Pyrrolo¬1,2-a|pyrazine spla2 inhibitor

Details Pyrrolo¬1,2-a|pyrazine spla2 inhibitor Pyrrolo¬1,2-a|pyrazine spla2 inhibitor

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/495 (2006.01) A61K 31/4985 (2006.01) A61K 31/519 (2006.01) A61P 1/00 (2006.01) A61P 9/10 (2006.01) A61P 11/00 (2006.01) A61P 17/00 (2006.01) A61P 27/14 (2006.01) A61P 27/16 (2006.01) A61P 29/00 (2006.01) A61P 43/00 (2006.01) C07D 209/00 (2006.01) C07D 241/00 (2006.01)

Patent

CA 2326522

Formula (I), wherein R1 is -(L1)-R6 wherein L1 is a divalent linking group of 1 to 18 atoms or the like, and R6 is a carbocyclic ring substituted by at least one non-interfering substituent or the like; R2 is C1 to C3 alkyl, C3 to C4 cycloalkyl or the like group; R3 is -(L2)-(acidic group); R4 and R5 are hydrogen atoms, non-interfering substituents, carbocyclic groups or the like; RA is -C(=X)-C(=X)-NH2 or the like; and X is independently oxygen atom or sulfur atom; the prodrugs thereof, their pharmaceutically acceptable salts, or their solvates, and a composition for inhibiting sPLA2 containing them as effective ingredients.

L'invention concerne un composé de la formule (I) dans laquelle R?1¿ est -(L?1¿)-R?6¿ (L?1¿ étant un groupe de liaison bivalent de 1 à 18 atomes ou autres; et R?6¿ étant un noyau carbocyclique substitué par au moins un substituant passif ou autre); R?2¿ est un groupe alkyle C1-C3, cycloalkyle C3-C4 ou autre; R?3¿ est -(L?2¿)-(groupe acide); R?4¿ et R?5¿ sont des atomes d'hydrogène, des substituants passifs, des groupes carbocycliques ou autres; R?A¿ est -C(=X)-C(=X)-NH¿2? ou autre; et X est indépendamment un atome d'oxygène ou un atome de soufre. L'invention concerne en outre des promédicaments obtenus à partir dudit composé, leurs sels pharmaceutiquement acceptables ou leurs solvats, et une composition les contenant en tant que principes actifs et pouvant inhiber sPLA¿2?.

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