Thiazolidine carboxamide derivatives as modulators of the...

C - Chemistry – Metallurgy – 07 – D

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C07D 417/12 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61P 15/06 (2006.01) C07D 277/06 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2477265

The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. G is selected from the group consisting of C1-C6-alkyl aryl, C1-C6-alkyl heteroaryl, C1-C6 Alkyl cycloalkyl, C1-C6-alkyl heteroaryl, aryl, heteroaryl, C3-C8-cycloalkyl or -heterocyclo~alkyl, said cycloalkyl or aryl or heteroaryl groups may be fused with cycloalkyl or aryl or heteroaryl groups. R1 is selected from the group consisting of aryl, heteroaryl, C3-C8-cycloalkyl or - heterocyclo-alkyl, said (hetero)cycloalkyl or aryl or heteroaryl groups may be fused with (hetero)cycloalkyl or aryl or heteroaryl groups. R2 is selected from the group consisting of H, carboxy, acyl, alkoxycarbonyl, amino~carbonyl, C1-C5-alkyl carboxy, C1-C5-alkyl acyl, C1-C5-alkyl alkoxycarbonyl, C1-C5-alkyl aminocarbonyl, C1-C5-alkyl acyloxy, C1-C5-alkyl acylamino, C1 -C5-alkyl ureido, C1-C5alkyl amino, C1-C5-alkyl alkoxy, C1-C5-alkyl sulfanyl, C1-C5- alkyl sulfinyl, C1-C5-alkyl sulfonyl, C1-C5-alkyl sulfonylamino, C1-C5-alkyl sulfonyloxy, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl, heteroaryl, C3- C8-cycloalkyl, heterocycloalkyl, C1-C6-alkyl aryl, C2-C6-alkyl heteroaryl, C1- C6-alkyl cycloalkyl, C1-C6-alkyl heterocycloalkyl, C2-C6-alkenyl aryl, C2-C6- alkenyl heteroaryl, C2-C6-alkynyl aryl, or C2-C6-alkynyl heteroaryl.

La présente invention concerne des dérivés de thiazolidine carboxamide représentés par la formule (II) qui sont utiles pour le traitement et/ou la prophylaxie de l'accouchement prématuré, de la naissance avant terme, de la dysménorrhée et pour arrêter le travail avant la naissance par césarienne. Dans la formule, G est sélectionné dans le groupe formé par aryl alkyle C¿1?-C¿6?, hétéroaryl alkyle C¿1?-C¿6?, cycloalkyl alkyle C¿1?-C¿6?,hétéroaryl alkyle C¿1?-C¿6?, aryle, hétéroaryle, cycloalkyle C¿3?-C¿8?- ou hétérocyclo-alkyle, lesdits groupes cycloalkyle ou aryle ou hétéroaryle pouvant être condensés avec des groupes cycloalkyle ou aryle ou hétéroaryle. R?1¿ est sélectionné dans le groupe formé par aryle, hétéroaryle, cycloalkyle C¿3?-C¿8? ou hétérocyclo-alkyle, lesdits groupes (hétéro)cycloalkyle ou aryle ou hétéroaryle pouvant être condensés avec des groupes (hétéro)cycloalkyle ou aryle ou hétéroaryle. R?2¿ est sélectionné dans le groupe formé par H, carboxy, acyle, alcoxycarbonyle, amino-carbonyle, carboxy alkyle C¿1?-C¿5?, acyl alkyle C¿1?-C¿5?, alcoxycarbonyl alkyle C¿1?-C¿5?, aminocarbonyl alkyle C¿1?-C¿5?, acyloxy alkyle C¿1?-C¿5?, acylamino alkyle C¿1?-C¿5?, uréido alkyle C¿1? -C¿5?, amino alkyle C¿1?-C¿5?, alcoxy alkyle C¿1?-C¿5?, sulfanyl alkyle C¿1?-C¿5?, sulfinyl alkyle C¿1?-C¿5?, sulfonyl alkyle C¿1?-C¿5?, sulfonylamino alkyle C¿1?-C¿5?, sulfonyloxy alkyle C¿1?-C¿5?, alkyle C¿1?-C¿6?, alcényle C¿2?-C¿6?, alcynyle C¿2?-C¿6?, aryle, hétéroaryle, cycloalkyle C¿3?-C¿8?, hétérocycloalkyle, aryl alkyle C¿1?-C¿6?, hétéroaryl alkyle C¿2?-C¿6?, cycloalkyl alkyle C¿1?-C¿6?, hétérocycloalkyl alkyle C¿1?-C¿6?, aryl alcényle C¿2?-C¿6?, hétéroaryl alcényle C¿2?-C¿6?, aryl alcynyle C¿2?-C¿6?, ou hétéroaryl alcynyle C¿2?-C¿6?. Formule (II)

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