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1. 发明授权

US5929092A Lipophilic benzothiophenes for treating estrogen deficiency 失效
标题翻译：用于治疗雌激素缺乏症的亲脂苯并噻吩类
公开(公告)号：US5929092A
公开(公告)日：1999-07-27
申请号：US943749
申请日：1997-10-03
申请人： George Joseph Cullinan , Raymond Francis Kauffman
发明人： George Joseph Cullinan , Raymond Francis Kauffman
IPC分类号： A61K31/00 , A61K31/40 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61P3/00 , A61P3/06 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/10 , C07D333/56 , C07D333/52
CPC分类号： C07D333/56
摘要： The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl;R.sub.2 and R.sub.3 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl), or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogenR.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ;R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen;n is 0-4; and pharmaceutically acceptable salts and solvates thereof, and further provides pharmaceutical compositions containing compounds of formula I, and the use of such compounds.
摘要翻译：本发明提供新的式（I）的苯并噻吩：其中R1是N-吡咯烷基或N-哌啶基; R 2和R 3独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） - （C 10 -C 22炔基）或-CO-（CH 2）n COOR 4; 提供的R 2和R 3不是十二酰基，R 2或R 3中的一个不是氢。R4是-3-胆甾醇基或-O（CH 2）2（OR 5）CH 2 OR 6; R 5和R 6独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） CO-（C 10 -C 22炔基）; 提供一个R5或R6不是氢; n为0-4; 以及其药学上可接受的盐和溶剂合物，并且还提供含有式I化合物的药物组合物和这些化合物的用途。

2. 发明授权

US5726168A Lipophilic benzothiophenes 失效
公开(公告)号：US5726168A
公开(公告)日：1998-03-10
申请号：US707680
申请日：1996-09-04
申请人： George Joseph Cullinan , Raymond Francis Kauffman
发明人： George Joseph Cullinan , Raymond Francis Kauffman
IPC分类号： A61K31/00 , A61K31/40 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61P3/00 , A61P3/06 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/10 , C07D333/56 , A61K31/56 , A61K31/44 , C07D333/52
CPC分类号： C07D333/56
摘要： The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl; R.sub.2 and R.sub.3 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl), or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogen R.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ; R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen; n is 0-4; and pharmaceutically acceptable salts and solvates thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, and the use of such compounds.

3. 发明授权

US5789400A Lipophilic benzothiophenes 失效
标题翻译：亲脂苯并噻吩
公开(公告)号：US5789400A
公开(公告)日：1998-08-04
申请号：US943689
申请日：1997-10-03
申请人： George Joseph Cullinan , Raymond Francis Kauffman
发明人： George Joseph Cullinan , Raymond Francis Kauffman
IPC分类号： A61K31/00 , A61K31/40 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61P3/00 , A61P3/06 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/10 , C07D333/56 , A61K31/56
CPC分类号： C07D333/56
摘要： The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl; R.sub.2 and R.sub.3 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl),or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogen R.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ; R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen; n is 0-4; and pharmaceutically acceptable salts and solvates thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, and the use of such compounds.
摘要翻译：本发明提供了式（I）的新型苯并噻吩：其中R 1是N-吡咯烷基或N-哌啶基; R 2和R 3独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） - （C 10 -C 22炔基）或-CO-（CH 2）n COOR 4; 提供的R 2和R 3不是十二酰基，R 2或R 3中的一个不是氢。R4是-3-胆甾醇基或-O（CH 2）2（OR 5）CH 2 OR 6; R 5和R 6独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） CO-（C 10 -C 22炔基）; 提供一个R5或R6不是氢; n为0-4; 及其药学上可接受的盐和溶剂化物。本发明还提供含有式I化合物的药物组合物，以及这些化合物的用途。

4. 发明授权

US6147092A Lipophilic benzothiophenes 失效
标题翻译：亲脂苯并噻吩
公开(公告)号：US6147092A
公开(公告)日：2000-11-14
申请号：US294238
申请日：1999-04-19
申请人： George Joseph Cullinan , Raymond Francis Kauffman
发明人： George Joseph Cullinan , Raymond Francis Kauffman
IPC分类号： A61K31/00 , A61K31/40 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61P3/00 , A61P3/06 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/10 , C07D333/56 , A61K31/56
CPC分类号： C07D333/56
摘要： The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl; R.sub.2 and R.sub.3 are independently hydrogen,--CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl),or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogenR.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ;R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen;n is 0-4; and pharmaceutically acceptable salts and solvates thereof.The present invention further provides pharmaceutical compositions containing compounds of formula I, and the use of such compounds.
摘要翻译：本发明提供新的式（I）的苯并噻吩：其中R1是N-吡咯烷基或N-哌啶基; R 2和R 3独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） - （C 10 -C 22炔基）或-CO-（CH 2）n COOR 4; 提供的R 2和R 3不是十二酰基，R 2或R 3中的一个不是氢。R4是-3-胆甾醇基或-O（CH 2）2（OR 5）CH 2 OR 6; R 5和R 6独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） CO-（C 10 -C 22炔基）; 提供一个R5或R6不是氢; n为0-4; 及其药学上可接受的盐和溶剂化物。本发明还提供含有式I化合物的药物组合物，以及这些化合物的用途。

5. 发明授权

US5827844A Lipophilic benzothiophenes used for treating endometriosis 失效
标题翻译：用于治疗子宫内膜异位症的亲脂苯并噻吩类
公开(公告)号：US5827844A
公开(公告)日：1998-10-27
申请号：US943340
申请日：1997-10-03
申请人： George Joseph Cullinan , Raymond Francis Kauffman
发明人： George Joseph Cullinan , Raymond Francis Kauffman
IPC分类号： A61K31/00 , A61K31/40 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61P3/00 , A61P3/06 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/10 , C07D333/56 , A61K31/58
CPC分类号： C07D333/56
摘要： The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl; R.sub.2 and R.sub.3 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl), or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogen R.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ; R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen; n is 0-4; and pharmaceutically acceptable salts and solvates thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, and the use of such compounds.
摘要翻译：本发明提供了式（I）的新型苯并噻吩：其中R 1是N-吡咯烷基或N-哌啶基; R 2和R 3独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） - （C 10 -C 22炔基）或-CO-（CH 2）n COOR 4; 提供的R 2和R 3不是十二酰基，R 2或R 3中的一个不是氢。R4是-3-胆甾醇基或-O（CH 2）2（OR 5）CH 2 OR 6; R 5和R 6独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） CO-（C 10 -C 22炔基）; 提供一个R5或R6不是氢; n为0-4; 及其药学上可接受的盐和溶剂化物。本发明还提供含有式I化合物的药物组合物，以及这些化合物的用途。

6. 发明授权

US5811415A Lipophilic benzothiophenes 失效
标题翻译：亲脂苯并噻吩
公开(公告)号：US5811415A
公开(公告)日：1998-09-22
申请号：US942967
申请日：1997-10-03
申请人： George Joseph Cullinan , Raymond Francis Kauffman
发明人： George Joseph Cullinan , Raymond Francis Kauffman
IPC分类号： A61K31/00 , A61K31/40 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61P3/00 , A61P3/06 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/10 , C07D333/56 , A61K31/58
CPC分类号： C07D333/56
摘要： The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl; R.sub.2 and R.sub.3 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl), or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogen R.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ; R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen; n is 0-4; and pharmaceutically acceptable salts and solvates thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, and the use of such compounds.
摘要翻译：本发明提供了式（I）的新型苯并噻吩：其中R 1是N-吡咯烷基或N-哌啶基; R 2和R 3独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） - （C 10 -C 22炔基）或-CO-（CH 2）n COOR 4; 提供的R 2和R 3不是十二酰基，R 2或R 3中的一个不是氢。R4是-3-胆甾醇基或-O（CH 2）2（OR 5）CH 2 OR 6; R 5和R 6独立地是氢，-CO-（C 10 -C 22烷基），-CO-（C 10 -C 22支链烷基），-CO-（C 10 -C 22烯基），-CO-（C 10 -C 22聚链烯基） CO-（C 10 -C 22炔基）; 提供一个R5或R6不是氢; n为0-4; 及其药学上可接受的盐和溶剂化物。本发明还提供含有式I化合物的药物组合物，以及这些化合物的用途。

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