A1 adenosine receptor antagonists

Details A1 adenosine receptor antagonists A1 adenosine receptor antagonists

C - Chemistry, Metallurgy

07

D

C07D 473/06 (2006.01) A61K 31/522 (2006.01) A61P 3/04 (2006.01) A61P 3/10 (2006.01) A61P 9/04 (2006.01) A61P 11/06 (2006.01) A61P 13/12 (2006.01) A61P 25/16 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01) A61P 29/00 (2006.01) A61P 37/08 (2006.01)

Patent

CA 2528367

This invention relates to compounds of formula (I): wherein R1 is a branched or straight chain C1-C8 alkyl; R2 is of the formula (II), wherein n is an integer ranging from 1 to 8; R5 is H or (CH2)pCH3, and R6 is H or (CH2)mOH, wherein p is an integer ranging from 1 to 7 and m is an integer ranging from 1 to 8; R3 is of the formula (III), wherein q is an integer ranging from 1 to 8; and R7 is selected from the group consisting of H, OH, NH2, (CH2)tOH, and R9COOH; wherein R9 is a straight or branched chain alkylene or alkenylene group having 1 to 8 carbon atoms, and t is an integer ranging from 1 to 8; R4 is of the formula (IV), wherein r is an integer ranging from 1 to 8 and R8 is selected from the group consisting of H, OH, (CH2)fNH2, (CH2)sOH, and R10COOH; wherein f is 0 or f and s are independently integers ranging from 1 to 8; and, R10 is a C1-C8 straight or branched chain alkylene or alkenylene; and; salts, solvates, and hydrates thereof. The present invention further provides methods of preparing the compounds of formula (I) and their use as therapeutic agents and diagnostic agents.

L'invention concerne des composés de formule (I), dans laquelle R¿1? est alkyle C¿1?-C¿8? à chaîne droite ou ramifiée; R¿2? est de formule (II), dans laquelle n est un entier compris entre 1 et 8; R¿5? est H ou (CH¿2?)¿p?CH¿3?, et R¿6? est H ou (CH¿2?)¿m?OH, sachant que p est un entier compris entre 1 et 7 et que m est un entier compris entre 1 et 8; R¿3? est de formule (III), dans laquelle q est un entier compris entre 1 et 8; et R¿7? peut être H, OH, NH¿2?, (CH¿2?)¿t?OH, et R¿9?COOH; en l'occurrence, R¿9? est un groupe alkylène ou alcénylène à chaîne droite ou ramifiée ayant entre 1 et 8 atomes de carbone, et t est un entier compris entre 1 et 8; R4 est de formule (IV), dans laquelle r est un entier compris entre 1 et 8 et R¿8? peut être un groupe comprenant H, OH, (CH¿2?)¿f?NH¿2?, (CH¿2?)¿s?OH, et R¿10?COOH; en l'occurrence, f vaut 0 ou f et s sont des entiers indépendants compris entre 1 et 8; et, R¿10? est alkylène or alcénylène C¿1?-C¿8? à chaîne droite ou ramifiée ; y compris les sels, solvates et hydrates correspondants. L'invention concerne également des procédés relatifs à l'élaboration des composés de formule (I), et leur utilisation comme agents thérapeutiques et agents diagnostiques.

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