Pyrimidine-2, 4-dione derivatives as gonadotropin-releasing...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/54 (2006.01) A61K 31/506 (2006.01) A61K 31/513 (2006.01) A61P 5/04 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2531508

GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

La présente invention concerne deux antagonistes du récepteur GnRH qui convienne pour le traitement d'une variété de pathologie liées aux hormones sexuelles tant chez l'homme que chez la femme. Des composés de cette invention possèdent la structure dans laquelle: R¿1a?, R¿1b?, R¿1c?, R¿2a?, R¿2b?, R¿3?, R¿4?, R¿5?, R¿6? et X sont tels que définis dans les descriptions, comprenant des stéréo-isomères, des promédicaments et des sels de ceux-ci répondant aux normes pharmaceutiques. Cette invention concerne aussi des compositions contenant un composé de cette invention en combinaison avec un véhicule répondant aux normes pharmaceutiques, ainsi que des techniques d'utilisation de celui-ci destiné à antagoniser une hormone libérant de la gonadotrophine chez un sujet nécessitant ce traitement.

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