BR0107532A - Composto, uso do composto, método para o tratamento de disfunções neurológicas associadas com a produção de b-amilóide, método de inibição da atividade de y-secretase e composição farmacêutica - Google Patents

Composto, uso do composto, método para o tratamento de disfunções neurológicas associadas com a produção de b-amilóide, método de inibição da atividade de y-secretase e composição farmacêutica

Info

Publication number
BR0107532A
BR0107532A BR0107532-2A BR0107532A BR0107532A BR 0107532 A BR0107532 A BR 0107532A BR 0107532 A BR0107532 A BR 0107532A BR 0107532 A BR0107532 A BR 0107532A
Authority
BR
Brazil
Prior art keywords
compound
amyloid
pharmaceutical composition
inhibiting
production
Prior art date
Application number
BR0107532-2A
Other languages
English (en)
Inventor
Richard E Olson
Michael G Yang
Original Assignee
Bristol Myers Squibb Pharma Co
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 Bristol Myers Squibb Pharma Co filed Critical Bristol Myers Squibb Pharma Co
Publication of BR0107532A publication Critical patent/BR0107532A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/16Benzazepines; Hydrogenated benzazepines
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4015Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
    • 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
    • A61K31/435Heterocyclic 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
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D223/08Oxygen atoms
    • C07D223/10Oxygen atoms attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/02Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D223/06Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D223/12Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D223/00Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
    • C07D223/14Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D223/18Dibenzazepines; Hydrogenated dibenzazepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D243/00Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/141,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/161,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/181,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06191Dipeptides containing heteroatoms different from O, S, or N
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

"COMPOSTO, USO DO COMPOSTO, MéTODO PARA O TRATAMENTO DE DISFUNçõES NEUROLóGICAS ASSOCIADAS COM A PRODUçãO DE <225>-AMILóIDE, MéTODO DE INIBIçãO DA ATIVIDADE DE <sym>-SECRETASE E COMPOSIçãO FARMACêUTICA". A presente invenção refere-se a novas malonamidas cíclicas que possuem a fórmula (1); suas composições farmacêuticas e seus métodos de utilização. Estes novos compostos inibem o processamento de proteínas precursoras de amilóides e, mais especificamente, inibem a produção do A<225>-peptídeo, de forma a agir para evitar a formação de depósitos neurológicos de proteínas de amilóide. Mais especificamente, a presente invenção refere-se ao tratamento de disfunções neurológicas relativas à produção de <255>-amilóide, tais como o mal de Alzheimer e a Síndrome de Down.
BR0107532-2A 2000-04-03 2001-04-03 Composto, uso do composto, método para o tratamento de disfunções neurológicas associadas com a produção de b-amilóide, método de inibição da atividade de y-secretase e composição farmacêutica BR0107532A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US19450300P 2000-04-03 2000-04-03
PCT/US2001/010667 WO2001074783A1 (en) 2000-04-03 2001-04-03 Cyclic lactams as inhibitors of a βετα protein production

Publications (1)

Publication Number Publication Date
BR0107532A true BR0107532A (pt) 2004-11-03

Family

ID=22717849

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0107532-2A BR0107532A (pt) 2000-04-03 2001-04-03 Composto, uso do composto, método para o tratamento de disfunções neurológicas associadas com a produção de b-amilóide, método de inibição da atividade de y-secretase e composição farmacêutica

Country Status (10)

Country Link
US (8) US6759404B2 (pt)
EP (1) EP1268433A1 (pt)
JP (1) JP2003535046A (pt)
CN (1) CN1436175A (pt)
AU (1) AU2001253090A1 (pt)
BR (1) BR0107532A (pt)
CA (1) CA2404023A1 (pt)
IL (1) IL151576A0 (pt)
MX (1) MXPA02009755A (pt)
WO (1) WO2001074783A1 (pt)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1436175A (zh) 2000-04-03 2003-08-13 布里斯托尔-迈尔斯斯奎布药品公司 作为Aβ-蛋白生产抑制剂的环状内酰胺
US6878363B2 (en) 2000-05-17 2005-04-12 Bristol-Myers Squibb Pharma Company Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging
NZ538870A (en) 2002-09-20 2007-04-27 Arrow Therapeutics Ltd Benzodiazepine derivatives and pharmaceutical compositions containing them
GB0221923D0 (en) * 2002-09-20 2002-10-30 Arrow Therapeutics Ltd Chemical compounds
EP1592684B1 (en) * 2003-02-04 2008-07-30 F. Hoffmann-La Roche Ag Malonamide derivatives as gamma-secretase inhibitors
US7163937B2 (en) 2003-08-21 2007-01-16 Bristol-Myers Squibb Company Cyclic derivatives as modulators of chemokine receptor activity
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
BRPI0520554A2 (pt) 2005-09-19 2009-06-13 Arrow Therapeutics Ltd uso de uma benzodiazepina ou um sal farmaceuticamente aceitável do mesmo, método para tratar ou prevenir uma infecção por hcv em um paciente, derivado de benzodiazepina ou um sal famaceuticamente aceitável do mesmo, e, composição farmacêutica
WO2007110337A1 (en) 2006-03-29 2007-10-04 F. Hoffmann-La Roche Ag Pyridine and pyrimidine derivatives as mglur2 antagonists
KR101150574B1 (ko) * 2007-02-02 2012-05-30 에프. 호프만-라 로슈 아게 6-옥소-6,7-다이하이드로-5h-다이벤조[b,d]아제핀-7-일 유도체
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
JP2010526825A (ja) * 2007-05-10 2010-08-05 エーエムアール テクノロジー インコーポレイテッド アリール置換およびヘテロアリール置換テトラヒドロベンゾ−1,4−ジアゼピンならびにノルエピネフリン、ドーパミンおよびセロトニンの再取り込みを遮断するためのその使用
EP2222636B1 (en) 2007-12-21 2013-04-10 Ligand Pharmaceuticals Inc. Selective androgen receptor modulators (sarms) and uses thereof
EP2291181B9 (en) 2008-04-18 2013-09-11 University College Dublin National University Of Ireland, Dublin Captodiamine for the treatment of depression symptoms
EP2349484A2 (en) * 2008-07-15 2011-08-03 Novartis AG Heteroaryl derivatives as dgat1 inhibitors
JP2010116364A (ja) * 2008-11-14 2010-05-27 Banyu Pharmaceut Co Ltd アゼピノン誘導体
US8383812B2 (en) 2009-10-13 2013-02-26 Bristol-Myers Squibb Company N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-A][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes
TWI530489B (zh) 2011-03-22 2016-04-21 必治妥美雅史谷比公司 雙(氟烷基)-1,4-苯二氮呯酮化合物
CN104797584A (zh) 2012-09-21 2015-07-22 百时美施贵宝公司 作为notch抑制剂的三环杂环化合物
TWI614238B (zh) 2012-09-21 2018-02-11 必治妥美雅史谷比公司 雙(氟烷基)-1,4-苯并二氮呯酮化合物及其前藥
CN105308030A (zh) 2012-09-21 2016-02-03 百时美施贵宝公司 烷基、氟烷基-1,4-苯并二氮杂*酮化合物
CN104797569A (zh) 2012-09-21 2015-07-22 百时美施贵宝公司 取代的1,5-苯并二氮杂*酮化合物
US9242940B2 (en) 2012-09-21 2016-01-26 Bristol-Myers Squibb Company N-substituted bis(fluoroalkyl)-1,4-benzodiazepinone compounds
WO2014047370A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Fluoroalkyl dibenzodiazepinone compounds
EP2897942B1 (en) 2012-09-21 2016-08-31 Bristol-Myers Squibb Company Fluoroalkyl and fluorocycloalkyl 1,4-benzodiazepinone compounds as notch inhibitors
WO2014047392A1 (en) 2012-09-21 2014-03-27 Bristol-Myers Squibb Company Fluoroalkyl-1,4-benzodiazepinone compounds
JP2015531792A (ja) 2012-09-21 2015-11-05 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 1,4−ベンゾジアゼピノン化合物のプロドラッグ
TWI637951B (zh) 2013-02-15 2018-10-11 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類
EP2981267A1 (en) 2013-04-04 2016-02-10 Bristol-Myers Squibb Company Combination therapy for the treatment of proliferative diseases
US10441567B2 (en) 2014-01-17 2019-10-15 Ligand Pharmaceuticals Incorporated Methods and compositions for modulating hormone levels
IL287136B2 (en) 2016-02-05 2023-09-01 Denali Therapeutics Inc Receptor inhibitors - interacting with protein kinase 1
JP7208137B2 (ja) 2016-12-09 2023-01-18 デナリ セラピューティクス インコーポレイテッド 化合物、組成物および方法
WO2020214834A1 (en) 2019-04-19 2020-10-22 Ligand Pharmaceuticals Inc. Crystalline forms and methods of producing crystalline forms of a compound
TW202334164A (zh) 2022-01-12 2023-09-01 美商戴納立製藥公司 (S)-5-苄基-N-(5-甲基-4-側氧基-2,3,4,5-四氫吡啶並[3,2-b][1,4]氧氮呯-3-基)-4H-1,2,4-三唑-3-甲醯胺的晶型

Family Cites Families (99)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4897489A (en) * 1984-12-18 1990-01-30 Takeda Chemical Industries, Ltd. Antibiotic derivatives, their production and use
US4666829A (en) * 1985-05-15 1987-05-19 University Of California Polypeptide marker for Alzheimer's disease and its use for diagnosis
JPS62123444A (ja) * 1985-08-07 1987-06-04 Japan Synthetic Rubber Co Ltd ポジ型感放射線性樹脂組成物
FR2630440B1 (fr) 1988-04-25 1991-09-20 Jouveinal Sa Benzodiazepines, leur procede et intermediaires de preparation et leurs applications en therapeutique
DK0411668T4 (da) 1989-08-04 1999-08-09 Merck Sharp & Dohme Central-chlolecystokinin-antagonister til behandling af psykiske forstyrrelser
US5175159A (en) 1989-10-05 1992-12-29 Merck & Co., Inc. 3-substituted-1,4-benzodiazepines as oxytocin antagonists
CA2026856A1 (en) 1989-10-05 1991-04-06 Mark G. Bock 3-substituted-1,4-benzodiazepines useful as oxytocin
CA2032427A1 (en) 1989-12-18 1991-06-19 Mark G. Bock Benzodiazepines analogs
US5206235A (en) 1991-03-20 1993-04-27 Merck & Co., Inc. Benzo-fused lactams that promote the release of growth hormone
GB9107368D0 (en) 1991-04-08 1991-05-22 Smithkline Beecham Plc Novel compounds
IT1260444B (it) 1992-01-24 1996-04-09 Mario Brufani Derivati della 8-(1-amminocicloalchil)1,3-dialchilxantina, procedimenbto di preparazione e loro composizioni farmaceutiche antidepressive, nootropiche e psicostimolanti
US5766846A (en) * 1992-07-10 1998-06-16 Athena Neurosciences Methods of screening for compounds which inhibit soluble β-amyloid peptide production
EP0652871B1 (en) 1992-07-29 2001-10-17 MERCK SHARP &amp; DOHME LTD. Benzodiazepine derivatives
US5283241A (en) 1992-08-28 1994-02-01 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
ES2197160T3 (es) 1992-12-21 2004-01-01 Smithkline Beecham Corp Antagonistas fibronogeno bicicliclos.
MX9308016A (es) 1992-12-22 1994-08-31 Lilly Co Eli Compuestos inhibidores de la proteasa del virus de la inmunodeficiencia humana, procedimiento para su preparacion y formulacion farmaceutica que los contiene.
AU6909194A (en) 1993-05-14 1994-12-12 Board Of Regents, The University Of Texas System Preparation of n-cyanodithioimino-carbonates and 3-mercapto-5-amino-1h-1,2,4-triazole
WO1994029273A1 (en) 1993-06-09 1994-12-22 Smithkline Beecham Corporation Bicyclic fibrinogen antagonists
NZ264143A (en) 1993-08-09 1996-11-26 Lilly Co Eli Use of an aspartyl protease inhibitor to inhibit beta-amyloid peptide production
US5602156A (en) 1993-09-17 1997-02-11 The United States Of America As Represented By The Department Of Health And Human Services Method for inhibiting metalloproteinase expression
US5545735A (en) 1993-10-04 1996-08-13 Merck & Co., Inc. Benzo-Fused Lactams promote release of growth hormone
US5426185A (en) 1993-11-22 1995-06-20 Merck & Co., Inc. Antiarrhythmic benzodiazepines
US5770573A (en) 1993-12-06 1998-06-23 Cytel Corporation CS-1 peptidomimetics, compositions and methods of using the same
GB9401919D0 (en) 1994-02-01 1994-03-30 Bridport Aviat Prod Luggage bins for the cabins of passenger aircraft
US5514716A (en) 1994-02-25 1996-05-07 Sterling Winthrop, Inc. Hydroxamic acid and carboxylic acid derivatives, process for their preparation and use thereof
JPH10504545A (ja) 1994-07-29 1998-05-06 藤沢薬品工業株式会社 ベンゾジアゼピン誘導体
US5661161A (en) 1994-09-29 1997-08-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1996017833A1 (en) 1994-12-09 1996-06-13 Smithkline Beecham Corporation Bicyclic fibrinogen antagonists
EP0799189A4 (en) 1994-12-13 1999-03-17 Smithkline Beecham Corp BICYCLIC FIBRINOGENIC ANTAGONISTS
US5639746A (en) 1994-12-29 1997-06-17 The Procter & Gamble Company Hydroxamic acid-containing inhibitors of matrix metalloproteases
US5672598A (en) 1995-03-21 1997-09-30 The Procter & Gamble Company Lactam-containing hydroxamic acids
US5856326A (en) 1995-03-29 1999-01-05 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5578629A (en) 1995-03-29 1996-11-26 Merck & Co., Inc. Benzamide-containing inhibitors of farnesyl-protein transferase
GB9507799D0 (en) 1995-04-18 1995-05-31 British Biotech Pharm Metalloproteinase inhibitors
US5710171A (en) 1995-05-24 1998-01-20 Merck & Co., Inc. Bisphenyl inhibitors of farnesyl-protein transferase
FI974368A7 (fi) 1995-05-29 1997-11-28 Pfizer Kasvuhormonin vapautumista edistäviä dipeptidejä
US5756528A (en) 1995-06-06 1998-05-26 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5919765A (en) * 1995-06-07 1999-07-06 Cor Therapeutics, Inc. Inhibitors of factor XA
EP0761680A3 (en) 1995-09-12 1999-05-06 Ono Pharmaceutical Co., Ltd. Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity
WO1997012861A1 (en) 1995-10-05 1997-04-10 Chiroscience Limited Mercaptoamide derivatives and their therapeutic use
ATE205184T1 (de) 1995-11-23 2001-09-15 British Biotech Pharm Metalloproteinase inhibitoren
AU703203B2 (en) 1996-01-30 1999-03-18 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5968965A (en) 1996-01-30 1999-10-19 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5891889A (en) 1996-04-03 1999-04-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2250353A1 (en) 1996-04-03 1997-10-09 Christopher J. Dinsmore Inhibitors of farnesyl-protein transferase
US5859012A (en) 1996-04-03 1999-01-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU2555997A (en) 1996-04-03 1997-10-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US6001835A (en) 1996-04-03 1999-12-14 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036877A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5919785A (en) 1996-04-03 1999-07-06 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5885995A (en) 1996-04-03 1999-03-23 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5852010A (en) 1996-04-03 1998-12-22 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5965578A (en) 1996-04-03 1999-10-12 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5869682A (en) 1996-04-03 1999-02-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
DE19614100C2 (de) 1996-04-10 2000-12-07 Bosch Gmbh Robert Vorrichtung zur Ermittlung des Zustandes eines Wischerblattes
US5770673A (en) * 1996-04-10 1998-06-23 Bayer Corporation Non-sagging, light stable polyurethane compositions, a process for producing them, and their use as seam sealants
CA2251955A1 (en) 1996-04-18 1997-10-23 Nancy E. Kohl A method of treating cancer
EP0934270A1 (en) 1996-05-30 1999-08-11 Merck & Co., Inc. A method of treating cancer
US5703129A (en) 1996-09-30 1997-12-30 Bristol-Myers Squibb Company 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives as inhibitors of β-amyloid protein production
JP2001504810A (ja) 1996-10-11 2001-04-10 シーオーアール・セラピューティックス・インコーポレーテッド 選択的第Xa因子阻害剤
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
DE19647382A1 (de) 1996-11-15 1998-05-20 Hoechst Ag Heterocyclen als Inhibitoren der Leukozytenadhäsion und VLA-4-Antagonisten
JP2001504498A (ja) 1996-11-22 2001-04-03 エラン・ファーマシューティカルズ・インコーポレイテッド N―(アリール/ヘテロアリール/アルキルアセチル)アミノ酸アミドおよびその医薬組成物、並びに該化合物を用いたβ―アミロイドペプチドの放出および/またはその合成を阻害する方法
CA2272433A1 (en) 1996-11-22 1998-05-28 James E. Audia N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions, and methods for inhibiting beta-amyloid peptide release and/or its synthesis
JP2001505204A (ja) 1996-11-22 2001-04-17 エラン・ファーマシューティカルズ・インコーポレイテッド N―(アリール/ヘテロアリールアセチル)アミノ酸エステル、それを含有する医薬組成物および該化合物を用いてβ―アミロイドペプチドの放出および/または合成を阻害する方法
TR199901132T2 (xx) 1996-11-22 1999-08-23 Elan Pharmaceuticals, Inc. N-(aril/heteoaril) amino asit t�revleri, bunlar� i�eren farmas�tik bile�imler ve b�yle bile�ikler kullan�larak �-amiloid peptidinin sal�nmas�n� ve/veya sentezini inhibe etmek i�in y�ntemler.
TW523506B (en) 1996-12-18 2003-03-11 Ono Pharmaceutical Co Sulfonamide or carbamide derivatives and drugs containing the same as active ingredients
HUP0001232A3 (en) * 1996-12-23 2001-02-28 Elan Pharmaceuticals Inc San F Cycloalkyl, lactam, lactone derivatives and their thio analogues inhibiting betha-amyloid peptide release and/or its synthesis and pharmaceutical compositions containing the compounds
CA2276081A1 (en) 1996-12-30 1998-07-09 Lekhanh O. Tran Inhibitors of farnesyl-protein transferase
US6093737A (en) 1996-12-30 2000-07-25 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
GB2338957B (en) 1997-02-19 2001-08-01 Berlex Lab N-heterocyclic derivatives as nos inhibitors
US6432947B1 (en) 1997-02-19 2002-08-13 Berlex Laboratories, Inc. N-heterocyclic derivatives as NOS inhibitors
WO1998041510A1 (en) 1997-03-14 1998-09-24 Shionogi & Co., Ltd. Novel benzolactam derivatives and medicinal compositions comprising the same
US5985900A (en) 1997-04-01 1999-11-16 Agouron Pharmaceuticals, Inc. Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses
AU724216B2 (en) 1997-04-07 2000-09-14 Merck & Co., Inc. A method of treating cancer
US6060038A (en) 1997-05-15 2000-05-09 Merck & Co., Inc. Radiolabeled farnesyl-protein transferase inhibitors
DE19726427A1 (de) 1997-06-23 1998-12-24 Boehringer Mannheim Gmbh Pyrimidin-2,4,6-trion-Derivate, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel
GB9715030D0 (en) 1997-07-18 1997-09-24 British Biotech Pharm Metalloproteinase inhibitors
CA2299610A1 (en) 1997-08-11 1999-02-18 Cor Therapeutics, Inc. Selective factor xa inhibitors
US6333321B1 (en) 1997-08-11 2001-12-25 Cor Therapeutics, Inc. Selective factor Xa inhibitors
ATE211482T1 (de) 1997-08-11 2002-01-15 Cor Therapeutics Inc Selektive inhibitoren des faktors x, eine azepinonstruktur enthaltend
US6228854B1 (en) 1997-08-11 2001-05-08 Cor Therapeutics, Inc. Selective factor Xa inhibitors
AU735366B2 (en) 1997-09-29 2001-07-05 Bristol-Myers Squibb Company Inhibitors of farnesyl protein transferase
US6297239B1 (en) 1997-10-08 2001-10-02 Merck & Co., Inc. Inhibitors of prenyl-protein transferase
US6440965B1 (en) 1997-10-15 2002-08-27 Krenitsky Pharmaceuticals, Inc. Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system
IL135564A0 (en) 1997-12-22 2001-05-20 Elan Pharm Inc POLYCYCLIC α-AMINO-ɛ-CAPROLACTAMS AND RELATED COMPOUNDS
US6297373B1 (en) * 1997-12-26 2001-10-02 Asahi Kasei Kabushiki Kaisha Method for acylating hexakis (arylmethyl) hexaazaisowurtzitane
ATE500532T1 (de) 1998-02-20 2011-03-15 Puredepth Ltd Mehrschichtige anzeigevorrichtung und verfahren zur darstellung von bildern auf einer solchen anzeigevorrichtung
WO1999067221A1 (en) * 1998-06-22 1999-12-29 Elan Pharmaceuticals, Inc. Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
CA2324475A1 (en) * 1998-06-22 1999-12-29 Elan Pharmaceuticals, Inc. Cyclic amino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting .beta.-amyloid peptide release and/or its synthesis by use of such compounds
JP2002518481A (ja) 1998-06-22 2002-06-25 エラン ファーマシューティカルズ,インコーポレイテッド β−アミロイドペプチドの放出および/またはその合成を阻害するための化合物
AU5204799A (en) 1998-06-22 2000-01-10 Elan Pharmaceuticals, Inc. Compounds for inhibiting beta-amyloid peptide release and/or its synthesis
WO2000002903A1 (en) 1998-07-10 2000-01-20 Cytel Corporation Cs-1 peptidomimetics, compositions and methods of using the same
HRP990246A2 (en) 1998-08-07 2000-06-30 Du Pont Pharm Co Succinoylamino benzodiazepines as inhibitors of a beta protein production
AU1618000A (en) 1998-11-12 2000-05-29 Du Pont Pharmaceuticals Company Use of radioligands to screen inhibitors of amyloid-beta peptide production
WO2000038618A2 (en) 1998-12-24 2000-07-06 Du Pont Pharmaceuticals Company SUCCINOYLAMINO BENZODIAZEPINES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
CA2395862A1 (en) 2000-02-17 2001-08-23 Hong Liu Succinoylamino carbocycles and heterocycles as inhibitors of a.beta. protein production
CN1436175A (zh) * 2000-04-03 2003-08-13 布里斯托尔-迈尔斯斯奎布药品公司 作为Aβ-蛋白生产抑制剂的环状内酰胺
US6424455B1 (en) * 2000-10-03 2002-07-23 Tycom (Us) Inc. Wide bandwidth fiber raman amplifier

Also Published As

Publication number Publication date
US7390896B2 (en) 2008-06-24
CA2404023A1 (en) 2001-10-11
IL151576A0 (en) 2003-04-10
AU2001253090A1 (en) 2001-10-15
US7276496B2 (en) 2007-10-02
US7053081B2 (en) 2006-05-30
US20080275024A1 (en) 2008-11-06
US6759404B2 (en) 2004-07-06
CN1436175A (zh) 2003-08-13
EP1268433A1 (en) 2003-01-02
US20100009965A1 (en) 2010-01-14
US20050009807A1 (en) 2005-01-13
US20090264419A1 (en) 2009-10-22
WO2001074783A1 (en) 2001-10-11
JP2003535046A (ja) 2003-11-25
US20020103184A1 (en) 2002-08-01
US20100041639A1 (en) 2010-02-18
US7528249B2 (en) 2009-05-05
US20060135762A1 (en) 2006-06-22
MXPA02009755A (es) 2003-03-27
US20080021014A1 (en) 2008-01-24

Similar Documents

Publication Publication Date Title
BR0107532A (pt) Composto, uso do composto, método para o tratamento de disfunções neurológicas associadas com a produção de b-amilóide, método de inibição da atividade de y-secretase e composição farmacêutica
BR0110051A (pt) Composto, uso do composto, composição farmacêutica e método de tratamento do mal de alzheimer
BR9917082A (pt) Compostos inibidores da produção de proteìnas a&#34;beta&#34;, método de tratamento de disfunções neurológicas associadas com a produção de &#34;beta&#34;-amilóide, composição farmacêutica e, método de inibição da atividade de y-secretase
BR0106717A (pt) Compostos, composição farmacêutica e usos dos compostos de lactama inovadora
BR9912969A (pt) Composto, composição farmacêutica, método para o tratamento dos distúrbios neurológicos associados com a produção de b-amilóide, método para o tratamento da doença de alzheimer associada com a produção de b-amilóide, método para o tratamento dos distúrbios neurológicos associados com a produção de b-amilóide e método para inibir a atividade de y-secretase
BR0116605A (pt) Composto, processo para a preparação de um composto, composição farmacêutica que compreende o mesmo, sua utilização e processo para o tratamento e profilaxia de distúrbios do sistema nervoso central, distúrbios cardiovasculares, distúrbios gastrintestinais e apnéia do sono
BR0116201A (pt) Composto, processo para a preparação de um composto, composição farmacêutica que compreende o composto, utilização do composto, processo para o tratamento e profilaxia de distúrbios e para o tratamento de obesidade
BR0014269A (pt) Compostos de lactamas, seus sais e pró-drogas farmaceuticamente aceitáveis, composição farmacêutica, método de tratamento de disfunções neurológicas associadas com a produção de &#34;beta&#34;-amilóide, método de inibição da atividade da &#34;alfa&#34;-secretase e usos dos compostos
BR0112918A (pt) Composto, utilização do mesmo, processo de tratamento de distúrbios, processo para a preparação de composto, composição farmacêutica que compreende esse composto, processo para preparar uma composição e processo de tratamento de obesidade em um ser humano
BR0312216A (pt) Composto, processo para a produção de um composto, composição farmacêutica, uso do composto, método para o tratamento de um sujeito que sofre de uma doença ou condição patológica e combinação de produto
BR0210721A (pt) Composto, sal ou éster farmaceuticamente aceitável, método para fabricar um composto, e, método para tratar um paciente que tem, ou para evitar que o paciente adquira uma doença ou condição
BR0111980A (pt) Amina substituìda, composto protegido, métodos para tratar um paciente que tenha ou para prevenir que um paciente contraia uma doença ou condição, para inibir a atividade da beta-secretase, para inibir a clivagem da proteìna precursora de amilóide (app), para inibir a produção do peptìdeo beta amilóide (a beta) em uma célula, para inibir a produção de placa beta0amilóide em um animal, e para tratar ou prevenir uma doença compreendendo depósitos de beta-amilóide no cérebro, composição método para produzir um complexo de beta-secretase, conjunto, e, uso de amina substituìda
BR0012590A (pt) Composto, processo para a preparação do mesmo, formulação farmacêutica, uso de um composto, e, métodos para tratamento ou profilaxia de dor ou desconforto, e para tratamento ou profilaxia de dor neuropática ou central
BR0211119A (pt) Composto, método de tratar um paciente que tenha, ou de prevenir um paciente de pegar, uma doença ou condição, uso de um composto, e, método para fabricar um composto
NO961326L (no) Inhibitorer av -amyloidproteinproduksjon
BR0209821A (pt) Compostos, processo para a manufatura desses compostos, composições farmacêuticas que compreendem os mesmos, processo para o tratamento e/ou profilaxia de enfermidades e utilização dos compostos
DE60126980D1 (de) Therapeutische agentien und methoden ihrer verwendung zur behandlung von amyloidogenen erkrankungen
SE0104340D0 (sv) New compounds
CY1108900T1 (el) Πολυθειωμενα γλυκοζιδια και αλατα αυτων
BR0208111A (pt) Composto, utilização de um composto, processo de tratamento de distúrbios, processo para preparação de composto, composição farmacêutica que compreende o composto e processo de tratamento de obesidade
BRPI0507786A (pt) composto e sais farmaceuticamente aceitáveis do mesmo, formulação farmacêutica, uso de um composto, método de tratar uma doença, e, processo para a preparação de compostos
BR0211118A (pt) Composto, métodos para o tratamento ou prevenção de doenças e para fabricar um composto, intermediário, e, uso de um composto ou sal
BR0207978A (pt) N-but-3enil norbuprenorfina e métodos de uso
BRPI0409151A (pt) uso de derivados de 10-hidróxi-10,11-diidrocarbamazepina para o tratamento de transtornos afetivos
BRPI0518907A2 (pt) compostos, processo para a sua manufatura, composiÇÕes farmacÊuticas que os compreendem, mÉtodo para o tratamento e/ou prevenÇço de enfermidades que estço associadas com a modulaÇço de receptores de h3 e sua utilizaÇço

Legal Events

Date Code Title Description
B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]