发明公开
EP0265119A1 1,2-Beta-methylene-4-substituted androstene-3,17-dione derivatives and process for their preparation
失效
1,2-β-亚甲基-4-取代基 - 雄甾-3,17-二酮衍生物和Verfahren zu ihrer Herstellung。
- 专利标题： 1,2-Beta-methylene-4-substituted androstene-3,17-dione derivatives and process for their preparation
- 专利标题（中）： 1,2-β-亚甲基-4-取代基 - 雄甾-3,17-二酮衍生物和Verfahren zu ihrer Herstellung。
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申请号： EP87308891.8申请日： 1987-10-07
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公开(公告)号： EP0265119A1公开(公告)日： 1988-04-27
- 发明人: Buzzetti, Franco , Di Salle, Enrico , Lombardi, Paolo
- 申请人： FARMITALIA CARLO ERBA S.r.l.
- 申请人地址： Via Carlo Imbonati 24 I-20159 Milano IT
- 专利权人： FARMITALIA CARLO ERBA S.r.l.
- 当前专利权人： FARMITALIA CARLO ERBA S.r.l.
- 当前专利权人地址： Via Carlo Imbonati 24 I-20159 Milano IT
- 代理机构： Woods, Geoffrey Corlett
- 优先权： GB8624251 19861009
- 主分类号： C07J53/00
- IPC分类号： C07J53/00 ; A61K31/565
摘要：
The invention relates to new aromatase inhibitor agents having the general formula (I)
wherein R 1 is hydrogen or a group = CHR 3 wherein R 3 is hydrogen or C 1 -C 6 alkyl; the symbol ----- indicates - the presence of a single or double bond in such a way that, when R 1 is hydrogen, (a) is single bond and (b) is either single or double bond, while, when R 1 is a group = CHR 3 as defined above, (a) is double bond and (b) is single bond; R 2 is hydrogen or fluorine; and R is
1) a group -OR 4 wherein R 4 is
a) hydrogen;
b) C 1 -C 6 alkyl;
c) a phenyl or benzyl group, each unsubstituted or ring-substituted by one or more substituents chosen from C 1 -C 4 alkl, halogen, trifluoromethyl, nitro, amino, hydroxy and C 1 -C 4 alkoxy;
d) a group - COR 5 wherein R 5 is
(i) a C 1 -C 22 saturated or C 2 -C 22 unsaturated aliphatic hydrocarbon radical;
(ii) a C 4 -C 7 monocycloalkyl group; or
(iii) a phenyl or benzyl group, each unsubstituted or ring substituted as reported above; or
e) a hydroxy protecting group;
2) a group - SR 6 wherein R 6 either has one of the meanings (a) to (d) indicated above for R 4 or is a group -SR 7 wherein, R 7 is
(iv) C 1 -C 6 alkyl;
(v) a phenyl or benzyl group, each unsubstituted or ring-substituted as reported above; or
(vi) a steroidic residue of formula
wherein R 1 , R 2 , (a), (b) and the symbol --- are as defined above;
3) the group -N 3 ; or
4). a group
wherein each of R s and R 9 , independently, is hydrogen or C 1 -C 6 alkyl, and the pharmaceutically acceptable salts thereof, which are useful in therapy, in particular, as anti-cancer agents.
wherein R 1 is hydrogen or a group = CHR 3 wherein R 3 is hydrogen or C 1 -C 6 alkyl; the symbol ----- indicates - the presence of a single or double bond in such a way that, when R 1 is hydrogen, (a) is single bond and (b) is either single or double bond, while, when R 1 is a group = CHR 3 as defined above, (a) is double bond and (b) is single bond; R 2 is hydrogen or fluorine; and R is
1) a group -OR 4 wherein R 4 is
a) hydrogen;
b) C 1 -C 6 alkyl;
c) a phenyl or benzyl group, each unsubstituted or ring-substituted by one or more substituents chosen from C 1 -C 4 alkl, halogen, trifluoromethyl, nitro, amino, hydroxy and C 1 -C 4 alkoxy;
d) a group - COR 5 wherein R 5 is
(i) a C 1 -C 22 saturated or C 2 -C 22 unsaturated aliphatic hydrocarbon radical;
(ii) a C 4 -C 7 monocycloalkyl group; or
(iii) a phenyl or benzyl group, each unsubstituted or ring substituted as reported above; or
e) a hydroxy protecting group;
2) a group - SR 6 wherein R 6 either has one of the meanings (a) to (d) indicated above for R 4 or is a group -SR 7 wherein, R 7 is
(iv) C 1 -C 6 alkyl;
(v) a phenyl or benzyl group, each unsubstituted or ring-substituted as reported above; or
(vi) a steroidic residue of formula
wherein R 1 , R 2 , (a), (b) and the symbol --- are as defined above;
3) the group -N 3 ; or
4). a group
wherein each of R s and R 9 , independently, is hydrogen or C 1 -C 6 alkyl, and the pharmaceutically acceptable salts thereof, which are useful in therapy, in particular, as anti-cancer agents.
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