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1. 发明授权

US4656185A 7-oxabicycloheptane substituted aminoalkyl amide prostaglandin analogs 失效
标题翻译： 7-氧杂双环庚烷取代的氨基烷基酰胺前列腺素类似物
公开(公告)号：US4656185A
公开(公告)日：1987-04-07
申请号：US804729
申请日：1985-12-05
申请人： Steven E. Hall , Masami Nakane
发明人： Steven E. Hall , Masami Nakane
IPC分类号： A61K31/557 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/08 , C07D493/08 , C07D405/14
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted diacid diamide prostaglandin analogs are provided having the structural formula ##STR1## wherein m is 0 to 4; A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; R is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt, --CH.sub.2 OH ##STR2## wherein R.sup.4 and R.sup.5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R.sup.4 and R.sup.5 being other than hydroxy and lower alkoxy; p is 1 to 4; R.sup.1 is H or lower alkyl; q is 1 to 12; R.sup.2 and R.sup.3 are the same or different and are H, lower alkly, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aralkyloxy, cycloalkyl or cycloalkylalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
摘要翻译：提供7-氧杂双环庚烷取代的二酸二酰胺前列腺素类似物，其结构式为：其中m为0至4; A是-CH = CH-或-CH 2 -CH 2 - ; n为1至5; R为CO 2 H，CO 2烷基，CO 2碱金属，CO 2多羟基胺盐，-CH 2 OH其中R 4和R 5相同或不同，为H，低级烷基，羟基，低级烷氧基或芳基，R 4和R 5中的至少一个为羟基和低级烷氧基; p为1〜4; R1是H或低级烷基; q为1〜12; R2和R3相同或不同，为H，低级烷基，低级烯基，低级炔基，芳基，芳烷基，低级烷氧基，芳烷氧基，环烷基或环烷基烷基。这些化合物是可用于例如治疗血栓形成疾病的心血管药。

2. 发明授权

US4456616A 7-Oxabicycloheptane substituted amino prostaglandin analogs and their use in inhibiting platelet aggregation and bronchoconstriction 失效
标题翻译： 7-氧杂双环庚烷取代的氨基前列腺素类似物及其在抑制血小板聚集和支气管收缩中的应用
公开(公告)号：US4456616A
公开(公告)日：1984-06-26
申请号：US453849
申请日：1982-12-27
申请人： Martin F. YHaslanger , Masami Nakane , Steven E. Hall
发明人： Martin F. YHaslanger , Masami Nakane , Steven E. Hall
IPC分类号： A61K31/34 , A61K31/557 , A61P9/00 , C07C29/10 , C07D317/12 , C07D317/22 , C07D493/08 , C07D307/00
CPC分类号： C07D493/08 , C07C247/00 , C07C29/103 , C07C309/00 , C07D317/12 , C07D317/22 , Y10S514/822
摘要： 7-Oxabicycloheptane substituted amino prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译：提供7-氧杂双环庚烷取代的氨基前列腺素类似物，其具有结构式Ⅰ和其所有立体异构体。该化合物是可用于例如治疗溶栓性疾病的心血管药。

3. 发明授权

US4652578A 7-oxabicycloheptane substituted amide prostaglandin analogs 失效
标题翻译： 7-氧杂双环庚烷取代酰胺前列腺素类似物
公开(公告)号：US4652578A
公开(公告)日：1987-03-24
申请号：US832543
申请日：1986-02-24
申请人： Masami Nakane , Steven E. Hall
发明人： Masami Nakane , Steven E. Hall
IPC分类号： C07D493/08 , A61K31/34 , A61K31/41 , C07D405/14
CPC分类号： C07D493/08
摘要： Cis-exo 7-oxabicycloheptane substituted amide prostaglandin analogs are provided having the structural formula ##STR1## wherein A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; R is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt, --CH.sub.2 OH, ##STR2## wherein R.sup.2 and R.sup.3 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R.sup.2 and R.sup.3 being other than hydroxy and lower alkoxy; X is O, NH, CH.dbd.CH, or --(CH.sub.2).sub.x wherein x is 0 or 1; and R.sup.1 is lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, amino, alkylamino, arylamino, arylthio or alkylthio.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
摘要翻译：提供具有结构式为其中A为-CH = CH-或-CH 2 -CH 2 - 的结构式的7-氧杂双环庚烷取代的酰基前列腺素类似物; n为1至5; R为CO 2 H，CO 2烷基，CO 2碱金属，CO 2多羟基胺盐，-CH 2 OH，其中R 2和R 3相同或不同，为H，低级烷基，羟基，低级烷氧基或芳基，R 2和R 3中的至少一个为其它羟基和低级烷氧基; X是O，NH，CH = CH或 - （CH 2）x，其中x是0或1; R 1为低级烷基，低级烯基，低级炔基，芳基，芳基烷基，低级烷氧基，芳氧基，氨基，烷基氨基，芳基氨基，芳硫基或烷硫基。这些化合物是可用于例如治疗血栓形成疾病的心血管药。

4. 发明授权

US5371091A Heteroaromatic amine thrombin inhibitors 失效
标题翻译：杂芳胺凝血酶抑制剂
公开(公告)号：US5371091A
公开(公告)日：1994-12-06
申请号：US76224
申请日：1993-06-14
申请人： Raj N. Misra , Steven E. Hall
发明人： Raj N. Misra , Steven E. Hall
IPC分类号： C07D213/38 , C07D213/74 , C07D237/20 , C07D239/42 , C07D241/20 , C07D401/12 , A61K31/445 , A61K31/415 , A61K31/42 , C07D215/14
CPC分类号： C07D213/74 , C07D213/38 , C07D237/20 , C07D239/42 , C07D241/20 , C07D401/12
摘要： Sulfonamide thrombin inhibitors are provided which have the structure ##STR1## including all stereoisomers thereof, wherein n is 1, 2 or 3; m is 0, 1 or 2; R.sup.1 and R.sup.2 are independently H, lower alkyl, cycloalkyl, aryl, heteroaryl or heteroaryl-alkyl, or R.sup.1 and R.sup.2 can be taken together with the N atom to which they are attached to form a 4- to 8-membered ring; R.sup.3 is monocyclic heteroaryl; and R.sup.4 is alkyl, cycloalkyl, aryl, heteroaryl, quinolinyl or tetrahydroquinolinyl, and pharmaceutically acceptable salts thereof.
摘要翻译：提供磺酰胺凝血酶抑制剂，其具有包括其所有立体异构体的结构，其中n为1,2或3; m为0,1或2; R 1和R 2独立地为H，低级烷基，环烷基，芳基，杂芳基或杂芳基 - 烷基，或者R 1和R 2可以与它们所连接的N原子一起形成4-至8-元环; R3是单环杂芳基; 和R4是烷基，环烷基，芳基，杂芳基，喹啉基或四氢喹啉基，及其药学上可接受的盐。

5. 发明授权

US4626548A 7-oxabicycloheptane substituted prostaglandin compounds useful in the treatment of thrombotic disease 失效
标题翻译：用于治疗血栓性疾病的7-氧杂双环庚烷取代的前列腺素化合物
公开(公告)号：US4626548A
公开(公告)日：1986-12-02
申请号：US767312
申请日：1985-08-19
申请人： Steven E. Hall
发明人： Steven E. Hall
IPC分类号： C07D493/08 , A61K31/34 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted prostaglandin alcohols are provided having the structural formula ##STR1## wherein A is --CH.dbd.CH-- or (CH.sub.2).sub.2 ; m is 1 to 5; Q is --CH.dbd.CH-- or (CH.sub.2).sub.2 ; R is H, alkali metal or alkyl; and R.sup.2 is ##STR2## wherein R.sup.3 is H or lower alkyl and R.sup.4 is H or I and including all steroisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
摘要翻译：提供具有结构式为“IMAGE”的7-氧杂二环庚烷取代的前列腺素醇，其中A为-CH = CH-或（CH 2）2; m为1〜5; Q是-CH = CH-或（CH 2）2; R是H，碱金属或烷基; 并且R 2是其中R 3是H或低级烷基且R 4是H或I并且包括其所有立体异构体。这些化合物是可用于例如治疗血栓形成疾病的心血管药。

6. 发明授权

US4560698A 7-Oxabicycloheptane substituted thio prostaglandin analogs and their use in the treatment in thrombolytic disease 失效
标题翻译： 7-氧杂双环庚烷取代的硫代前列腺素类似物及其在溶栓性疾病治疗中的应用
公开(公告)号：US4560698A
公开(公告)日：1985-12-24
申请号：US617201
申请日：1984-06-04
申请人： Steven E. Hall , Martin F. Haslanger
发明人： Steven E. Hall , Martin F. Haslanger
IPC分类号： A61K31/34 , A61P7/02 , A61P29/00 , C07D493/08 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted thio prostaglandin analogs are provided having the structural formula ##STR1## wherein p is 0 to 4; A is CH.dbd.CH, (CH.sub.2).sub.2, or a single bond; m is 0 to 8; R is H, lower alkyl, alkali metal or tris(hydroxymethyl)aminomethane; n is 1 to 4; n' is 0, 1 or 2; q is 1 to 12; X is ##STR2## wherein R.sup.2 and R.sup.3 may be the same or different and are H or lower alkyl; t is 0 to 5; and R.sup.1 is H, lower alkyl, aryl, aralkyl, cycloalkyl or cycloalkylalkyl, and including all stereoisomers thereof.The compounds are cardiovascular agents and antiinflammatory agents useful, for example, in the treatment of thrombolytic disease, inflammation and pain.
摘要翻译：提供7-氧杂双环庚烷取代的硫代前列腺素类似物，其结构式为：其中p为0至4; A是CH = CH，（CH 2）2或单键; m为0〜8; R为H，低级烷基，碱金属或三（羟甲基）氨基甲烷; n为1〜4; n'为0,1或2; q为1〜12; X为，其中R2和R3可以相同或不同，为H或低级烷基; t为0〜5; 且R 1为H，低级烷基，芳基，芳烷基，环烷基或环烷基烷基，并且包括其所有立体异构体。所述化合物是可用于例如治疗溶栓性疾病，炎症和疼痛的心血管药物和抗炎剂。

7. 发明授权

US4542157A 7-Oxabicycloheptane substituted oxa prostaglandin analogs and their use in the treatment of thrombolytic disease 失效
标题翻译： 7-氧杂双环庚烷取代的oxa前列腺素类似物及其在治疗溶栓性疾病中的应用
公开(公告)号：US4542157A
公开(公告)日：1985-09-17
申请号：US604717
申请日：1984-04-27
申请人： Steven E. Hall , Martin F. Haslanger
发明人： Steven E. Hall , Martin F. Haslanger
IPC分类号： A61K31/34 , A61P9/00 , A61P25/04 , A61P29/00 , A61P43/00 , C07D493/08 , A61K31/557 , C07D307/00
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted oxo prostaglandin analogs are provided having the structural formula ##STR1## wherein R is hydrogen, lower alkyl, alkali metal or tris(hydroxymethyl)aminomethane, R.sup.1 is hydrogen, lower alkyl, aryl, aralkyl, cycloalkyl or cycloalkylalkyl, A is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --, y is 0 to 4, m is 0 to 8, and n is 1 to 4, p is 1 to 12 and q is 0 to 5, and including all stereoisomers thereof.The compounds are antiinflammatory agents useful, for example, in the treatment of inflammatory diseases and analgesic agents as well as cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译：提供具有结构式为其中R为氢，低级烷基，碱金属或三（羟甲基）氨基甲烷，R 1为氢，低级烷基，芳基，芳烷基，环烷基或环烷基烷基的结构式的7-氧杂双环庚烷取代的氧代前列腺素类似物，A为 -CH = CH-或 - （CH 2）2 - ，y为0〜4，m为0〜8，n为1〜4，p为1〜12，q为0〜5，包括其全部立体异构体。所述化合物是可用于例如治疗炎性疾病和止痛剂以及可用于治疗溶栓性疾病的心血管药物的抗炎药。

8. 发明授权

US5290799A 7-oxabicycloheptyl substituted heterocyclic thioamide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease 失效
标题翻译：可用于治疗血栓形成和血管痉挛性疾病的7-氧杂二环庚基取代的杂环硫代酰胺前列腺素类似物
公开(公告)号：US5290799A
公开(公告)日：1994-03-01
申请号：US584969
申请日：1990-09-19
申请人： Raj N. Misra , Philip M. Sher , Philip D. Stein , Steven E. Hall , David Floyd , Joel C. Barrish
发明人： Raj N. Misra , Philip M. Sher , Philip D. Stein , Steven E. Hall , David Floyd , Joel C. Barrish
IPC分类号： A61K31/415 , A61K31/42 , A61K31/425 , A61P7/02 , A61P9/08 , A61P43/00 , C07D493/08 , C07D403/04 , C07D413/04 , C07D417/04
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasospastic disease have the structural formula ##STR1## wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH.sub.2).sub.2 --, --CH.dbd.CH-- or ##STR2## wherein Y is O, a single bond or vinyl, with the proviso that when n is O, if Z is ##STR3## then Y cannot be O, and when Z is --CH.dbd.CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO.sub.2 H, CO.sub.2 lower alkyl, CH.sub.2 OH, CO.sub.2 alkali metal, CONHSOR.sup.3, CONHR.sup.3a or --CH.sub.2 -5-tetrazolyl, X is O, S or NH; and where R.sup.1, R.sup.2, R.sup.3 and R.sup.3a are as defined herein.
摘要翻译：可用于治疗血栓形成和血管痉挛性疾病的7-氧杂双环庚烷取代的前列腺素类似物具有结构式（*化学结构*），其中m为1,2或3; n为1,2,3或4; Z是 - （CH 2）2 - ， - CH = CH-或（*化学结构*）其中Y是O，单键或乙烯基，条件是当n是O时，如果Z是（*化学结构*）那么Y不能是O，当Z是-CH = CH-时，n是1,2,3或4; 当Y =乙烯基时，n = 0; R是CO 2 H，CO 2低级烷基，CH 2 OH，CO 2碱金属，CONHSOR 3，CONHR 3 a或-CH 2 5-四唑基，X是O，S或NH; 并且其中R 1，R 2，R 3和R 3a如本文所定义。

9. 发明授权

US4977174A 7-oxabicycloheptane imidazole prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease 失效
标题翻译：用于治疗血栓和血管痉挛症的7-氧杂双环庚烷咪唑前列腺素类似物
公开(公告)号：US4977174A
公开(公告)日：1990-12-11
申请号：US492504
申请日：1990-03-12
申请人： Philip D. Stein , Steven E. Hall
发明人： Philip D. Stein , Steven E. Hall
IPC分类号： A61K31/415 , A61K31/557 , A61K38/43 , A61K38/46 , A61P7/02 , A61P9/08 , A61P9/10 , A61P11/08 , A61P13/02 , A61P15/00 , A61P43/00 , C07D493/08
CPC分类号： C07D493/08
摘要： 7-Oxabicycloheptane imidazole prostaglandin analogs are provided which are useful in treating thrombotic and vasospastic disease and have the structural formula ##STR1## wherein m is 0, 1, 2, 3 or 4; n is 1, 2 or 3; and p is 1, 2 or 3; Z is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 -- or ##STR2## wherein Y is 1 or a single bond; R is CO.sub.2 H, CO.sub.2 lower alkyl, CO.sub.2 alkali metal, CONHSO.sub.2 R.sub.2 (wherein R.sub.2 is lower alkyl or aryl) or --CH.sub.2 -5-tetrazolyl; A is CHOH, C.dbd.O, ##STR3## (wherein R.sub.3 is H or lower alkyl), or a single bond; R.sub.1 is lower alkyl, aryl, cycloalkyl or H, R.sub.1 can be H only when A is a single bond.
摘要翻译：提供了7-氧杂双环庚烷咪唑前列腺素类似物，其可用于治疗血栓形成和血管痉挛性疾病，并具有结构式：其中m为0,1,2,3或4; n为1,2或3; p为1,2或3; Z是-CH = CH-，-CH 2 CH 2 - 或者其中Y是1或单键; R是CO 2 H，CO 2低级烷基，CO 2碱金属，CONHSO 2 R 2（其中R 2是低级烷基或芳基）或-CH 2 5-四唑基; A是CHOH，C = O，（其中R 3是H或低级烷基）或单键; R 1是低级烷基，芳基，环烷基或H，当A是单键时，R 1可以是H。

10. 发明授权

US4965279A Cyclopropyl aza prostaglandin analogs 失效
标题翻译：环丙基氮杂前列腺素类似物
公开(公告)号：US4965279A
公开(公告)日：1990-10-23
申请号：US272953
申请日：1988-11-18
申请人： Raj N. Misra , David M. Floyd , Steven E. Hall
发明人： Raj N. Misra , David M. Floyd , Steven E. Hall
IPC分类号： C07C233/36 , C07C233/78 , C07C235/30 , C07C235/50 , C07C237/22 , C07C271/22 , C07C271/54 , C07C311/19 , C07C311/51
CPC分类号： C07C311/19 , C07C233/36 , C07C233/78 , C07C235/30 , C07C235/50 , C07C237/22 , C07C271/22 , C07C271/54 , C07C311/51 , C07C2101/02 , C07C2101/14
摘要： Novel cyclopropyl aza prostaglandin analogs are disclosed having the formula ##STR1## wherein A can be carbonyl, sulfonyl or a single bond. These compounds are useful, for example, as thromboxane antagonists.
摘要翻译：公开了具有式（IMAGE）的新型环丙基氮杂前列腺素类似物，其中A可以是羰基，磺酰基或单键。这些化合物可用作例如血栓烷拮抗剂。

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