PE20040806A1 - COMPUESTOS HETEROBICICLOS NITROGENADOS SUSTITUIDOS COMO INHIBIDORES DEL FACTOR Xa - Google Patents

COMPUESTOS HETEROBICICLOS NITROGENADOS SUSTITUIDOS COMO INHIBIDORES DEL FACTOR Xa

Info

Publication number
PE20040806A1
PE20040806A1 PE2003001281A PE2003001281A PE20040806A1 PE 20040806 A1 PE20040806 A1 PE 20040806A1 PE 2003001281 A PE2003001281 A PE 2003001281A PE 2003001281 A PE2003001281 A PE 2003001281A PE 20040806 A1 PE20040806 A1 PE 20040806A1
Authority
PE
Peru
Prior art keywords
alkyl
carbonyl
chloro
substituted
benzimidazol
Prior art date
Application number
PE2003001281A
Other languages
English (en)
Inventor
Henning Priepke
Roland Pfau
Kai Gerlach
Uwe Ries
Wolfgang Wienen
Eckhart Bauer
Herbert Nar
Original Assignee
Boehringer Ingelheim Pharma
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 Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of PE20040806A1 publication Critical patent/PE20040806A1/es

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
    • C07D409/02—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
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 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
    • 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)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

SE REFIERE A HETEROBICICLOS NITROGENADOS SUSTITUIDOS DE FORMULA I, DONDE R1 ES AMINO, ALQUIL(C1-C5)-AMINO, CICLOALQUIL(C3-C7)-AMINO O (FENILALQUIL(C1-C3))-AMINO, QUE PUEDEN ESTAR SUSTITUIDOS POR ALQUILO(C1-C5) O ALQUIL(C1-C5)-CARBONILO EN EL NITROGENO AMINICO POR UN GRUPO FENILCARBONILO O FENILSULFONILO, CICLOALQUILENIMINOCARBONILO O CICLOAQUILENIMINOSULFONIO DE 4 A 7 MIEMBROS,ENTRE OTROS Y OPCIONALMENTE SUSTITUIDOS; R2 ES H, F, Cl, Br, ALQUILO C1-C3 QUE PUEDE ESTAR SUSTITUIDO POR F, ALQUENILO(C2-C3), ALQUINILO(C2-C3), ENTRE OTROS; R3 ES H O ALQUILO(C1-C3), R4 ES H O ALQUILO(C1-C5) LINEAL O RAMIFICADA, OPCIONALMENTE SUSTITUIDO POR F, ALQUENILO(C2-C3), ENTRE OTROS; R5 ES H O ALQUILO C1-C3; O BIEN R4 Y R5 JUNTO CON EL CARBONO AL QUE ESTAN UNIDOS FORMAN UN GRUPO CICLOALQUILO C3-C7; B PUEDE SER UN BENZIMIDAZOL, INDOL, BENZOTIAZOL, ENTRE OTROS; X1, X2 Y X3 SON N, OXIDO-N, CH SUSTITUIDO POR ALQUILO C1-C3, EN QUE AL MENOS UNO Y COMO MAXIMO DOS SON N. SON COMPUESTOS PREFERIDOS: 4-[(5-CLORO-1H-BENZIMIDAZOL-2-IL)-METILAMINO]-7-(PIRROLIDIN-1-IL-CARBONIL)-QUINOLINA, 6-CLORO-4-[C-(5-CLORO-1H-BENZIMIDAZOL-2-IL)-METILAMINO]-7-(PIRROLIDIN-1-IL-CARBONIL)-QUINAZOLINA, 4-[C-(5-CLORO-1H-BENZIMIDAZOL-2-IL)METILAMINO]-7-(PIRROLIDIN-1-IL-CARBONIL)-QUINAZOLINA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE ELABORACION, ESTOS COMPUESTOS SON INHIBIDORES DEL FACTOR Xa Y/O INHIBIDOR DE SERINA PROTEASA AMPARENTADAS Y PRESENTAN ACTIVIDAD ANTITROMBOTICA
PE2003001281A 2002-12-23 2003-12-12 COMPUESTOS HETEROBICICLOS NITROGENADOS SUSTITUIDOS COMO INHIBIDORES DEL FACTOR Xa PE20040806A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10260730A DE10260730A1 (de) 2002-12-23 2002-12-23 Neue substituierte stickstoffhaltige Heterobicyclen, deren Herstellung und deren Verwendung als Arzneimittel

Publications (1)

Publication Number Publication Date
PE20040806A1 true PE20040806A1 (es) 2004-12-23

Family

ID=32404214

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003001281A PE20040806A1 (es) 2002-12-23 2003-12-12 COMPUESTOS HETEROBICICLOS NITROGENADOS SUSTITUIDOS COMO INHIBIDORES DEL FACTOR Xa

Country Status (11)

Country Link
EP (1) EP1583757A1 (es)
JP (1) JP2006515301A (es)
AR (1) AR043685A1 (es)
AU (1) AU2003298192A1 (es)
CA (1) CA2511349A1 (es)
CL (1) CL2003002697A1 (es)
DE (1) DE10260730A1 (es)
PE (1) PE20040806A1 (es)
TW (1) TW200424194A (es)
UY (1) UY28143A1 (es)
WO (1) WO2004058743A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101087609B (zh) 2004-10-26 2012-11-14 詹森药业有限公司 因子Xa化合物
EP2220079A2 (en) 2007-11-15 2010-08-25 Boehringer Ingelheim International GmbH Substituted amides, manufacturing and use thereof as medicaments
CN103265524B (zh) * 2013-05-15 2016-01-20 华东师范大学 β-氨基-2,5-二氧六环内酯衍生物的制备方法

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9514265D0 (en) * 1995-07-13 1995-09-13 Wellcome Found Hetrocyclic compounds
PE121699A1 (es) * 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma Heterociclos biciclicos disustituidos como inhibidores de la trombina
US20030114448A1 (en) * 2001-05-31 2003-06-19 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
PE20040804A1 (es) * 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa

Also Published As

Publication number Publication date
TW200424194A (en) 2004-11-16
CL2003002697A1 (es) 2005-01-14
JP2006515301A (ja) 2006-05-25
CA2511349A1 (en) 2004-07-15
DE10260730A1 (de) 2004-07-01
WO2004058743A1 (de) 2004-07-15
EP1583757A1 (de) 2005-10-12
AU2003298192A1 (en) 2004-07-22
UY28143A1 (es) 2004-07-30
AR043685A1 (es) 2005-08-10

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