Compounds having tafia inhibitory activity

Details Compounds having tafia inhibitory activity Compounds having tafia inhibitory activity

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/4745 (2006.01) A61K 31/5383 (2006.01) A61K 31/55 (2006.01) A61P 3/04 (2006.01) A61P 7/02 (2006.01) A61P 9/10 (2006.01) A61P 11/00 (2006.01) A61P 13/12 (2006.01) A61P 27/02 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 43/00 (2006.01) C07D 471/14 (2006.01) C07D 487/04 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2741783

Provided are compounds having superior TAFIa inhibitory activity. Specifically, there are provided compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof: (see formula I) wherein A is a benzene ring or a pyridine ring; X is the formula -(CH2)-, the formula -(CH2)2-, an oxygen atom, a nitrogen atom or a single bond; Y is the formula -(CH2)3-NH- R3, the formula -(CH2) 4-NH-R3 or a 2-aminopyridyl group; R3 is a hydrogen atom, a C1-6 alkyl group, or the formula - CO2R4; R4 is a C1-6 alkyl group, the formula -CHR5OC(O)R6, or a substituent having the structure represented by the following formula Ia; (see formula I a) R5 is a C1-6 alkyl group; R6 is a C1-6 alkyl group, a C3-8 cycloalkyl group, or a phenyl group; R7 is a C1-6 alkyl group or a phenyl group; R1 is a hydrogen atom, a halogen atom, a C1-4 alkyl group substituted by 1-3 halogen atoms, a C1-10 alkyl group, a C1-8 alkoxy group, a C3-8 cycloalkyl group, a C3-8 cycloalkoxy group, a C4-14 cycloalkylalkyl group, or a phenyl group; R 2 is CO2R8, or a tetrazolyl group; R8 is a hydrogen atom, a C1-10 alkyl group, or a substituent having the structure represented by the following formula Ib or Ic; (see formula Ib) (see formula Ic) m and n are each an integer of zero or one.

La présente invention concerne un composé ayant une excellente activité inhibitrice des TAFIa. L'invention concerne spécifiquement un composé représenté par la formule (I) ou un sel de celui-ci. Dans la formule, A représente un cycle benzénique ou un cycle pyridine ; X représente -(CH2)-, -(CH2)2-, un atome doxygène, un atome dazote ou une liaison simple ; Y représente -(CH2)3-NH-R3, -(CH2)4-NH-R3 ou un groupe 2-aminopyridyle ; R3 représente un atome d'hydrogène ou équivalent ; R1 représente un atome d'hydrogène ou équivalent ; R2 représente CO2R8, un groupe tétrazolyle ou équivalent ; R8 représente un atome dhydrogène, un groupe alkyle en C1 à C10 ou un groupe ayant une structure de formule (Ib) ou (Ic) ; et m et n représentent chacun un entier tel que 0 ou 1.

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