Title:
CARBOXAMIDE-SUBSTITUTED BENZIMIDAZOL DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS TRYPTASE INHIBITORS
Document Type and Number:
WIPO Patent Application WO2001034572
Kind Code:
A3
Abstract:
The invention relates to carboxamide-substituted benzimidazol derivatives of general formula (I), wherein R<1> represents an optionally substituted residue from the group C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, phenyl-C1-C4-alkyl, heterocyclyl, heterocyclyl-C1-C4-alkyl; R<2> represents -C(=NH)NH2, -CH2-NH2; R<3> represents an optionally substituted residue from the group C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C4 alkoxy-C1-C4-alkyl, heterocyclyl, heterocyclyl-C1-C4-alkyl, heterocyclyl-C2-C4-alkenyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl-C1-C4-alkyl, naphthyl-C1-C4-alkyl, and; R<4> represents hydrogen and an optionally substituted C1-C6 alkyl, optionally provided in the form of their tautomers, racemates, enantiomers, diastereomers, mixtures thereof and pharmacologically safe acid addition salts thereof. The invention also relates to methods for the producing said carboxamide-substituted benzimidazol derivatives and to their use as medicaments having a tryptase-inhibiting effect. The invention additionally relates to so-called prodrugs , wherein R<2> represents C(=NR<7>)NH2 and intermediate products, wherein R<2> represents -CN.
Inventors:
ANDERSKEWITZ RALF (DE)
BRAUN CHRISTINE (CH)
BRIEM HANS (DE)
DISSE BERND (DE)
HOENKE CHRISTOPH (DE)
JENNEWEIN HANS MICHAEL (DE)
SPECK GEORG (DE)
BRAUN CHRISTINE (CH)
BRIEM HANS (DE)
DISSE BERND (DE)
HOENKE CHRISTOPH (DE)
JENNEWEIN HANS MICHAEL (DE)
SPECK GEORG (DE)
Application Number:
PCT/EP2000/010996
Publication Date:
October 11, 2001
Filing Date:
November 08, 2000
Export Citation:
Assignee:
BOEHRINGER INGELHEIM PHARMA (DE)
ANDERSKEWITZ RALF (DE)
BRAUN CHRISTINE (CH)
BRIEM HANS (DE)
DISSE BERND (DE)
HOENKE CHRISTOPH (DE)
JENNEWEIN HANS MICHAEL (DE)
SPECK GEORG (DE)
ANDERSKEWITZ RALF (DE)
BRAUN CHRISTINE (CH)
BRIEM HANS (DE)
DISSE BERND (DE)
HOENKE CHRISTOPH (DE)
JENNEWEIN HANS MICHAEL (DE)
SPECK GEORG (DE)
International Classes:
A61K31/4184; A61K31/4439; A61K31/454; A61K31/496; A61P1/00; A61P1/02; A61P1/04; A61P9/10; A61P11/00; A61P11/02; C07D235/14; A61P11/06; A61P17/00; A61P17/04; A61P17/06; A61P19/02; A61P27/02; A61P27/16; A61P35/00; A61P37/02; A61P37/06; A61P37/08; A61P43/00; C07D235/00; C07D235/16; C07D401/12; C07D403/12; (IPC1-7): C07D235/16; C07D401/12; C07D403/12; A61K31/415; A61K31/445; A61K31/44; A61P11/06; A61P17/00; A61P19/02; A61P37/08
Domestic Patent References:
| WO1999040072A1 | 1999-08-12 | |||
| WO2000008014A1 | 2000-02-17 | |||
| WO2001014342A1 | 2001-03-01 | |||
| WO2001023359A1 | 2001-04-05 |
Other References:
CHEMICAL ABSTRACTS, vol. 132, no. 20, 15 May 2000, Columbus, Ohio, US; abstract no. 265201, SUZUKI, N. ET AL.: "Preparation of imidazole derivatives as gonadotropin-releasing hormone antagonists" XP002165472
CHEMICAL ABSTRACTS, vol. 133, no. 1, 3 July 2000, Columbus, Ohio, US; abstract no. 805, KUBO, K. ET AL.: "Benzimidazole derivatives as neovascularization inhibitors and pharmaceutical compositions containing them" XP002165473
CHEMICAL ABSTRACTS, vol. 133, no. 1, 3 July 2000, Columbus, Ohio, US; abstract no. 805, KUBO, K. ET AL.: "Benzimidazole derivatives as neovascularization inhibitors and pharmaceutical compositions containing them" XP002165473
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