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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Japan
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alkyl
alkylene
independently
unsubstituted
mmol
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JP2010547079A
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Japanese (ja)
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JP2011512368A5 (enExample
JP2011512368A (ja
Inventor
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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Sanofi SA
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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
    • 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
    • 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic 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
    • C07D333/26—Heterocyclic 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D333/40—Thiophene-2-carboxylic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • 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
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (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 2008-02-21
EP08290279.2 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)

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

Family

ID=39637695

Family Applications (1)

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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)

Country Link
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
CN103732589B (zh) 2011-05-25 2016-03-30 百时美施贵宝公司 可用作抗细胞凋亡bcl抑制剂的取代的磺酰胺
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
WO2014174102A1 (en) * 2013-04-26 2014-10-30 Sanofi Tartrate salt of 5-chloro-thiophene-2-carboxylic acid [(s)-2-[methyl-3-(2-oxo-pyrrolidin-1-yl)-benzenesulfonylamino]-3-(4-methyl piperazin-1 -yl)-3-oxo-propryl]amide
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
US10851051B2 (en) 2015-08-14 2020-12-01 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
CA2279927A1 (en) * 1997-02-06 1998-08-13 Merck & Co., Inc. Fibrinogen receptor antagonist prodrugs
WO2000075129A1 (en) * 1999-06-07 2000-12-14 Shire Biochem Inc. Thiophene integrin inhibitors
CA2392576A1 (en) 1999-11-24 2001-05-31 Lingyan Wang .beta.-amino acid-, aspartic acid- and diaminopropionic-based inhibitors of factor xa
GB0228552D0 (en) * 2002-12-06 2003-01-15 Glaxo Group Ltd Chemical compounds
CA2511500A1 (en) 2002-12-24 2004-07-15 Daiichi Pharmaceutical Co., Ltd. Novel ethylenediamine derivatives
US20070197640A1 (en) 2005-11-02 2007-08-23 Cytokinetics, Inc. Certain chemical entities, compositions, and methods

Also Published As

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

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