ATE396174T1 - Hydroxyalkylaminderivate als beta-secretase- inhibitoren und deren verwendung zur behandlung der alzheimerschen krankheit oder ähnlicher krankheiten - Google Patents

Hydroxyalkylaminderivate als beta-secretase- inhibitoren und deren verwendung zur behandlung der alzheimerschen krankheit oder ähnlicher krankheiten

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Publication number
ATE396174T1
ATE396174T1 AT02741841T AT02741841T ATE396174T1 AT E396174 T1 ATE396174 T1 AT E396174T1 AT 02741841 T AT02741841 T AT 02741841T AT 02741841 T AT02741841 T AT 02741841T AT E396174 T1 ATE396174 T1 AT E396174T1
Authority
AT
Austria
Prior art keywords
disease
alzheimer
hydroxyalkylamine
beta
derivatives
Prior art date
Application number
AT02741841T
Other languages
English (en)
Inventor
John Freskos
David Brown
Larry Fang
Yvette Fobian
John Varghese
Arthur Romero
Original Assignee
Elan Pharm Inc
Pharmacia & Upjohn Co Llc
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 Elan Pharm Inc, Pharmacia & Upjohn Co Llc filed Critical Elan Pharm Inc
Application granted granted Critical
Publication of ATE396174T1 publication Critical patent/ATE396174T1/de

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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
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    • C07C317/50—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
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    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
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    • C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
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    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/40—Oxygen atoms
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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AT02741841T 2001-06-01 2002-05-31 Hydroxyalkylaminderivate als beta-secretase- inhibitoren und deren verwendung zur behandlung der alzheimerschen krankheit oder ähnlicher krankheiten ATE396174T1 (de)

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Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004502664A (ja) 2000-06-30 2004-01-29 イーラン　ファーマスーティカルズ、インコーポレイテッド アルツハイマー病処置用化合物
MXPA03011046A (es) * 2001-06-01 2004-06-25 Elan Pharm Inc Hidroxialquilaminas.
AU2002360508A1 (en) * 2001-12-06 2003-06-23 Elan Pharmaceuticals, Inc. Substituted hydroxyethylamines
UY27967A1 (es) * 2002-09-10 2004-05-31 Pfizer Acetil 2-hindroxi-1,3-diaminoalcanos
CA2507484A1 (en) * 2002-11-27 2004-06-17 Elan Pharmaceuticals, Inc. Substituted ureas and carbamates
GB0300804D0 (en) * 2003-01-14 2003-02-12 Novo Pharmaceuticals De Ltd Compounds and their use
US7521481B2 (en) 2003-02-27 2009-04-21 Mclaurin Joanne Methods of preventing, treating and diagnosing disorders of protein aggregation
US7763609B2 (en) 2003-12-15 2010-07-27 Schering Corporation Heterocyclic aspartyl protease inhibitors
WO2005070407A1 (en) * 2004-01-21 2005-08-04 Elan Pharmaceuticals, Inc. Methods of treatment of amyloidosis using aspartyl-protease inihibitors
JP2007528400A (ja) 2004-03-09 2007-10-11 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 置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬
JP2007528402A (ja) * 2004-03-09 2007-10-11 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 置換ヒドロキシエチルアミン系のアスパラギン酸プロテアーゼ阻害薬
WO2006010095A2 (en) * 2004-07-09 2006-01-26 Elan Pharmaceuticals Inc. Oxime derivative substituted hydroxyethylamine aspartyl protease inhibitors
US20060128715A1 (en) * 2004-07-09 2006-06-15 Jennifer Sealy Oxime derivative hydroxyethylamine aspartyl-protease inhibitors
US8178077B2 (en) 2004-10-19 2012-05-15 Reverse Proteomics Research Institute Co., Ltd. Drug development target protein and target gene, and method of screening
NZ562314A (en) 2005-04-08 2010-02-26 Comentis Inc Compounds which inhibit beta-secretase activity and methods of use thereof
WO2007047305A1 (en) 2005-10-12 2007-04-26 Elan Pharmaceuticals, Inc. Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors
US8278345B2 (en) 2006-11-09 2012-10-02 Probiodrug Ag Inhibitors of glutaminyl cyclase
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
CA2676715A1 (en) 2007-02-12 2008-08-21 Merck & Co., Inc. Piperazine derivatives for treatment of ad and related conditions
JP5930573B2 (ja) 2007-03-01 2016-06-15 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の新規使用
EP2142514B1 (de) 2007-04-18 2014-12-24 Probiodrug AG Thioharnstoffderivate als glutaminylcyclaseinhibitoren
EP2291181B9 (de) 2008-04-18 2013-09-11 University College Dublin National University Of Ireland, Dublin Captodiamine zur Behandlung von depressionartigen Symptomen
WO2009129532A1 (en) * 2008-04-18 2009-10-22 University Of Connecticut Compounds for lysosomal modulation and methods of use
JP5934645B2 (ja) 2009-09-11 2016-06-15 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ヘテロ環式誘導体
JP6026284B2 (ja) 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
NZ602312A (en) 2010-03-10 2014-02-28 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
EP2686313B1 (de) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazolderivate als glutaminylcyclase-hemmer
EP3509590A4 (de) 2016-09-07 2020-12-02 Pliant Therapeutics, Inc. N-acyl-aminosäure-verbindungen und verfahren zur verwendung
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa
FI3761980T3 (fi) 2018-03-07 2024-02-21 Pliant Therapeutics Inc Aminohappoyhdisteitä ja käyttömenetelmiä
CN114173803A (zh) 2019-04-08 2022-03-11 普利安特治疗公司 氨基酸化合物的剂型和方案

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3587742A (en) * 1969-09-08 1971-06-28 Shell Oil Co Consolidation of shallow formations with acid modified epoxy resinous material
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5211811A (en) * 1989-02-15 1993-05-18 Union Camp Patent Holding, Inc. Process for high consistency oxygen delignification of alkaline treated pulp followed by ozone delignification
ES2217250T3 (es) 1990-06-15 2004-11-01 Scios Inc. Mamifero transgenico, no humano que muestra la patologia de formacion amiloides de la enfermedad de alzheimer.
US5912410A (en) 1990-06-15 1999-06-15 Scios Inc. Transgenic non-human mice displaying the amyloid-forming pathology of alzheimer's disease
ES2236682T5 (es) 1991-01-21 2011-03-31 Elan Pharmaceuticals, Inc. Ensayo y modelo para la enfermedad de alzheimer.
AU671093B2 (en) 1992-01-07 1996-08-15 Elan Pharmaceuticals, Inc. Transgenic animal models for alzheimer's disease
US5441870A (en) 1992-04-15 1995-08-15 Athena Neurosciences, Inc. Methods for monitoring cellular processing of β-amyloid precursor protein
US5604102A (en) 1992-04-15 1997-02-18 Athena Neurosciences, Inc. Methods of screening for β-amyloid peptide production inhibitors
US5766846A (en) 1992-07-10 1998-06-16 Athena Neurosciences Methods of screening for compounds which inhibit soluble β-amyloid peptide production
US5783701A (en) * 1992-09-08 1998-07-21 Vertex Pharmaceuticals, Incorporated Sulfonamide inhibitors of aspartyl protease
AU702293B2 (en) 1993-10-27 1999-02-18 Athena Neurosciences, Inc. Transgenic animals harboring APP allele having Swedish mutation
US5877399A (en) 1994-01-27 1999-03-02 Johns Hopkins University Transgenic mice expressing APP-Swedish mutation develop progressive neurologic disease
US5744346A (en) 1995-06-07 1998-04-28 Athena Neurosciences, Inc. β-secretase
JPH11507538A (ja) * 1995-06-07 1999-07-06 アテナ ニューロサイエンシズ インコーポレイティド β−セクレターゼ、β−セクレターゼに対する抗体、及びβ−セクレターゼ阻害を検出するためのアッセイ
WO1998022597A2 (en) 1996-11-20 1998-05-28 Oklahoma Medical Research Foundation Cloning and characterization of napsin, an aspartic protease
US6191166B1 (en) 1997-11-21 2001-02-20 Elan Pharmaceuticals, Inc. Methods and compounds for inhibiting β-amyloid peptide release and/or its synthesis
EP0958293B1 (de) * 1997-02-04 2005-01-19 The Regents Of The University Of California Nanomolare, non-peptidische inhibitoren von cathepsin d
GB9812189D0 (en) 1998-06-05 1998-08-05 Glaxo Group Ltd Methods and compositions for increasing penetration of HIV protease inhibitors
WO2000003819A1 (en) 1998-07-17 2000-01-27 The Penn State Research Foundation Full form roll finishing technique
PL205294B1 (pl) 1998-09-24 2010-03-31 Upjohn Co Izolowany lub oczyszczony polipeptyd, oczyszczony lub izolowany polinukleotyd, wektor, wektor ekspresyjny, komórka gospodarza, sposób wytwarzania polipeptydu, sposoby identyfikowania czynnika obniżającego, modulującego lub hamującego aktywność, zastosowanie takiego czynnika, izolowany kwas nukleinowy, obejmujący go wektor i ich zastosowanie, sposoby zmniejszania komórkowego wytwarzania beta amyloidu i zastosowanie antysensownego reagenta
GB2364059B (en) 1999-02-10 2004-01-14 Elan Pharm Inc Beta-Secretase enzyme compositions and methods
JP2002539260A (ja) * 1999-03-24 2002-11-19 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア アスパルチルプロテアーゼインヒビターを使用して神経変性障害を処置する方法
WO2001010387A2 (en) 1999-08-09 2001-02-15 Vanderbilt University Antiviral therapy use of p-glycoprotein modulators
WO2001023533A2 (en) 1999-09-23 2001-04-05 Pharmacia & Upjohn Company Alzheimer's disease secretase, app substrates therefor, and uses therefor
JP2003520266A (ja) 2000-01-24 2003-07-02 メルク シャープ エンド ドーム リミテッド γ−セクレターゼ阻害薬
GB0005251D0 (en) 2000-03-03 2000-04-26 Merck Sharp & Dohme Therapeutic compounds
DE60124080T2 (de) * 2000-03-23 2007-03-01 Elan Pharmaceuticals, Inc., San Francisco Verbindungen und verfahren zur behandlung der alzheimerschen krankheit
JP2004502664A (ja) 2000-06-30 2004-01-29 イーラン　ファーマスーティカルズ、インコーポレイテッド アルツハイマー病処置用化合物
MXPA03011046A (es) * 2001-06-01 2004-06-25 Elan Pharm Inc Hidroxialquilaminas.

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