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公开(公告)号:US6093821A
公开(公告)日:2000-07-25
申请号:US943853
申请日:1997-10-08
申请人: Todd K. Jones , Mark E. Goldman , Charlotte L. F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi
发明人: Todd K. Jones , Mark E. Goldman , Charlotte L. F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi
IPC分类号: C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , C07D215/12 , C07D215/18 , C07D215/38
CPC分类号: C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
摘要翻译: 公开了用于类固醇受体的高亲和力,高选择性调节剂的非甾体化合物。 还公开了掺入这种化合物的药物组合物,使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物,可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。
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公开(公告)号:US06696459B1
公开(公告)日:2004-02-24
申请号:US08950032
申请日:1997-10-14
申请人: Todd K. Jones , Mark E. Goldman , Charlotte L. F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi , Lawrence G. Hamann , Luc J. Farmer , Robert L. Davis
发明人: Todd K. Jones , Mark E. Goldman , Charlotte L. F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi , Lawrence G. Hamann , Luc J. Farmer , Robert L. Davis
IPC分类号: A61K314353
CPC分类号: C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
摘要翻译: 公开了用于类固醇受体的高亲和力,高选择性调节剂的非甾体化合物。 还公开了掺入这种化合物的药物组合物,使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物,可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。
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公开(公告)号:US5696133A
公开(公告)日:1997-12-09
申请号:US465556
申请日:1995-06-05
申请人: Todd K. Jones , Mark E. Goldman , Charlotte L.F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi , Lawrence G. Hamann , Luc J. Farmer , Robert L. Davis
发明人: Todd K. Jones , Mark E. Goldman , Charlotte L.F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi , Lawrence G. Hamann , Luc J. Farmer , Robert L. Davis
IPC分类号: C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , A61K31/47
CPC分类号: C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiting steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
摘要翻译: 公开了用于类固醇受体的高亲和力,高选择性调节剂的非甾体化合物。 还公开了掺入这种化合物的药物组合物,使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物,可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。
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公开(公告)号:US5688810A
公开(公告)日:1997-11-18
申请号:US464541
申请日:1995-06-05
申请人: Todd K. Jones , Mark E. Goldman , Charlotte L.F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi
发明人: Todd K. Jones , Mark E. Goldman , Charlotte L.F. Pooley , David T. Winn , James P. Edwards , Sarah J. West , Christopher M. Tegley , Lin Zhi
IPC分类号: C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , A61K31/47 , C07D215/12 , C07D215/18 , C07D215/36 , C07D215/38
CPC分类号: C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
摘要翻译: 公开了用于类固醇受体的高亲和力,高选择性调节剂的非甾体化合物。 还公开了掺入这种化合物的药物组合物,使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物,可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。
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公开(公告)号:US5693647A
公开(公告)日:1997-12-02
申请号:US464546
申请日:1995-06-05
申请人: Todd K. Jones , Lin Zhi , Christopher M. Tegley , David T. Winn , Lawrence G. Hamann , James P. Edwards , Sarah J. West
发明人: Todd K. Jones , Lin Zhi , Christopher M. Tegley , David T. Winn , Lawrence G. Hamann , James P. Edwards , Sarah J. West
IPC分类号: C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , A61K31/47 , C07D221/16 , C07D491/48 , C07D491/52
CPC分类号: C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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公开(公告)号:US5688808A
公开(公告)日:1997-11-18
申请号:US463231
申请日:1995-06-05
申请人: Todd K. Jones , David T. Winn , Lin Zhi , Lawrence G. Hamann , Christopher M. Tegley , Charlotte L. F. Pooley
发明人: Todd K. Jones , David T. Winn , Lin Zhi , Lawrence G. Hamann , Christopher M. Tegley , Charlotte L. F. Pooley
IPC分类号: C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , A61K31/47 , C07D221/16 , C07D491/48 , C07D491/52
CPC分类号: C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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公开(公告)号:US5696127A
公开(公告)日:1997-12-09
申请号:US465429
申请日:1995-06-05
IPC分类号: C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , A61K31/44 , A61K31/47 , C07D491/52
CPC分类号: C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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公开(公告)号:US06448405B1
公开(公告)日:2002-09-10
申请号:US08947428
申请日:1997-10-08
IPC分类号: C07D491052
CPC分类号: C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
摘要翻译: 公开了用于类固醇受体的高亲和力,高选择性调节剂的非甾体化合物。 还公开了掺入这种化合物的药物组合物,使用所公开的化合物的方法和用于治疗需要类固醇受体激动剂或拮抗剂治疗的患者的组合物,可用于制备化合物的中间体和用于制备类固醇受体调节剂化合物的方法。
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公开(公告)号:US5693646A
公开(公告)日:1997-12-02
申请号:US464360
申请日:1995-06-05
IPC分类号: C07D215/06 , C07D221/18 , C07D311/80 , C07D401/04 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/052 , A61K31/44 , C07D491/52
CPC分类号: C07D401/04 , C07D215/06 , C07D221/18 , C07D311/80 , C07D413/04 , C07D417/04 , C07D471/04 , C07D491/04
摘要: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
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公开(公告)号:US08476262B2
公开(公告)日:2013-07-02
申请号:US12915211
申请日:2010-10-29
申请人: Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , Christopher M. Tegley , James P. Edwards
发明人: Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , Christopher M. Tegley , James P. Edwards
IPC分类号: A61K31/535
CPC分类号: C07D403/04 , A61K31/405 , A61K31/5415 , C07D413/04
摘要: This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein, T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.
摘要翻译: 本发明提供具有以下结构的式1的孕酮受体拮抗剂,其中T为O,S或不存在; R 1和R 2各自独立地为氢,烷基,取代的烷基; 或R 1和R 2一起形成环,并且一起含有-CH 2(CH 2)n CH 2 - , - CH 2 CH 2 CH 2 CH 2 CH 2 - , - O(CH 2)p CH 2 - , - O(CH 2)q O - , - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 CH 2 CH 2 - n = 1-5; p = 1-4; q = 1-4; R3是氢,OH,NH2,烷基,取代的烷基,烯基,取代的烯基,炔基,取代的炔基或CORA; RA是氢,烷基,取代的烷基,烷氧基,取代的烷氧基,氨基烷基或取代的氨基烷基; R4是氢,卤素,CN,NH2,烷基,取代的烷基,烷氧基,取代的烷氧基,氨基烷基或取代的氨基烷基; R5是氢,烷基或取代的烷基; R6是氢,烷基,取代的烷基或CORB; RB是氢,烷基,取代的烷基,烷氧基,取代的烷氧基,氨基烷基或取代的氨基烷基; R7是氢或烷基; 或其药学上可接受的盐。
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