CN1237978A - N－(芳基/杂芳基)氨基酸衍生物、包括这些衍生物的药用组合物以及用这些化合物抑制β－淀粉样肽释放和或其合成的方法 - Google Patents
N－(芳基/杂芳基)氨基酸衍生物、包括这些衍生物的药用组合物以及用这些化合物抑制β－淀粉样肽释放和或其合成的方法 Download PDFInfo
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- CN1237978A CN1237978A CN97199776A CN97199776A CN1237978A CN 1237978 A CN1237978 A CN 1237978A CN 97199776 A CN97199776 A CN 97199776A CN 97199776 A CN97199776 A CN 97199776A CN 1237978 A CN1237978 A CN 1237978A
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- Prior art keywords
- dichlorophenyl
- alanyl
- alkyl
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- heteroaryl
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- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- PTIBVSAWRDGWAE-UHFFFAOYSA-K trisodium;phosphate;heptahydrate Chemical class O.O.O.O.O.O.O.[Na+].[Na+].[Na+].[O-]P([O-])([O-])=O PTIBVSAWRDGWAE-UHFFFAOYSA-K 0.000 description 1
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- ORQXBVXKBGUSBA-QMMMGPOBSA-N β-cyclohexyl-alanine Chemical compound OC(=O)[C@@H](N)CC1CCCCC1 ORQXBVXKBGUSBA-QMMMGPOBSA-N 0.000 description 1
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)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75533496A | 1996-11-22 | 1996-11-22 | |
| US08/755,334 | 1996-11-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1237978A true CN1237978A (zh) | 1999-12-08 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN97199776A Pending CN1237978A (zh) | 1996-11-22 | 1997-11-20 | N－(芳基/杂芳基)氨基酸衍生物、包括这些衍生物的药用组合物以及用这些化合物抑制β－淀粉样肽释放和或其合成的方法 |
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) |
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN102532055A (zh) * | 2003-03-14 | 2012-07-04 | 匹兹堡大学联邦制高等教育 | 苯并噻唑衍生物化合物、组合物及用途 |
| US8691185B2 (en) | 2003-08-22 | 2014-04-08 | University of Pittsburgh—of the Commonwealth System of Higher Education | Benzothiazole derivative compounds, compositions and uses |
| US8911707B2 (en) | 2000-08-24 | 2014-12-16 | University of Pittsburgh—of the Commonwealth System of Higher Education | Thioflavin derivatives for use in antemortem diagnosis of alzheimer's disease and in vivo imaging and prevention of amyloid deposition |
| US9833458B2 (en) | 2000-08-24 | 2017-12-05 | University of Pittsburgh—of the Commonwealth System of Higher Education | Thioflavin derivatives for use in the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition |
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|---|---|---|---|---|
| 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 |
| US6486350B1 (en) | 1998-09-30 | 2002-11-26 | Elan Pharmaceuticals Inc. | Biological reagents and methods for determining the mechanism in the generation of β-amyloid peptide |
| 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 |
| AU778005B2 (en) | 1998-12-24 | 2004-11-11 | Bristol-Myers Squibb Pharma Company | Succinoylamino benzodiazepines as inhibitors of Abeta 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 |
| US6960576B2 (en) | 1999-09-13 | 2005-11-01 | Bristol-Myers Squibb Pharma Company | Hydroxyalkanoylaminolactams and related structures as inhibitors of Aβ 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$g(b) |
| WO2001060826A2 (fr) | 2000-02-17 | 2001-08-23 | Bristol-Myers Squibb Pharma Company | CARBOCYCLES ET HETEROCYCLES SUCCINOYLAMINO UTILISES EN TANT QU'INHIBITEURS DE LA PRODUCTION DE LA PROTEINE A$g(b) |
| US6713476B2 (en) | 2000-04-03 | 2004-03-30 | Dupont Pharmaceuticals Company | Substituted cycloalkyls as inhibitors of a beta protein production |
| MXPA02009755A (es) | 2000-04-03 | 2003-03-27 | Bristol Myers Squibb Pharma Co | Lactamas ciclicas como inhibidores de la produccion de proteina a-beta. |
| AU2001257006A1 (en) | 2000-04-11 | 2001-10-23 | Du Pont Pharmaceuticals Company | Substituted lactams as inhibitors of abeta protein production |
| 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 |
| IL147629A0 (en) | 2000-06-01 | 2002-08-14 | Bristol Myers Squibb Pharma Co | LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF Aβ PROTEIN PRODUCTION |
| US6432944B1 (en) | 2000-07-06 | 2002-08-13 | Bristol-Myers Squibb Company | Benzodiazepinone β-amyloid inhibitors: arylacetamidoalanyl derivatives |
| US6657070B2 (en) | 2000-12-13 | 2003-12-02 | Wyeth | Production of chirally pure α-amino acids and N-sulfonyl α-amino acids |
| SI1341779T1 (sl) | 2000-12-13 | 2006-12-31 | Wyeth Corp | Heterociklicni sulfonamidni inhibitorji produkcije beta amiloida |
| 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 |
| RU2342374C2 (ru) | 2003-03-31 | 2008-12-27 | Уайт | Фтор- и трифторалкилсодержащие гетероциклические сульфонамидные ингибиторы образования бета-амилоида и их производные |
| EP2511267A1 (fr) | 2003-06-05 | 2012-10-17 | Elan Pharmaceuticals Inc. | 3-((aminoacyl n-acylé)amino)pyrazoles comme inhibiteurs de la production de peptide beta-amyloide utiles pour le traitement de la maladie d'alzheimer |
| EP1709003B1 (fr) | 2004-01-16 | 2009-09-23 | Wyeth | Inhibiteurs a base de sulfonamides heterocycliques de la production des beta-amyloides contenant un azole |
| JP4805909B2 (ja) | 2004-03-03 | 2011-11-02 | スミスクライン ビーチャム コーポレーション | 選択的アンドロゲン受容体モジュレーターとしてのアニリン誘導体 |
| WO2006113552A2 (fr) * | 2005-04-15 | 2006-10-26 | Smithkline Beecham Corporation | Cyanoarylamines |
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2171882C (fr) * | 1993-10-01 | 2001-12-04 | Barbara Cordell | Inhibiteurs de la production de proteines de .beta.-amyloide |
| US5872101A (en) * | 1995-01-06 | 1999-02-16 | Sibia Neurosciences, Inc. | Methods of treating neurodegenerative disorders using protease inhibitors |
-
1997
- 1997-11-20 WO PCT/US1997/018704 patent/WO1998022493A2/fr not_active Application Discontinuation
- 1997-11-20 TR TR1999/01132T patent/TR199901132T2/xx unknown
- 1997-11-20 ID IDW990395A patent/ID22275A/id unknown
- 1997-11-20 JP JP52364998A patent/JP2001519769A/ja active Pending
- 1997-11-20 BR BR9714358A patent/BR9714358A/pt not_active IP Right Cessation
- 1997-11-20 CA CA002270876A patent/CA2270876A1/fr not_active Abandoned
- 1997-11-20 IL IL12947797A patent/IL129477A0/xx unknown
- 1997-11-20 NZ NZ335157A patent/NZ335157A/xx unknown
- 1997-11-20 HU HU0001383A patent/HUP0001383A3/hu unknown
- 1997-11-20 AU AU53543/98A patent/AU5354398A/en not_active Abandoned
- 1997-11-20 CN CN97199776A patent/CN1237978A/zh active Pending
- 1997-11-20 EP EP97950576A patent/EP0942923A2/fr not_active Withdrawn
-
1999
- 1999-05-20 NO NO992426A patent/NO992426L/no not_active Application Discontinuation
Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8911707B2 (en) | 2000-08-24 | 2014-12-16 | University of Pittsburgh—of the Commonwealth System of Higher Education | Thioflavin derivatives for use in antemortem diagnosis of alzheimer's disease and in vivo imaging and prevention of amyloid deposition |
| US9808541B2 (en) | 2000-08-24 | 2017-11-07 | University of Pittsburgh—Of the Commonwealth System of Higher Eduation | Thioflavin derivatives for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition |
| US9833458B2 (en) | 2000-08-24 | 2017-12-05 | University of Pittsburgh—of the Commonwealth System of Higher Education | Thioflavin derivatives for use in the antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition |
| US10137210B2 (en) | 2000-08-24 | 2018-11-27 | The University of Pittsburgh—Of the Commonwealth System of Higher Education | Thioflavin derivatives for use in antemortem diagnosis of Alzheimer's disease and in vivo imaging and prevention of amyloid deposition |
| CN102532055A (zh) * | 2003-03-14 | 2012-07-04 | 匹兹堡大学联邦制高等教育 | 苯并噻唑衍生物化合物、组合物及用途 |
| CN102532055B (zh) * | 2003-03-14 | 2016-05-11 | 匹兹堡大学联邦制高等教育 | 苯并噻唑衍生物化合物、组合物及用途 |
| US8691185B2 (en) | 2003-08-22 | 2014-04-08 | University of Pittsburgh—of the Commonwealth System of Higher Education | Benzothiazole derivative compounds, compositions and uses |
| US9134328B2 (en) | 2003-08-22 | 2015-09-15 | University of Pittsburgh—of the Commonwealth System of Higher Education | Methods of using benzothiazole derivative compounds and compositions |
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| IL129477A0 (en) | 2000-02-29 |
| ID22275A (id) | 1999-09-23 |
| TR199901132T2 (xx) | 1999-08-23 |
| HUP0001383A1 (hu) | 2001-05-28 |
| CA2270876A1 (fr) | 1998-05-28 |
| AU5354398A (en) | 1998-06-10 |
| WO1998022493A2 (fr) | 1998-05-28 |
| HUP0001383A3 (en) | 2001-11-28 |
| NO992426L (no) | 1999-06-30 |
| NZ335157A (en) | 2001-01-26 |
| BR9714358A (pt) | 2000-03-21 |
| JP2001519769A (ja) | 2001-10-23 |
| NO992426D0 (no) | 1999-05-20 |
| EP0942923A2 (fr) | 1999-09-22 |
| WO1998022493A3 (fr) | 1998-07-23 |
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