Prodrugs to d-prolines

Details Prodrugs to d-prolines Prodrugs to d-prolines

C - Chemistry, Metallurgy

07

D

C07D 207/16 (2006.01) A61K 31/401 (2006.01) A61K 31/407 (2006.01) A61P 25/28 (2006.01) C07D 498/14 (2006.01)

Patent

CA 2470037

The invention relates to compounds of formulae (I) or (IA), wherein R1 and R2 are independently from each other and signify lower alkoxy, lower alkenyloxy, benzyloxy, hydroxy, -OCH(CH3)OC(O)-lower alkyl or OCH2C(O)N(R3)(R4), with the proviso that only one of R1 or R2 may be hydroxy; R3 and R4 are independently from each other and signify hydrogen, lower alkyl, lower alkenyl or cycloalkyl; or R1 and R2 form together with the carbon atom, to which they are attached the linking group X, wherein X is -O(CH2)nCH=CH(CH2)n0- or -O(CH2)mO- ; n is l, 2 or 3; and m is 4-8. as well as pharmaceutically acceptable salts of said compounds. Compounds of the present invention can be used for the treatment of diseases where Serum Amyloid P Component depletion has a beneficial effect, in particular in the treatment or prevention of all forms of central and systemic amyloidosis.

L'invention concerne des composés de formules (I) ou (IA), dans lesquelles R?1¿ et R?2¿ représentent, indépendamment l'un de l'autre, alcoxy inférieur, benzyloxy, hydroxy, -OCH(CH¿3?)OC(O)-alkyle inférieur ou OCH¿2?C(O)N(R?3¿)(R?4¿), à condition que seulement un des groupes R?1¿ ou R?2¿ puisse représenter hydroxy; R?3¿ et R?4¿ représentent, indépendamment l'un de l'autre, hydrogène, alkyle inférieur, alcényle inférieur ou cycloalkyle; ou R?1¿ et R?2¿ forment conjointement avec l'atome de carbone, auquel ils sont liés, le groupe de liaison X, ce dernier représentant -O(CH¿2?)¿n?CH=CH(CH¿2?)¿n?0- ou -O(CH¿2?)¿m?O-; n valant 1, 2 ou 3; et m étant compris entre 4 et 8. L'invention concerne également les sels pharmaceutiquement acceptables desdits composés. Les composés selon l'invention peuvent être utilisés pour le traitement de maladies, sur lesquelles la réduction du taux de composant amyloïde P sérique a un effet favorable, en particulier pour le traitement ou la prévention de toutes les formes d'amylose centrale et systémique.

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