PA8816101A1 - 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
PA8816101A1
PA8816101A1 PA20098816101A PA8816101A PA8816101A1 PA 8816101 A1 PA8816101 A1 PA 8816101A1 PA 20098816101 A PA20098816101 A PA 20098816101A PA 8816101 A PA8816101 A PA 8816101A PA 8816101 A1 PA8816101 A1 PA 8816101A1
Authority
PA
Panama
Prior art keywords
compounds
factor
formula
thrombin
present
Prior art date
Application number
PA20098816101A
Other languages
English (en)
Inventor
Jean-Michel Altenburger
Markus Follmann
Jean-Pascal Herault
Gilbert Lasalle
Jerome Meneyrol
Frederic Petit
Volkmar Wehner
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 PA8816101A1 publication Critical patent/PA8816101A1/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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Hematology (AREA)
  • Diabetes (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

LA PRESENTE INVENCIÓN SE REFIERE A COMPUESTOS DE LA FÒRMULA I, EN LA QUE R1; R2; R3; R4; R5; R13, R16, X Y M TIENEN LOS SIGNIFICADOS INDICADOS EN LAS REIVINDICACIONES. LOS COMPUESTOS DE LA FÓRMULA I SON COMPUESTOS FARMACOLÓGICAMENTE ACTIVOS VALIOSOS. PRESENTAN UN FUERTE EFECTO ANTITROMBÓTICO Y SON ADECUADOS, POR EJEMPLO, PARA LA TERAPIA Y PROFILAXIS DE TRASTORNOS CARDIOVASCULARES TALES COMO ENFERMEDADES TROMBOEMBÓLICAS O RESTENOSIS. SON INHIBIDORES REVERSIBLES DE LAS ENZIMAS DE COAGULACIÓN SANGUÍNEA FACTOR XA (FXA) Y TROMBINA Y EN GENERAL SE PUEDEN APLICAR EN ENFERMEDADES EN LAS QUE ESTÁ PRESENTE UNA ACTIVIDAD INDESEADA DEL FACTOR XA Y/O DE LA TROMBINA O EN LAS QUE PARA LA CURACIÓN O PREVENCIÓN DE LAS MISMAS SE INTENTA UNA INHIBICIÓN DEL FACTOR XA Y DE LA TROMBINA. LA INVENCIÓN SE REFIERE ADEMÁS A PROCEDIMIENTOS PARA LA PREPARACIÓN DE COMPUESTOS DE LA FÓRMULA I, A SU USO, EN PARTICULAR COMO INGREDIENTES ACTIVOS EN PRODUCTOS FARMACÉUTICOS, Y A PREPARACIONES FARMACÉUTICAS QUE LOS CONTIENEN.
PA20098816101A 2008-02-21 2009-02-16 Clorotiofeno - amidas como inhibidores de los factores de coagulacion xa y trombina PA8816101A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PA8816101A1 true PA8816101A1 (es) 2009-09-17

Family

ID=39637695

Family Applications (1)

Application Number Title Priority Date Filing Date
PA20098816101A PA8816101A1 (es) 2008-02-21 2009-02-16 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
EP2714681B1 (en) 2011-05-25 2015-06-24 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
JP6393310B2 (ja) 2013-04-26 2018-09-19 サノフイＳａｎｏｆｉ ５−クロロ−チオフェン−２−カルボン酸［（ｓ）−２−［メチル−３−（２−オキソ−ピロリジン−１−イル）−ベンゼンスルホニルアミノ］−３−（４−メチル−ピペラジン−１−イル）−３−オキソ−プロプリル］アミドの酒石酸塩
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
JP7546172B2 (ja) 2021-09-03 2024-09-05 バイエル・アクチエンゲゼルシヤフト 置換ｓ－アラニナート誘導体
WO2024175450A1 (en) 2023-02-21 2024-08-29 Bayer Aktiengesellschaft Substituted s-alaninate derivatives

Family Cites Families (8)

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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
AU5379900A (en) * 1999-06-07 2000-12-28 Shire Biochem Inc. Thiophene integrin inhibitors
AU1770001A (en) 1999-11-24 2001-06-04 Cor Therapeutics, Inc. Beta-amino acid-, aspartic acid- and diaminopropionic-based inhibitors of factorxa
GB0228552D0 (en) 2002-12-06 2003-01-15 Glaxo Group Ltd Chemical compounds
ZA200504813B (en) 2002-12-24 2006-10-25 Daiichi Seiyaku Co Novel ethylenediamine derivatives
WO2007056056A2 (en) 2005-11-02 2007-05-18 Cytokinetics, Inc. Mitotic kinesin inhibitors

Also Published As

Publication number Publication date
WO2009103440A1 (en) 2009-08-27
EP2254881A1 (en) 2010-12-01
EP2254881B1 (en) 2012-09-12
US8378092B2 (en) 2013-02-19
JP2011512368A (ja) 2011-04-21
AU2009217075A1 (en) 2009-08-27
CA2714654A1 (en) 2009-08-27
JP5422570B2 (ja) 2014-02-19
CN102015675A (zh) 2011-04-13
US20110112075A1 (en) 2011-05-12
CN102015675B (zh) 2014-07-02
HK1156607A1 (en) 2012-06-15
ES2394550T3 (es) 2013-02-01
PE20091729A1 (es) 2009-12-01
AU2009217075B2 (en) 2013-05-16
TW200948366A (en) 2009-12-01
CL2009000367A1 (es) 2009-06-26
DK2254881T3 (da) 2012-12-10
AR070441A1 (es) 2010-04-07
PT2254881E (pt) 2012-12-10
UY31666A1 (es) 2009-09-30

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