PL2475428T3 - Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej - Google Patents

Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej

Info

Publication number
PL2475428T3
PL2475428T3 PL10751952T PL10751952T PL2475428T3 PL 2475428 T3 PL2475428 T3 PL 2475428T3 PL 10751952 T PL10751952 T PL 10751952T PL 10751952 T PL10751952 T PL 10751952T PL 2475428 T3 PL2475428 T3 PL 2475428T3
Authority
PL
Poland
Prior art keywords
heterocylcic
inhibitors
derivatives
glutaminyl cyclase
glutaminyl
Prior art date
Application number
PL10751952T
Other languages
English (en)
Inventor
Ulrich Heiser
Robert Sommer
Daniel Ramsbeck
Antje Meyer
Torsten Hoffmann
Livia Boehme
Hans-Ulrich Demuth
Original Assignee
Probiodrug Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Probiodrug Ag filed Critical Probiodrug Ag
Publication of PL2475428T3 publication Critical patent/PL2475428T3/pl

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/427Thiazoles not condensed and containing further heterocyclic rings
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
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    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
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    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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PL10751952T 2009-09-11 2010-09-13 Pochodne heterocykliczne jako inhibitory cyklazy glutaminowej PL2475428T3 (pl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US24143209P 2009-09-11 2009-09-11
EP10751952.2A EP2475428B1 (en) 2009-09-11 2010-09-13 Heterocylcic derivatives as inhibitors of glutaminyl cyclase
PCT/EP2010/063341 WO2011029920A1 (en) 2009-09-11 2010-09-13 Heterocylcic derivatives as inhibitors of glutaminyl cyclase

Publications (1)

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PL2475428T3 true PL2475428T3 (pl) 2015-12-31

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US (3) US8486940B2 (pl)
EP (1) EP2475428B1 (pl)
JP (1) JP5934645B2 (pl)
KR (1) KR101755737B1 (pl)
CN (1) CN102695546B (pl)
AU (1) AU2010294214B2 (pl)
BR (1) BR112012008346B1 (pl)
CA (1) CA2772488C (pl)
DK (1) DK2475428T3 (pl)
EA (1) EA022007B1 (pl)
ES (1) ES2548913T3 (pl)
IL (1) IL218259A (pl)
MX (1) MX2012002993A (pl)
NZ (1) NZ598685A (pl)
PL (1) PL2475428T3 (pl)
SG (1) SG178953A1 (pl)
WO (1) WO2011029920A1 (pl)
ZA (1) ZA201201366B (pl)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8530670B2 (en) 2011-03-16 2013-09-10 Probiodrug Ag Inhibitors
SG194770A1 (en) * 2011-05-27 2013-12-30 Probiodrug Ag Radiolabelled glutaminyl cyclase inhibitors
KR20160003652A (ko) * 2013-03-15 2016-01-11 캔써 리써치 테크놀로지, 엘엘씨 감마―글루타밀 주기 조절 방법 및 조성물
KR20210091830A (ko) * 2013-03-15 2021-07-22 비보리온 테라퓨틱스 아게 신규한 억제제
TWI477479B (zh) * 2013-07-18 2015-03-21 Daxin Materials Corp 二胺苯化合物、聚合物、配向膜用組成物、配向膜以及液晶顯示元件
DE102015011780A1 (de) * 2015-09-16 2017-03-16 Hochschule Anhalt Neue Glutaminylcyclase-lnhibitoren
GB201705263D0 (en) * 2017-03-31 2017-05-17 Probiodrug Ag Novel inhibitors
ES2938445T3 (es) 2017-07-24 2023-04-11 Stichting Het Nederlands Kanker Inst Antoni Van Leeuwenhoek Ziekenhuis Tratamiento de estados patológicos mediante acción selectiva directa e indirecta sobre la interacción SIRPA-CD47
ES2812698T3 (es) * 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
AU2018348359C1 (en) 2017-10-10 2023-10-12 Douglas Pharmaceuticals Ltd. Extended release pharmaceutical formulation and methods of treatment
US10869838B2 (en) 2017-10-10 2020-12-22 Douglas Pharmaceuticals, Ltd. Extended release pharmaceutical formulation
EP3521308B1 (en) 2018-01-31 2024-03-13 Vivoryon Therapeutics N.V. Humanized and de-immunized antibodies
US20210261539A1 (en) * 2018-02-06 2021-08-26 Shanghai Haihe Pharmaceutical Co., Ltd. Compound having bet inhibitory activity and preparation method and use therefor
KR102743609B1 (ko) 2018-02-23 2024-12-16 프라운호퍼-게젤샤프트 츄어 푀르더룽 데어 안게반텐 포르슝에.파우. 치주 및 관련 질환의 치료에 사용하기 위한 박테리아 글루타미닐 사이클라제에 대한 새로운 저해제
TWI715156B (zh) * 2018-08-31 2021-01-01 財團法人國家衛生研究院 苯并咪唑化合物及其用於治療阿茲海默症或亨丁頓氏症之用途
SG11202101274XA (en) * 2018-08-31 2021-03-30 National Health Res Inst Benzimidazole compounds and use thereof for treating alzheimer's disease or huntington's disease
GB201918410D0 (en) * 2019-12-13 2020-01-29 Z Factor Ltd Compounds and their use for the treatment of alpha1-antitrypsin deficiency
CN118019737A (zh) 2021-06-24 2024-05-10 英矽智能科技知识产权有限公司 用于治疗疾病的β-内酰胺衍生物
AU2022203580A1 (en) * 2021-09-17 2023-04-06 Academia Sinica Methods of Increasing Cell Phagocytosis
CN115448892B (zh) * 2022-09-19 2023-07-07 郑州铁路职业技术学院 一种苯并噻二唑杂环化合物的合成方法
EP4455142A1 (en) 2023-04-26 2024-10-30 Scenic Immunology B.V. Novel inhibitor of qpctl and/or qc
US20250026738A1 (en) 2023-06-16 2025-01-23 Vivoryon Therapeutics N.V. Crystalline pharmaceutically acceptable salt and polymorphic form of the glutaminyl cyclase inhibitor varoglutamstat
WO2025021012A1 (en) * 2023-07-21 2025-01-30 Insilico Medicine Ip Limited Crystalline beta-lactam derivatives and uses thereof
WO2025224179A1 (en) 2024-04-23 2025-10-30 Vivoryon Therapeutics N.V. Glutaminyl cyclase inhbitors for use in the treatment of kidney disease
WO2025224169A1 (en) 2024-04-23 2025-10-30 Vivoryon Therapeutics N.V. Dose regimens for the glutaminyl cyclase inhibitor varoglutamstat

Family Cites Families (596)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6137764A (ja) 1984-07-31 1986-02-22 Suntory Ltd 抗プロリルエンドペプチダ−ゼ活性を有する新規生理活性化合物
JPS6172439A (ja) 1984-09-18 1986-04-14 Sanyo Electric Co Ltd デ−タ転送方式
JPH0623190B2 (ja) 1985-04-16 1994-03-30 サントリー株式会社 インヒビタ−活性を有するn−アシルピロリジン誘導体及びその製法並びに用途
US4772587A (en) 1985-04-16 1988-09-20 Suntory Limited Dipeptide derivative of fatty acid
EP0201741B1 (en) 1985-04-16 1991-07-31 Suntory Limited Dipeptide derivatives, processes for preparing them, pharmaceutical composition and use
JPS62114957A (ja) 1985-11-13 1987-05-26 Suntory Ltd プロリルエンドペプチダ−ゼ阻害作用を有する新規ピロリジン誘導体およびその製法並びに用途
JPH0714878B2 (ja) 1985-11-14 1995-02-22 サントリー株式会社 ピロリジンアミドを有効成分とするプロリルエンドペプチダーゼ阻害剤
JPH0764834B2 (ja) 1985-11-29 1995-07-12 サントリー株式会社 プロリルエンドペプチダーゼ阻害活性を有する新規ピロリジンアミド誘導体およびその製法並びに用途
US5198458A (en) 1986-02-04 1993-03-30 Suntory Limited Pyrrolidineamide derivatives of acylamino acid and pharmaceutical composition containing the same
CA1320734C (en) 1986-02-04 1993-07-27 Suntory Limited Pyrrolidineamide derivative of acylamino acid and pharmaceutical composition containing the same
CA1334092C (en) 1986-07-11 1995-01-24 David John Carini Angiotensin ii receptor blocking imidazoles
US5223482A (en) 1986-11-17 1993-06-29 Scios Nova Inc. Recombinant Alzheimer's protease inhibitory amyloid protein and method of use
JPH08806B2 (ja) 1986-11-18 1996-01-10 サントリー株式会社 プロリルエンドペプチダ−ゼ阻害作用を有する新規ピロリジンアミド誘導体
DE3786229T2 (de) 1986-11-20 1993-10-07 Ono Pharmaceutical Co Prolinalderivate.
US5254550A (en) 1986-11-20 1993-10-19 Ono Pharmaceutical Co., Ltd. Prolinal derivatives and pharmaceutical compositions thereof
JPS63162672A (ja) 1986-12-25 1988-07-06 Ono Pharmaceut Co Ltd 新規なプロリナ−ル誘導体、それらの製造方法およびそれらを含有する抗健忘症剤
DE3783754T2 (de) 1986-12-29 1993-08-05 Ono Pharmaceutical Co Prolin-derivate.
JPH089591B2 (ja) 1986-12-29 1996-01-31 小野薬品工業株式会社 新規なプロリナール誘導体
US5262431A (en) 1986-12-29 1993-11-16 Ono Pharmaceutical Co., Ltd. Prolinal derivatives and pharmaceutical compositions thereof
EP0277588B1 (en) 1987-02-04 1993-03-24 Ono Pharmaceutical Co., Ltd. Prolinal derivatives
JP2528343B2 (ja) 1987-02-04 1996-08-28 小野薬品工業株式会社 新規なプロリナ―ル誘導体
ES2052619T3 (es) 1987-02-23 1994-07-16 Ono Pharmaceutical Co Un procedimiento para la preparacion de los nuevos derivados de tiazolidina.
JPS6442465A (en) 1987-08-07 1989-02-14 Wakunaga Pharma Co Ltd N-acylprolylpyrrolidine derivative, production and use thereof
JP2649237B2 (ja) 1988-03-07 1997-09-03 キッセイ薬品工業 株式会社 チアゾリジン誘導体
US4857524A (en) 1987-08-08 1989-08-15 Kissei Pharmaceutical Co., Ltd. Thiazolidine compounds and therapeutic method
JP2515558B2 (ja) 1987-09-10 1996-07-10 株式会社ヤクルト本社 新規なペプチドおよびそれを有効成分とする抗健忘症剤
CA1339014C (en) 1987-10-08 1997-03-25 Ronald E. Majocha Antibodies to a4 amyloid peptide
JPH0742309B2 (ja) 1987-11-30 1995-05-10 キッセイ薬品工業株式会社 チアゾリジン誘導体
JPH01250370A (ja) 1987-12-23 1989-10-05 Zeria Pharmaceut Co Ltd 新規アミノ酸イミド誘導体、製法ならびに用途
US5053414A (en) 1988-04-08 1991-10-01 Ono Pharmaceutical Co., Ltd. Heterocyclic compounds
US5328899A (en) 1988-07-15 1994-07-12 The Salk Institute For Biological Studies NPY peptide analogs
ZA896376B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y agonists
ZA896374B (en) 1988-08-26 1990-05-30 Merrell Dow Pharma Neuropeptide y antagonists
JP2531989B2 (ja) 1988-09-14 1996-09-04 吉富製薬株式会社 ピリジン化合物
CA2004028C (en) 1988-12-08 1998-09-22 Motoki Torizuka Condensed benzene derivative
JPH02207070A (ja) 1989-02-07 1990-08-16 Zeria Pharmaceut Co Ltd アミノ酸イミド誘導体、それを含有する医薬及び該化合物の製造中間体
EP0419683A4 (en) 1989-04-13 1992-03-11 Japan Tobacco Inc. New amino acid derivatives having prolylendopeptidase inhibitor activity
WO1990012871A1 (en) 1989-04-14 1990-11-01 Research Foundation For Mental Hygiene, Inc. Cerebrovascular amyloid protein-specific monoclonal antibody sv17-6e10
WO1990012870A1 (en) 1989-04-14 1990-11-01 Research Foundation For Mental Hygiene, Inc. Monoclonal antibody to amyloid peptide
EP0403159B1 (en) 1989-06-14 2000-03-01 Smithkline Beecham Corporation Imidazolyl-alkenoic acids
JPH082791B2 (ja) 1989-07-24 1996-01-17 キッセイ薬品工業株式会社 健忘症治療剤
DE3939797A1 (de) 1989-12-01 1991-06-06 Basf Ag Neue vom neuropeptid y abgeleitete peptide
US4985560A (en) 1990-01-12 1991-01-15 American Home Products Corporation Pyridazino(4,5-b)indolizines
PH30484A (en) 1990-02-19 1997-05-28 Ciba Geigy Acy compounds pharmaceutical composition containing said compound and method of use thereof
JPH04211648A (ja) 1990-07-27 1992-08-03 Nippon Kayaku Co Ltd ケト酸アミド誘導体
JPH03255080A (ja) 1990-03-05 1991-11-13 Yoshitomi Pharmaceut Ind Ltd ベンゼン化合物
TW201738B (pl) 1990-03-20 1993-03-11 Sanofi Co
US4999349A (en) 1990-03-22 1991-03-12 Bristol-Myers Squibb Co. BU-4164E - A and B, prolyl endopeptidase inhibitors
US5073549A (en) 1990-03-22 1991-12-17 Bristol-Myers Squibb Company BU-4164E - A and B, prolyl endopeptidase inhibitors and their methods of use
US5196444A (en) 1990-04-27 1993-03-23 Takeda Chemical Industries, Ltd. 1-(cyclohexyloxycarbonyloxy)ethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate and compositions and methods of pharmaceutical use thereof
JPH049367A (ja) 1990-04-26 1992-01-14 Zeria Pharmaceut Co Ltd アリールアルカノイル誘導体,該化合物の製造中間体及びそれらを含有する医薬
JP2511605B2 (ja) 1990-06-04 1996-07-03 ファイザー・インコーポレーテッド 芳香性ピロリジンおよびチアゾリヂンアミド類
WO1991018877A1 (en) 1990-06-07 1991-12-12 Zeria Pharmaceutical Co., Ltd. Novel arylalkanoylamine derivative and drug containing the same
US5506256A (en) 1990-07-27 1996-04-09 Yoshitomi Pharmaceutical Industries, Ltd. Proline derivatives possessing prolyl endopeptidase-inhibitory activity
EP0468469A2 (en) 1990-07-27 1992-01-29 Japan Tobacco Inc. Proline derivatives
JPH07108897B2 (ja) 1990-07-27 1995-11-22 日本たばこ産業株式会社 新規なプロリン誘導体
JPH05186498A (ja) 1991-12-27 1993-07-27 Japan Tobacco Inc プロリン誘導体
JPH04235162A (ja) 1990-08-09 1992-08-24 Zeria Pharmaceut Co Ltd 新規コハク酸アミド誘導体およびそれを含有する医薬
JPH04208299A (ja) 1990-11-30 1992-07-29 Ajinomoto Co Inc プロリルエンドペプチターゼ阻害ペプチド
IE920540A1 (en) 1991-02-21 1992-08-26 Sankyo Co 1-biphenylmethylimidazole derivatives, their preparation and¹their therapetuic use
US5104880A (en) 1991-05-01 1992-04-14 Mayo Foundation For Medical Education And Research Huperzine a analogs as acetylcholinesterase inhibitors
WO1992021333A2 (en) 1991-05-24 1992-12-10 Pharmavene, Inc. Treatment of drug withdrawal symptoms and drug craving with type b monoamine oxidase inhibitors
WO1993000361A1 (en) 1991-06-20 1993-01-07 Snow Brand Milk Products Co., Ltd. Novel prolyl endopeptidase inhibitors sna-115 and sna-115t, production thereof, and strain which produces said inhibitors
DE4121975A1 (de) 1991-07-03 1993-01-07 Basf Ag Thermoplastische formmassen auf der basis von polycarbonaten, styrol/acrylnitril-polymerisaten und polyolefinen
JP3010795B2 (ja) 1991-07-04 2000-02-21 不二製油株式会社 ペプチドの苦味除去方法
EP0597956A1 (en) 1991-07-29 1994-05-25 Warner-Lambert Company Quinazoline derivatives as acetylcholinesterase inhibitors
TW226375B (pl) 1991-10-24 1994-07-11 American Home Prod
EP0672054A4 (en) 1991-12-19 1996-02-07 Garvan Inst Med Res NEW MOLECULE INHIBITING THE BIOLOGICAL FUNCTION OF THE TYROSINE NEUROPEPTIDE.
JPH05301826A (ja) 1991-12-24 1993-11-16 Snow Brand Milk Prod Co Ltd プロリルエンドペプチダーゼ阻害剤
JPH05201970A (ja) 1992-01-24 1993-08-10 Japan Tobacco Inc 新規プロリン誘導体
JP3318622B2 (ja) 1992-05-27 2002-08-26 独立行政法人産業技術総合研究所 プロリルエンドペプチダーゼ阻害剤
GB9212308D0 (en) 1992-06-10 1992-07-22 Ici Plc Therapeutic compositions
GB9213215D0 (en) 1992-06-20 1992-08-05 Wellcome Found Peptides
JPH06116284A (ja) 1992-10-02 1994-04-26 Yamanouchi Pharmaceut Co Ltd 新規ペプチド
DK0664291T3 (da) 1992-10-05 2000-10-30 Ube Industries Pyrimidinforbindelse
US5260286A (en) 1992-10-16 1993-11-09 Japan Tobacco, Inc. 2-piperidinecarboxylic acid derivatives useful as NMDA receptor antagonists
WO1994012474A1 (fr) 1992-11-20 1994-06-09 Japan Tobacco Inc. Compose inhibant la prolyle endopeptidase et utilisation pharmaceutique de ce dernier
US5354758A (en) 1992-12-16 1994-10-11 Japan Tobacco Inc. Benzomorphans useful as NMDA receptor antagonists
JPH06192298A (ja) 1992-12-24 1994-07-12 Mitsui Toatsu Chem Inc 新規機能性ペプチド
DE4326465A1 (de) 1993-01-20 1995-02-09 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
US5750349A (en) 1993-01-25 1998-05-12 Takeda Chemical Industries Ltd. Antibodies to β-amyloids or their derivatives and use thereof
JPH06234693A (ja) 1993-02-09 1994-08-23 Snow Brand Milk Prod Co Ltd 新規イソテトラセノン系物質及びその製造法
FR2701480B1 (fr) 1993-02-15 1995-05-24 Sanofi Elf Composés à groupe sulfamoyle et amidino, leur procédé de préparation et les compositions pharmaceutiques les contenant.
EP0611769A1 (en) 1993-02-16 1994-08-24 Merrell Dow Pharmaceuticals Inc. Silylated acetylcholinesterase inhibitors
WO1994020476A1 (fr) 1993-03-02 1994-09-15 Fujisawa Pharmaceutical Co., Ltd. Nouveau compose heterocyclique
FR2702150B1 (fr) 1993-03-03 1995-04-07 Rhone Poulenc Rorer Sa Application de dérivés de 2H-1,2-4-benzothiadiazine-3(4H)-one-1,1-dioxyde comme antagonistes non compétitifs du récepteur NMDA.
FR2703050B1 (fr) 1993-03-24 1995-04-28 Adir Nouveaux dérivés bicycliques azotés, leur procédé de préparation et les compositions pharmaceutiques qui les contiennent.
EP0627400A1 (en) 1993-06-04 1994-12-07 Merrell Dow Pharmaceuticals Inc. Aromatic acetylcholinesterase inhibitors
WO1995000161A1 (en) 1993-06-18 1995-01-05 University Of Cincinnati Neuropeptide y antagonists and agonists
WO1995001352A1 (en) 1993-06-30 1995-01-12 Zeria Pharmaceutical Co., Ltd. Thiazolidine derivative and medicine containing the same
FR2707645B1 (fr) 1993-07-16 1995-08-11 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pirazine-4-one, leur préparation et les médicaments les contenant.
FR2707643B1 (fr) 1993-07-16 1995-08-11 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pyrazine-4-one, leur préparation et les médicaments les contenant.
EP0709373B1 (en) 1993-07-23 2001-10-17 Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai Pyrrolidine derivative
FR2711993B1 (fr) 1993-11-05 1995-12-01 Rhone Poulenc Rorer Sa Médicaments contenant des dérivés de 7H-imidazol[1,2-a]pyrazine-8-one, les nouveaux composés et leur préparation.
HUT74687A (en) 1993-12-02 1997-01-28 Merrell Pharma Inc Pyrrole and thiazolidine derivatives of prolyl endopeptidase inhibitor activity and pharmaceutical compositions containing the same
IL111785A0 (en) 1993-12-03 1995-01-24 Ferring Bv Dp-iv inhibitors and pharmaceutical compositions containing them
FR2717805B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Dérivés de 5H-indeno[1,2-b]pyrazine-2,3-dione, leur préparation et les médicaments les contenant .
FR2717812B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Indeno[1,2-e]pyrazine-4-ones, leur préparation et les médicaments les contenant.
FR2717813B1 (fr) 1994-03-28 1996-05-10 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]indeno[1,2-e]pyrazine-4-one, leur préparation et les médicaments les contenant .
FR2717811B1 (fr) 1994-03-28 1996-04-26 Rhone Poulenc Rorer Sa Dérivés d'imidazo[1,2-a]pyrazine-4-one, leur préparation et les médicaments les contenant.
JPH07267988A (ja) 1994-03-31 1995-10-17 Yamanouchi Pharmaceut Co Ltd 新規ペプチド
GB9410320D0 (en) 1994-05-24 1994-07-13 Fisons Corp Novel therapeutic method
GB9418443D0 (en) 1994-09-13 1994-11-02 Pfizer Ltd Therapeutic agents
US6562862B1 (en) 1994-10-20 2003-05-13 Eli Lilly And Company Methods of inhibiting physiological conditions associated with an excess of neuropeptide Y
IL115613A0 (en) 1994-10-20 1996-01-19 Lilly Co Eli Bicyclic neuropeptide y receptor antagonists
US5663192A (en) 1994-10-20 1997-09-02 Eli Lilly And Company Heterocyclic neuropeptide Y receptor antagonists
FR2726275B1 (fr) 1994-11-02 1996-12-06 Rhone Poulenc Rorer Sa Spiro heterocycle-imidazo(1,2-a)indeno(1,2-e)pyrazine)-4'- ones, leur preparation et les medicaments les contenants
IL116584A0 (en) 1994-12-29 1996-03-31 Res Dev Foundation Novel flavin adenine dinucleotide analogue inhibitors of monoamine oxidase
US5691368A (en) 1995-01-11 1997-11-25 Hoechst Marion Roussel, Inc. Substituted oxazolidine calpain and/or cathepsin B inhibitors
GB9500601D0 (en) 1995-01-12 1995-03-01 Wellcome Found Modified peptides
US5786180A (en) 1995-02-14 1998-07-28 Bayer Corporation Monoclonal antibody 369.2B specific for β A4 peptide
US5552411A (en) 1995-05-26 1996-09-03 Warner-Lambert Company Sulfonylquinolines as central nervous system and cardiovascular agents
IL117997A0 (en) 1995-06-07 1996-10-31 Pfizer Neuropeptide Y1 specific ligands
US5635503A (en) 1995-06-07 1997-06-03 Bristol-Myers Squibb Company Dihydropyridine npy antagonists: piperazine derivatives
US5668151A (en) 1995-06-07 1997-09-16 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: piperidine derivatives
US5554621A (en) 1995-06-07 1996-09-10 Bristol-Myers Squibb Company Dihydropyridine NPY antagonists: nitrogen heterocyclic derivatives
JP3727383B2 (ja) 1995-07-31 2005-12-14 月桂冠株式会社 プロリルエンドペプチダーゼ阻害剤
IL120724A0 (en) 1995-09-01 1997-08-14 Lilly Co Eli Indolyl neuropeptide Y receptor antagonists
AU6966696A (en) 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
ES2100129B1 (es) 1995-10-11 1998-02-16 Medichem Sa Nuevos compuestos aminopiridinicos policiclicos inhibidores de acetilcolinesterasa, procedimiento para su preparacion y su utilizacion.
DE19544685A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE19544686A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
DE19544687A1 (de) 1995-11-30 1997-06-05 Thomae Gmbh Dr K Aminosäurederivate, diese Verbindungen enthaltende Arzneimittel und Verfahren zu ihrer Herstellung
AU7692996A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Receptor antagonists
WO1997019682A1 (en) 1995-12-01 1997-06-05 Synaptic Pharmaceutical Corporation Aryl sulfonamide and sulfamide derivatives and uses thereof
AU7626496A (en) 1995-12-01 1997-06-27 Ciba-Geigy Ag Heteroaryl compounds
WO1997020821A1 (en) 1995-12-01 1997-06-12 Novartis Ag Heteroaryl derivatives
AU7692896A (en) 1995-12-01 1997-06-27 Novartis Ag Quinazolin-2,4-diazirines as NPY receptor antagonist
JPH09157253A (ja) 1995-12-12 1997-06-17 Yamanouchi Pharmaceut Co Ltd 新規アミノ酸誘導体
ZA9610745B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Subsituted piperidine analogs and their use as subtype selective nmda receptor antagonists
ZA9610736B (en) 1995-12-22 1997-06-27 Warner Lambert Co 2-Substituted piperidine analogs and their use as subtypeselective nmda receptor antagonists
ZA9610741B (en) 1995-12-22 1997-06-24 Warner Lambert Co 4-Substituted piperidine analogs and their use as subtype selective nmda receptor antagonists
AU2242197A (en) 1996-01-09 1997-08-01 Eli Lilly And Company Benzimidzolyl neuropeptide y receptor antagonists
GB9605027D0 (en) 1996-03-09 1996-05-08 Pfizer Ltd Quinoxalinediones
US5662723A (en) 1996-03-22 1997-09-02 Libbey Glass Inc. Apparatus and method for forming a decorative pattern on glassware having an edge
CA2252039C (en) 1996-04-12 2002-12-24 Hoechst Marion Roussel, Inc. Isatin derivatives as acetylcholinesterase inhibitors and analgesics
DE122010000020I1 (de) 1996-04-25 2010-07-08 Prosidion Ltd Verfahren zur Senkung des Blutglukosespiegels in Säugern
AU3295297A (en) 1996-06-04 1998-01-05 Synaptic Pharmaceutical Corporation Methods of modifying feeding behavior, compounds useful in such methods, and dna encoding a hypothalamic atypical neuropeptide y/peptide yy receptor (y5)
PT942751E (pt) 1996-07-05 2003-02-28 Wwk Trust The Composicoes para o tratamento de neuropatias perifericas contendo antiodepressivos e/ou inibidores da monoamino-oxidase e/ou vitamina b12 e/ou precursores ou indutores de neurotransmissores
DK0915859T3 (da) 1996-07-23 2003-03-03 Neurogen Corp Visse substituerede benzylaminderivater; en ny klasse af Neuropeptid Y1-specifikke ligander
JP2000515151A (ja) 1996-07-23 2000-11-14 ニューロジェン・コーポレーション 特定の置換ベンジルアミン誘導体;新規クラスの神経ペプチド―y1特異的リガンド
PT918761E (pt) 1996-07-23 2003-09-30 Neurogen Corp Algumas amidas e aminas substituidas com derivados de benzilamina uma nova classe de ligandos especificos do neuropeptido y1
AU3967297A (en) 1996-08-01 1998-02-25 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
EP0927167A1 (en) 1996-08-14 1999-07-07 Warner-Lambert Company 2-phenyl benzimidazole derivatives as mcp-1 antagonists
US6849733B1 (en) 1996-08-23 2005-02-01 Agouron Pharmaceuticals, Inc. Neuropeptide-Y ligands
JP3880664B2 (ja) 1996-09-04 2007-02-14 月桂冠株式会社 プロリルエンドペプチダーゼ阻害ペプチド
WO1998010757A2 (en) 1996-09-11 1998-03-19 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services The use of functional n-methyl-d-aspartate antagonists to ameliorate or prevent aminoglycoside-induced ototoxicity
WO1998015647A1 (en) 1996-10-08 1998-04-16 Novartis Ag Modulation of apoptosis
FR2754709B1 (fr) 1996-10-23 1999-03-05 Sanofi Sa Composition cosmetique contenant un antagoniste des recepteurs du neuropeptide gamma et alpha 2 antagonistes susceptibles d'etre incorpores dans une telle composition
TW492957B (en) 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
US6011155A (en) 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
AU5716898A (en) 1997-01-08 1998-08-03 Warner-Lambert Company Acetylcholinesterase inhibitors in combination with muscarinic agonists for the treatment of alzheimer's disease
US20030068316A1 (en) 1997-02-05 2003-04-10 Klein William L. Anti-ADDL antibodies and uses thereof
JP2894445B2 (ja) 1997-02-12 1999-05-24 日本たばこ産業株式会社 Cetp活性阻害剤として有効な化合物
WO1998040102A1 (en) 1997-03-13 1998-09-17 The Provost, Fellows And Scholars Of The College Of The Holy And Undivided Trinity Of Queen Elizabeth Near Dublin Cytoprotective agents comprising monoamine oxidase inhibitors
DE69839808D1 (de) 1997-04-09 2008-09-11 Intellect Neurosciences Inc Für die termini des beta-amyloids spezifische, rekombinante antikörper, dafür kodierende dna und verfahren zu ihrer verwendung
US8173127B2 (en) 1997-04-09 2012-05-08 Intellect Neurosciences, Inc. Specific antibodies to amyloid beta peptide, pharmaceutical compositions and methods of use thereof
DE69808266D1 (de) 1997-04-16 2002-10-31 Arqule Inc Herstellung und verwendung von alpha-ketoamid derivate und anordnunge
WO1998050075A1 (en) 1997-05-07 1998-11-12 Algos Pharmaceutical Corporation Cox-2 inhibitors in combination with nmda-blockers for treating pain
WO1998050044A1 (en) 1997-05-07 1998-11-12 Algos Pharmaceutical Corporation Composition and method combining an antidepressant with an nmda receptor antagonist, for treating neuropathic pain
ATE240936T1 (de) 1997-06-30 2003-06-15 Merz & Co Gmbh & Co 1-amino-alkylcyclohexane als nmda-rezeptor- antagonisten
GB9716657D0 (en) 1997-08-07 1997-10-15 Zeneca Ltd Chemical compounds
GB9716879D0 (en) 1997-08-08 1997-10-15 Shire Int Licensing Bv Treatment of attention deficit disorders
WO1999007413A1 (en) 1997-08-11 1999-02-18 Algos Pharmaceutical Corporation Substance p inhibitors in combination with nmda-blockers for treating pain
SE9703376D0 (sv) 1997-09-18 1997-09-18 Astra Ab A new combination
SE9703414D0 (sv) 1997-09-23 1997-09-23 Astra Ab New compounds
US7964192B1 (en) 1997-12-02 2011-06-21 Janssen Alzheimer Immunotherapy Prevention and treatment of amyloidgenic disease
US7179892B2 (en) 2000-12-06 2007-02-20 Neuralab Limited Humanized antibodies that recognize beta amyloid peptide
TWI239847B (en) 1997-12-02 2005-09-21 Elan Pharm Inc N-terminal fragment of Abeta peptide and an adjuvant for preventing and treating amyloidogenic disease
EP2823812A1 (en) 1998-02-02 2015-01-14 Trustees Of Tufts College Dipeptidylpeptidase IV inhibitors for use in the treatment of Type II diabetes
JP2002506075A (ja) 1998-03-09 2002-02-26 フォンダテッヒ・ベネルクス・ナムローゼ・フェンノートシャップ セリンペプチダーゼ調節剤
US6007841A (en) 1998-03-13 1999-12-28 Algos Pharmaceutical Corporation Analgesic composition and method for treating pain
GB9805561D0 (en) 1998-03-16 1998-05-13 Merck Sharp & Dohme A combination of therapeutic agents
US6541208B1 (en) 1998-03-17 2003-04-01 University Of Maryland Biotechnology Institute Diagnostic method for distinguishing HIV-associated dementia from other forms of dementia
DE19812331A1 (de) 1998-03-20 1999-09-23 Merck Patent Gmbh Piperidinderivate
US6054451A (en) 1998-04-21 2000-04-25 Algos Pharmaceutical Corporation Analgesic composition and method for alleviating pain
US6303617B1 (en) 1998-05-04 2001-10-16 Neotherapeutics, Inc. Serotonin-like 9-substituted hypoxanthine and methods of use
WO1999057119A1 (en) 1998-05-04 1999-11-11 Neotherapeutics, Inc. Novel dopamine-like 9-substituted hypoxanthine and methods of use
AU4007599A (en) 1998-05-21 1999-12-06 University Of Tennessee Research Corporation, The Methods for amyloid removal using anti-amyloid antibodies
DE19823831A1 (de) 1998-05-28 1999-12-02 Probiodrug Ges Fuer Arzneim Neue pharmazeutische Verwendung von Isoleucyl Thiazolidid und seinen Salzen
DE19828114A1 (de) 1998-06-24 2000-01-27 Probiodrug Ges Fuer Arzneim Produgs instabiler Inhibitoren der Dipeptidyl Peptidase IV
DE19828113A1 (de) 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
PE20000728A1 (es) 1998-06-26 2000-08-21 Cocensys Inc Heterociclos 4-bencil piperidina alquilsulfoxido y su uso como antagonistas receptores subtipo-selectivo nmda
DE19834591A1 (de) 1998-07-31 2000-02-03 Probiodrug Ges Fuer Arzneim Verfahren zur Steigerung des Blutglukosespiegels in Säugern
IT1304904B1 (it) 1998-09-11 2001-04-05 Eisai Co Ltd Derivati anticolinesterasici per il trattamento delle sindromidolorose funzionali e/o organiche
JP2002538078A (ja) 1998-11-12 2002-11-12 アルゴス ファーマシューティカル コーポレーション 痛みを治療するnmda−ブロッカーと組み合わされたcox−2阻害剤
WO2000030674A1 (en) 1998-11-26 2000-06-02 Ferring Bv Neuropeptide y y4 agents in the treatment of reproductive disorders
GB9902455D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902453D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902459D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902461D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
GB9902452D0 (en) 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
US6495587B1 (en) 1999-03-23 2002-12-17 Sumitomo Pharmaceuticals Company, Limited Tricyclic indole-2-carboxylic acid compound used as NMDA receptor antagonist
JP2002542261A (ja) 1999-04-15 2002-12-10 メルク フロスト カナダ アンド カンパニー カスパーゼにより切断されたappを認識する抗体及びその使用法
US6121311A (en) 1999-04-28 2000-09-19 Japan Tobacco Inc. Method for treating cocainism
CA2373035A1 (en) 1999-05-05 2000-11-16 Scott Dax 3a,4,5,9b-tetrahydro-1h-benz[e]indol-2-yl amine-derived neuropeptide y receptors ligands useful in the treatment of obesity and other disorders
JP3148739B2 (ja) 1999-05-19 2001-03-26 ドーマー株式会社 プロリルエンドペプチダーゼ阻害剤
DK1409654T3 (da) 1999-06-16 2008-12-08 Boston Biomedical Res Inst Immunologisk styring af beta-amyloid-niveauer in vivo
US6107317A (en) 1999-06-24 2000-08-22 Novartis Ag N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6172081B1 (en) 1999-06-24 2001-01-09 Novartis Ag Tetrahydroisoquinoline 3-carboxamide derivatives
US6110949A (en) 1999-06-24 2000-08-29 Novartis Ag N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
US6524616B1 (en) 1999-06-25 2003-02-25 Wake Forest University Health Services Compositions and methods for treating or preventing neurodegeneration and cognitive decline and dysfunction associated with alzheimer's disease, aging, other dementia related disorders and estrogen deficiency related conditions
US6316449B1 (en) 1999-07-08 2001-11-13 Millennium Pharmaceuticals, Inc. Chemokine receptor antagonists
DE19936719A1 (de) 1999-08-06 2001-02-15 Gruenenthal Gmbh Substituierte 1,5-Dihydropyrrol-2-on-Derivate
DE19936521A1 (de) 1999-08-06 2001-02-15 Gruenenthal Gmbh Substituierte Pyrrolidin-2,3,4-trion-3-oxim-Derivate
EP1307219A4 (en) 1999-08-13 2005-04-06 Univ Columbia METHODS OF INHIBITING BETA FIBRILLE BINDING BETA TO RAGE RECEPTOR, AND CONSEQUENCES THEREOF
EP1078632A1 (en) 1999-08-16 2001-02-28 Sanofi-Synthelabo Use of monoamine oxydase inhibitors for the manufacture of drugs intended for the treatment of obesity
DE19940130A1 (de) 1999-08-24 2001-03-01 Probiodrug Ges Fuer Arzneim Neue Effektoren der Dipeptidyl Peptidase IV zur topischen Anwendung
TWI283577B (en) 1999-10-11 2007-07-11 Sod Conseils Rech Applic Pharmaceutical composition of imidazole derivatives acting as modulators of sodium channels and the use thereof
UA72558C2 (uk) 1999-11-01 2005-03-15 Мерц Фарма Гмбх Унд Ко. Кгаа 1-аміноалкілциклогексанові антагоністи рецептора nmda
JP2003535034A (ja) 1999-11-12 2003-11-25 ギルフォード ファーマシューティカルズ インコーポレイテッド ジペプチジルペプチダーゼiv阻害剤並びにジペプチジルペプチダーゼiv阻害剤の製造及び使用法
US20020094335A1 (en) 1999-11-29 2002-07-18 Robert Chalifour Vaccine for the prevention and treatment of alzheimer's and amyloid related diseases
GB9928330D0 (en) 1999-11-30 2000-01-26 Ferring Bv Novel antidiabetic agents
EP1254108A1 (en) 2000-01-24 2002-11-06 MERCK SHARP & DOHME LTD. Gamma-secretase inhibitors
WO2001055105A1 (en) 2000-01-24 2001-08-02 Novo Nordisk A/S N-substituted 2-cyanopyroles and -pyrrolines which are inhibitors of the enzyme dpp-iv
CA2399080C (en) 2000-02-03 2013-05-21 Millennium Pharmaceuticals, Inc. Humanized anti-ccr2 antibodies and methods of use therefor
CA2400559C (en) 2000-02-24 2012-05-01 Washington University Humanized antibodies that sequester .alpha..beta. peptide
GB0005251D0 (en) 2000-03-03 2000-04-26 Merck Sharp & Dohme Therapeutic compounds
AU2001239052A1 (en) 2000-03-06 2001-09-17 Immune Network Ltd. Compositions for prevention and treatment of dementia
US6395767B2 (en) 2000-03-10 2002-05-28 Bristol-Myers Squibb Company Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
US6992081B2 (en) 2000-03-23 2006-01-31 Elan Pharmaceuticals, Inc. Compounds to treat Alzheimer's disease
WO2001070672A2 (en) 2000-03-23 2001-09-27 Elan Pharmaceuticals, Inc. Compounds and methods to treat alzheimer's disease
GB0008710D0 (en) 2000-04-07 2000-05-31 Merck Sharp & Dohme Therapeutic compounds
JP4150519B2 (ja) 2000-04-13 2008-09-17 エーザイ・アール・アンド・ディー・マネジメント株式会社 1−ベンジルピリジニウム塩を含有してなるアセチルコリンエステラーゼ阻害剤
GB0010183D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
GB0010188D0 (en) 2000-04-26 2000-06-14 Ferring Bv Inhibitors of dipeptidyl peptidase IV
EE200200612A (et) 2000-04-26 2004-06-15 Warner-Lambert Company Tsükloheksüülamiini derivaadid kui alatüübi selektiivsed NMDA-retseptori antagonistid
US20010036949A1 (en) 2000-05-09 2001-11-01 Coe Jotham Wadsworth Pharmaceutical composition and method of treatment of diseases of cognitive dysfunction in a mammal
WO2001092204A1 (en) 2000-06-01 2001-12-06 Warner-Lambert Company Cyclohexylamine derivatives as subtype selective nmda receptor antagonists
AU2001263130A1 (en) 2000-06-06 2001-12-17 Warner Lambert Company Bicyclic cyclohexylamines and their use as nmda receptor antagonists
JP2004501145A (ja) 2000-06-22 2004-01-15 ファーモス コーポレイション 向精神作用をもたない新規なカンナビノイド
GB0015488D0 (en) 2000-06-23 2000-08-16 Merck Sharp & Dohme Therapeutic agents
US6713276B2 (en) 2000-06-28 2004-03-30 Scios, Inc. Modulation of Aβ levels by β-secretase BACE2
US6686449B2 (en) 2000-06-30 2004-02-03 Pharmacia & Upjohn Company Mutant presenilin 1 polypeptides
AU2001271686A1 (en) 2000-06-30 2002-01-14 Elan Pharmaceuticals, Inc. Compounds to treat alzheimer's disease
MXPA02012272A (es) 2000-07-04 2003-04-25 Novo Nordisk As Compuestos heterociclicos que son inhibidores de la enzima dipeptidilpeptidasa-iv.
GB0016681D0 (en) 2000-07-06 2000-08-23 Merck Sharp & Dohme Therapeutic compounds
US6556971B1 (en) 2000-09-01 2003-04-29 Snap-On Technologies, Inc. Computer-implemented speech recognition system training
WO2002020500A2 (en) * 2000-09-01 2002-03-14 Icos Corporation Materials and methods to potentiate cancer treatment
WO2002027418A2 (en) 2000-09-25 2002-04-04 Motorwiz, Inc. Model-based machine diagnostics and prognostics using theory of noise and communications
US20020151591A1 (en) 2000-10-17 2002-10-17 Anabella Villalobos Combination use of acetylcholinesterase inhibitors and GABAa inverse agonists for the treatment of cognitive disorders
HU227197B1 (en) 2000-10-24 2010-10-28 Richter Gedeon Nyrt Nmda receptor antagonist carboxylic acid amide derivatives and pharmaceutical compositions containing them
AU1074702A (en) 2000-11-02 2002-05-15 Merck Sharp & Dohme Sulfamides as gamma-secretase inhibitors
AU2002239765A1 (en) 2000-11-03 2002-06-03 Proteotech, Inc. Antibody pti-hs7 for treatment of alzheimer's disease and other amyloidoses and parkinson's disease
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives
TWI255272B (en) 2000-12-06 2006-05-21 Guriq Basi Humanized antibodies that recognize beta amyloid peptide
US6495335B2 (en) 2000-12-07 2002-12-17 Mario Chojkier Compositions and methods for diagnosing alzheimer's disease
US6670364B2 (en) 2001-01-31 2003-12-30 Telik, Inc. Antagonists of MCP-1 function and methods of use thereof
TWI245761B (en) 2001-03-01 2005-12-21 Telik Inc Antagonists of MCP-1 function and methods of use thereof
JP2005506292A (ja) 2001-03-08 2005-03-03 エモリー ユニバーシティ pHに依存するNMDAレセプターアンタゴニスト
US6649196B2 (en) 2001-03-12 2003-11-18 Mayo Foundation For Medical Education And Research Methods of reducing β-amyloid polypeptides
US6815175B2 (en) 2001-03-16 2004-11-09 Cornell Research Foundation, Inc. Anti-amyloid peptide antibody based diagnosis and treatment of a neurological disease or disorder
US6677365B2 (en) 2001-04-03 2004-01-13 Telik, Inc. Antagonists of MCP-1 function and methods of use thereof
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
US7318923B2 (en) 2001-04-30 2008-01-15 Eli Lilly And Company Humanized anti-βantibodies
AU2002257162A1 (en) 2001-04-30 2002-11-11 Eli Lilly And Company Humanized antibodies
FR2824825B1 (fr) 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
SI20922A (sl) 2001-05-18 2002-12-31 Krka Tovarna Zdravil, D.D., Novo Mesto Monoklonsko protitelo, ki nevtralizira aktivnost katepsina B, in njegove uporabe
US6562783B2 (en) 2001-05-30 2003-05-13 Neurologic, Inc. Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
EP1395551B1 (en) 2001-06-01 2008-05-21 Elan Pharmaceuticals, Inc. Hydroxy alkyl amine derivatives as beta-secretase inhibitors and their use for the treatment of alzheimer's disease and similar diseases
JP2005500308A (ja) 2001-06-20 2005-01-06 メルク エンド カムパニー インコーポレーテッド 糖尿病を治療するためのジペプチジルペプチダーゼ阻害剤
AU2002344820B2 (en) 2001-06-20 2006-12-14 Merck & Co., Inc. Dipeptidyl peptidase inhibitors for the treatment of diabetes
GB0115517D0 (en) 2001-06-25 2001-08-15 Ferring Bv Novel antidiabetic agents
CA2452039A1 (en) 2001-06-27 2003-01-09 Elan Pharmaceuticals, Inc. Beta-hydroxyamine derivatives useful in treatment of alzheimer's disease
EP1406873B1 (en) 2001-06-27 2007-09-26 Smithkline Beecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
DE10150203A1 (de) 2001-10-12 2003-04-17 Probiodrug Ag Peptidylketone als Inhibitoren der DPIV
DE60223920T2 (de) 2001-06-27 2008-11-13 Smithkline Beecham Corp. Pyrrolidine als dipeptidyl-peptidase-inhibitoren
ATE370943T1 (de) 2001-06-27 2007-09-15 Smithkline Beecham Corp Fluoropyrrolidine als dipeptidyl-peptidase inhibitoren
DE10154689A1 (de) 2001-11-09 2003-05-22 Probiodrug Ag Substituierte Aminoketonverbindungen
CN1471538A (zh) 2001-06-27 2004-01-28 前体生物药物股份有限公司 用于竞争性调节二肽基肽酶iv催化的肽结构
WO2003002596A2 (en) 2001-06-27 2003-01-09 Probiodrug Ag Use of dipeptidyl peptidase iv inhibitors as therapeutics for neurological disorders
DE60225556D1 (de) 2001-07-03 2008-04-24 Novo Nordisk As Dpp-iv-inhibierende purin-derivative zur behandlung von diabetes
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
SK287726B6 (en) 2001-07-24 2011-07-06 Richter Gedeon Vegyeszet Carboxylic acid amide derivatives, their preparation, pharmaceutical compositions containing them and process for preparing pharmaceutical compositions
US20040234990A1 (en) 2001-07-31 2004-11-25 Hiroto Komano Method of screening alzheimer's disease-associated gene
JP4729717B2 (ja) 2001-08-03 2011-07-20 株式会社医学生物学研究所 GM1ガングリオシド結合型アミロイドβタンパク質を認識する抗体、及び該抗体をコードするDNA
TWI242555B (en) 2001-08-03 2005-11-01 Schering Corp Novel gamma secretase inhibitors
EP1411944A1 (en) 2001-08-03 2004-04-28 Schering Corporation Sulfonamide derivatives as gamma secretase inhibitors
EP1519740A4 (en) 2001-08-17 2005-11-09 Lilly Co Eli FASTER IMPROVEMENT OF COGNITION IN DISEASES ASSOCIATED WITH A-BETA
US20040192898A1 (en) 2001-08-17 2004-09-30 Jia Audrey Yunhua Anti-abeta antibodies
JP2005502680A (ja) 2001-08-30 2005-01-27 オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド 抗痙攣剤およびアセチルコリンエステラーゼ阻害剤による痴呆および記憶障害の処置
KR20040033048A (ko) 2001-09-14 2004-04-17 미츠비시 웰파마 가부시키가이샤 티아졸리딘 유도체 및 이의 약학적 용도
JP2005509603A (ja) 2001-09-19 2005-04-14 ノボ ノルディスク アクティーゼルスカブ Dpp−iv酵素の阻害剤であるヘテロ環化合物
GB0125445D0 (en) 2001-10-23 2001-12-12 Ferring Bv Protease Inhibitors
GB0125446D0 (en) 2001-10-23 2001-12-12 Ferring Bv Novel anti-diabetic agents
AU2002359301B2 (en) 2001-10-23 2008-07-03 Comentis, Inc. Beta-secretase inhibitors and methods of use
US6861440B2 (en) 2001-10-26 2005-03-01 Hoffmann-La Roche Inc. DPP IV inhibitors
EP1448601A4 (en) 2001-11-02 2006-04-26 Diagenics Internat Corp METHOD AND COMPOSITIONS OF MONOCLONAL ANTIBODIES SPECIFIC TO BETA-AMYLOIDE PROTEINS
US7304040B2 (en) 2001-11-02 2007-12-04 Kensuke Egashira Suppression of post-transplant arteriosclerosis
WO2003040183A2 (en) 2001-11-09 2003-05-15 The Genetics Company, Inc Compounds for the diagnosis/prevention/treatment of alzheimer's disease
GEP20074045B (en) 2001-11-19 2007-02-26 Elan Pharm Inc (4-phenyl) piperidin-3-yl-phenylcarboxylate derivatives and related compounds as beta-secretase inhibitors for the treatment of alzheimer's disease
EP1572894B1 (en) 2001-11-21 2016-04-13 New York University Synthetic immunogenic but non-deposit-forming polypeptides and peptides homologous to amyloid beta, prion protein, amylin, alpha synuclein, or polyglutamine repeats for induction of an immune response thereto
EP1469873A4 (en) 2001-11-26 2007-10-03 Tufts College PEPTIDOMIMETIC INHIBITORS FROM BEHIND PROLIN SPLENDING ENZYMES
WO2003048204A1 (en) 2001-12-06 2003-06-12 Takeda Chemical Industries, Ltd. Alzheimer’s disease-associated gene and protein and use thereof
US20050227941A1 (en) 2001-12-17 2005-10-13 Karen Duff Sequestration of ass in the periphery in the absence of immunomodulating agent as a therapeutic approach for the treatment or prevention of beta-amyloid related diseases
BR0215240A (pt) 2001-12-19 2004-10-26 Atherogenics Inc Derivados de calcona e seu uso no tratamento de doenças
US20060210555A1 (en) 2001-12-21 2006-09-21 Antigenics, Inc. Compositions comprising immunoreactive reagents and saponins, and methods of use thereof
AU2002360732A1 (en) 2001-12-26 2003-07-24 Guilford Pharmaceuticals Change inhibitors of dipeptidyl peptidase iv
US6727261B2 (en) 2001-12-27 2004-04-27 Hoffman-La Roche Inc. Pyrido[2,1-A]Isoquinoline derivatives
WO2003057204A2 (en) 2002-01-08 2003-07-17 Nordic Bioscience A/S Modulation of iamt (pimt or pcmt) in immune system
WO2003059346A1 (en) 2002-01-18 2003-07-24 The Genetics Company Inc. Beta-secretase inhibitors
WO2003063760A2 (en) 2002-01-31 2003-08-07 Tel Aviv University Future Technology Development L.P. Peptides antibodies directed thereagainst and methods using same for diagnosing and treating amyloid-associated diseases
US20040171614A1 (en) 2002-02-06 2004-09-02 Schering-Plough Corporation Novel gamma secretase inhibitors
TW200302717A (en) 2002-02-06 2003-08-16 Schering Corp Novel gamma secretase inhibitors
PL371678A1 (pl) 2002-02-13 2005-06-27 F.Hoffmann-La Roche Ag Nowe pochodne pirydyny i pirymidyny
BR0307576A (pt) 2002-02-13 2005-01-11 Hoffmann La Roche Compostos; processo para a fabricação de compostos; composições farmacêuticas; método para o tratamento e/ou profilaxia de doenças associadas com o dpp iv; e uso de compostos
AR038568A1 (es) 2002-02-20 2005-01-19 Hoffmann La Roche Anticuerpos anti-a beta y su uso
HUP0200849A2 (hu) 2002-03-06 2004-08-30 Sanofi-Synthelabo N-aminoacetil-2-ciano-pirrolidin-származékok, e vegyületeket tartalmazó gyógyszerkészítmények és eljárás előállításukra
MY139983A (en) 2002-03-12 2009-11-30 Janssen Alzheimer Immunotherap Humanized antibodies that recognize beta amyloid peptide
JP2005526811A (ja) 2002-03-25 2005-09-08 メルク エンド カムパニー インコーポレーテッド 糖尿病の治療または予防用β−アミノ複素環式ジペプチジルペプチダーゼ阻害剤
ES2297141T3 (es) 2002-03-29 2008-05-01 EISAI R&D MANAGEMENT CO., LTD. Derivados de (1-indanona)-(1,2,3,6-tetrahidropiridina).
AU2003226356A1 (en) 2002-04-12 2003-10-27 Ramot At Tel Aviv University Ltd. Prevention of brain inflammation as a result of induced autoimmune response
AU2003218560B2 (en) 2002-04-19 2009-09-03 The Governing Council Of The University Of Toronto Immunological methods and compositions for the treatment of alzheimer's disease
WO2003091278A1 (fr) 2002-04-24 2003-11-06 Hiroshi Mori Inhibiteurs de gamma secretase
CA2484217A1 (en) 2002-04-26 2003-11-06 Schering Corporation Muscarinic antagonists
AU2003230392A1 (en) 2002-05-17 2003-12-12 Merck And Co., Inc. Beta-secretase inhibitors
ATE414519T1 (de) 2002-05-31 2008-12-15 Lundbeck & Co As H Kombination aus einem nmda-antagonist und acetylcholinesterase-hemmern zur behandlung der alzheimer-krankheit
EP1513808A2 (en) 2002-06-04 2005-03-16 Pfizer Products Inc. Fluorinated cyclic amides as dipeptidyl peptidase iv inhibitors
WO2003101449A2 (en) 2002-06-04 2003-12-11 Pfizer Products Inc. Process for the preparation of 3,3,4,4-tetrafluoropyrrolidine and derivatives thereof
JP3675813B2 (ja) 2002-06-06 2005-07-27 エーザイ株式会社 新規縮合イミダゾール誘導体
US20050171300A1 (en) 2002-06-19 2005-08-04 Luc Moens Semi-gloss powder coating compositions
JPWO2004007446A1 (ja) 2002-07-10 2005-11-10 アステラス製薬株式会社 新規なアゼチジン誘導体又はその塩
US7208498B2 (en) 2002-07-15 2007-04-24 Merck & Co., Inc. Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes
AU2003251993A1 (en) 2002-07-19 2004-02-09 Inge Grundke-Iqbal NMDA RECEPTOR ANTAGONISTS AND THEIR USE IN INHIBITING ABNORMAL HYPERPHOSPHORYLATION OF MICROTUBULE ASSOCIATED PROTEIN tau
US7557137B2 (en) 2002-08-05 2009-07-07 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
JP4233524B2 (ja) 2002-08-21 2009-03-04 ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト 8−[3−アミノ−ピペリジン−1−イル]−キサンチン、その製造およびその薬理組成物としての使用
DE10238470A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Xanthinderivate, deren Herstellung und deren Verwendung als Arzneimittel
DE10238477A1 (de) 2002-08-22 2004-03-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Purinderivate, deren Herstellung und deren Verwendung als Arzneimittel
WO2006039807A1 (en) 2004-10-15 2006-04-20 Biopharmacopae Design International Inc. Methods and therapeutic compositions comprising plant extracts for the treatment of cancer
ES2201929B1 (es) 2002-09-12 2005-05-16 Araclon Biotech, S.L. Anticuerpos policlonales, metodo de preparacion y uso de los mismos.
CA2498407A1 (en) 2002-09-12 2004-03-25 The Regents Of The University Of California Immunogens and corresponding antibodies specific for high molecular weight aggregation intermediates common to amyloids formed from proteins of differing sequence
WO2010011999A2 (en) 2008-07-25 2010-01-28 The Regents Of The University Of California Methods and compositions for eliciting an amyloid-selective immune response
WO2010012004A2 (en) 2008-07-25 2010-01-28 The Regents Of The University Of California Monoclonal antibodies specific for pathological amyoid aggregates common to amyloids formed from proteins of differing sequence
JP4426449B2 (ja) 2002-09-12 2010-03-03 財団法人化学及血清療法研究所 ヒト抗ヒトmcp−1抗体及び該抗体フラグメント
NZ538567A (en) 2002-09-19 2007-04-27 Abbott Lab Pyrrolidine-2-carbonitrile derivatives and their pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
WO2004026851A1 (en) 2002-09-20 2004-04-01 Axys Pharmaceuticals, Inc. 3-(3,5-disubstituted-4-hydroxyphenyl)propionamide derivatives as cathepsin b inhibitors
US7273889B2 (en) 2002-09-25 2007-09-25 Innovative Drug Delivery Systems, Inc. NMDA receptor antagonist formulation with reduced neurotoxicity
WO2004029629A1 (en) 2002-09-27 2004-04-08 Janssen Pharmaceutica N.V. N-11 truncated amyloid-beta nomoclonal antibodies, compositions, methods and uses
CA2501091A1 (en) 2002-10-01 2004-04-15 Northwestern University Amyloid beta-derived diffusible ligands (addls), addl-surrogates, addl-binding molecules, and uses thereof
GB0223039D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
GB0223038D0 (en) 2002-10-04 2002-11-13 Merck Sharp & Dohme Therapeutic compounds
AU2003275404A1 (en) 2002-10-07 2004-05-04 Merck & Co., Inc. Antidiabetic beta-amino heterocyclic dipeptidyl peptidase inhibitors
WO2004033455A2 (en) 2002-10-08 2004-04-22 Novo Nordisk A/S Hemisuccinate salts of heterocyclic dpp-iv inhibitors
GB0223494D0 (en) 2002-10-09 2002-11-13 Neuropharma Sa Dual binding site acetylcholinesterase inhibitors for the treatment of alzheimer's disease
PL377769A1 (pl) 2002-10-09 2006-02-20 Rinat Neuroscience Corp. Sposób leczenia choroby Alzheimera z zastosowaniem przeciwciał skierowanych przeciw peptydowi beta amyloidu i ich kompozycje
KR20050067418A (ko) 2002-10-18 2005-07-01 머크 앤드 캄파니 인코포레이티드 당뇨병을 치료 또는 예방하기 위한 베타-아미노헤테로사이클릭 디펩티딜 펩티다제 억제제
EP2260839A3 (en) 2002-10-24 2012-05-02 Merz Pharma GmbH & Co. KGaA Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase inhibitors
US20040082543A1 (en) 2002-10-29 2004-04-29 Pharmacia Corporation Compositions of cyclooxygenase-2 selective inhibitors and NMDA receptor antagonists for the treatment or prevention of neuropathic pain
AU2003286776A1 (en) 2002-10-30 2004-06-07 Guilford Pharmaceuticals Inc. Novel inhibitors of dipeptidyl peptidase iv
WO2004039773A2 (en) 2002-10-30 2004-05-13 Nordic Bioscience A/S Coumpounds modulating the activity of gapdh and/or iamt
US7452911B2 (en) 2002-10-31 2008-11-18 Boehringer Ingelheim Pharma Gmbh & Co. Kg Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds
GB0225474D0 (en) 2002-11-01 2002-12-11 Merck Sharp & Dohme Therapeutic agents
FR2846667B1 (fr) 2002-11-06 2004-12-31 Pasteur Institut Fragments variables d'anticorps de camelides a chaine unique diriges contre le peptide beta-amyloide 1-42 et leurs applications pour le diagnostic et le traitement des maladies neuroagregatives
RU2005117383A (ru) 2002-11-07 2006-01-20 Мерк энд Ко., Инк. (US) Производные фенилаланина в качестве ингибиторов дипептидилпептидазы для лечения или профилактики диабета
US7109217B2 (en) 2002-11-12 2006-09-19 Merck & Co., Inc. Phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
AU2002952946A0 (en) 2002-11-27 2002-12-12 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
JP2006510630A (ja) 2002-12-04 2006-03-30 メルク エンド カムパニー インコーポレーテッド 糖尿病を治療又は予防するためのジペプチジルペプチダーゼ阻害剤としてのフェニルアラニン誘導体
US7420079B2 (en) 2002-12-09 2008-09-02 Bristol-Myers Squibb Company Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
US20040181075A1 (en) 2002-12-19 2004-09-16 Weingarten M. David Process of making chalcone derivatives
AU2003297219A1 (en) 2002-12-20 2004-07-22 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CA2512111A1 (en) 2003-01-07 2004-07-29 Merck And Co., Inc. Macrocyclic beta-secretase inhibitors for treatment of alzheimer's disease
WO2004064778A2 (en) 2003-01-17 2004-08-05 Merck & Co. Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JP2006516573A (ja) 2003-01-31 2006-07-06 メルク エンド カムパニー インコーポレーテッド 糖尿病の治療および予防のためのジペプチジルペプチダーゼ阻害薬としての3−アミノ−4−フェニルブタン酸誘導体
DE10303974A1 (de) 2003-01-31 2004-08-05 Abbott Gmbh & Co. Kg Amyloid-β(1-42)-Oligomere, Verfahren zu deren Herstellung und deren Verwendung
KR20050118669A (ko) 2003-02-01 2005-12-19 뉴랄랩 리미티드 가용성 a-베타에 대한 항체를 생성하기 위한 능동 면역화
KR100810810B1 (ko) 2003-02-04 2008-03-06 에프. 호프만-라 로슈 아게 감마-세크레타제 억제제로서 말론아마이드 유도체
ATE468886T1 (de) 2003-02-10 2010-06-15 Applied Molecular Evolution Abeta-bindende moleküle
WO2004071454A2 (en) 2003-02-13 2004-08-26 Guilford Pharmaceuticals Inc. Substituted azetidine compounds as inhibitors of dipeptidyl peptidase iv
CA2516259A1 (en) 2003-02-18 2004-09-02 Roskamp Research, Llc Anti-angiogenic and anti-tumoral properties of beta and gamma secretase inhibitors
US8663650B2 (en) 2003-02-21 2014-03-04 Ac Immune Sa Methods and compositions comprising supramolecular constructs
AU2003207881A1 (en) 2003-02-28 2004-09-17 Aic Dipeptidyl peptidase inhibitors
WO2004076434A1 (en) 2003-02-28 2004-09-10 Aic Dipeptidyl peptidase inhibitors
EP1454627A1 (en) 2003-03-06 2004-09-08 MyoContract Ltd. Alpha-Keto carbonyl calpain inhibitors
WO2004084830A2 (en) 2003-03-21 2004-10-07 Buck Institute Method for treating alzheimer’s dementia
US20040191334A1 (en) 2003-03-24 2004-09-30 Pang-Chui Shaw Use of transhinone derivates as cholinesterase inhibitors in treating related diseases
EP1608317B1 (en) 2003-03-25 2012-09-26 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
KR20060054174A (ko) 2003-03-28 2006-05-22 센토코 인코포레이티드 항-아밀로이드 항체, 조성물, 방법 및 용도
EP1613321A2 (en) 2003-03-28 2006-01-11 Acadia Pharmaceuticals Inc. Muscarinic m1 receptor agonists for pain management
BRPI0409255A (pt) 2003-04-09 2006-03-28 Wyeth Corp derivados de ácido 2-(8,9-dioxo-2,6-diazabi-ciclo(5.2.0)non-1(7)-en-2-il)alquil fosfÈnico e seu uso como antagonistas de receptores de d-asparto de -n-metila (nmda)
GB0308382D0 (en) 2003-04-10 2003-05-21 Univ Cambridge Tech Therapeutic methods and means
GB0308318D0 (en) 2003-04-10 2003-05-14 Merck Sharp & Dohme Therapeutic agents
WO2004089362A1 (en) 2003-04-11 2004-10-21 Novo Nordisk A/S 2-cyanopyrroles and their analogues as ddp-iv inhibitors
WO2004098625A2 (en) 2003-05-05 2004-11-18 Probiodrug Ag Medical use of inhibitors of glutaminyl and glutamate cyclases
WO2004098591A2 (en) 2003-05-05 2004-11-18 Probiodrug Ag Inhibitors of glutaminyl cyclase and their use in the treatment of neurological diseases
WO2004099134A2 (en) 2003-05-05 2004-11-18 Prosidion Ltd. Glutaminyl based dp iv-inhibitors
ES2246177B1 (es) 2003-05-08 2007-03-01 Universidad De Zaragoza. Uso de anticuerpos para el tratamiento de enfermedades amiloideas.
AU2003902260A0 (en) 2003-05-09 2003-05-29 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
DE602004015110D1 (de) 2003-05-13 2008-08-28 Schering Corp Verbrückte n-arylsulfonylpiperidine als gamma-sekretaseinhibitoren
EP1625122A1 (en) 2003-05-14 2006-02-15 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7560455B2 (en) 2003-05-14 2009-07-14 Merck & Co., Inc. 3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
WO2004101538A1 (en) 2003-05-16 2004-11-25 Merck Sharp & Dohme Limited Cyclohexyl sulphones as gamma-secretase inhibitors
AU2004251636B2 (en) 2003-05-27 2006-11-09 Merz Pharma Gmbh & Co. Kgaa Combination of an NMDA receptor antagonist and a selective serotonin reuptake inhibitor for the treatment of depression and other mood disorders
TWI374893B (en) 2003-05-30 2012-10-21 Janssen Alzheimer Immunotherap Humanized antibodies that recognize beta amyloid peptide
AU2003902828A0 (en) 2003-06-05 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
CN1798556A (zh) 2003-06-06 2006-07-05 麦克公司 作为治疗或者预防糖尿病的二肽基肽酶抑制剂的稠合吲哚
AU2003902946A0 (en) 2003-06-12 2003-06-26 Fujisawa Pharmaceutical Co., Ltd. Dpp-iv inhibitor
EP1638950A4 (en) 2003-06-17 2010-06-30 Merck Sharp & Dohme CYCLOHEXYLGLYCIN DERIVATIVES AS DIPEPTIDYLPEPTIDASEINHIBITORS FOR THE TREATMENT OF BZW. PREVENTION OF DIABETES
DE602004030244D1 (de) 2003-06-20 2011-01-05 Hoffmann La Roche Itoren
ES2327740T3 (es) 2003-06-20 2009-11-03 F. Hoffmann-La Roche Ag Hexahidropiridoisoquinolinas como inhibidoras de la dpp-iv.
JP5137400B2 (ja) 2003-06-30 2013-02-06 テル アヴィヴ ユニヴァーシティ フューチャー テクノロジー ディヴェロップメント エル.ピー. アミロイド関連疾患を診断および処置するためのペプチド、それに対する抗体、ならびにその使用方法
US7291620B2 (en) 2003-06-30 2007-11-06 Merck + Co., Inc. N-alkyl phenylcarboxamide beta-secretase inhibitors for the treatment of Alzheimer's disease
CN1909897A (zh) 2003-07-01 2007-02-07 默克公司 用于治疗阿尔茨海默病的苯基羧化物β-分泌酶抑制剂
WO2005007614A1 (en) 2003-07-03 2005-01-27 The Government Of The United States Of America As Represented By The Secretary, Department Of Health And Human Services 6011 Monoamine oxidase inhibitors
JP2007528862A (ja) 2003-07-16 2007-10-18 アールブイエックス セラピューティクス, インコーポレイテッド TGF−βの効果を下方制御するための化合物および方法
WO2005008250A1 (en) 2003-07-21 2005-01-27 Angiogenetics Sweden Ab Compounds and methods for promoting angiogenesis by using a gamma-secretase inhibitor or inhibiting the gamma-secretase pathway
WO2005014041A2 (en) 2003-07-24 2005-02-17 Novartis Ag Use of an amyloid beta dna vaccine for the treatment and/or prevention of amyloid diseases
CA2529674A1 (en) 2003-07-28 2005-02-03 Merz Pharma Gmbh & Co. Kgaa The use of 1-amino-alkylcyclohexane compounds in the treatment of pain hypersensitivity
DE602004018503D1 (de) 2003-07-31 2009-01-29 Merck & Co Inc Hexahydrodiazepinone als inhibitoren des dipeptidylpeptidase-iv zur behandlung bzw. prävention von diabetes
US20050124016A1 (en) 2003-08-01 2005-06-09 Enh Research Institute Antibodies specific for toxic amyloid beta protein oligomers
GB0318447D0 (en) 2003-08-05 2003-09-10 Merck Sharp & Dohme Therapeutic agents
US7790736B2 (en) 2003-08-13 2010-09-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005018545A2 (en) 2003-08-14 2005-03-03 Merck & Co., Inc. Macrocyclic beta-secretase inhibitors for the treatment of alzheimer's disease
WO2005018424A2 (en) 2003-08-18 2005-03-03 Research Foundation For Mental Hygiene, Inc. Antibodies specific for fibrillar amyloid and a procedure to detect fibrillar amyloid deposits
WO2005023762A1 (en) 2003-09-04 2005-03-17 Abbott Laboratories Pyrrolidine-2-carbonitrile derivatives and their use as inhibitors of dipeptidyl peptidase-iv (dpp-iv)
AU2003298171A1 (en) 2003-09-05 2005-03-29 Cellzome Ag Protein complexes associated with app-processing
WO2005026148A1 (en) 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2005030751A2 (en) 2003-09-08 2005-04-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
WO2005025554A2 (en) 2003-09-09 2005-03-24 Japan Tobacco Inc. Dipeptidyl peptidase iv inhibitor
EP1666061A1 (en) 2003-09-09 2006-06-07 Takeda Pharmaceutical Company Limited Use of antibody
JP2007527865A (ja) 2003-09-12 2007-10-04 ザ・レジェンツ・オブ・ザ・ユニバーシティ・オブ・カリフォルニア 種々の配列を有するタンパク質から形成されたアミロイドに共通の高分子量凝集中間体に特異的なモノクローナル抗体
GB0322140D0 (en) 2003-09-22 2003-10-22 Pfizer Ltd Combinations
US7514459B2 (en) 2003-09-24 2009-04-07 Merck Sharp & Dohme Ltd. Gamma-secretase inhibitors
US7829597B2 (en) 2003-10-03 2010-11-09 Merck, Sharp & Dohme, Inc. Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease
JP2007516154A (ja) 2003-10-06 2007-06-21 トレント・ファーマシューティカルズ・リミテッド アゾリジンカーボニトリル類及びそれらのdpp−iv阻害剤としての用途
CN1894217B (zh) 2003-10-06 2011-09-21 弗·哈夫曼-拉罗切有限公司 用作γ-分泌酶抑制剂的取代的二苯并氮杂*和苯并二氮杂*
CA2541831A1 (en) 2003-10-08 2005-04-21 Pfizer Inc. 1-'2-(4-hydroxyphenyl)-2-hydroxyethyl!-piperidin-4-ol compounds as nmda receptor antagonists
AU2004283461B2 (en) 2003-10-15 2010-02-11 Probiodrug Ag Use of effectors of glutaminyl and glutamate cyclases
GB0324236D0 (en) 2003-10-16 2003-11-19 Astrazeneca Ab Chemical compounds
NZ547152A (en) 2003-10-16 2009-12-24 Neurosearch As Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an acetylcholinesterase inhibitor
TW200519105A (en) 2003-10-20 2005-06-16 Lg Life Science Ltd Novel inhibitors of DPP-IV, methods of preparing the same, and pharmaceutical compositions containing the same as an active agent
US20050113458A1 (en) 2003-10-22 2005-05-26 Forest Laboratories, Inc. Use of 1-aminocyclohexane derivatives to modify deposition of fibrillogenic a-beta peptides in amyloidopathies
EP1824846A2 (en) 2003-11-03 2007-08-29 Probiodrug AG Novel compounds for the treatment of neurological disorders
US7238683B2 (en) 2003-11-04 2007-07-03 Merck & Co., Inc. Fused phenylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
PL1685142T3 (pl) 2003-11-11 2008-06-30 Hoffmann La Roche Pochodne kwasu fosfinowego, inhibitory beta-sekterazy do leczenia choroby Alzheimera
NZ547752A (en) 2003-11-12 2009-12-24 Phenomix Corp Heterocyclic boronic acid compounds for inhibiting dipeptidyl peptidase-IV
EP1689713B1 (en) 2003-11-24 2011-07-27 Merck Sharp & Dohme Corp. Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer s disease
DE10355304A1 (de) 2003-11-27 2005-06-23 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 8-(Piperazin-1-yl)-und 8-([1,4]Diazepan-1-yl)-xanthine, deren Herstellung und deren Verwendung als Arzneimittel
UY28650A1 (es) 2003-12-05 2005-02-28 Forest Laboratories Memantina para la prevencion o disminucion de la conducta suicida y para el tratamiento de la depresion mayor asociada con esta conducta
EP1541143A1 (en) 2003-12-09 2005-06-15 Graffinity Pharmaceuticals Aktiengesellschaft Dpp-iv inhibitors
EP1541148A1 (en) 2003-12-09 2005-06-15 Graffinity Pharmaceuticals Aktiengesellschaft Dpp-iv inhibitors
WO2005058849A1 (en) 2003-12-15 2005-06-30 Glenmark Pharmaceuticals Ltd. New dipeptidyl peptidase in inhibitors; process for their preparation and compositions containing them
US7550481B2 (en) 2003-12-19 2009-06-23 Merck & Co., Inc. Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
WO2005070429A1 (en) 2004-01-22 2005-08-04 Neurosearch A/S Pharmaceutical composition comprising a monoamine neurotransmitter re-uptake inhibitor and an n-methyl-d-aspartate (nmda) receptors antagonist
EP1715843A1 (en) 2004-01-29 2006-11-02 Neuromolecular Inc. Combination of a nmda receptor antagonist and a mao-inhibitor or a gadph-inhibitor for the treatment of central nervous system-related conditions
WO2005075426A1 (en) 2004-02-03 2005-08-18 Glenmark Pharmaceuticals Ltd. Novel dipeptidyl peptidase iv inhibitors; processes for their preparation and compositions thereof
EP1713780B1 (en) * 2004-02-05 2012-01-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
AU2005215775B2 (en) 2004-02-13 2011-02-03 Neuromolecular, Inc. Combination of a NMDA receptor antagonist and an anti-depressive drug MAO-inhibitor or a GADPH-inhibitor for the treatment of psychiatric conditions
US20050182044A1 (en) 2004-02-17 2005-08-18 Bruinsma Gosse B. Combinatorial therapy with an acetylcholinesterase inhibitor and (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3,-b]indol-5-yl phenylcarbamate
EP2119717B1 (de) 2004-02-18 2018-01-17 Boehringer Ingelheim International GmbH 8-[3-amino-piperidin-1-yl]-Xanthine, deren Herstellung und deren Verwendung als DPP IV Hemmer
WO2005080435A1 (ja) 2004-02-20 2005-09-01 Immuno-Biological Laboratories Co., Ltd. モノクローナル抗体およびその利用
MXPA06009589A (es) 2004-02-23 2007-03-26 Tufts College Inhibidores de dipeptidil peptidasa iv par regular el metabolismo de glucosa.
EP1593671A1 (en) 2004-03-05 2005-11-09 Graffinity Pharmaceuticals AG DPP-IV inhibitors
EP1729774A4 (en) 2004-03-09 2009-05-06 Nat Health Research Institutes PYRROLIDINE CONNECTIONS
EA013427B1 (ru) 2004-03-15 2010-04-30 Такеда Фармасьютикал Компани Лимитед Ингибиторы дипептидилпептидазы
US20070213388A1 (en) 2004-03-19 2007-09-13 Bruinsma Gosse B Acetylcholinesterase Inhibitors and N-Methyl-D-Aspartate Antagonists Useful in the Treatment of of Cognitive Disorders
WO2005095339A1 (en) 2004-03-31 2005-10-13 Pfizer Products Inc. Dicyanopyrrolidines as dipeptidyl peptidase iv inhibitors
WO2005097103A2 (en) 2004-04-01 2005-10-20 Axys Pharmaceuticals, Inc. Diabetes and metabolic syndrome therapy utilizing cathepsin b inhibitors
CN1950358A (zh) 2004-04-05 2007-04-18 先灵公司 新颖的γ分泌酶抑制剂
US7968571B2 (en) 2004-04-20 2011-06-28 Merck, Sharp & Dohme, Corp. 2,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's Disease
JP2007533743A (ja) 2004-04-20 2007-11-22 メルク エンド カムパニー インコーポレーテッド アルツハイマー病治療のためのβ−セクレターゼ阻害薬として有用な1,3,5−置換フェニル誘導体化合物
WO2005102390A2 (en) 2004-04-22 2005-11-03 Pfizer Japan, Inc. Combinations comprising alpha-2-delta ligands and nmda receptor antagonists
US9549895B2 (en) 2004-04-23 2017-01-24 Massachusetts Eye And Ear Infirmary Methods and compositions for preserving the viability of photoreceptor cells
JPWO2005105998A1 (ja) 2004-04-27 2008-07-31 財団法人化学及血清療法研究所 ヒト抗アミロイドβペプチド抗体およびその抗体フラグメント
AU2005241056A1 (en) 2004-05-04 2005-11-17 Merck & Co., Inc. 1,2,4-oxadiazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
BRPI0510284A (pt) 2004-05-12 2007-10-30 Pfizer Prod Inc derivados de prolina e seu uso como inibidores da dipeptidil peptidase iv
JP2007537257A (ja) 2004-05-13 2007-12-20 メルク エンド カムパニー インコーポレーテッド アルツハイマー病の治療用ベータセクレターゼ阻害剤として有用なフェニルカルボキサミド化合物
CA2564884A1 (en) 2004-05-18 2005-12-08 Merck & Co., Inc. Cyclohexylalanine derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
EP1598341A1 (en) 2004-05-21 2005-11-23 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
US7687638B2 (en) 2004-06-04 2010-03-30 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
DE602005022871D1 (de) 2004-06-07 2010-09-23 Univ Ramot Verfahren zur passiven immunisierung gegen eine durch amyloidaggregation gekennzeichnete krankheit oder erkrankung mit vermindertem nervenentzündungsrisiko
EP1604980A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1604989A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft DPP-IV inhibitors
EP1604662A1 (en) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft 1-[(3R)-Amino-4-(2-fluoro-phenyl)-butyl]-pyrrolidine-(2R)-carboxylic acid benzyl amine derivatives and related compounds as dipeptidyl peptidase IV (DPP-IV) inhibitors for the treatment of type 2 diabetes mellitus
AU2005257904A1 (en) 2004-06-15 2006-01-05 Merck Sharp & Dohme Corp. Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
GB0413389D0 (en) 2004-06-16 2004-07-21 Astrazeneca Ab Chemical compounds
AU2005265148B2 (en) 2004-06-21 2011-01-20 Merck Sharp & Dohme Corp. Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
SE0401601D0 (sv) 2004-06-21 2004-06-21 Bioarctic Neuroscience Ab Protofibril specific antibodies and uses thereof
US7371825B2 (en) 2004-06-30 2008-05-13 Centocor, Inc. Anti-MCP-1 antibodies, compositions, methods and uses
CA2570183A1 (en) 2004-06-30 2006-01-12 Schering Corporation Substituted n-arylsulfonylheterocyclic amines as gamma-secretase inhibitors
CA2572602A1 (en) 2004-07-02 2006-02-09 Northwestern University Monolocal antibodies that target pathological assemblies of amyloid .beta. (abeta)
US7786163B2 (en) 2004-07-12 2010-08-31 Forest Laboratories Holdings Limited (BM) Constrained cyano compounds
WO2006019965A2 (en) 2004-07-16 2006-02-23 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
WO2006014638A2 (en) 2004-07-19 2006-02-09 The General Hospital Corporation ANTIBODIES TO CROSS-LINKED AMYLOID β OLIGOMERS
US20080038192A1 (en) 2004-07-19 2008-02-14 Neurochem Inc. Diagnostic Methods Of Multiple Organ Amyloidosis
CA2574218A1 (en) 2004-07-22 2006-02-09 Schering Corporation Substituted amide beta secretase inhibitors
WO2006014944A1 (en) 2004-07-28 2006-02-09 Schering Corporation Macrocyclic beta-secretase inhibitors
HUP0401523A3 (en) 2004-07-29 2007-05-02 Richter Gedeon Vegyeszet Indole-2-carboxamide derivatives, pharmaceutical compositions containing them and process for producing them
CA2575663C (en) 2004-07-30 2013-04-23 Rinat Neuroscience Corp. Antibodies directed against amyloid-beta peptide and methods using same
EP1623983A1 (en) 2004-08-05 2006-02-08 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Heterocyclic compounds useful as DPP-IV inhibitors
WO2006016644A1 (ja) 2004-08-11 2006-02-16 Mitsubishi Chemical Corporation 抗体及びその利用
US7625888B2 (en) 2004-08-23 2009-12-01 Merck & Co., Inc. Fused triazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
CA2577987A1 (en) 2004-08-25 2006-03-02 Santhera Pharmaceuticals (Schweiz) Ag Alpha-keto carbonyl calpain inhibitors
AU2005276635A1 (en) 2004-08-25 2006-03-02 Santhera Pharmaceuticals (Schweiz) Ag Alpha-keto carbonyl calpain inhibitors
US7388007B2 (en) 2004-08-26 2008-06-17 Bristol-Myers Squibb Company Gamma-lactams as beta-secretase inhibitors
TWI374935B (en) 2004-08-27 2012-10-21 Pfizer Ireland Pharmaceuticals Production of α-abeta
EP1791818A1 (en) 2004-09-14 2007-06-06 The Genetics Company, Inc. Hydrazone derivatives and their use as beta secretase inhibitors
AU2005286844A1 (en) 2004-09-17 2006-03-30 Comentis, Inc Bicyclic compounds which inhibit beta-secretase activity and methods of use thereof
WO2006034296A2 (en) 2004-09-17 2006-03-30 Comentis, Inc. Amino-containing compounds which inhibit memapsin 2 beta-secretase activity and methods of use thereof
WO2006058064A2 (en) 2004-11-29 2006-06-01 Merck & Co., Inc. Fused aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2006039470A2 (en) 2004-09-29 2006-04-13 Centocor, Inc. Anti- amyloid antibodies, compositions, methods and uses
WO2006039325A2 (en) 2004-10-01 2006-04-13 Merck & Co., Inc. Aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2006042103A2 (en) 2004-10-05 2006-04-20 Axys Pharmaceuticals, Inc. Reversible inhibitors of cathepsin b
BRPI0516446A (pt) 2004-10-08 2008-09-02 Novartis Ag combinação de compostos orgánicos
US9186345B2 (en) 2004-10-12 2015-11-17 Hakon Hakonarson Method of treating skin diseases
WO2006044497A2 (en) 2004-10-13 2006-04-27 Merck & Co., Inc. Spiropiperidine compounds useful as beta-secretase inhibitors for the treatment of alzhermer’s disease
BRPI0516962A (pt) 2004-10-25 2008-09-30 Univ Northwestern anticorpo isolado, ou fragmento do mesmo, composição farmacêutica, métodos para prevenir a ligação de ligantes difundìveis derivados de abeta a um neurÈnio, para inibir a constituição de ligantes difundìveis, para bloquear a fosforilação de proteìna, para tratar profilaticamente ou terapeuticamente uma doença, para identificar um agente terapêutico, para detectar ligantes difundìveis, e para diagnosticar uma doença, e, kit para detectar ligantes difundìveis
WO2006047248A1 (en) 2004-10-25 2006-05-04 Novartis Ag Combination of dpp-iv inhibitor, ppar antidiabetic and metformin
WO2006046644A1 (ja) 2004-10-28 2006-05-04 Sanko Junyaku Co., Ltd. アルツハイマー病の検定方法及び診断試薬
US7932275B2 (en) 2004-10-29 2011-04-26 Merck, Sharp & Dohme Corp. 2-aminopyridine compounds useful as β-secretase inhibitors for the treatment of alzheimer's disease
CA2587083A1 (en) 2004-11-17 2006-05-26 Merck & Co., Inc. Macrocyclic tertiary amine beta-secretase inhibitors for the treatment of alzheimer's disease
RU2404750C2 (ru) 2004-11-23 2010-11-27 Адамас Фармасьютикалс, Инк. Композиция, содержащая основу или покрытие для замедленного высвобождения и антагонист nmda рецептора, способ введения такого nmda антагониста субъекту
CA2587360A1 (en) 2004-11-23 2006-06-01 Merck & Co., Inc. 2,3,4,6-substituted pyridyl derivative compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease
WO2006057983A1 (en) 2004-11-23 2006-06-01 Merck & Co., Inc. Macrocyclic aminopyridyl beta-secretase inhibitors for the treatment of alzheimer's disease
EP2623099A1 (en) 2004-11-24 2013-08-07 Neuromolecular Pharmaceuticals, Inc Composition and method for treating neurological disease
MX2007006239A (es) 2004-11-30 2007-07-20 Hoffmann La Roche Benzoquinolisinas sustituidas como inhibidores de dipeptidil peptidasa iv (dpp-iv) para tratamiento de diabetes.
EP1827478A4 (en) 2004-12-03 2009-08-05 Mucosal Therapeutics Llc METHODS OF TREATING JOINED OR SICK JOINTS
TW200636066A (en) 2004-12-15 2006-10-16 Elan Pharm Inc Humanized antibodies that recognize beta amyloid peptide
PE20061401A1 (es) 2004-12-15 2006-12-23 Neuralab Ltd ANTICUERPOS Aß PARA MEJORAR LA COGNICION
AR052051A1 (es) 2004-12-15 2007-02-28 Neuralab Ltd Anticuerpos ab humanizados usados en mejorar la cognicion
WO2006066233A1 (en) 2004-12-15 2006-06-22 Neuralab Limited An immunoprecipitation-based assay for predicting in vivo efficacy of beta-amyloid antibodies
US7411093B2 (en) 2004-12-20 2008-08-12 Hoffman-La Roche Inc. Aminocycloalkanes as DPP-IV inhibitors
EP1831165A1 (en) 2004-12-20 2007-09-12 F. Hoffmann-Roche AG 4-aminopiperidine derivatives
US7872124B2 (en) 2004-12-21 2011-01-18 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
JP2008525439A (ja) 2004-12-23 2008-07-17 ボイジャー・ファーマシューティカル・コーポレーション アルツハイマー病の治療のための酢酸ロイプロリド及びアセチルコリンエステラーゼインヒビターまたはnmdaレセプターアゴニスト
EP1831172B1 (en) 2004-12-28 2009-02-18 Council of Scientific and Industrial Research Substituted carbamic acid quinolin-6-yl esters useful as acetylcholinesterase inhibitors
CN101098700A (zh) 2005-01-06 2008-01-02 默克公司 治疗炎性疾病的药物组合疗法和药用组合物
EP1855679B1 (en) 2005-01-19 2016-06-29 Merck Sharp & Dohme Corp. Aminomethyl beta-secretase inhibitors for the treatment of alzheimer's disease
EP1841455A1 (en) 2005-01-24 2007-10-10 Amgen Inc. Humanized anti-amyloid antibody
US20060216331A1 (en) 2005-02-28 2006-09-28 Lines Thomas C Composition for treating mental health disorders
EP1858501A1 (en) 2005-03-07 2007-11-28 Michael Hermanussen Nmda receptor antagonists in the medical intervention of metabolic disorders
ES2259270B1 (es) 2005-03-09 2007-11-01 Consejo Superior De Investigaciones Cientificas Metodo de diagnostico in vitro de la enfermedad de alzheimer mediante un anticuerpo monoclonal.
US7745470B2 (en) 2005-03-10 2010-06-29 Bristol-Myers Squibb Company Isophthalates as beta-secretase inhibitors
FR2883285B1 (fr) 2005-03-17 2007-05-18 Sanofi Aventis Sa Sel besylate de la 7-(2-(4-(3-trifluoromethyl-phenyl) -1,2,3,6-tetrahudro-pyrid-1-yl)ethyl) isoquinoleine, sa preparation et son utilisation en therapeutique
ES2318918B1 (es) 2005-04-01 2010-02-16 Biotherapix Molecular Medicines, S.L.U. Anticuerpos humanos con capacidad de union al peptido beta-amiloide y sus aplicaciones.
CA2605771A1 (en) 2005-04-27 2006-11-02 Novartis Ag Methods of treating atherosclerosis
PE20061323A1 (es) 2005-04-29 2007-02-09 Rinat Neuroscience Corp Anticuerpos dirigidos contra el peptido amiloide beta y metodos que utilizan los mismos
PA8675801A1 (es) 2005-05-19 2006-12-07 Centocor Inc Anticuerpos anti-mcp-1, composiciones, metodos y usos
AU2006254335A1 (en) 2005-06-01 2006-12-07 Ucb Pharma, S.A. 2-oxo-1-pyrrolidine derivatives and their therapeutic use on the central nervous system
US7741448B2 (en) 2005-06-21 2010-06-22 Medical & Biological Laboratories Co., Ltd. Antibody having inhibitory effect on amyloid fibril formation
WO2007011833A2 (en) 2005-07-18 2007-01-25 Merck & Co., Inc. Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
US20090182021A1 (en) 2005-08-03 2009-07-16 Nanternet Philippe G Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
US20090170830A1 (en) 2005-08-03 2009-07-02 Nantermet Philippe G Tricyclic Beta-Secretase Inhibitors for the Treatment of Alzheimer's Disease
WO2007021793A1 (en) 2005-08-12 2007-02-22 Bristol-Myers Squibb Company Macrocyclic diaminopropanes as beta-secretase inhibitors
CA2619725C (en) 2005-08-18 2016-06-07 Ramot At Tel Aviv University Ltd. Single chain antibodies against beta-amyloid peptide
EP1931656B1 (en) 2005-09-28 2011-02-09 Robert Ternansky Novel drugs for dementia
WO2007051333A1 (en) 2005-11-02 2007-05-10 Oncalis Ag Triazine beta-secretase inhibitors
RS53291B (sr) 2005-12-12 2014-08-29 Ac Immune S.A. Beta 1-42 specifična monoklonska antitela sa terapeutskim svojstvima
ES2407429T3 (es) 2005-12-12 2013-06-12 Ac Immune S.A. Vacuna terapéurica
CA2637897A1 (en) 2006-01-20 2007-07-26 Schering Corporation Carbocyclic and heterocyclic arylsulfones as gamma secretase inhibitors
CN101421299A (zh) 2006-02-22 2009-04-29 株式会社林原生物化学研究所 用于诱导产生抗淀粉样β肽抗体的肽疫苗
GB0704100D0 (en) 2006-03-17 2007-04-11 Vodafone Plc Improvements in an ehspa architecture
CN103539857A (zh) 2006-03-30 2014-01-29 葛兰素集团有限公司 针对β-淀粉样蛋白肽的抗体
CL2007002070A1 (es) 2006-07-14 2008-02-08 Ac Immune S A Genentech Inc Anticuerpo quimerico o humanizado, o fragmentos de ellos, que se adhieren especificamente a por lo menos un epitopo en la proteina beta-amiloide; molecula de acido nucleico que lo codifica; composicion que lo comprende; su uso para tratar enfermedade
BRPI0719763A2 (pt) 2006-10-02 2014-01-28 Ac Immune Sa Anticorpo, molécula de ácido nucleico, vetor de expressão, célula, composição, mistura, uso de um anticorpo quimérico ou um fragmento do mesmo ou um anticorpo humanizado ou um fragmento do mesmo e/ou uma parte funcional e/ou uma composição farmacêutica ou uma mistura, métodos para a preparação de uma composição farmacêutica ou de uma mistura, para prevenir, tratar ou aliviar os efeitos de uma doença, de diagnóstico de uma doença ou condição associada com amilóide em um paciente e de determinação do grau da carga de placa amiloidogênica em um tecido e/ou fluidos corporais, kits de teste para a detecção e diagnóstico de doenças e condições associadas com amilóide, região variável de cadeia leve, região variável de cadeia pesada, linhagem de célula, gene de anticorpo, e, métodos para desagregar fibras de beta-amilóide pré formadas, para prevenir a degradação de neurônio induzida por abeta, para diagnosticar uma predisposição a uma doença ou condição associada com amilóide em um paciente, para monitorar doença residual mínima em um paciente, para prognosticar a responsividade de um paciente que é tratado com um anticorpo ou uma composição de vacina, para reduzir a carga de placa no cérebro de um animal, para reduzir a quantidade de placas no cérebro de um animal, para diminuir a quantidade total de abeta solúvel no cérebro de um animal e para reter ou aumentar a capacidade de memória cognitiva em um mamífero.
CA2668065A1 (en) 2006-10-30 2008-05-08 Merck & Co., Inc. Spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
EP2091945B1 (en) 2006-11-09 2014-01-15 Probiodrug AG Novel inhibitors of glutaminyl cyclase
EP2086960B1 (en) 2006-11-09 2014-03-05 Probiodrug AG Novel inhibitors of glutaminyl cyclase
US9126987B2 (en) 2006-11-30 2015-09-08 Probiodrug Ag Inhibitors of glutaminyl cyclase
US20100216875A1 (en) 2006-12-20 2010-08-26 Gregory Hook Methods of treating alzheimer's disease
CA2672213C (en) * 2006-12-22 2016-02-16 Astex Therapeutics Limited Bicyclic amine derivatives as protein tyrosine kinase inhibitors
JP5612860B2 (ja) 2007-03-09 2014-10-22 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのイミダゾ[1,5−a]ピリジン誘導体
JP5667440B2 (ja) 2007-04-18 2015-02-12 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体
US8227498B2 (en) 2007-04-18 2012-07-24 Probiodrug Ag Inhibitors of glutaminyl cyclase
JP5675341B2 (ja) 2007-04-18 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのチオキソキナゾリノン誘導体
EP2146968B1 (en) 2007-04-18 2015-09-23 Probiodrug AG Urea derivatives as glutaminyl cyclase inhibitors
JP5675344B2 (ja) 2007-04-18 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのニトロビニルジアミン誘導体
DK2142513T3 (da) 2007-04-18 2014-06-10 Probiodrug Ag Nitrovinyl-diamin-derivater som glutaminyl-cyclase-inhibitorer
MX2009011281A (es) * 2007-04-20 2010-03-08 Univ New York State Res Found Benzimidazol y composiciones farmaceuticas del mismo.
WO2008128984A1 (en) 2007-04-20 2008-10-30 Probiodrug Ag Aminopyrimidine derivatives as glutaminyl cyclase inhibitors
NZ582039A (en) 2007-05-25 2012-02-24 Elan Pharm Inc Pyrazolopyrrolidines as inhibitors of gamma secretase
AR066987A1 (es) 2007-06-12 2009-09-23 Ac Immune Sa Anticuerpo monoclonal contra proteina beta-amiloide
WO2008151927A2 (en) 2007-06-15 2008-12-18 Nycomed Gmbh 6-n-substituted benz imidazole derivatives as acid pump antagonists
BRPI0814256A8 (pt) 2007-07-05 2016-02-10 Schering Corp Inibidores de tetrahidropiranocromeno gama secretase
US8618123B2 (en) 2007-07-17 2013-12-31 Merck Sharp & Dohme Corp. Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
WO2009029272A2 (en) 2007-08-27 2009-03-05 Agadjanyan Michael G Epitope vaccine for prevention and reversion of ad pathology
WO2009033743A1 (en) 2007-09-13 2009-03-19 University Of Zurich Prorektorat Forschung Monoclonal amyloid beta (abeta)-specific antibody and uses thereof
WO2009042694A1 (en) 2007-09-24 2009-04-02 Comentis, Inc. (3-hydroxy-4-amino-butan-2-yl) -3- (2-thiazol-2-yl-pyrrolidine-1-carbonyl) benzamide derivatives and related compounds as beta-secretase inhibitors for treating
US20100267712A1 (en) 2007-09-27 2010-10-21 The United States of America, as represented by the Secretary, Department of Health and Isoindoline compounds for the treatment of spinal muscular atrophy and other uses
JP5219225B2 (ja) 2007-10-25 2013-06-26 国立大学法人 鹿児島大学 アミロイドβペプチドのミミック分子を用いたペプチドワクチン
GB0720912D0 (en) 2007-10-25 2007-12-05 Univ Cardiff Monoclonal Anitbody for APP
MY155144A (en) 2007-10-29 2015-09-15 Inst Nat Sante Rech Med NEW ANTIBODIES SPECIFIC OF THE ß-AMYLOID PEPTIDES AND THEIR USES AS DIAGNOSTIC AGENTS OR DRUGS
MX2010003828A (es) 2007-11-16 2010-04-27 Univ Rockefeller Anticuerpos especificos para la forma de protofibrillas de la proteina beta-amiloide.
US9345753B2 (en) 2008-01-16 2016-05-24 Yeda Research And Development Co. Ltd. At The Weizmann Institute Of Science Vaccine for alzheimer's disease
ITNA20080006A1 (it) 2008-01-28 2009-07-29 Consiglio Nazionale Ricerche Proteine chimeriche capaci di formare particelle virus-like, che contengono sequenze peptidiche del beta-amiloide e la componente e2 della alfachetoacido deidrogenasi di "geobacillus stearothermophilus", utili per l'induzione di una risposta anticorp
CA2714058A1 (en) 2008-02-28 2009-09-03 Ivory D. Hills 2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease
WO2009134750A1 (en) 2008-04-28 2009-11-05 Janssen Pharmaceutica Nv Benzoimidazoles as prolyl hydroxylase inhibitors
AU2009271019A1 (en) * 2008-07-14 2010-01-21 Gilead Sciences, Inc. Fused heterocyclyc inhibitors of histone deacetylase and/or cyclin-dependent kinases
US20110092445A1 (en) 2008-07-25 2011-04-21 Abbott Laboratories Amyloid ß peptide analogues, oligomers thereof, processes for preparing and composi-tions comprising said analogues or oligomers, and their uses
CN102256620B (zh) 2008-08-07 2016-11-16 莫西亚药物公司 用于治疗阿尔茨海默氏病的免疫治疗组合物
EP2324032B1 (en) 2008-08-19 2014-10-01 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
MX2011002106A (es) 2008-09-04 2011-04-07 Probiodrug Ag Inhibidores novedosos.
WO2010044464A1 (ja) 2008-10-16 2010-04-22 財団法人化学及血清療法研究所 改変アミロイドβペプチド
JP4932065B2 (ja) 2008-11-23 2012-05-16 ファイザー・インク βセクレターゼ阻害剤としてのラクタム
US8609897B2 (en) 2009-02-06 2013-12-17 Merck Sharp & Dohme Corp. Trifluoromethylsulfonamide gamma secretase inhibitor
WO2010094242A1 (en) 2009-02-20 2010-08-26 Merck Sharp & Dohme Corp. Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer's disease

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