CA2714654A1 - Chlorothiophene-amides as inhibitors of coagulation factors xa and thrombin - Google Patents

Chlorothiophene-amides as inhibitors of coagulation factors xa and thrombin Download PDF

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Publication number
CA2714654A1
CA2714654A1 CA2714654A CA2714654A CA2714654A1 CA 2714654 A1 CA2714654 A1 CA 2714654A1 CA 2714654 A CA2714654 A CA 2714654A CA 2714654 A CA2714654 A CA 2714654A CA 2714654 A1 CA2714654 A1 CA 2714654A1
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CA
Canada
Prior art keywords
alkyl
alkylene
unsubstituted
heterocyclyl
mono
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2714654A
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English (en)
French (fr)
Inventor
Markus Follmann
Volkmar Wehner
Jerome Meneyrol
Jean-Michel Altenburger
Frederic Petit
Gilbert Lassalle
Jean-Pascal Herault
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sanofi Aventis France
Original Assignee
Sanofi Aventis France
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sanofi Aventis France filed Critical Sanofi Aventis France
Publication of CA2714654A1 publication Critical patent/CA2714654A1/en
Abandoned legal-status Critical Current

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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)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CA2714654A 2008-02-21 2009-02-10 Chlorothiophene-amides as inhibitors of coagulation factors xa and thrombin Abandoned CA2714654A1 (en)

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 (1)

Publication Number Publication Date
CA2714654A1 true CA2714654A1 (en) 2009-08-27

Family

ID=39637695

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2714654A Abandoned CA2714654A1 (en) 2008-02-21 2009-02-10 Chlorothiophene-amides as inhibitors of coagulation factors xa and thrombin

Country Status (16)

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

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
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
EP4669644A1 (en) 2023-02-21 2025-12-31 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
WO2000075129A1 (en) * 1999-06-07 2000-12-14 Shire Biochem 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
CA2511500A1 (en) * 2002-12-24 2004-07-15 Daiichi Pharmaceutical Co., Ltd. Novel ethylenediamine derivatives
WO2007056056A2 (en) 2005-11-02 2007-05-18 Cytokinetics, Inc. Mitotic kinesin inhibitors

Also Published As

Publication number Publication date
CN102015675A (zh) 2011-04-13
WO2009103440A1 (en) 2009-08-27
CL2009000367A1 (es) 2009-06-26
PT2254881E (pt) 2012-12-10
AU2009217075B2 (en) 2013-05-16
AU2009217075A1 (en) 2009-08-27
EP2254881A1 (en) 2010-12-01
JP2011512368A (ja) 2011-04-21
EP2254881B1 (en) 2012-09-12
DK2254881T3 (da) 2012-12-10
PE20091729A1 (es) 2009-12-01
JP5422570B2 (ja) 2014-02-19
UY31666A1 (es) 2009-09-30
AR070441A1 (es) 2010-04-07
TW200948366A (en) 2009-12-01
PA8816101A1 (es) 2009-09-17
HK1156607A1 (en) 2012-06-15
ES2394550T3 (es) 2013-02-01
US8378092B2 (en) 2013-02-19
CN102015675B (zh) 2014-07-02
US20110112075A1 (en) 2011-05-12

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20140123

FZDE Discontinued

Effective date: 20160801