JP5422570B2 - 凝固第Xa因子及びトロンビンの阻害剤としてのクロロチオフェン−アミド類 - Google Patents

凝固第Xa因子及びトロンビンの阻害剤としてのクロロチオフェン−アミド類 Download PDF

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JP5422570B2
JP5422570B2 JP2010547079A JP2010547079A JP5422570B2 JP 5422570 B2 JP5422570 B2 JP 5422570B2 JP 2010547079 A JP2010547079 A JP 2010547079A JP 2010547079 A JP2010547079 A JP 2010547079A JP 5422570 B2 JP5422570 B2 JP 5422570B2
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alkyl
alkylene
independently
unsubstituted
mmol
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JP2011512368A5 (enExample
JP2011512368A (ja
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マルクス・フォールマン
フォルクマー・ヴェーナー
ジェローム・メネロール
ジャン−ミシェル・アルタンブルジェ
フレデリック・ペティ
ジルベール・ラサル
ジャン−パスカル・エロル
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Sanofi SA
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D333/40Thiophene-2-carboxylic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2010547079A 2008-02-21 2009-02-10 凝固第Xa因子及びトロンビンの阻害剤としてのクロロチオフェン−アミド類 Expired - Fee Related JP5422570B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08290279.2 2008-02-21
EP08290279 2008-02-21
PCT/EP2009/000903 WO2009103440A1 (en) 2008-02-21 2009-02-10 Chlorothiophene-amides as inhibitors of coagulation factors xa and thrombin

Publications (3)

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JP2011512368A JP2011512368A (ja) 2011-04-21
JP2011512368A5 JP2011512368A5 (enExample) 2012-03-29
JP5422570B2 true JP5422570B2 (ja) 2014-02-19

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JP2010547079A Expired - Fee Related JP5422570B2 (ja) 2008-02-21 2009-02-10 凝固第Xa因子及びトロンビンの阻害剤としてのクロロチオフェン−アミド類

Country Status (16)

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US (1) US8378092B2 (enExample)
EP (1) EP2254881B1 (enExample)
JP (1) JP5422570B2 (enExample)
CN (1) CN102015675B (enExample)
AR (1) AR070441A1 (enExample)
AU (1) AU2009217075B2 (enExample)
CA (1) CA2714654A1 (enExample)
CL (1) CL2009000367A1 (enExample)
DK (1) DK2254881T3 (enExample)
ES (1) ES2394550T3 (enExample)
PA (1) PA8816101A1 (enExample)
PE (1) PE20091729A1 (enExample)
PT (1) PT2254881E (enExample)
TW (1) TW200948366A (enExample)
UY (1) UY31666A1 (enExample)
WO (1) WO2009103440A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012162365A1 (en) 2011-05-25 2012-11-29 Bristol-Myers Squibb Company Substituted sulfonamides useful as antiapoptotic bcl inhibitors
CN102924442B (zh) * 2012-11-15 2014-10-29 沈阳药科大学 含有噻唑环的色满类化合物及其类似物和医药用途
KR102388926B1 (ko) * 2013-04-26 2022-04-22 베이징 리앤신 파마수티컬 씨오., 엘티디. 5-클로로-티오펜-2-카복실산 [(s)-2-[메틸-3-(2-옥소-피롤리딘-1-일)-벤젠설포닐아미노]-3-(4-메틸 피페라진-1-일)-3-옥소-프로필]아미드의 타르트레이트 염
CN104557928B (zh) * 2015-02-14 2016-08-24 佛山市赛维斯医药科技有限公司 一种含二环酰胺结构凝血因子Xa抑制剂、其制备方法及其用途
US9701671B2 (en) * 2015-02-20 2017-07-11 Canon Kabushiki Kaisha Organic compound, electrochromic element containing the same, optical filter, lens unit, imaging device, and window component
WO2017030987A1 (en) * 2015-08-14 2017-02-23 The Broad Institute, Inc. Compositions and methods for treating multiple myeloma
US20250002483A1 (en) 2021-09-03 2025-01-02 Bayer Aktiengesellschaft Substituted s-alaninate derivatives
WO2024175450A1 (en) 2023-02-21 2024-08-29 Bayer Aktiengesellschaft Substituted s-alaninate derivatives

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9322976D0 (en) * 1993-11-08 1994-01-05 Pfizer Ltd Therapeutic agents
US6313242B1 (en) * 1996-05-20 2001-11-06 Fina Technology, Inc. Stereorigid bis-fluorenyl metallocenes
JP2001512439A (ja) * 1997-02-06 2001-08-21 メルク エンド カンパニー インコーポレーテッド 線維素原受容体拮抗薬プロドラッグ
US6274620B1 (en) * 1999-06-07 2001-08-14 Biochem Pharma Inc. Thiophene integrin inhibitors
WO2001038309A1 (en) 1999-11-24 2001-05-31 Cor Therapeutics, Inc. β-AMINO ACID-, ASPARTIC ACID- AND DIAMINOPROPIONIC-BASED INHIBITORS OF FACTOR Xa
GB0228552D0 (en) * 2002-12-06 2003-01-15 Glaxo Group Ltd Chemical compounds
WO2004058728A1 (ja) 2002-12-24 2004-07-15 Daiichi Pharmaceutical Co., Ltd. 新規なエチレンジアミン誘導体
WO2007056056A2 (en) 2005-11-02 2007-05-18 Cytokinetics, Inc. Mitotic kinesin inhibitors

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Publication number Publication date
JP2011512368A (ja) 2011-04-21
UY31666A1 (es) 2009-09-30
CN102015675B (zh) 2014-07-02
EP2254881B1 (en) 2012-09-12
AU2009217075A1 (en) 2009-08-27
EP2254881A1 (en) 2010-12-01
CN102015675A (zh) 2011-04-13
HK1156607A1 (en) 2012-06-15
WO2009103440A1 (en) 2009-08-27
CL2009000367A1 (es) 2009-06-26
AR070441A1 (es) 2010-04-07
US20110112075A1 (en) 2011-05-12
US8378092B2 (en) 2013-02-19
DK2254881T3 (da) 2012-12-10
PA8816101A1 (es) 2009-09-17
PE20091729A1 (es) 2009-12-01
PT2254881E (pt) 2012-12-10
AU2009217075B2 (en) 2013-05-16
TW200948366A (en) 2009-12-01
CA2714654A1 (en) 2009-08-27
ES2394550T3 (es) 2013-02-01

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