Disubstituted maleimide compound and pharmaceutical use thereof

Details Disubstituted maleimide compound and pharmaceutical use thereof Disubstituted maleimide compound and pharmaceutical use thereof

C - Chemistry, Metallurgy

07

D

C07D 401/14 (2006.01) A61K 31/40 (2006.01) A61K 31/41 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) A61K 31/445 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) C07D 403/04 (2006.01) C07D 403/14 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 498/04 (2006.01) C07D 498/06 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2338866

Disubstituted maleimide compounds represented by general formula [I] or pharmaceutically acceptable salts thereof; and medicinal compositions and protein kinase (PKC) .beta.-inhibitors containing these compounds. Because of selectively inhibiting PKC.beta., these compounds are usable as efficacious and safe remedies and preventives for diseases caused by PKC such as complications of diabetes, wherein R1 represents hydrogen or alkyl; R2 represents aryl, cycloalkyl or a heterocycle; R3, R5, R6, R7 and R8 represent each hydrogen, halogeno, hydroxy, amino, alkyl or alkoxy; and R4 is W, or R4 and R3 or R4 and R5 may form together a ring substituted by W thereon (wherein W represents -(CH2)1-(Y)m-(CH2)n-Z).

L'invention concerne des composés de maléimide disubstitués représentés par la formule générale [I] suivante ou des sels pharmaceutiquement acceptables de ces derniers. L'invention a aussi pour objet des compositions médicinales et des inhibiteurs -.beta. (PCK) de la protéine kinase contenant ces composés. Ces composés, qui inhibent la PKC.beta. peuvent être utilisés comme produits thérapeutiques efficaces et sans danger et comme produits prophylactiques pour les maladies provoquées par la PKC, comme des complications du diabète. Dans la formule [I], R?1¿ représente hydrogène ou alkyle ; R?2¿ représente aryle, cycloalkyle ou un hétérocycle; R?3¿, R?5¿, R?6¿, R?7¿ et R?8¿ représentent chacun hydrogène, halogéno, hydroxy, amino, alkyle ou alcoxy; et R?4¿ représente W ou R?4¿ et R?3¿ ou R?4¿ et R?5¿ peuvent former ensemble une chaîne substituée par W (où W représente -CH¿2?)¿1?-(Y)¿m?-(CH¿2?)¿n?-Z).

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