ATE177752T1 - Neue inhibitoren von faktor xa - Google Patents
Neue inhibitoren von faktor xaInfo
- Publication number
- ATE177752T1 ATE177752T1 AT94904466T AT94904466T ATE177752T1 AT E177752 T1 ATE177752 T1 AT E177752T1 AT 94904466 T AT94904466 T AT 94904466T AT 94904466 T AT94904466 T AT 94904466T AT E177752 T1 ATE177752 T1 AT E177752T1
- Authority
- AT
- Austria
- Prior art keywords
- factor
- novel compounds
- disclosed
- inhibitors
- new inhibitors
- Prior art date
Links
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
- C07K5/06008—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
- C07K5/0207—Peptides 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)4-C(=0), e.g. 'isosters', replacing two amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US99120492A | 1992-12-15 | 1992-12-15 |
Publications (1)
Publication Number | Publication Date |
---|---|
ATE177752T1 true ATE177752T1 (de) | 1999-04-15 |
Family
ID=25536978
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AT94904466T ATE177752T1 (de) | 1992-12-15 | 1993-12-15 | Neue inhibitoren von faktor xa |
Country Status (7)
Country | Link |
---|---|
US (2) | US5883077A (de) |
EP (1) | EP0675899B1 (de) |
JP (1) | JPH08504769A (de) |
AT (1) | ATE177752T1 (de) |
CA (1) | CA2151044A1 (de) |
DE (1) | DE69324041D1 (de) |
WO (1) | WO1994013693A1 (de) |
Families Citing this family (66)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6759384B1 (en) * | 1994-04-26 | 2004-07-06 | Aventis Pharmaceuticals Inc. | Factor Xa inhibitors |
US5696231A (en) * | 1994-12-21 | 1997-12-09 | Corvas International, Inc. | N-substituted glycine derivatives as enzyme inhibitors |
US6025472A (en) * | 1994-12-21 | 2000-02-15 | Corvas International, Inc. | N-substituted glycine derivatives as enzyme inhibitors |
ES2208737T3 (es) * | 1995-03-10 | 2004-06-16 | Berlex Laboratories, Inc. | Derivados de benzamidina, su preparacion y su utilizacion como anticoagulantes. |
US5691364A (en) * | 1995-03-10 | 1997-11-25 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
US5612363A (en) * | 1995-06-02 | 1997-03-18 | Berlex Laboratories, Inc. | N,N-di(aryl) cyclic urea derivatives as anti-coagulants |
US5612378A (en) * | 1995-06-06 | 1997-03-18 | 3-Dimensional Pharmaceuticals, Inc. | Bis-arylsulfonylaminobenzamide derivatives and the use thereof as factor Xa inhibitors |
US5741819A (en) * | 1995-06-07 | 1998-04-21 | 3-Dimensional Pharmaceuticals, Inc. | Arylsulfonylaminobenzene derivatives and the use thereof as factor Xa inhibitors |
US5919765A (en) * | 1995-06-07 | 1999-07-06 | Cor Therapeutics, Inc. | Inhibitors of factor XA |
US6022861A (en) * | 1995-06-07 | 2000-02-08 | Cor Therapeutics, Inc. | Ketoheterocyclic inhibitors of factor Xa |
US6046169A (en) * | 1995-06-07 | 2000-04-04 | Cor Therapeutics, Inc. | Inhibitors of factor XA |
US5721214A (en) * | 1995-06-07 | 1998-02-24 | Cor Therapeutics, Inc. | Inhibitors of factor Xa |
US6069130A (en) | 1995-06-07 | 2000-05-30 | Cor Therapeutics, Inc. | Ketoheterocyclic inhibitors of factor Xa |
US5849759A (en) * | 1995-12-08 | 1998-12-15 | Berlex Laboratories, Inc. | Naphthyl-substituted benzimidazole derivatives as anti-coagulants |
US5994375A (en) | 1996-02-12 | 1999-11-30 | Berlex Laboratories, Inc. | Benzamidine derivatives substituted by amino acid and hydroxy acid derivatives and their use as anti-coagulants |
HU222199B1 (hu) * | 1996-06-05 | 2003-05-28 | Gyógyszerkutató Intézet Kft. | Véralvadásgátló hatású peptid-aldehid-származékok és a vegyületeket tartalmazó gyógyszerkészítmények |
US6245743B1 (en) | 1996-06-05 | 2001-06-12 | Cor Therapeutics, Inc. | Inhibitors of factor Xa |
US5693641A (en) * | 1996-08-16 | 1997-12-02 | Berlex Laboratories Inc. | Bicyclic pyrimidine derivatives and their use as anti-coagulants |
US5753635A (en) * | 1996-08-16 | 1998-05-19 | Berlex Laboratories, Inc. | Purine derivatives and their use as anti-coagulants |
US6008234A (en) * | 1996-09-12 | 1999-12-28 | Berlex Laboratories, Inc. | Benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives and their use as anti-coagulants |
DE69717474T2 (de) | 1996-09-12 | 2003-06-26 | Schering Ag | Durch cyclische aminosäuren oder cyclische hydroxysäuren substituierte benzamidinderivate und deren verwendung als antikoagulantien |
US6004985A (en) * | 1996-10-09 | 1999-12-21 | Berlex Laboratories, Inc. | Thio acid derived monocylic N-heterocyclics as anticoagulants |
US6194435B1 (en) | 1996-10-11 | 2001-02-27 | Cor Therapeutics, Inc. | Lactams as selective factor Xa inhibitors |
US6262047B1 (en) | 1996-10-11 | 2001-07-17 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6369080B2 (en) | 1996-10-11 | 2002-04-09 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6063794A (en) | 1996-10-11 | 2000-05-16 | Cor Therapeutics Inc. | Selective factor Xa inhibitors |
EP0977772A1 (de) | 1997-04-14 | 2000-02-09 | Cor Therapeutics, Inc. | Selektive faktor xa-inhibitoren |
JP2002514214A (ja) | 1997-04-14 | 2002-05-14 | シーオーアール セラピューティクス インコーポレイテッド | 選択的Xa因子阻害剤 |
US6133256A (en) * | 1997-04-14 | 2000-10-17 | Cor Therapeutics Inc | Selective factor Xa inhibitors |
AU7603098A (en) * | 1997-06-06 | 1998-12-21 | Emory University | Exosite assay for anticoagulants |
US6228854B1 (en) | 1997-08-11 | 2001-05-08 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6333321B1 (en) | 1997-08-11 | 2001-12-25 | Cor Therapeutics, Inc. | Selective factor Xa inhibitors |
US6218382B1 (en) | 1997-08-11 | 2001-04-17 | Cor Therapeutics, Inc | Selective factor Xa inhibitors |
US6204384B1 (en) | 1997-11-26 | 2001-03-20 | Corvas International, Inc. | Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors (II) |
US6011047A (en) * | 1997-11-26 | 2000-01-04 | Corvas International Inc. | Substituted 3-amino-2-hydroxyphenylacetamide derivatives as enzyme inhibitors |
US6686364B2 (en) | 1997-12-08 | 2004-02-03 | Berlex Laboratories, Inc. | Benzamidine derivatives and their use as anti-coagulants |
US6140351A (en) * | 1997-12-19 | 2000-10-31 | Berlex Laboratories, Inc. | Ortho-anthranilamide derivatives as anti-coagulants |
DE69821985T2 (de) | 1997-12-19 | 2005-05-04 | Schering Ag | Ortho-anthranilamide derivate als antikoagulantien |
AP1224A (en) | 1998-03-19 | 2003-11-14 | Bristol Myers Squibb Co | Biphasic controlled release delivery system for high solubility pharmaceuticals and method. |
US6787612B1 (en) | 1998-07-24 | 2004-09-07 | Dendreon Corporation | Resin derivatization method and uses thereof |
US6262088B1 (en) | 1998-11-19 | 2001-07-17 | Berlex Laboratories, Inc. | Polyhydroxylated monocyclic N-heterocyclic derivatives as anti-coagulants |
US6127376A (en) * | 1998-12-04 | 2000-10-03 | Berlex Laboratories, Inc. | Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants |
CA2361428A1 (en) | 1999-02-11 | 2000-08-17 | Cor Therapeutics, Inc. | Inhibitors of factor xa |
US6350761B1 (en) | 1999-07-30 | 2002-02-26 | Berlex Laboratories, Inc. | Benzenamine derivatives as anti-coagulants |
US6677473B1 (en) | 1999-11-19 | 2004-01-13 | Corvas International Inc | Plasminogen activator inhibitor antagonists |
AU2001250783A1 (en) | 2000-02-29 | 2001-09-12 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
US7157596B2 (en) | 2000-09-08 | 2007-01-02 | Dendreon Corporation | Inhibitors of serine protease activity of matriptase or MTSP1 |
DE60122750T2 (de) | 2000-09-11 | 2006-12-21 | Genentech, Inc., South San Francisco | Amidin-Inhibitoren von Serin-Proteasen |
US7312235B2 (en) | 2001-03-30 | 2007-12-25 | Millennium Pharmaceuticals, Inc. | Benzamide inhibitors of factor Xa |
US6777431B2 (en) | 2001-07-13 | 2004-08-17 | Corvas International, Inc. | Non-convalent thrombin inhibitors |
WO2003010130A1 (en) * | 2001-07-24 | 2003-02-06 | Pharmacore, Inc. | Amino acid derivatives |
AU2003223702A1 (en) * | 2002-04-23 | 2003-11-10 | Vddi Pharmaceuticals | Inhibition of platelet aggregation |
US6872827B2 (en) | 2002-04-26 | 2005-03-29 | Chembridge Research Laboratories, Inc. | Somatostatin analogue compounds |
PT1569912E (pt) | 2002-12-03 | 2015-09-15 | Pharmacyclics Llc | Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia |
US7019019B2 (en) * | 2002-12-23 | 2006-03-28 | Dendreon Corporation | Matriptase inhibitors and methods of use |
CA2525854C (en) | 2003-05-20 | 2009-12-15 | Genentech, Inc. | Acylsulfamide inhibitors of factor viia |
JP2007500221A (ja) | 2003-05-20 | 2007-01-11 | ジェネンテック・インコーポレーテッド | 第VIIa因子のベンゾフラン阻害剤 |
ATE453626T1 (de) | 2003-10-09 | 2010-01-15 | Millennium Pharm Inc | Thioethersubstituierte benzamide als inhibitoren von faktor xa |
KR101195801B1 (ko) | 2004-06-18 | 2012-11-05 | 밀레니엄 파머슈티컬스 인코퍼레이티드 | Xa 인자 억제제 |
US7612089B2 (en) | 2004-11-19 | 2009-11-03 | Portola Pharmaceuticals, Inc. | Tetrahydroisoquinolines as factor Xa inhibitors |
WO2006063113A2 (en) | 2004-12-07 | 2006-06-15 | Portola Pharmaceuticals, Inc. | Ureas as factor xa inhibitors |
WO2007056517A2 (en) | 2005-11-08 | 2007-05-18 | Millennium Pharmaceuticals, Inc. | Pharmaceutical salts and polymorphs of n- (5-chl0r0-2-pyridinyl) -2- [ [4- [ (dimethylamino) iminomethyl] benzoyl] amino] -5-meth oxy-benzamide, a factor xa inhibitor |
CA2667488C (en) | 2006-11-02 | 2015-07-07 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing pharmaceutical salts of a factor xa inhibitor |
CN103153288B (zh) | 2010-07-09 | 2017-02-15 | 詹姆斯·特林卡·格林 | 用于包括瑞格列净的短半衰期药物的组合立即/延迟释放递送系统 |
EA036091B1 (ru) | 2014-08-20 | 2020-09-25 | Портола Фармасьютикалз, Инк. | ВОДНЫЕ СОСТАВЫ АНТИДОТОВ ФАКТОРА Xa (fXa) ДЛЯ ПРЕДУПРЕЖДЕНИЯ ИЛИ УМЕНЬШЕНИЯ КРОВОТЕЧЕНИЯ И ИХ ПРИМЕНЕНИЕ |
WO2017147522A1 (en) * | 2016-02-24 | 2017-08-31 | Portola Pharmaceuticals, Inc. | Lyophilized formulations for factor xa antidote |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4847201A (en) * | 1985-02-05 | 1989-07-11 | Cetus Corporation | DNA encoding for CSF-1 and accompanying recombinant systems |
US4882145A (en) * | 1986-12-09 | 1989-11-21 | Scripps Clinic And Research Foundation | T cell epitopes of the hepatitis B virus nucleocapsid protein |
US5187157A (en) * | 1987-06-05 | 1993-02-16 | Du Pont Merck Pharmaceutical Company | Peptide boronic acid inhibitors of trypsin-like proteases |
US5200510A (en) * | 1987-06-16 | 1993-04-06 | Zymogenetics, Inc. | Method for purifying factor viii:c, von willebrand factor and complexes thereof |
JPH075634B2 (ja) * | 1987-10-30 | 1995-01-25 | 日東紡績株式会社 | トリペプチド類及びこれを含有する抗プラスミン剤 |
US5141862A (en) * | 1990-04-17 | 1992-08-25 | Smithkline Beecham Corporation | Method of purifying tpa or plasminogen activator using a tripeptide of the formula: -X-Y-argininal wherein X and Y are selected from the group consisting of pro,phe,trp and tyr |
JPH0813834B2 (ja) * | 1990-08-01 | 1996-02-14 | 日東紡績株式会社 | トリペプチド誘導体及びそれを有効成分とする蛋白分解酵素阻害剤 |
US5283293A (en) * | 1990-12-14 | 1994-02-01 | Corvas, Inc. | Reagents for automated synthesis of peptide analogs |
US5367072A (en) * | 1990-12-14 | 1994-11-22 | Corvas International, Inc. | Reagents for automated synthesis of peptide analogs |
WO1993008211A1 (en) * | 1991-10-23 | 1993-04-29 | The Procter & Gamble Company | Tripeptide derivative anti-inflammatory agents |
AU1339092A (en) * | 1991-12-13 | 1993-07-19 | Corvas International, Inc. | Reagents for automated synthesis of peptide analogs |
US5534498A (en) * | 1992-01-30 | 1996-07-09 | Corvas International, Inc. | Trypsin inhibitors |
-
1993
- 1993-12-15 EP EP94904466A patent/EP0675899B1/de not_active Expired - Lifetime
- 1993-12-15 JP JP6514525A patent/JPH08504769A/ja not_active Ceased
- 1993-12-15 AT AT94904466T patent/ATE177752T1/de not_active IP Right Cessation
- 1993-12-15 DE DE69324041T patent/DE69324041D1/de not_active Expired - Lifetime
- 1993-12-15 US US08/168,964 patent/US5883077A/en not_active Expired - Lifetime
- 1993-12-15 WO PCT/US1993/012255 patent/WO1994013693A1/en active IP Right Grant
- 1993-12-15 CA CA002151044A patent/CA2151044A1/en not_active Abandoned
-
1995
- 1995-06-05 US US08/465,115 patent/US5739112A/en not_active Expired - Lifetime
Also Published As
Publication number | Publication date |
---|---|
JPH08504769A (ja) | 1996-05-21 |
WO1994013693A1 (en) | 1994-06-23 |
EP0675899B1 (de) | 1999-03-17 |
US5883077A (en) | 1999-03-16 |
EP0675899A4 (de) | 1996-01-24 |
CA2151044A1 (en) | 1994-06-23 |
EP0675899A1 (de) | 1995-10-11 |
US5739112A (en) | 1998-04-14 |
DE69324041D1 (de) | 1999-04-22 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |