Hydroxyformamidine derivatives and medicines containing the...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 213/74 (2006.01) A61K 31/44 (2006.01) A61K 31/443 (2006.01) A61K 31/4433 (2006.01) A61K 31/4436 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61K 31/4545 (2006.01) A61K 31/522 (2006.01) A61K 31/5377 (2006.01) A61P 9/00 (2006.01) A61P 9/10 (2006.01) A61P 13/12 (2006.01) C07D 401/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 417/12 (2006.01) C07D 473/08 (2006.01)

Patent

CA 2411418

Pharmaceutical agents for inhibiting the production of 20-HETE which participates in constriction or dilation of microvessels in major organs such as the kidneys and the cerebral blood vessels, or participates in causing cell proliferation are provided. The present invention relates to hydroxyamidine compounds represented by the formula: (see above formula) wherein R1 represents a group represented by the formula: R2-(CH2)m- (wherein R2 represents a C3-8 cycloalkyl group, a C2-6 alkoxycarbonyl group, a C2-10 alkenyl group, a C2-6 alkynyl group, a substituted or non-substituted aryl group, or the like, and m is an integer of 1 to 8), a group represented by the formula: R3-A- (wherein R3 represents a hydrogen atom, a C1-6 alkoxy group, a C3-8 cycloalkoxy group, or the like, and A represents a straight-chain C2-10 alkylene group which may be substituted with a C1-6 alkyl group or a trifluoromethyl group), or a C3-8 cycloalkyl group, and X represents an oxygen atom or a sulfur atom, or pharmaceutically acceptable salts thereof, and relates to medicines including the same as active ingredients.

L'invention concerne des inhibiteurs d'enzymes qui produisent l'acide 20-HETE, lequel participe à la constriction ou à la dilatation de vaisseaux sanguins de très petite taille dans les principaux organes, y compris les vaisseaux sanguins des reins et cérébraux, à la prolifération cellulaire, etc.. L'invention concerne également les composés hydroxyformamidine de la formule générale (I) ou les sels pharmaceutiquement acceptables de ceux-ci, et les médicaments contenant ces composés ou ces sels en tant que principes actifs. Dans ladite formule (I) : R<1> représente un groupe de la formule générale : R<2> (CH2)m (où R<2 >représente cycloalkyle C 3-8, alkoxycarbonyle C 2-6, alcényle C 2-10, alkynyle C 2-10, aryle éventuellement substitué, ou analogue et m représente un nombre entier de 1 à 8), un groupe de la formule générale : R<3>-A- (où R<3> représente hydrogène, alcoxy C 1-6, cycloalcoxy C 3-8, ou analogue et A représente un alkylène C 2-10 linéaire qui peut être substitué par un alkyle C 1-6 ou un trifluorométhyle), ou bien C 3-8 cycloalkyle ; et X représente oxygène ou soufre.

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