PE20010954A1 - BENZHIMIDAZOLES, ITS PREPARATION AND ITS USE AS MEDICINES - Google Patents

BENZHIMIDAZOLES, ITS PREPARATION AND ITS USE AS MEDICINES

Info

Publication number
PE20010954A1
PE20010954A1 PE2000001365A PE0013652000A PE20010954A1 PE 20010954 A1 PE20010954 A1 PE 20010954A1 PE 2000001365 A PE2000001365 A PE 2000001365A PE 0013652000 A PE0013652000 A PE 0013652000A PE 20010954 A1 PE20010954 A1 PE 20010954A1
Authority
PE
Peru
Prior art keywords
alkyl
preparation
benzhimidazoles
medicines
amidine
Prior art date
Application number
PE2000001365A
Other languages
Spanish (es)
Inventor
Wolfgang Wienen
Norbert Hauel
Henning Priepke
Uwe Ries
Jean Marie Stassen
Herbert Nar
Iris Kauffmann-Hefner
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 PE20010954A1 publication Critical patent/PE20010954A1/en

Links

Classifications

    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A BENCIMIDAZOLES DE FORMULA I, DONDE Ra ES ALQUILO C1-C3 SUSTITUIDO CON FLUOR, PIRROLIDINOCARBONILO, AMINO, ALQUILO C1-C3, ENTRE OTROS; Rb ES ALQUILO C1-C3; Rc ES AMIDINO, CIANO, 1,2,4-OXADIZOL-3-ILO SUSTITUIDO EN POSICION 5 POR ALQUILO C1-C3, FENILO; SON COMPUESTOS PREFERIDOS 2-[4-(N-FENILCARBONIL-AMIDINO)-FENILAMINOMETIL]-1-METIL-5-[1-(n-BUTILOXICARBONILMETILAMINO)-1-(PIRROLIDINOCARBONIL)-ETIL]BENCIMIDAZOL, 2-(4-AMIDINOFENILAMINOMETIL)-1-METIL-5-[1-(TETRAZOL-5-IL-METILAMINO)-1-(PIRROLIDINOCARBONIL)-ETIL]BENCIMIDAZOL, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS I PUEDEN SER UTILES COMO ANTITROMBOTICOSREFERS TO BENZYMIDAZOLES OF FORMULA I, WHERE Ra IS C1-C3 ALKYL SUBSTITUTE WITH FLUORINE, PYRROLIDINE CARBONYL, AMINE, C1-C3 ALKYL, AMONG OTHERS; Rb IS C1-C3 ALKYL; Rc IS AMIDINE, CYANE, 1,2,4-OXADIZOL-3-ILO SUBSTITUTED AT POSITION 5 BY C1-C3 ALKYL, PHENYL; PREFERRED COMPOUNDS ARE 2- [4- (N-PHENYLCARBONYL-AMIDINE) -PHENYLAMINOMETHYL] -1-METHYL-5- [1- (n-BUTYLOXYCARBONYLMETHYLAMINE) -1- (PYRROLIDINOCARBONYL) -ETHYL] BENZIMIDAZOLE, 2- (4-AMIDOMETHYLLINOPHENE ) -1-METHYL-5- [1- (TETRAZOL-5-IL-METHYLAMINE) -1- (PYRROLIDINE CARBONYL) -ETHYL] BENZIMIDAZOLE, AMONG OTHERS. IT ALSO REFERS TO A PROCEDURE FOR PREPARATION. COMPOUNDS I MAY BE USEFUL AS ANTI-THROMBOTICS

PE2000001365A 1999-12-23 2000-12-19 BENZHIMIDAZOLES, ITS PREPARATION AND ITS USE AS MEDICINES PE20010954A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE19962329A DE19962329A1 (en) 1999-12-23 1999-12-23 New substituted 2-(phenylaminomethyl)-benzimidazoles, used as thrombin inhibitors, serine protease inhibitors, antithrombotic agents and intermediates

Publications (1)

Publication Number Publication Date
PE20010954A1 true PE20010954A1 (en) 2001-10-09

Family

ID=7934028

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001365A PE20010954A1 (en) 1999-12-23 2000-12-19 BENZHIMIDAZOLES, ITS PREPARATION AND ITS USE AS MEDICINES

Country Status (10)

Country Link
EP (1) EP1244636A1 (en)
JP (1) JP2003519129A (en)
AR (1) AR027050A1 (en)
AU (1) AU2011501A (en)
CA (1) CA2393916A1 (en)
DE (1) DE19962329A1 (en)
MX (1) MXPA02006299A (en)
PE (1) PE20010954A1 (en)
UY (1) UY26492A1 (en)
WO (1) WO2001047896A1 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10125478A1 (en) * 2001-05-25 2002-11-28 Boehringer Ingelheim Pharma Treatment or prophylaxis of arterial thrombosis, using 5-quinolinesulfonylamino-benzimidazole derivatives having combined thrombin inhibiting and fibrinogen receptor inhibiting action
US7169934B2 (en) 2002-06-20 2007-01-30 Boehringer Ingelheim International Gmbh (R) 2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1 (pyrrolidinocarbonyl)-ethyl]-benzimidazole, the monohydrochloride thereof, preparation thereof and the use as pharmaceutical composition
DE10227666A1 (en) * 2002-06-20 2004-01-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg (R) -2- (4-amidinophenylaminomethyl) -1-methyl-5- [1- (carboxymethylamino) -1- (pyrrolidinocarbonyl) ethyl] benzimidazole, its monohydrochloride, process for its preparation and use as a medicament
PE20040804A1 (en) * 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma CARBOXAMID DERIVATIVES AS INHIBITORS OF THE Xa FACTOR
US7371743B2 (en) * 2004-02-28 2008-05-13 Boehringer Ingelheim International Gmbh Carboxylic acid amides, the preparation thereof and their use as medicaments
EP1609784A1 (en) * 2004-06-25 2005-12-28 Boehringer Ingelheim Pharma GmbH & Co.KG Process for the preparation of 4-(benzimidazolylmethylamino)-benzamidines
DE102005061623A1 (en) 2005-12-21 2007-06-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Improved process for the preparation of 4- (benzimidazolylmethylamino) -benzamidines and their salts
DE102005061624A1 (en) 2005-12-21 2007-06-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Improved process for the preparation of salts of 4- (benzimidazolylmethylamino) -benzamidines
US10077251B2 (en) 2012-10-29 2018-09-18 Biophore India Pharmaceuticals Pvt. Ltd. Process for the synthesis of Dabigatran Etexilate and its intermediates
US9533971B2 (en) 2012-10-29 2017-01-03 Biophore India Pharmaceuticals Pvt. Ltd Process for the synthesis of dabigatran and its intermediates
RU2623439C1 (en) * 2016-10-14 2017-06-26 федеральное государственное автономное образовательное учреждение высшего образования "Южный федеральный университет" 1-substituted-3-{[2-(3,5-di-tret-4-hydroxyphenyl)-2-oxoethyl]}-2aminobenzimidazolium bromides with antiplatelet and antioxidant properties

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4129603A1 (en) * 1991-09-06 1993-03-11 Thomae Gmbh Dr K CONDENSED 5-LOW HETEROCYCLES, METHOD FOR THE PRODUCTION THEREOF, AND MEDICAMENTS CONTAINING THESE COMPOUNDS
JP2002502844A (en) * 1998-02-03 2002-01-29 ベーリンガー インゲルハイム ファルマ コマンディトゲゼルシャフト 5-membered heterocyclic fused benzo derivatives, their preparation and their use as pharmaceuticals
TWI248435B (en) * 1998-07-04 2006-02-01 Boehringer Ingelheim Pharma Benzimidazoles, the preparation thereof and their use as pharmaceutical compositions
DE19829964A1 (en) * 1998-07-04 2000-01-05 Boehringer Ingelheim Pharma New benzimidazolyl amidine or nitrile compounds, used as thrombin inhibitors, antithrombotic agents or intermediates

Also Published As

Publication number Publication date
WO2001047896A1 (en) 2001-07-05
DE19962329A1 (en) 2001-06-28
CA2393916A1 (en) 2001-07-05
UY26492A1 (en) 2001-07-31
AR027050A1 (en) 2003-03-12
EP1244636A1 (en) 2002-10-02
JP2003519129A (en) 2003-06-17
MXPA02006299A (en) 2002-12-09
AU2011501A (en) 2001-07-09

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