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公开(公告)号:EP0138504A3
公开(公告)日:1986-03-12
申请号:EP84306715
申请日:1984-10-02
发明人: Bowler, Jean , Tait, Brian Steele
IPC分类号: C07J41/00 , A61K31/565 , C07J31/00
CPC分类号: C07J51/00 , C07C53/21 , C07C309/00 , C07F7/1856 , C07F9/5407 , C07J1/007 , C07J1/0096 , C07J17/00 , C07J31/006 , C07J41/0072 , C07J41/0094
摘要: A steroid derivative of the formula:
wherein ST is a 7a-linked steroid nucleus of the general formula:
wherein the double bond(s) carbon atoms 6 and 7 and/or carbon atoms 8 and 9 are optional; wherein the aromatic ring A may optionally bear one or two halogen or alkyl substituents; wherein R 3 is hydrogen, alkyl, or acyl; wherein R 16 is hydrogen, alkyl or hydroxy; wherein either R 17 is hydroxy or acyloxy and R 27 is hydrogen, alkyl, alkenyl or alkynyl, or R 17 and R 27 together form oxo (=0); wherein R 18 is alkyl; wherein A is alkylene, alkenylene or alkynylene optionally fluorinated and optionally interrupted by -0-, -S-, -SO-, -S0 2 -, -CO-, -NR-, -NRCO-, -CONR-, -COO-, -OCO- or phenylene, wherein R is hydrogen or alkyl; wherein R 1 is hydrogen, alkyl, alkenyl, cycloalkyl, halogenoalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl, arylalkyl, or dialkylaminoalkyl, or R 1 is joined to R 2 as defined below; and wherein X is -CONR 2 -, -CSNR 2- , -NR 12 CO-, -NR 12 CS-, N R 2 2 -NR 12 CONR 2 -, NR 12 -C-NR 2 -, -SO 2 NR 2 -, or-CO-; or, when R 1 is not hydrogen, is -O-, -NR 2 -, -(NO)R 2 -, -(PO)R 2 -, -NR 12 COO-; -NR 12 SO 2 -, -S-, -SO- or -S0 2 -; wherein R 2 is hydrogen or alkyl or R 1 annd R 2 together form alkylene or halogenoalkylene; wherein R 12 is hydrogen or alkyl and wherein R 22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.-
公开(公告)号:EP0163416A3
公开(公告)日:1986-10-08
申请号:EP85302881
申请日:1985-04-24
发明人: Bowler, Jean , Glen, Alasdair Thomas , Crawley, Graham Charles , Large, Michael Stewart , Edwards, Philip Neil , Tait, Brian Steele
IPC分类号: C07C103/34 , C07C147/14 , C07C147/02 , C07C149/18 , C07C149/20 , C07C149/26 , C07C149/273 , A61K31/16 , A61K31/215 , A61K31/10
CPC分类号: C07C323/16 , C07C45/46 , C07C45/515 , C07C45/68 , C07C49/755 , C07C49/757 , C07C65/40 , C07C317/18 , C07C2602/10 , C07F7/1856 , C07F9/5031
摘要: A phenol derivative of the formula
wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl- hydroxyindanyl, phenyl-hydroxybenzothienyl or mono- hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R' is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkozyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R' is joined to R 2 , and wherein X is -CONR 2 -, CSNR 2 -, -NR 12 CO-, -NR 12 CS-, -NR 12 CONR 2 -,
-SO 2 NR 2 - or -CO-, or, when R 1 is not hydrogen, is-NR 12 COO-,-(PO)R 2 -, -S-, -SO- or -S0 2 -, wherein R 2 is hydrogen or alkyl, or R 1 and R 2 together form alkylene; wherein R' 2 is hydrogen or alkyl, and wherein R 22 is hydrogen, cyano or nitro, or a salt thereof when appropriate. The compounds possess antioestrogenic activity and may be used for the treatment of hormone-dependent breast tumours or of anovulatory infertility.-
公开(公告)号:EP0163416B1
公开(公告)日:1989-05-31
申请号:EP85302881.9
申请日:1985-04-24
发明人: Bowler, Jean , Glen, Alasdair Thomas , Crawley, Graham Charles , Large, Michael Stewart , Edwards, Philip Neil , Tait, Brian Steele
IPC分类号: C07C103/34 , C07C147/14 , C07C147/02 , C07C149/18 , C07C149/20 , C07C149/26 , C07C149/273 , A61K31/16 , A61K31/215 , A61K31/10
CPC分类号: C07C323/16 , C07C45/46 , C07C45/515 , C07C45/68 , C07C49/755 , C07C49/757 , C07C65/40 , C07C317/18 , C07C2602/10 , C07F7/1856 , C07F9/5031
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公开(公告)号:EP0138504B1
公开(公告)日:1988-07-20
申请号:EP84306715.8
申请日:1984-10-02
发明人: Bowler, Jean , Tait, Brian Steele
IPC分类号: C07J41/00 , A61K31/565 , C07J31/00
CPC分类号: C07J51/00 , C07C53/21 , C07C309/00 , C07F7/1856 , C07F9/5407 , C07J1/007 , C07J1/0096 , C07J17/00 , C07J31/006 , C07J41/0072 , C07J41/0094
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公开(公告)号:EP0163416A2
公开(公告)日:1985-12-04
申请号:EP85302881.9
申请日:1985-04-24
发明人: Bowler, Jean , Glen, Alasdair Thomas , Crawley, Graham Charles , Large, Michael Stewart , Edwards, Philip Neil , Tait, Brian Steele
IPC分类号: C07C103/34 , C07C147/14 , C07C147/02 , C07C149/18 , C07C149/20 , C07C149/26 , C07C149/273 , A61K31/16 , A61K31/215 , A61K31/10
CPC分类号: C07C323/16 , C07C45/46 , C07C45/515 , C07C45/68 , C07C49/755 , C07C49/757 , C07C65/40 , C07C317/18 , C07C2602/10 , C07F7/1856 , C07F9/5031
摘要: A phenol derivative of the formula
wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl- hydroxyindanyl, phenyl-hydroxybenzothienyl or mono- hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R' is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkozyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R' is joined to R 2 , and wherein X is -CONR 2 -, CSNR 2 -, -NR 12 CO-, -NR 12 CS-, -NR 12 CONR 2 -,
-SO 2 NR 2 - or -CO-, or, when R 1 is not hydrogen, is-NR 12 COO-,-(PO)R 2 -, -S-, -SO- or -S0 2 -, wherein R 2 is hydrogen or alkyl, or R 1 and R 2 together form alkylene; wherein R' 2 is hydrogen or alkyl, and wherein R 22 is hydrogen, cyano or nitro, or a salt thereof when appropriate. The compounds possess antioestrogenic activity and may be used for the treatment of hormone-dependent breast tumours or of anovulatory infertility.摘要翻译: 式NU-A-X-R1的酚衍生物,其中NU是包括苯基 - 羟基萘基的定义的酚核; 羟萘; 苯基 - 羟基茚满基,苯基 - 羟基苯并噻吩基或单羟基苯基 - 乙烯或亚乙烯基核; 其中A是可被亚苯基或其它键连接的亚烷基,亚烯基或亚炔基,其中R 1是氢或烷基,烯基,炔基,环烷基,卤代烷基,烷氧基烷基,卤代烷氧基烷基,芳基或芳基烷基,或R 1与R 2连接, 其中X是-CONR 2 + 13,-CSNR 2 - , - NR 12 CO - , - NR 12 CS - , - NR 12 CONR 2 - , - SO 2 NR 2 - 或-CO-,或者当R 1不是氢时,是-NR 12 COO-, - ( PO)R213,-S-,-SO-或-SO2-,其中R2是氢或烷基,或R1和R2一起形成亚烷基; 其中R 12是氢或烷基,并且其中R 22是氢,氰基或硝基; 或其盐。 该化合物具有抗雌激素活性,可用于治疗激素依赖性乳腺肿瘤或无排卵性不育症。
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公开(公告)号:EP0138504A2
公开(公告)日:1985-04-24
申请号:EP84306715.8
申请日:1984-10-02
发明人: Bowler, Jean , Tait, Brian Steele
IPC分类号: C07J41/00 , A61K31/565 , C07J31/00
CPC分类号: C07J51/00 , C07C53/21 , C07C309/00 , C07F7/1856 , C07F9/5407 , C07J1/007 , C07J1/0096 , C07J17/00 , C07J31/006 , C07J41/0072 , C07J41/0094
摘要: A steroid derivative of the formula:
wherein ST is a 7a-linked steroid nucleus of the general formula:
wherein the double bond(s) carbon atoms 6 and 7 and/or carbon atoms 8 and 9 are optional;
wherein the aromatic ring A may optionally bear one or two halogen or alkyl substituents;
wherein R 3 is hydrogen, alkyl, or acyl;
wherein R 16 is hydrogen, alkyl or hydroxy;
wherein either R 17 is hydroxy or acyloxy and R 27 is hydrogen, alkyl, alkenyl or alkynyl, or R 17 and R 27 together form oxo (=0);
wherein R 18 is alkyl;
wherein A is alkylene, alkenylene or alkynylene optionally fluorinated and optionally interrupted by -0-, -S-, -SO-, -S0 2 -, -CO-, -NR-, -NRCO-, -CONR-, -COO-, -OCO- or phenylene, wherein R is hydrogen or alkyl;
wherein R 1 is hydrogen, alkyl, alkenyl, cycloalkyl, halogenoalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl, arylalkyl, or dialkylaminoalkyl, or R 1 is joined to R 2 as defined below; and wherein X is -CONR 2 -, -CSNR 2- , -NR 12 CO-, -NR 12 CS-, N R 2 2 -NR 12 CONR 2 -, NR 12 -C-NR 2 -, -SO 2 NR 2 -, or-CO-; or, when R 1 is not hydrogen, is -O-, -NR 2 -, -(NO)R 2 -, -(PO)R 2 -, -NR 12 COO-; -NR 12 SO 2 -, -S-, -SO- or -S0 2 -;
wherein R 2 is hydrogen or alkyl or R 1 annd R 2 together form alkylene or halogenoalkylene;
wherein R 12 is hydrogen or alkyl and wherein R 22 is hydrogen, cyano or nitro;
or a salt thereof when appropriate.
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