ZA200602448B - Thrombin receptor antagonists - Google Patents
Thrombin receptor antagonists Download PDFInfo
- Publication number
- ZA200602448B ZA200602448B ZA200602448A ZA200602448A ZA200602448B ZA 200602448 B ZA200602448 B ZA 200602448B ZA 200602448 A ZA200602448 A ZA 200602448A ZA 200602448 A ZA200602448 A ZA 200602448A ZA 200602448 B ZA200602448 B ZA 200602448B
- Authority
- ZA
- South Africa
- Prior art keywords
- compound represented
- pharmaceutically acceptable
- following structural
- structural formula
- alkyl
- Prior art date
Links
- 239000003856 thrombin receptor antagonist Substances 0.000 title description 12
- 150000001875 compounds Chemical class 0.000 claims description 110
- 229910052739 hydrogen Inorganic materials 0.000 claims description 43
- 150000003839 salts Chemical class 0.000 claims description 28
- 239000012453 solvate Substances 0.000 claims description 24
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 201000006474 Brain Ischemia Diseases 0.000 claims description 9
- 206010008120 Cerebral ischaemia Diseases 0.000 claims description 9
- 208000006011 Stroke Diseases 0.000 claims description 9
- 206010008118 cerebral infarction Diseases 0.000 claims description 9
- 208000027866 inflammatory disease Diseases 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- 208000007536 Thrombosis Diseases 0.000 claims description 6
- 208000000884 Airway Obstruction Diseases 0.000 claims description 5
- 206010006458 Bronchitis chronic Diseases 0.000 claims description 5
- 208000001132 Osteoporosis Diseases 0.000 claims description 5
- 206010063897 Renal ischaemia Diseases 0.000 claims description 5
- 206010006451 bronchitis Diseases 0.000 claims description 5
- 208000023819 chronic asthma Diseases 0.000 claims description 5
- 208000007451 chronic bronchitis Diseases 0.000 claims description 5
- 206010012601 diabetes mellitus Diseases 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 5
- 210000001035 gastrointestinal tract Anatomy 0.000 claims description 5
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- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 5
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- 102000003790 Thrombin receptors Human genes 0.000 claims description 3
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- QAOWNCQODCNURD-UHFFFAOYSA-M hydrogensulfate Chemical compound OS([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-M 0.000 claims description 2
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- 238000004519 manufacturing process Methods 0.000 claims 4
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- IMCGHZIGRANKHV-AJNGGQMLSA-N tert-butyl (3s,5s)-2-oxo-5-[(2s,4s)-5-oxo-4-propan-2-yloxolan-2-yl]-3-propan-2-ylpyrrolidine-1-carboxylate Chemical compound O1C(=O)[C@H](C(C)C)C[C@H]1[C@H]1N(C(=O)OC(C)(C)C)C(=O)[C@H](C(C)C)C1 IMCGHZIGRANKHV-AJNGGQMLSA-N 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 description 125
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P11/08—Bronchodilators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- Organic Chemistry (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
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| US10/671,216 US7488742B2 (en) | 2000-06-15 | 2003-09-25 | Thrombin receptor antagonists |
Publications (1)
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| ZA200602448B true ZA200602448B (en) | 2007-09-26 |
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| JP (1) | JP4694490B2 (https=) |
| KR (1) | KR20060128848A (https=) |
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| MX (1) | MXPA06003379A (https=) |
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| PE (1) | PE20050471A1 (https=) |
| RU (1) | RU2367660C9 (https=) |
| SG (1) | SG147466A1 (https=) |
| TW (1) | TWI331608B (https=) |
| WO (1) | WO2005030712A2 (https=) |
| ZA (1) | ZA200602448B (https=) |
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| US6346510B1 (en) | 1995-10-23 | 2002-02-12 | The Children's Medical Center Corporation | Therapeutic antiangiogenic endostatin compositions |
| US20040192753A1 (en) * | 2000-06-15 | 2004-09-30 | Samuel Chackalamannil | Methods of use of thrombin receptor antagonists |
| BRPI0309309B8 (pt) * | 2002-04-16 | 2021-05-25 | Merck Sharp & Dohme | antagonistas de receptor de trombina tricíclicos |
| ES2427166T3 (es) * | 2003-06-23 | 2013-10-29 | Ono Pharmaceutical Co., Ltd. | Compuesto heterocíclico tricíclico novedoso |
| CN1984905B (zh) * | 2004-05-28 | 2011-06-22 | 先灵公司 | 作为凝血酶受体拮抗剂的约束喜巴辛类似物 |
| US20060063930A1 (en) * | 2004-08-20 | 2006-03-23 | Agoston Gregory E | Compositions and methods comprising proteinase activated receptor antagonists |
| US8563511B2 (en) * | 2004-10-06 | 2013-10-22 | University Of Rochester | Treatment of pulmonary hypertension using an agent that inhibits a tissue factor pathway |
| US7488752B2 (en) * | 2004-10-08 | 2009-02-10 | Schering Corporation | Thrombin receptor antagonists |
| WO2006068164A1 (ja) * | 2004-12-22 | 2006-06-29 | Ono Pharmaceutical Co., Ltd. | 三環式化合物およびその用途 |
| CA2875768C (en) | 2005-01-14 | 2018-03-06 | George G. Wu | Process for the preparation of phosphonate compounds useful in the preparation of himbacine analogs |
| US7776889B2 (en) * | 2005-03-31 | 2010-08-17 | Schering Corporation | Spirocyclic thrombin receptor antagonists |
| WO2007075808A2 (en) * | 2005-12-20 | 2007-07-05 | Schering Corporation | Methods for preventing and/or treating a cell proliferative disorder |
| JP2009521458A (ja) * | 2005-12-22 | 2009-06-04 | シェーリング コーポレイション | トロンビン受容体アンタゴニストとしてのオキサゾロイソキノリン誘導体 |
| JP2009521472A (ja) * | 2005-12-22 | 2009-06-04 | シェーリング コーポレイション | 心肺手術の合併症の予防としてのトロンビンレセプターアンタゴニスト |
| AU2007243657A1 (en) * | 2006-03-29 | 2007-11-08 | Schering Corporation | Monocyclic and bicyclic himbacine derivatives useful as thrombin receptor antagonists |
| TW200812619A (en) * | 2006-04-06 | 2008-03-16 | Schering Corp | TRA combination therapies |
| US8003803B2 (en) * | 2006-04-13 | 2011-08-23 | Schering Corporation | Fused ring thrombin receptor antagonists |
| EP2032560B1 (en) * | 2006-06-29 | 2013-05-01 | Merck Sharp & Dohme Corp. | Substituted bicyclic and tricyclic thrombin receptor antagonists |
| TWI367112B (en) * | 2006-06-30 | 2012-07-01 | Schering Corp | Immediate-release tablet formulations of a thrombin receptor antagonist |
| DE102006036023A1 (de) * | 2006-08-02 | 2008-02-07 | Sanofi-Aventis | Imino-imidazo-pyridinderivate mit antithrombotischer Aktivität |
| TWI343262B (en) * | 2006-09-26 | 2011-06-11 | Schering Corp | Rapidly disintegrating lyophilized oral formulations of a thrombin receptor antagonist |
| EP2069326B1 (en) | 2006-10-04 | 2015-03-18 | Merck Sharp & Dohme Corp. | Bicyclic and tricyclic derivatives as thrombin receptor antagonists |
| EP2120879A2 (en) * | 2006-12-22 | 2009-11-25 | Schering Corporation | Disintegration promoters in solid dose wet granulation formulations |
| BRPI0809095A2 (pt) * | 2007-03-23 | 2014-09-09 | Schering Corp | Redução de eventos adversos após intervenção percutânea através de uso de um antagonista de receptor de trombina |
| SI2242740T1 (sl) | 2008-02-05 | 2013-03-29 | Sanofi | SF5-derivati kot PAR1 inhibitorji, njihova priprava in uporaba kot zdravila |
| RS52264B (sr) | 2008-02-05 | 2012-10-31 | Sanofi | Triazolopiridazini kao inhibitori par1, njihovo dobijanje i upotreba kao lekova |
| RU2494100C2 (ru) * | 2008-02-05 | 2013-09-27 | Санофи-Авентис | Соли триазолия в качестве ингибиторов par1, их получение и применение в качестве лекарственного средства |
| EP2438060B1 (en) | 2009-06-04 | 2013-10-02 | Merck Sharp & Dohme Corp. | Active metabolite of a thrombin receptor antagonist |
| JP2012529431A (ja) | 2009-06-08 | 2012-11-22 | メルク・シャープ・アンド・ドーム・コーポレーション | トロンビン受容体アンタゴニストおよびクロピドグレルの固定用量錠剤 |
| ES2532902T3 (es) | 2010-04-16 | 2015-04-01 | Sanofi | Piridil-vinil-pirroles tricíclicos como inhibidores de PAR1 |
| WO2011128420A1 (de) | 2010-04-16 | 2011-10-20 | Sanofi | Pyridyl-vinyl-pyrazolo-chinoline als par1-inhibitoren |
| WO2013134012A1 (en) | 2012-03-06 | 2013-09-12 | Merck Sharp & Dohme Corp. | Preparation and use of bicyclic himbacine derivatives as par-receptor antagonists |
| WO2015013083A1 (en) | 2013-07-22 | 2015-01-29 | Merck Sharp & Dohme Corp. | Co-crystal of the par-1 receptor antagonist vorapaxar and aspirin |
| WO2015026685A1 (en) * | 2013-08-22 | 2015-02-26 | Merck Sharp & Dohme Corp. | 7a-heterocycle substituted- 6, 6-difluoro bicyclic himbacine derivatives |
| EP3035928B1 (en) * | 2013-08-22 | 2023-10-18 | Merck Sharp & Dohme LLC | 3'-pyridyl substituted- 6,6-difluoro bicyclic himbacine derivatives |
| EP3035929B1 (en) * | 2013-08-22 | 2024-07-03 | Merck Sharp & Dohme LLC | 7a-amide substituted-6,6-difluoro bicyclic himbacine derivatives |
| WO2016114386A1 (ja) * | 2015-01-15 | 2016-07-21 | 国立研究開発法人国立精神・神経医療研究センター | 進行型免疫性脱髄疾患治療剤 |
| CN110407819B (zh) * | 2019-08-02 | 2020-06-26 | 牡丹江医学院 | 一种作为预防外科手术并发症的凝血酶受体拮抗剂 |
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| JP2000229961A (ja) * | 1998-12-11 | 2000-08-22 | Sagami Chem Res Center | ヒドロナフト［２，３−ｃ］フラン誘導体およびその製造方法 |
| US6063847A (en) * | 1997-11-25 | 2000-05-16 | Schering Corporation | Thrombin receptor antagonists |
| CZ298578B6 (cs) * | 1997-11-25 | 2007-11-14 | Schering Corporation | Heterocyklickou skupinou substituovaná tricyklická sloucenina a farmaceutický prostredek ji obsahující |
| AU6690001A (en) | 2000-06-15 | 2001-12-24 | Schering Corp | Thrombin receptor antagonists |
| US20040192753A1 (en) * | 2000-06-15 | 2004-09-30 | Samuel Chackalamannil | Methods of use of thrombin receptor antagonists |
| US7235567B2 (en) * | 2000-06-15 | 2007-06-26 | Schering Corporation | Crystalline polymorph of a bisulfate salt of a thrombin receptor antagonist |
| KR100960170B1 (ko) * | 2001-10-18 | 2010-05-26 | 쉐링 코포레이션 | 트롬빈 수용체 길항제로서의 힘바신 동족체 |
| BRPI0309309B8 (pt) * | 2002-04-16 | 2021-05-25 | Merck Sharp & Dohme | antagonistas de receptor de trombina tricíclicos |
| CN1984905B (zh) * | 2004-05-28 | 2011-06-22 | 先灵公司 | 作为凝血酶受体拮抗剂的约束喜巴辛类似物 |
| JP2008526254A (ja) * | 2005-01-14 | 2008-07-24 | シェーリング コーポレイション | ヒンバシン類似物のキラルプロパルギルアルコールおよびエステル中間体の調製 |
| CA2875768C (en) * | 2005-01-14 | 2018-03-06 | George G. Wu | Process for the preparation of phosphonate compounds useful in the preparation of himbacine analogs |
| US7541471B2 (en) * | 2005-01-14 | 2009-06-02 | Schering Corporation | Synthesis of himbacine analogs |
| WO2006076452A2 (en) * | 2005-01-14 | 2006-07-20 | Schering Corporation | An exo-selective synthesis of himbacine analogs |
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2008
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| US20090069383A1 (en) | 2009-03-12 |
| CN101128457A (zh) | 2008-02-20 |
| EP1663965B1 (en) | 2014-04-09 |
| US20040152736A1 (en) | 2004-08-05 |
| MY143834A (en) | 2011-07-15 |
| WO2005030712A8 (en) | 2007-12-21 |
| CA2540163C (en) | 2012-06-05 |
| CO5680428A2 (es) | 2006-09-29 |
| WO2005030712A2 (en) | 2005-04-07 |
| RU2367660C9 (ru) | 2010-08-10 |
| AU2004276327B2 (en) | 2010-10-07 |
| CA2540163A1 (en) | 2005-04-07 |
| JP2007523051A (ja) | 2007-08-16 |
| JP4694490B2 (ja) | 2011-06-08 |
| TW200524914A (en) | 2005-08-01 |
| TWI331608B (en) | 2010-10-11 |
| MXPA06003379A (es) | 2006-06-08 |
| IL174538A0 (en) | 2006-08-01 |
| RU2367660C2 (ru) | 2009-09-20 |
| US20090076088A1 (en) | 2009-03-19 |
| BRPI0414592A (pt) | 2006-11-07 |
| US7488742B2 (en) | 2009-02-10 |
| KR20060128848A (ko) | 2006-12-14 |
| NO20061797L (no) | 2006-05-19 |
| SG147466A1 (en) | 2008-11-28 |
| EP1663965A2 (en) | 2006-06-07 |
| AU2004276327A1 (en) | 2005-04-07 |
| WO2005030712A3 (en) | 2007-09-20 |
| RU2006113638A (ru) | 2007-11-10 |
| PE20050471A1 (es) | 2005-08-24 |
| AR045809A1 (es) | 2005-11-16 |
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