2-furancarboxylic acid hydrazides and pharmaceutical...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 307/68 (2006.01) A61K 31/341 (2006.01) A61K 31/381 (2006.01) A61K 31/40 (2006.01) A61K 31/404 (2006.01) A61K 31/443 (2006.01) A61K 31/4709 (2006.01) A61K 31/5377 (2006.01) A61P 1/00 (2006.01) A61P 1/18 (2006.01) A61P 3/04 (2006.01) A61P 3/06 (2006.01) A61P 3/10 (2006.01) A61P 9/00 (2006.01) A61P 9/04 (2006.01) A61P 9/10 (2006.01) A61P 43/00 (2006.01) C07D 405/04 (2006.01) C07D 405/12 (2006.01) C07D 409/04 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2473591

The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula (I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof, methods for producing them and pharmaceutical compositions containing them: (see formula I) wherein A is a group represented by Formula (a) or the like: (see formula a) (wherein either R4 or R5 represents cyano, nitro or the like, and the other represents a hydrogen atom or the like); either R1 or R2 represents a group: -D-(X)m-R6 or the like, and the other represents a group: -E-(Y)n-R7, hydrogen atom, aryl or the like; R3 is a hydrogen atom or the like; D and E independently represent aryl; X and Y independently represent O or the like; R6 and R7 independently represent alkyl, aryl, arylalkyl or the like; and m and n are independently 0 or 1, provided that the aryl is optionally substituted. Such compounds exhibit a potent antagonistic activity on glucagon receptor and are of use as preventive and/or therapeutic agents for symptoms and diseases in which glucagon is involved.

L'invention concerne des hydrazides d'acide 2-furancarboxylique représentés par la formule générale (I), des promédicaments ou des sels physiologiquement acceptables de ceux-ci, des hydrates ou des solvates de ceux-ci, des procédés de préparations de ceux-ci, ainsi que des compositions pharmaceutiques les contenant. Dans la formule générale (I), A représente un groupe représenté par la formule générale (a) ou similaire, dans laquelle l'un de R?4¿ et R?5¿ représente cyano, nitro ou similaire et l'autre représente hydrogène ou similaire, l'un de R?1¿ et R?2¿ représente D-(X)m-R?6¿ ou similaire, et l'autre représente E-(Y)n-R?7¿, hydrogène, aryle ou similaire, R?3¿ représente hydrogène ou similaire, D et E représentent chacun aryle, X et Y représentent chacun O ou similaire, R?6¿ et R?7¿ représentent chacun alkyle, aryle, arylalkyle ou similaire, et m et n valent chacun 0 ou 1, à condition que chaque aryle puisse être substitué. Ces composés font preuve d'un puissant antagonisme au récepteur du glucagon et sont utiles en tant que médicaments préventifs et/ou thérapeutiques pour des symptômes et des maladies impliquant le glucagon.

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