Hexahydroindenopyridine compounds having antispermatogenic...

C - Chemistry – Metallurgy – 07 – D

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C07D 221/16 (2006.01) A61K 31/435 (2006.01) A61K 51/00 (2006.01)

Patent

CA 2279293

Hexahydroindenopyridine compounds having formula (I) and relative stereochemistry where R1 is C1-6 alkyl; R2 is hydrogen or C1-6 alkyl; R3 is carboxyl or a group which is metabolized to a carboxyl group under mammalian physiological conditions; R4 is halogen; mixtures of said compound and acid addition salts thereof exhibit potent antispermatogenic activity and are useful in a method or inhibiting spermatogenesis in mammals.

L'invention concerne des composés d'hexahydroindénopyridine présentant la structure stéréochimique relative de formule (I), dans laquelle R<1> représente alkyle C1-6; R<2> représente hydrogène ou alkyle C1-6; R<3> représente carboxyle ou un groupe métabolisé en un groupe carboxyle dans des conditions physiologiques mammaliennes; R<4> représente halogène. Des mélanges dudit composé et ses sels d'addition d'acide présentent une forte activité antispermatogène et sont utiles pour inhiber la spermatogenèse chez les mammifères.

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