发明公开
EP0253681A2 Cycloalkyl-substituted 4-pyridyl derivatives and process for their preparation
失效
环烷基取代基4-Pyridylderivate und Verfahren zu ihrer Herstellung。
- 专利标题： Cycloalkyl-substituted 4-pyridyl derivatives and process for their preparation
- 专利标题（中）： 环烷基取代基4-Pyridylderivate und Verfahren zu ihrer Herstellung。
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申请号： EP87306379.6申请日： 1987-07-17
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公开(公告)号： EP0253681A2公开(公告)日： 1988-01-20
- 发明人: Crugnola, Angelo , 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： GB8617596 19860718; GB8628029 19861124
- 主分类号： C07D213/56
- IPC分类号： C07D213/56 ; C07D213/55 ; C07D213/50 ; C07D213/40 ; C07D213/38 ; C07D213/30 ; C07D213/18 ; C07D213/16 ; A61K31/44
摘要：
The invention relates to cycloalkyl-substituted 4-pyridyl derivatives of formula (I)
wherein
R is C₁-C₄ alkyl;
each of R₁ and R₂ is, independently, hydrogen or C₁-C₄ alkyl;
n is an integer of 1 to 5; and either
(a) A is >C=O and B is -O-, -NH- or -CH₂-; or
(b) A is -CH₂- and B is -O-, -NH-, -CH₂- or >C=O; or
(c) A is -O- and B is >C=O or -CH₂-; or
(d) A is -NH- and B is >C=O or -CH₂-,
and their pharmaceutically acceptable salts.
The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hyperplasia.
wherein
R is C₁-C₄ alkyl;
each of R₁ and R₂ is, independently, hydrogen or C₁-C₄ alkyl;
n is an integer of 1 to 5; and either
(a) A is >C=O and B is -O-, -NH- or -CH₂-; or
(b) A is -CH₂- and B is -O-, -NH-, -CH₂- or >C=O; or
(c) A is -O- and B is >C=O or -CH₂-; or
(d) A is -NH- and B is >C=O or -CH₂-,
and their pharmaceutically acceptable salts.
The compounds of the invention show aromatase inhibiting activity and can be useful, e.g., in treating hormone-dependent tumors and prostatic hyperplasia.
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