发明名称 UNSATURATED 17-SUBSTITUTED 3-CARBOXY STEROIDS
摘要 The present invention concerns steroidic 5 alpha -reductase inhibitors having the following formula (I) <CHEM> wherein Y is oxygen or sulphur; R is a group: a) -OR4, wherein R4 is hydrogen or a C1-C6 alkyl group; b) <CHEM> wherein each of R5 and R6, independently, is hydrogen or a C1-C6 alkyl group; c) <CHEM> wherein R7 is hydrogen or a C1-C6 alkyl group and W is a group: (i) <CHEM> wherein R8 is a C1-C6 alkyl group, a C5-C6 cycloalkyl group, a C6-C9 cycloalkylalkyl group, a phenyl group or a benzyl group; or (ii) <CHEM> wherein R9 is a C1-C6 alkyl group or a C5-C6 cycloalkyl group; or (iii) <CHEM> wherein R5 and R6 are as defined above; d) <CHEM> wherein each of R10 and R11 is, independently, hydrogen or a C1-C6 alkyl group or taken together with the nitrogen atom to which they are linked form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen, and n is an integer of 2 to 4; R1 is hydrogen, a C1-C6 alkyl group, a C5-C6 cycloalkyl group, a C6-C9 cycloalkyalkyl group or an aryl group; each of R2 and R3 is, independently, selected from the group consisting of hydrogen, C1-C6 alkyl, C5-C6 cycloalkyl, C6-C9 cycloalkylalkyl and aryl or R2 and R3, taken together with the nitrogen atom to which they are linked, form a pentatomic or hexatomic saturated heteromonocyclic ring, optionally containing at least one additional heteroatom selected from oxygen and nitrogen; and the symbol (----) represents a single or a double bond provided that when it is a double bond the hydrogen in the 5 alpha position doesn't exist and the pharmaceutically acceptable salts thereof. In view of their 5- alpha reductase inhibiting activity the compounds of the invention can be useful for the treatment of androgen dependent conditions.
申请公布号 ZA9203758(B) 申请公布日期 1993.01.27
申请号 ZA19920003758 申请日期 1992.05.22
申请人 FARMITALIA CARLO ERBA S.R.L. 发明人 ACHILLE PANZERI;MARCELLA NESI;ENRICO DI SALLE
分类号 A61K31/565;A61K31/56;A61K31/58;A61P5/24;A61P5/28;A61P13/02;A61P15/00;A61P17/00;A61P17/02;A61P17/14;A61P35/00;A61P43/00;C07J;C07J41/00;C07J43/00 主分类号 A61K31/565
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