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PE20091729A1 - CLOROTIOFENO-AMIDAS COMO INHIBIDORES DE LOS FACTORES DE COAGULACION Xa Y TROMBINA - Google Patents

CLOROTIOFENO-AMIDAS COMO INHIBIDORES DE LOS FACTORES DE COAGULACION Xa Y TROMBINA

Info

Publication number
PE20091729A1
PE20091729A1 PE2009000243A PE2009000243A PE20091729A1 PE 20091729 A1 PE20091729 A1 PE 20091729A1 PE 2009000243 A PE2009000243 A PE 2009000243A PE 2009000243 A PE2009000243 A PE 2009000243A PE 20091729 A1 PE20091729 A1 PE 20091729A1
Authority
PE
Peru
Prior art keywords
oxo
alkyl
methyl
chlorothiophene
amides
Prior art date
Application number
PE2009000243A
Other languages
English (en)
Inventor
Markus Follmann
Volkmar Wehner
Jerome Meneyrol
Jean-Michel Altenburger
Frederic Petit
Gilbert Lassalle
Jean-Pascal Herault
Original Assignee
Sanofi Aventis
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 filed Critical Sanofi Aventis
Publication of PE20091729A1 publication Critical patent/PE20091729A1/es

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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

Landscapes

  • 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)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE CLOROTIOFENO AMIDAS DE FORMULA (I) DONDE M ES TIOFENILO, X ES HALOGENO, METILO O ETINILO; R1, R2 Y R3 SON CADA UNO H, -O-ALQUILO(C1-C4), -O-FLUOROALQUILO(C1-C3), ENTRE OTROS; R4 Y R5 SON CADA UNO H, ALQUILO(C1-C6), ALQUILENO(C0-C6)-CICLOALQUILO(C3-C8), ENTRE OTROS; R13 Y R16 SON CADA UNO H, -OH U -O-ALQUILO(C1-C4). SON COMPUESTOS PREFERIDOS: [(S)-2-[2-CLORO-3-(2-OXO-PIPERIDIN-1-IL)-BENCENOSULFONILAMINO]-3-(4-METIL-PIPERAZIN-1-IL)-3-OXO-PROPIL]-AMIDA DEL ACIDO 5-CLORO-TIOFENO-2-CARBOXILICO, [(S)-2-[2-ETIL-3-(2-OXO-PIRROLIDIN-1-IL)-BENCENOSULFONILAMINO]-3-((S)-3-METIL-MORFOLIN-4-IL)-3-OXO-PROPIL]-AMIDA DEL ACIDO 5-CLORO-TIOFENO-2-CARBOXILICO, ENTRE OTROS. SE REFIERE TAMBIEN A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES REVERSIBLES DE LAS ENZIMAS DE COAGULACION SANGUINEA FACTOR Xa (FXa) Y TROMBINA SIENDO UTILES EN EL TRATAMIENTO DE ENFERMEDADES TROMBOEMBOLICAS O RESTENOSIS
PE2009000243A 2008-02-21 2009-02-19 CLOROTIOFENO-AMIDAS COMO INHIBIDORES DE LOS FACTORES DE COAGULACION Xa Y TROMBINA PE20091729A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08290279 2008-02-21

Publications (1)

Publication Number Publication Date
PE20091729A1 true PE20091729A1 (es) 2009-12-01

Family

ID=39637695

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2009000243A PE20091729A1 (es) 2008-02-21 2009-02-19 CLOROTIOFENO-AMIDAS COMO INHIBIDORES DE LOS FACTORES DE COAGULACION Xa Y TROMBINA

Country Status (17)

Country Link
US (1) US8378092B2 (es)
EP (1) EP2254881B1 (es)
JP (1) JP5422570B2 (es)
CN (1) CN102015675B (es)
AR (1) AR070441A1 (es)
AU (1) AU2009217075B2 (es)
CA (1) CA2714654A1 (es)
CL (1) CL2009000367A1 (es)
DK (1) DK2254881T3 (es)
ES (1) ES2394550T3 (es)
HK (1) HK1156607A1 (es)
PA (1) PA8816101A1 (es)
PE (1) PE20091729A1 (es)
PT (1) PT2254881E (es)
TW (1) TW200948366A (es)
UY (1) UY31666A1 (es)
WO (1) WO2009103440A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9346795B2 (en) 2011-05-25 2016-05-24 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
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
WO1998034935A1 (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
KR20050092373A (ko) 2002-12-24 2005-09-21 다이이찌 세이야꾸 가부시기가이샤 신규한 에틸렌디아민 유도체
JP2009514865A (ja) 2005-11-02 2009-04-09 サイトキネティクス・インコーポレーテッド 有糸分裂キネシン阻害剤

Also Published As

Publication number Publication date
TW200948366A (en) 2009-12-01
DK2254881T3 (da) 2012-12-10
US8378092B2 (en) 2013-02-19
ES2394550T3 (es) 2013-02-01
AR070441A1 (es) 2010-04-07
AU2009217075A1 (en) 2009-08-27
CN102015675B (zh) 2014-07-02
US20110112075A1 (en) 2011-05-12
UY31666A1 (es) 2009-09-30
HK1156607A1 (en) 2012-06-15
CA2714654A1 (en) 2009-08-27
JP2011512368A (ja) 2011-04-21
EP2254881B1 (en) 2012-09-12
EP2254881A1 (en) 2010-12-01
CL2009000367A1 (es) 2009-06-26
JP5422570B2 (ja) 2014-02-19
AU2009217075B2 (en) 2013-05-16
PA8816101A1 (es) 2009-09-17
PT2254881E (pt) 2012-12-10
CN102015675A (zh) 2011-04-13
WO2009103440A1 (en) 2009-08-27

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