BRPI0410446A - derivados de benzimidazol como inibidores de fator xa - Google Patents

derivados de benzimidazol como inibidores de fator xa

Info

Publication number
BRPI0410446A
BRPI0410446A BRPI0410446-3A BRPI0410446A BRPI0410446A BR PI0410446 A BRPI0410446 A BR PI0410446A BR PI0410446 A BRPI0410446 A BR PI0410446A BR PI0410446 A BRPI0410446 A BR PI0410446A
Authority
BR
Brazil
Prior art keywords
factor
inhibitors
formula
compounds
benzimidazole derivatives
Prior art date
Application number
BRPI0410446-3A
Other languages
English (en)
Inventor
Marc Nazare
Michael Wagner
Volkmar Wehner
Hans Matter
Matthias Urmann
Kurt Ritter
Original Assignee
Sanofi Aventis Deutschland
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33040952&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0410446(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Sanofi Aventis Deutschland filed Critical Sanofi Aventis Deutschland
Publication of BRPI0410446A publication Critical patent/BRPI0410446A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • 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
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • C07D473/08—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1 and 3, e.g. theophylline
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

"DERIVADOS DE BENZIMIDAZOL COMO INIBIDORES DE FATOR Xa". A presente invenção refere-se um composto s da fórmula 1, onde R¬ 0¬, R¬ 1¬, R¬ 2¬, Q, V, G e M têm os significados indicados nas reivindicações. Os compostos da fórmula 1 são compostos farmacologicamente ativos valiosos. Eles exibem um efeito antitrombótico forte e são úteis, por exemplo, para a terapia e profilaxia de distúrbios cardiovasculares tipo restenoses ou doenças tromboembólicas. Eles são inibidores reversíveis fator Xa de enzimas de coagulação sangüínea (FXa) e/ou fator Vila (FVlla), e podem em geral ser aplicados em condições nas quais uma atividade indesejada de fator Xa e/ou fator Vlla está presente ou para a cura ou prevenção da qual uma inibição de fator Xa e/ou fator Vila é pretendida. A invenção também refere-se a processos para a preparação de compostos da fórmula 1, seu uso, em particular como ingredientes ativos em produtos farmacêuticos, e preparações farmacêuticas compreendendo-os.
BRPI0410446-3A 2003-05-19 2004-05-05 derivados de benzimidazol como inibidores de fator xa BRPI0410446A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP03011305A EP1479676A1 (en) 2003-05-19 2003-05-19 Benzimidazole-derivatives as factor xa inhibitors
PCT/EP2004/004750 WO2004101553A1 (en) 2003-05-19 2004-05-05 BENZIMIDAZOLE-DERIVATIVES AS FACTOR Xa INHIBITORS

Publications (1)

Publication Number Publication Date
BRPI0410446A true BRPI0410446A (pt) 2006-06-06

Family

ID=33040952

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0410446-3A BRPI0410446A (pt) 2003-05-19 2004-05-05 derivados de benzimidazol como inibidores de fator xa

Country Status (29)

Country Link
EP (2) EP1479676A1 (pt)
JP (1) JP4658940B2 (pt)
KR (1) KR20060014056A (pt)
CN (2) CN100484935C (pt)
AR (1) AR045683A1 (pt)
AT (1) ATE474838T1 (pt)
AU (1) AU2004238497B2 (pt)
BR (1) BRPI0410446A (pt)
CA (1) CA2526065A1 (pt)
CL (1) CL2004001078A1 (pt)
CR (1) CR8087A (pt)
DE (1) DE602004028240D1 (pt)
EC (1) ECSP056178A (pt)
MA (1) MA27798A1 (pt)
MX (1) MXPA05012231A (pt)
NO (1) NO20055910L (pt)
NZ (1) NZ543670A (pt)
OA (1) OA13168A (pt)
PA (1) PA8603501A1 (pt)
PE (1) PE20050198A1 (pt)
RS (1) RS20050856A (pt)
RU (1) RU2346944C2 (pt)
SA (1) SA04250196B1 (pt)
TN (1) TNSN05297A1 (pt)
TW (1) TW200503696A (pt)
UA (1) UA82100C2 (pt)
UY (1) UY28324A1 (pt)
WO (1) WO2004101553A1 (pt)
ZA (1) ZA200508151B (pt)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10342570A1 (de) * 2003-09-15 2005-04-14 Bayer Healthcare Ag Verfahren zur Herstellung von 4-(4-Aminophenyl)-3-morpholinon
EP1742637A4 (en) * 2004-04-23 2011-06-08 Paratek Pharm Innc TRANSCRIPTION FACTOR MODULATION COMPOUNDS AND METHODS OF USE
WO2008033739A2 (en) * 2006-09-12 2008-03-20 Neurogen Corporation Benzimidazole carboxamide derivatives
DE102010018299A1 (de) 2010-04-23 2011-10-27 Archimica Gmbh Verfahren zur Herstellung von 4-(4-Aminophenyl)-morpholin-3-on
EP3085700B1 (en) * 2013-12-20 2018-10-31 Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China Novel piperidine carboxamide compound, preparation method, and usage thereof
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
JP7050165B2 (ja) 2018-02-26 2022-04-07 ギリアード サイエンシーズ， インコーポレイテッド Ｈｂｖ複製阻害剤としての置換ピロリジン化合物

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GB1377642A (en) * 1971-01-14 1974-12-18 Koninklijke Gist Spiritus Penicillanic and cephalosporanic acid derivatives
US4269846A (en) * 1979-10-29 1981-05-26 Usv Pharmaceutical Corporation Heterocyclic compounds useful as anti-allergy agents
JPH0784462B2 (ja) * 1986-07-25 1995-09-13 日清製粉株式会社 ベンゾイミダゾ−ル誘導体
US4897401A (en) * 1987-06-19 1990-01-30 Janssen Pharmaceutical N.V. N-(4-piperidinyl) bicyclic condensed 2-imidazolamine derivatives useful in treating allergic diseases
DE3828537A1 (de) * 1988-08-23 1990-03-01 Basf Ag Neue n-substituierte benzimidazol-2-carbonsaeureanilide, deren verwendung als lichtschutzmittel, insbesondere polymere und diese anilide enthaltendes organisches material
JPH0324609A (ja) * 1989-06-21 1991-02-01 Mitsuba Electric Mfg Co Ltd Ｉ／ｏ用バッファｉｃ
JPH03184043A (ja) * 1989-12-14 1991-08-12 Fuji Photo Film Co Ltd ハロゲン化銀カラー写真感光材料
KR100190299B1 (ko) * 1990-07-19 1999-06-01 디르크 반테 신규한 옥사졸릴 유도체
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Also Published As

Publication number Publication date
NO20055910L (no) 2006-02-10
CL2004001078A1 (es) 2005-04-08
ECSP056178A (es) 2006-08-30
CN1791598A (zh) 2006-06-21
JP4658940B2 (ja) 2011-03-23
CR8087A (es) 2006-09-22
SA04250196B1 (ar) 2008-11-18
MXPA05012231A (es) 2006-08-18
TW200503696A (en) 2005-02-01
HK1089174A1 (zh) 2006-11-24
UY28324A1 (es) 2004-12-31
CN101139346A (zh) 2008-03-12
MA27798A1 (fr) 2006-03-01
AU2004238497A1 (en) 2004-11-25
KR20060014056A (ko) 2006-02-14
WO2004101553A1 (en) 2004-11-25
PE20050198A1 (es) 2005-04-25
EP1479676A1 (en) 2004-11-24
EP1636216A1 (en) 2006-03-22
EP1636216B1 (en) 2010-07-21
OA13168A (en) 2006-12-13
UA82100C2 (uk) 2008-03-11
RU2346944C2 (ru) 2009-02-20
ATE474838T1 (de) 2010-08-15
PA8603501A1 (es) 2004-11-26
TNSN05297A1 (en) 2007-07-10
AR045683A1 (es) 2005-11-09
WO2004101553B1 (en) 2005-03-03
CA2526065A1 (en) 2004-11-25
CN100484935C (zh) 2009-05-06
NZ543670A (en) 2008-09-26
ZA200508151B (en) 2007-02-28
RU2005139555A (ru) 2006-06-10
DE602004028240D1 (de) 2010-09-02
AU2004238497B2 (en) 2010-07-22
JP2006528213A (ja) 2006-12-14
RS20050856A (sr) 2007-11-15

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Legal Events

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 8A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2144 DE 07/02/2012.