CA2270876A1 - Derives de n-(aryl/heteroaryl) aminoacide, compositions pharmaceutiques les contenant et procedes permettant d'inhiber la liberation de peptide .beta. amyloide et/ou sa synthese al'aide de ces composes - Google Patents

Derives de n-(aryl/heteroaryl) aminoacide, compositions pharmaceutiques les contenant et procedes permettant d'inhiber la liberation de peptide .beta. amyloide et/ou sa synthese al'aide de ces composes Download PDF

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Publication number
CA2270876A1
CA2270876A1 CA002270876A CA2270876A CA2270876A1 CA 2270876 A1 CA2270876 A1 CA 2270876A1 CA 002270876 A CA002270876 A CA 002270876A CA 2270876 A CA2270876 A CA 2270876A CA 2270876 A1 CA2270876 A1 CA 2270876A1
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CA
Canada
Prior art keywords
dichlorophenyl
alanyl
group
methyl ester
alkyl
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002270876A
Other languages
English (en)
Inventor
James E. Audia
Beverly K. Folmer
Varghese John
Lee H. Latimer
Jeffrey S. Nissen
Warren J. Porter
Eugene D. Thorsett
Jing Wu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Elan Pharmaceuticals LLC
Eli Lilly and Co
Original Assignee
Individual
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 Individual filed Critical Individual
Publication of CA2270876A1 publication Critical patent/CA2270876A1/fr
Abandoned legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Public Health (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

L'invention a trait à des composés inhibant la libération de peptide .beta.-amyloïde et ou sa synthèse et, de ce fait, se révélant utiles s'agissant de traiter la maladie d'Alzheimer. Elle a également trait à des compositions pharmaceutiques contenant un composé inhibant la libération de peptide .beta.-amyloïde et ou sa synthèse ainsi qu'à des méthodes de traitement de la maladie d'Alzheimer, tant au plan prophylactique que thérapeutique, ces méthodes faisant intervenir lesdites compositions pharmaceutiques.
CA002270876A 1996-11-22 1997-11-20 Derives de n-(aryl/heteroaryl) aminoacide, compositions pharmaceutiques les contenant et procedes permettant d'inhiber la liberation de peptide .beta. amyloide et/ou sa synthese al'aide de ces composes Abandoned CA2270876A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US75533496A 1996-11-22 1996-11-22
US08/755,334 1996-11-22
PCT/US1997/018704 WO1998022493A2 (fr) 1996-11-22 1997-11-20 DERIVES DE N-(ARYL/HETEROARYL) AMINOACIDE, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT ET PROCEDES PERMETTANT D'INHIBER LA LIBERATION DE PEPTIDE β AMYLOIDE ET/OU SA SYNTHESE A L'AIDE DE CES COMPOSES

Publications (1)

Publication Number Publication Date
CA2270876A1 true CA2270876A1 (fr) 1998-05-28

Family

ID=25038718

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002270876A Abandoned CA2270876A1 (fr) 1996-11-22 1997-11-20 Derives de n-(aryl/heteroaryl) aminoacide, compositions pharmaceutiques les contenant et procedes permettant d'inhiber la liberation de peptide .beta. amyloide et/ou sa synthese al'aide de ces composes

Country Status (13)

Country Link
EP (1) EP0942923A2 (fr)
JP (1) JP2001519769A (fr)
CN (1) CN1237978A (fr)
AU (1) AU5354398A (fr)
BR (1) BR9714358A (fr)
CA (1) CA2270876A1 (fr)
HU (1) HUP0001383A3 (fr)
ID (1) ID22275A (fr)
IL (1) IL129477A0 (fr)
NO (1) NO992426L (fr)
NZ (1) NZ335157A (fr)
TR (1) TR199901132T2 (fr)
WO (1) WO1998022493A2 (fr)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ525513A (en) 1998-08-07 2004-09-24 Pont Pharmaceuticals Du Succinoylamino lactams as inhibitors of Abeta protein production
HRP990246A2 (en) 1998-08-07 2000-06-30 Du Pont Pharm Co Succinoylamino benzodiazepines as inhibitors of a beta protein production
EP1131634A2 (fr) 1998-09-30 2001-09-12 Elan Pharmaceuticals, Inc. Reactifs biologiques et procedes servant a determiner le mecanisme implique dans la generation du peptide beta-amyloide
US6737038B1 (en) 1998-11-12 2004-05-18 Bristol-Myers Squibb Company Use of small molecule radioligands to discover inhibitors of amyloid-beta peptide production and for diagnostic imaging
WO2000038618A2 (fr) 1998-12-24 2000-07-06 Du Pont Pharmaceuticals Company BENZODIAZEPINES SUCCINOYLAMINO UTILISEES COMME INHIBITEURS DE LA PRODUCTION DE PROTEINE A$g(b)
US6960576B2 (en) 1999-09-13 2005-11-01 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ protein production
US6503902B2 (en) 1999-09-13 2003-01-07 Bristol-Myers Squibb Pharma Company Hydroxyalkanoylaminolactams and related structures as inhibitors of a β protein production
EP1222176A1 (fr) 1999-10-08 2002-07-17 Bristol-Myers Squibb Pharma Company AMINO SULFONAMIDES DE LACTAME UTILISES COMME INHIBITEURS DE LA PRODUCTION DE PROTEINE A$g(b)
CA2395862A1 (fr) 2000-02-17 2001-08-23 Hong Liu Carbocycles et heterocycles succinoylamino utilises en tant qu'inhibiteurs de la production de la proteine a.beta.
EP1268434A1 (fr) 2000-04-03 2003-01-02 Bristol-Myers Squibb Pharma Company Lactames cycliques utiles en tant qu'inhibiteurs de la production de proteine a-beta
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
WO2001077086A1 (fr) 2000-04-11 2001-10-18 Dupont Pharmaceuticals Company LACTAMES SUBSTITUES UTILISES EN TANT QU'INHIBITEURS DE PRODUCTION DE PROTEINE A$g(b)
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
CN1386118A (zh) 2000-06-01 2002-12-18 布里斯托尔-迈尔斯斯奎布药品公司 作为Aβ蛋白产生抑制剂的被环状琥珀酸酯取代的内酰胺类化合物
US6432944B1 (en) 2000-07-06 2002-08-13 Bristol-Myers Squibb Company Benzodiazepinone β-amyloid inhibitors: arylacetamidoalanyl derivatives
US7270800B2 (en) 2000-08-24 2007-09-18 University Of Pittsburgh Thioflavin derivatives for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition
RU2324686C2 (ru) 2000-08-24 2008-05-20 Юнивесити Оф Питсбэг ПРОИЗВОДНЫЕ ТИОФЛАВИНА, СВЯЗЫВАЮЩИЕ АМИЛОИД, СПОСОБ ОБНАРУЖЕНИЯ in vivo ОТЛОЖЕНИЙ АМИЛОИДА И СПОСОБ РАСПОЗНАВАНИЯ БОЛЕЗНИ АЛЬЦГЕЙМЕРА
JP2004517892A (ja) 2000-12-13 2004-06-17 ワイス β−アミロイド産生の複素環スルホンアミド阻害剤
US6657070B2 (en) 2000-12-13 2003-12-02 Wyeth Production of chirally pure α-amino acids and N-sulfonyl α-amino acids
CH698246B1 (de) * 2001-12-20 2009-06-30 Hoffmann La Roche Test zur Identifizierung von Inhibitoren von Beta-Sekretasen.
DE10306202A1 (de) 2003-02-13 2004-08-26 Grünenthal GmbH Arzneimittel enthaltend substituierte 2-Aryl-Aminoessigsäure-Verbindungen und/oder substituierte 2-Heteroaryl-Aminoessigsäure-Verbindungen
PT1611115E (pt) * 2003-03-14 2012-12-07 Univ Pittsburgh Compostos derivados de benzotiazole, composições e utilizações
KR20060002908A (ko) 2003-03-31 2006-01-09 와이어쓰 베타 아밀로이드 생산 억제제인 플루오로- 및트리플루오로알킬-함유 헤테로사이클릭 설폰아미드 및 이의유도체
JP4220548B2 (ja) 2003-06-05 2009-02-04 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 アシル化されたアミノ酸・アミジルピラゾール、および関連化合物
US8236282B2 (en) 2003-08-22 2012-08-07 University of Pittsburgh—of the Commonwealth System of Higher Education Benzothiazole derivative compounds, compositions and uses
DE602005016775D1 (de) 2004-01-16 2009-11-05 Wyeth Corp Heterocyclische, ein azol enthaltende sulfonamidinhibitoren der beta-amyloid-produktion
US7514470B2 (en) 2004-03-03 2009-04-07 Smithkline Beecham Corporation Aniline derivatives as selective androgen receptor modulators
JP2008536868A (ja) * 2005-04-15 2008-09-11 スミスクライン・ビーチャム・コーポレイション シアノアリールアミン
CN100999546B (zh) * 2007-01-11 2010-08-11 清华大学 具有含氮杂环修饰的多肽类化合物及其应用
WO2012172449A1 (fr) 2011-06-13 2012-12-20 Pfizer Inc. Lactames convenant comme inhibiteurs des bêta-sécrétases
CN111777571B (zh) * 2020-06-28 2023-07-11 武汉药明康德新药开发有限公司 一种手性2-氨基-3 -(1,3-苯并噻唑-2-基)丙酸盐酸盐的合成方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ274074A (en) * 1993-10-01 1997-11-24 Merrell Pharma Inc Various dipeptide derivatives having a reduced carboxy group, the aldehyde being optionally substituted; pharmaceutical compositions
US5863902A (en) * 1995-01-06 1999-01-26 Sibia Neurosciences, Inc. Methods of treating neurodegenerative disorders using protease inhibitors

Also Published As

Publication number Publication date
WO1998022493A3 (fr) 1998-07-23
CN1237978A (zh) 1999-12-08
WO1998022493A2 (fr) 1998-05-28
HUP0001383A3 (en) 2001-11-28
EP0942923A2 (fr) 1999-09-22
ID22275A (id) 1999-09-23
AU5354398A (en) 1998-06-10
JP2001519769A (ja) 2001-10-23
NZ335157A (en) 2001-01-26
IL129477A0 (en) 2000-02-29
NO992426L (no) 1999-06-30
HUP0001383A1 (hu) 2001-05-28
BR9714358A (pt) 2000-03-21
NO992426D0 (no) 1999-05-20
TR199901132T2 (xx) 1999-08-23

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FZDE Discontinued