ATE190625T1 - Antagonisten gegen den thrombinrezeptor - Google Patents
Antagonisten gegen den thrombinrezeptorInfo
- Publication number
- ATE190625T1 ATE190625T1 AT93917028T AT93917028T ATE190625T1 AT E190625 T1 ATE190625 T1 AT E190625T1 AT 93917028 T AT93917028 T AT 93917028T AT 93917028 T AT93917028 T AT 93917028T AT E190625 T1 ATE190625 T1 AT E190625T1
- Authority
- AT
- Austria
- Prior art keywords
- thrombin receptor
- hydrophobic radical
- linkages
- formula
- image
- Prior art date
Links
- 102000003790 Thrombin receptors Human genes 0.000 title abstract 2
- 108090000166 Thrombin receptors Proteins 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title 1
- 230000002209 hydrophobic effect Effects 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 2
- 108090000190 Thrombin Proteins 0.000 abstract 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000006350 alkyl thio alkyl group Chemical group 0.000 abstract 1
- 125000003275 alpha amino acid group Chemical group 0.000 abstract 1
- 150000001413 amino acids Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 230000003197 catalytic effect Effects 0.000 abstract 1
- 230000001413 cellular effect Effects 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 125000001165 hydrophobic group Chemical group 0.000 abstract 1
- -1 hydroxy, amino Chemical group 0.000 abstract 1
- 230000002452 interceptive effect Effects 0.000 abstract 1
- 230000007935 neutral effect Effects 0.000 abstract 1
- 229960004072 thrombin Drugs 0.000 abstract 1
- 239000003856 thrombin receptor antagonist Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
-
- 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
- C07K5/10—Tetrapeptides
- C07K5/1002—Tetrapeptides with the first amino acid being neutral
- C07K5/1016—Tetrapeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/02—Linear peptides containing at least one abnormal peptide link
-
- 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)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92234092A | 1992-07-30 | 1992-07-30 | |
| US8078893A | 1993-06-28 | 1993-06-28 | |
| PCT/US1993/006428 WO1994003479A1 (en) | 1992-07-30 | 1993-07-08 | Thrombin receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE190625T1 true ATE190625T1 (de) | 2000-04-15 |
Family
ID=26763931
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT93917028T ATE190625T1 (de) | 1992-07-30 | 1993-07-08 | Antagonisten gegen den thrombinrezeptor |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US5866681A (de) |
| EP (1) | EP0656008B1 (de) |
| JP (1) | JP2675438B2 (de) |
| AT (1) | ATE190625T1 (de) |
| AU (1) | AU669922B2 (de) |
| CA (1) | CA2140543C (de) |
| DE (1) | DE69328104T2 (de) |
| IL (1) | IL106197A (de) |
| SG (1) | SG49772A1 (de) |
| WO (1) | WO1994003479A1 (de) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6063847A (en) | 1997-11-25 | 2000-05-16 | Schering Corporation | Thrombin receptor antagonists |
| JP3449620B2 (ja) * | 1997-11-25 | 2003-09-22 | シェーリング コーポレイション | トロンビンレセプターアンタゴニスト |
| US6017890A (en) * | 1998-02-19 | 2000-01-25 | Ortho-Mcneil Pharmaceutical, Inc. | Azole peptidomimetics as thrombin receptor antagonists |
| ES2183515T3 (es) * | 1998-02-19 | 2003-03-16 | Ortho Mcneil Pharm Inc | Peptidomimeticos de azol utilizados como antagonistas del receptor de la trombina. |
| GB2356198A (en) | 1999-10-29 | 2001-05-16 | Merck & Co Inc | Isoxazole thrombin receptor antagonists |
| US6515023B2 (en) | 2000-01-31 | 2003-02-04 | Merck & Co., Inc. | Thrombin receptor antagonists |
| US6403612B2 (en) | 2000-01-31 | 2002-06-11 | Merck & Co., Inc. | Thrombin receptor antagonists |
| US7235567B2 (en) | 2000-06-15 | 2007-06-26 | Schering Corporation | Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist |
| MY130642A (en) | 2000-06-15 | 2007-07-31 | Schering Corp | Nor-seco himbacine derivatives useful as thrombin receptor antagonists |
| EP1343751A2 (de) | 2000-12-20 | 2003-09-17 | Bristol-Myers Squibb Company | Cyclische derivate als modulatoren der chemokinrezeptoraktivität |
| AU2002241724A1 (en) | 2000-12-20 | 2002-07-01 | Bristol-Myers Squibb Company | Diamines as modulators of chemokine receptor activity |
| US20040096443A1 (en) * | 2002-03-08 | 2004-05-20 | Traynelis Stephen Francis | Treatment of neurodegenerative diseases and conditions using par1 antagonists |
| JP4307260B2 (ja) | 2001-10-18 | 2009-08-05 | シェーリング コーポレイション | トロンビンレセプタアンタゴニストとしてのヒンバシン類似物 |
| IL164376A0 (en) * | 2002-04-03 | 2005-12-18 | Applied Research Systems | Ox4or binding agents, their preparation and pharmaceutical compositions containing them |
| NZ575139A (en) | 2002-04-16 | 2010-08-27 | Schering Corp | Tricyclic thrombin receptor antagonists |
| US7074765B2 (en) | 2003-05-01 | 2006-07-11 | The Regents Of The University Of Michigan | Synthetic peptide analogs of Arg-Pro-Pro-Gly-Phe as selective inhibitors of thrombin and thrombin activation of protease activated receptors 1 and 4 |
| ATE406366T1 (de) * | 2004-05-28 | 2008-09-15 | Schering Corp | Gehinderte himbacinanaloga als thrombinrezeptorantagonisten |
| EP2075250B1 (de) | 2004-10-08 | 2015-03-04 | Merck Sharp & Dohme Corp. | Thrombinrezeptorantagonisten |
| JP2008534604A (ja) | 2005-03-31 | 2008-08-28 | シェーリング コーポレイション | スピロ環式トロンビンレセプターアンタゴニスト |
| KR20080104352A (ko) | 2006-03-29 | 2008-12-02 | 쉐링 코포레이션 | 트롬빈 수용체 길항제로서 유용한 모노사이클릭 및 비사이클릭 힘바신 유도체 |
| JP2009533450A (ja) | 2006-04-13 | 2009-09-17 | シェーリング コーポレイション | 縮合環トロンビンレセプターアンタゴニスト |
| WO2008005262A1 (en) | 2006-06-29 | 2008-01-10 | Schering Corporation | Substituted bicyclic and tricyclic thrombin receptor antagonists |
| KR20090074219A (ko) | 2006-10-04 | 2009-07-06 | 쉐링 코포레이션 | 트롬빈 수용체 길항제로서의 비사이클릭 및 트리사이클릭 유도체 |
| MX2009010268A (es) * | 2007-03-23 | 2009-11-09 | Schering Corp | Reduccion de eventos adversos despues de intervencion percutanea mediante el uso de un antagonista del receptor de trombina. |
| US20090022729A1 (en) * | 2007-04-13 | 2009-01-22 | Nigel Mackman | Methods and compositions for treating cardiac dysfunctions |
| JP5504259B2 (ja) | 2008-05-19 | 2014-05-28 | メルク・シャープ・アンド・ドーム・コーポレーション | 第ixa因子阻害剤としての複素環式化合物 |
| WO2011017296A1 (en) | 2009-08-04 | 2011-02-10 | Schering Corporation | 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors |
| EP2335717A1 (de) | 2009-11-16 | 2011-06-22 | Institut National De La Recherche Agronomique | PAR-1-Antagonisten zur Verwendung bei der Behandlung oder Prävention von Influenzavirus-Typ-A-Infektionen |
| EP2822557B1 (de) | 2012-03-06 | 2017-08-23 | Merck Sharp & Dohme Corp. | Herstellung und verwendung bicyclischer himbacinderivate als par-rezeptor-antagonisten |
| WO2015026686A1 (en) | 2013-08-22 | 2015-02-26 | Merck Sharp & Dohme Corp. | 3'-pyridyl substituted- 6,6-difluoro bicyclic himbacine derivatives |
| EP3035929B1 (de) | 2013-08-22 | 2024-07-03 | Merck Sharp & Dohme LLC | 7a-amid-substituierte bicyclische 6,6-difluorhimbacinderivate |
| EP3035930A4 (de) | 2013-08-22 | 2017-03-08 | Merck Sharp & Dohme Corp. | 7a-heterocyclus-substituierte 6,6-difluor-bicyclus-himbacinderivate |
| EP3131897B8 (de) | 2014-04-16 | 2022-08-03 | Merck Sharp & Dohme LLC | Faktor-ixa-hemmer |
| CA3189771A1 (en) | 2020-07-22 | 2022-01-27 | Janssen Pharmaceutica Nv | Compounds useful as factor xia inhibitors |
| US11919881B2 (en) | 2021-03-18 | 2024-03-05 | Janssen Pharmaceutica Nv | Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors |
| US11814364B2 (en) | 2021-03-18 | 2023-11-14 | Janssen Pharmaceutica Nv | Pyridine N-oxide derivatives useful as factor XIa inhibitors |
| US11845748B2 (en) | 2021-03-18 | 2023-12-19 | Janssen Pharmaceutica Nv | Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors |
| US11897880B2 (en) | 2021-04-30 | 2024-02-13 | Janssen Pharmaceutica Nv | 7,8-dihydrobenzo[e]pyrido[3,4-c]azocine-2,5(3H,6H)-dione derivatives useful as a factor XIa inhibitors |
| US11958856B2 (en) | 2021-07-22 | 2024-04-16 | Janssen Pharmaceutica Nv | Substituted 1,2,3,8,9,9a-hexahydro-5H-pyrrolo[1,2-a]azepin-5-ones as factor XIa inhibitors |
| US12286429B2 (en) | 2021-07-22 | 2025-04-29 | Janssen Pharmaceutica Nv | 5-oxo-1,2,3,5,8,8a-hexahydroindolizine-3-carboxamide derivatives useful as a factor XIa inhibitors |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2589720A1 (fr) * | 1985-11-14 | 1987-05-15 | Aubaniac Jean | Ensemble prothetique pour l'articulation du genou |
| US4859609A (en) * | 1986-04-30 | 1989-08-22 | Genentech, Inc. | Novel receptors for efficient determination of ligands and their antagonists or agonists |
| US5352664A (en) * | 1986-10-31 | 1994-10-04 | Board Of Regents, The University Of Texas System | Thrombin derived polypeptides; compositions and methods for use |
| AU618029B2 (en) * | 1987-11-02 | 1991-12-12 | Imperial Chemical Industries Plc | Polypeptide compounds |
| US5318899A (en) * | 1989-06-16 | 1994-06-07 | Cor Therapeutics, Inc. | Platelet aggregation inhibitors |
| US5688768A (en) * | 1991-02-19 | 1997-11-18 | Cor Therapeutics, Inc. | Recombinant thrombin receptor and related pharmaceuticals |
| US5256766A (en) * | 1991-02-19 | 1993-10-26 | The Regents Of The University Of California | Recombinant thrombin receptor and related pharmaceuticals |
| JPH07507995A (ja) * | 1992-03-02 | 1995-09-07 | バイオジェン,インコーポレイテッド | トロンビンレセプターアンタゴニスト |
-
1993
- 1993-06-30 IL IL10619793A patent/IL106197A/en not_active IP Right Cessation
- 1993-07-08 AU AU46685/93A patent/AU669922B2/en not_active Ceased
- 1993-07-08 EP EP93917028A patent/EP0656008B1/de not_active Expired - Lifetime
- 1993-07-08 CA CA002140543A patent/CA2140543C/en not_active Expired - Fee Related
- 1993-07-08 DE DE69328104T patent/DE69328104T2/de not_active Expired - Fee Related
- 1993-07-08 SG SG1996005407A patent/SG49772A1/en unknown
- 1993-07-08 JP JP6505310A patent/JP2675438B2/ja not_active Expired - Fee Related
- 1993-07-08 WO PCT/US1993/006428 patent/WO1994003479A1/en not_active Ceased
- 1993-07-08 AT AT93917028T patent/ATE190625T1/de not_active IP Right Cessation
-
1995
- 1995-03-20 US US08/407,468 patent/US5866681A/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| SG49772A1 (en) | 1998-06-15 |
| JPH07506115A (ja) | 1995-07-06 |
| US5866681A (en) | 1999-02-02 |
| DE69328104D1 (de) | 2000-04-20 |
| EP0656008A1 (de) | 1995-06-07 |
| AU669922B2 (en) | 1996-06-27 |
| CA2140543C (en) | 2001-04-10 |
| IL106197A (en) | 1999-11-30 |
| EP0656008B1 (de) | 2000-03-15 |
| DE69328104T2 (de) | 2000-12-21 |
| JP2675438B2 (ja) | 1997-11-12 |
| CA2140543A1 (en) | 1994-02-17 |
| IL106197A0 (en) | 1994-05-30 |
| WO1994003479A1 (en) | 1994-02-17 |
| AU4668593A (en) | 1994-03-03 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| UEP | Publication of translation of european patent specification | ||
| REN | Ceased due to non-payment of the annual fee |