C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 213/38 (2006.01) A61K 31/44 (2006.01) A61K 31/4418 (2006.01) A61K 31/4439 (2006.01) A61K 31/444 (2006.01) A61K 31/535 (2006.01) A61K 31/5377 (2006.01) A61K 31/55 (2006.01) C07D 213/30 (2006.01) C07D 213/55 (2006.01)
Patent
CA 2227877
The present invention is directed to compounds of formula (I) wherein n is 2 or 3; R is dimethylamino, diethylamino, 1-piperidinyl, 1-pyrrolidinyl, 4- morpholinyl, or 1-hexamethyleneimino; R1 is hydrogen, loweralkyl of C1-C4, phenyl, or mono- or di-substituted phenyl wherein each substituent is independently halo, methyl, hydroxy, C1-C6-alkoxy, benzyloxy, C1-C6- alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C1-C4-loweralkyl, or C1-C4-loweralkoxy, C1-C5-alkoxycarbonyloxy or C4-C6-alkylsulfonyloxy; R2 is hydrogen, hydroxy, C1- C6-alkoxy, benzyloxy, C1-C6-alkanoyloxy, benzoyloxy, substituted benzoyloxy bearing 1 to 3 substituents each of which is independently halo, C1-C4- loweralkyl, or C1-C4-loweralkoxy, C1-C5-alkoxycarbonyloxy, or C4-C6- alkylsulfonyloxy; and the pharmaceutically acceptable acid addition salts, which are for the treatment of post menopausal symptoms such as osteoporosis, cardiovascular conditions such as hyperlipidaemia, and the like.
Cette invention concerne des composés de Formule (I), ou n est 2 ou 3; R désigne un groupe diméthylamino, diéthylamino, pipéridinyle-1, pyrrolidinyle-1, morpholinyle-4, ou hexaméthylène-imino-1; R?1¿ désigne l'hydrogène, un groupe alkyle inférieur C¿1?-C¿4?, phényle, ou phényle mono ou bi-substitué, dans lequel chaque substituant est indépendamment l'un de l'autre un halogène, un groupe méthyle, hydroxy, alcoxy C¿1?-C¿6?, benzyloxy, alcanoyloxy C¿1?-C¿6? ou benzoyloxy, le benzoyloxy substitué portant 1 à 3 substituants dont chacun est indépendamment l'un de l'autre un halogène, un groupe alkyle inférieur C¿1?-C¿4?, alcoxy inférieur C¿1?-C¿4?, alcoxycarbonyloxy C¿1?-C¿5? ou alkylsulfonyloxy C¿4?-C¿6?; R?2¿ désigne l'hydrogène, un groupe hydroxy, alkoxy C¿1?-C¿6?, benzyloxy, alcanoyloxy C¿1?-C¿6? ou benzoyloxy, le benzoyloxy portant 1 à 3 substituants dont chacun est indépendamment l'un de l'autre un halogène, un groupe alkyle inférieur C¿1?-C¿4?, alcoxy inférieur C¿1?-C¿4?, alcoxycarbonyloxy C¿1?-C¿5?, ou alkylsulfonyloxy C¿4?-C¿6?. L'invention concerne également des sels d'addition d'acides pharmaceutiquement acceptables destinés au traitement des symptômes post-ménopausiques tels qu'ostéoporose et troubles cardio-vasculaires (hyperlipidémie par exemple), etc.
Bryant Henry Uhlman
Finley Don Richard
Matsumoto Ken
Eli Lilly And Company
Gowling Lafleur Henderson Llp
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