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1. 发明授权

US4588727A Intermediates for pyrrolo[1,2-b][1,2,5]triazepines 失效
标题翻译：吡咯并[1,2-b] [1,2,5]三氮杂的中间体
公开(公告)号：US4588727A
公开(公告)日：1986-05-13
申请号：US698196
申请日：1985-02-04
申请人： Richard C. Effland , Joseph T. Klein , R. Richard L. Hamer
发明人： Richard C. Effland , Joseph T. Klein , R. Richard L. Hamer
IPC分类号： C07D207/50 , C07D487/04 , A61K31/40
CPC分类号： C07D487/04 , C07D207/50
摘要： There are described novel pyrrolo[1,2-b][1,2,5]triazepines of the general formula ##STR1## where R is hydrogen, loweralkyl, loweralkylaminoloweralkyl or diloweralkylaminoloweralkyl; X is hydrogen, halogen (fluorine, chlorine, bromine or iodine), trifluoromethyl or nitro; and Y is hydrogen, halogen or loweralkyl. Also described are derivatives of 1-amino-2-benzoylpyrrole having the general formula ##STR2## where R, X and Y are as defined above, and R.sub.1 is hydrogen, ##STR3##Compounds I and II are useful as analgesic, anxiolytic and/or anticonvulsant agents, and many of Compounds II are useful as intermediates for synthesizing Compounds I.
摘要翻译：描述了通式“IMAGE”的新型吡咯并[1,2-b] [1,2,5]三氮，其中R是氢，低级烷基，低级烷基氨基低级烷基或二低烷基氨基低级烷基; X是氢，卤素（氟，氯，溴或碘），三氟甲基或硝基; Y是氢，卤素或低级烷基。还描述了具有通式为：其中R，X和Y如上所定义，并且R 1是氢的具有通式“（II）”的1-氨基-2-苯甲酰基吡咯的衍生物，其中R 1是氢，化合物I和II可用作止痛剂，抗焦虑剂和/或抗惊厥剂，许多化合物II可用作合成化合物I的中间体。

2. 发明授权

US4517195A Pyrrolo[1,2-b][1,2,5]triazepines and pharmaceutical compositions thereof 失效
标题翻译：吡咯并[1,2-b] [1,2,5]三氮杂及其药物组合物
公开(公告)号：US4517195A
公开(公告)日：1985-05-14
申请号：US627329
申请日：1984-07-02
申请人： Richard C. Effland , Joseph T. Klein , R. Richard L. Hamer
发明人： Richard C. Effland , Joseph T. Klein , R. Richard L. Hamer
IPC分类号： C07D207/48 , A61K31/40 , A61K31/55 , A61P25/04 , A61P25/08 , A61P25/20 , C07D207/50 , C07D403/04 , C07D403/12 , C07D487/04 , C07D255/02 , C07D255/04
CPC分类号： C07D487/04 , C07D207/50
摘要： There are described novel pyrrolo[1,2-b][1,2,5]triazepines of the general formula ##STR1## where R is hydrogen, loweralkyl, loweralkylaminoloweralkyl or diloweralkylaminoloweralkyl; X is hydrogen, halogen (fluorine, chlorine, bromine or iodine), trifluoromethyl or nitro; and Y is hydrogen, halogen or loweralkyl. Also described are derivatives of 1-amino-2-benzoylpyrrole having the general formula ##STR2## where R, X and Y are as defined above, and R.sub.1 is hydrogen, ##STR3## Compounds I and II are useful as analgesic, anxiolytic and/or anticonvulsant agents, and many of Compounds II are useful as intermediates for synthesizing Compounds I.
摘要翻译：描述了通式（I）的新颖的吡咯并[1,2-b] [1,2,5]三氮，其中R是氢，低级烷基，低级烷基氨基低级烷基或二低级烷基氨基低级烷基; X是氢，卤素（氟，氯，溴或碘），三氟甲基或硝基; Y是氢，卤素或低级烷基。还描述了具有通式为：其中R，X和Y如上所定义，并且R 1是氢的具有通式“（II）”的1-氨基-2-苯甲酰基吡咯的衍生物，其中R 1是氢，化合物I和II可用作止痛剂，抗焦虑剂和/或抗惊厥剂，许多化合物II可用作合成化合物I的中间体。

3. 发明授权

US5686483A Aminoalkyloximes 失效
公开(公告)号：US5686483A
公开(公告)日：1997-11-11
申请号：US457422
申请日：1995-06-01
申请人： Gregory M. Shutske , Brian S. Freed , John D. Tomer, IV , R. Richard L. Hamer
发明人： Gregory M. Shutske , Brian S. Freed , John D. Tomer, IV , R. Richard L. Hamer
IPC分类号： C07D233/60 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/445 , A61K31/454 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , C07D211/14 , C07D211/32 , C07D233/54 , C07D233/61 , C07D235/26 , C07D401/04 , C07D401/12 , C07D521/00 , C07D295/13 , C07D207/08 , C07D403/04 , C07D403/12
CPC分类号： C07D233/64 , C07D211/14 , C07D211/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

4. 发明授权

US5006563A Alkylamino- and alkylamino alkyl diarylketones 失效
标题翻译：烷基氨基和烷基氨基烷基二芳基酮
公开(公告)号：US5006563A
公开(公告)日：1991-04-09
申请号：US561202
申请日：1990-07-31
申请人： R. Richard L. Hamer , Brian Freed , Richard C. Allen
发明人： R. Richard L. Hamer , Brian Freed , Richard C. Allen
IPC分类号： C07C45/00 , C07C45/45 , C07C49/233 , C07C49/80 , C07C217/86 , C07C225/16 , C07C225/22
CPC分类号： C07C225/22 , C07C217/86 , C07C225/16 , C07C45/004 , C07C45/455 , C07C49/233 , C07C49/80
摘要： This invention relates to alkylamino and alkyl amino alkyl diarylketones of the formula ##STR1## where Ar is aryl of the formula ##STR2## where V is hydrogen, halogen, loweralkyl, loweralkoxy, CF.sub.3, No.sub.2 and u is an integer of 1 to 3; X and Y are independently CH.sub.2 --, --CH.sub.2 -- or --CHF--; Z and W are independently --CH.sub.2 --, --O--, --CHOH--, or --CHF--; m, n, p, q and t are integers which are independently 0 or 1; R.sub.1 is H or loweralkyl; R.sub.2 and R.sub.3 are loweralkyl; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic agents and as agents for alleviating various memory dysfunctions, characterized by a decreased cholinergic function, such as Alzheimer's disease.
摘要翻译：本发明涉及式（Ia）的烷基氨基和烷基氨基烷基二芳基酮，其中Ar是下式的芳基：其中V是氢，卤素，低级烷基，低级烷氧基，CF 3，NO 2，u是1至3的整数; X和Y独立地为CH 2 - ， - CH 2 - 或-CHF-; Z和W独立地是-CH 2 - ， - O - ， - CHOH-或-CHF-; m，n，p，q和t分别是0或1的整数; R1是H或低级烷基; R2和R3是低级烷基; 和其药学上可接受的酸加成盐，并且在适用的情况下为其几何和旋光异构体及其外消旋混合物。本发明的化合物显示出作为镇痛剂的用途，并且作为减轻各种记忆功能障碍的药剂，其特征在于胆碱能功能降低，如阿尔茨海默病。

5. 发明授权

US4786644A 1-aryl-3-quinolinecarboxamide 失效
标题翻译： 1-芳基-3-喹啉甲酰胺
公开(公告)号：US4786644A
公开(公告)日：1988-11-22
申请号：US125971
申请日：1987-11-27
申请人： Edward J. Glamkowski , R. Richard L. Hamer
发明人： Edward J. Glamkowski , R. Richard L. Hamer
IPC分类号： A61K31/47 , A61K31/472 , A61K31/495 , A61P25/04 , A61P29/00 , C07D215/56 , C07D217/26 , C07D401/12 , C07D413/12 , C07D417/12 , C07D215/00
CPC分类号： C07D401/12 , C07D215/56 , C07D217/26 , C07D413/12 , C07D417/12
摘要： Novel 1-aryl-3-quinolinecarboxamides and 1-aryl-3-isoquinolinecarboxamides, processes for the preparation thereof, and methods for treating pain and inflammation utilizing compounds and compositions thereof are disclosed.

6. 发明授权

US5770740A Aminoalkyloximers 失效
标题翻译：氨基酰肟酮
公开(公告)号：US5770740A
公开(公告)日：1998-06-23
申请号：US902462
申请日：1997-07-29
申请人： Gregory M. Shutske , Brian S. Freed , John D. Tomer, IV , R. Richard L. Hamer
发明人： Gregory M. Shutske , Brian S. Freed , John D. Tomer, IV , R. Richard L. Hamer
IPC分类号： C07D233/60 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/445 , A61K31/454 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , C07D211/14 , C07D211/32 , C07D233/54 , C07D233/61 , C07D235/26 , C07D401/04 , C07D401/12 , C07D521/00
CPC分类号： C07D233/64 , C07D211/14 , C07D211/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.
摘要翻译：描述了新的氨基肟基，其前体及其制备方法，以及治疗抑郁症和强迫症的方法。

7. 发明授权

US5686446A Aminoalkyloximes 失效
公开(公告)号：US5686446A
公开(公告)日：1997-11-11
申请号：US457681
申请日：1995-06-01
申请人： Gregory M. Shutske , Brian S. Freed , John D. Tomer, IV , R. Richard L. Hamer
发明人： Gregory M. Shutske , Brian S. Freed , John D. Tomer, IV , R. Richard L. Hamer
IPC分类号： C07D233/60 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/445 , A61K31/454 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , C07D211/14 , C07D211/32 , C07D233/54 , C07D233/61 , C07D235/26 , C07D401/04 , C07D401/12 , C07D521/00 , C07D403/12 , C07D207/08 , C07D295/13 , C07D403/04
CPC分类号： C07D233/64 , C07D211/14 , C07D211/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： Novel aminoalkyloximes, precursors and processes for the preparation thereof, and methods of treating depression and obsessive compulsive disorders are described.

8. 发明授权

US5550254A Memory enhancing and analgesic 1,2,3,3A,8,8A-hexahydro-3A,8 (and 1,3A,8)-di (and tri) methylpyrrolo[2,3-B] indoles 失效
标题翻译：记忆增强和镇痛剂1,2,3,3A，8,8A-六氢-3A，8（和1,3A，8） - 二（和三）甲基吡咯并[2,3-B]吲哚
公开(公告)号：US5550254A
公开(公告)日：1996-08-27
申请号：US483700
申请日：1995-06-07
申请人： R. Richard L. Hamer , Grover C. Helsley , Edward J. Glamkowski , Yulin Chiang
发明人： R. Richard L. Hamer , Grover C. Helsley , Edward J. Glamkowski , Yulin Chiang
IPC分类号： A61K31/40 , A61K31/44 , A61K31/495 , A61K31/535 , A61P25/04 , A61P25/28 , C07D487/04
CPC分类号： C07D487/04
摘要： There are described compounds of the formula ##STR1## where (a) X is O or S;(b) R is H, loweralkyl, ##STR2## where Y is O or S; R.sub.2 is alkyl, cycloalkyl, bicycloalkyl, cycloalkenyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl, R.sub.3 is H or alkyl, or the group --NR.sub.2 R.sub.3 taken as a whole is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl, 1-piperazinyl, 4-methyl-1-piperazinyl or 2-(2,6-dichlorophenylimino)-1-imidazolidinyl) and R.sub.4 is hydrogen, loweralkyl, arylloweralkyl, diarylloweralkyl, aryl or heteroaryl,(c) m is 1 or 2;(d) each Z is independently H, loweralkyl, halogen, nitro, --NH.sub.2, loweralkylcarbonylamino, arylcarbonylamino, loweralkoxycarbonylamino or loweralkylamino, and(e) R.sub.1 is H, loweralkyl, arylloweralkyl, heteroarylloweralkyl, cycloalkylmethyl or loweralkenylmethyl,with the proviso that when X is O, m is 1, Z is H and R.sub.1 is methyl, R is not --CONHCH.sub.3, --CONHC.sub.6 H.sub.5, hydrogen, methyl or ethyl, and that when X is O, m is 1 and Z and R.sub.1 are both hydrogen, R is not hydrogen or methyl, and pharmaceutically acceptable acid addition salts thereof which are useful as memory-enhancing and analgesic agents.
摘要翻译：描述了式（IMAGE）的化合物，其中（a）X是O或S; （b）R是H，低级烷基，其中Y是O或S; R2是烷基，环烷基，二环烷基，环烯基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，R3是H或烷基，或作为整体的基团-NR2R3是1-吡咯烷基，1-哌啶基，4-吗啉基，4-硫代吗啉基， 1-哌嗪基，4-甲基-1-哌嗪基或2-（2,6-二氯苯基亚氨基）-1-咪唑烷基），R4是氢，低级烷基，芳基低级烷基，二芳基低级烷基，芳基或杂芳基，（c）m是1或2; （d）每个Z独立地是H，低级烷基，卤素，硝基，-NH 2，低级烷基羰基氨基，芳基羰基氨基，低级烷氧基羰基氨基或低级烷基氨基，和（e）R 1是H，低级烷基，芳基低级烷基，杂芳基低级烷基，环烷基甲基或低级烯基甲基，条件是当X 是O，m是1，Z是H，R1是甲基，R不是-CONHCH3，-CONHC6H5，氢，甲基或乙基，当X是O时，m是1，Z和R1都是氢，R是不是氢或甲基，以及其药学上可接受的酸加成盐，其可用作记忆增强剂和止痛剂。

9. 发明授权

US5917057A N-hydroxy-dibenz�b,e!oxepinalkylamines, n-hydroxy-dibenz�b,e!oxepinalkanoic acid amides and related heterocyclic analogues 失效
标题翻译： N-羟基 - 二苯并[b，e]氧基烷基胺，正羟基 - 二苯并[b，e]氧代庚酸酰胺和相关杂环类似物
公开(公告)号：US5917057A
公开(公告)日：1999-06-29
申请号：US32240
申请日：1998-02-27
申请人： Richard C. Allen , Grover C. Helsley , R. Richard L. Hamer , Brian S. Freed , John I. White , Lawrence L. Martin
发明人： Richard C. Allen , Grover C. Helsley , R. Richard L. Hamer , Brian S. Freed , John I. White , Lawrence L. Martin
IPC分类号： C07D313/12 , C07D495/04 , C07D333/74 , A61K31/335 , A61K31/38 , C07D313/00
CPC分类号： C07D495/04 , C07D313/12
摘要： This invention relates to N-hydroxy-dibenz�b,e!oxepinalkylamines, N-hydroxy-dibenz�b,e!oxepinalkanoic acid amides and related heterocyclic analogues of the formula ##STR1## where X together with the carbon atoms to which it is attached forms a benzene or thiophene ring; W and Z are independently hydrogen, halogen, loweralkyl, or trifluoromethyl; R.sup.1 is hydrogen, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; R.sup.2 is loweralkyl, cycloalkyl, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; m is 0 or 1 and n is an integer of 0 to 4 or the pharmaceutically acceptable salts thereof. The compounds of this invention are useful as analgesics and topical antiinflammatory agents for the treatment of various dermatoses and agents for the treatment of conditions where accumulation of cyclooxygenase and/or lipoxygenase metabolites is a causative factor.
摘要翻译：本发明涉及N-羟基 - 二苯并[b，e]氧基烷基胺，N-羟基 - 二苯并[b，e]氧代庚酸酰胺和下式的相关杂环类似物，其中X与其连接的碳原子一起形成苯或噻吩环; W和Z独立地是氢，卤素，低级烷基或三氟甲基; R1是氢，芳基低级烷基，低级烷氧基羰基，低级烷基羰基，芳基羰基或芳基低级烷基羰基; R2是低级烷基，环烷基，芳基低级烷基，低级烷氧基羰基，低级烷基羰基，芳基羰基或芳基低级烷基羰基; m为0或1，n为0〜4的整数或其药学上可接受的盐。本发明的化合物可用作用于治疗各种皮肤病的止痛剂和局部抗炎剂和用于治疗环氧合酶和/或脂氧合酶代谢物积累是致病因素的病症的药剂。

10. 发明授权

US5840749A N-hydroxy-dibenz �b,e!oxepinalkylamines, N-hydroxy-dibenz �b,e!oxepinalkanoic acid amides and related heterocyclic analogues 失效
标题翻译： N-羟基 - 二苯并[b，e]氧基烷基胺，N-羟基 - 二苯并[b，e]氧代庚酸酰胺和相关杂环类似物
公开(公告)号：US5840749A
公开(公告)日：1998-11-24
申请号：US207464
申请日：1994-03-08
申请人： Richard C. Allen , Grover C. Helsley , R. Richard L. Hamer , Brian S. Freed , John I. White , Lawrence L. Martin
发明人： Richard C. Allen , Grover C. Helsley , R. Richard L. Hamer , Brian S. Freed , John I. White , Lawrence L. Martin
IPC分类号： C07D313/12 , C07D495/04 , A61K31/335
CPC分类号： C07D495/04 , C07D313/12
摘要： This invention relates to N-hydroxy-dibenz�b,e!oxepinalkylamines, N-hydroxy-dibenz�b,e!oxepinalkanoic acid amides and related heterocyclic analogues of the formula ##STR1## where X together with the carbon atoms to which it is attached forms a benzene or thiophene ring; W and Z are independently hydrogen, halogen, loweralkyl, or trifluoromethyl; R.sup.1 is hydrogen, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; R.sup.2 is loweralkyl, cycloalkyl, arylloweralkyl, loweralkoxycarbonyl, loweralkylcarbonyl, arylcarbonyl or arylloweralkylcarbonyl; m is 0 or 1 and n is an integer of 0 to 4 or the pharmaceutically acceptable salts thereof. The compounds of this invention are useful as analgesics and topical antiinflammatory agents for the treatment of various dermatoses and agents for the treatment of conditions where accumulation of cyclooxygenase and/or lipoxygenase metabolites is a causative factor.
摘要翻译：本发明涉及N-羟基 - 二苯并[b，e]氧基烷基胺，N-羟基 - 二苯并[b，e]氧代庚酸酰胺及其相关杂环类似物，其中X与它们的碳原子一起附着形成苯或噻吩环; W和Z独立地是氢，卤素，低级烷基或三氟甲基; R1是氢，芳基低级烷基，低级烷氧基羰基，低级烷基羰基，芳基羰基或芳基低级烷基羰基; R2是低级烷基，环烷基，芳基低级烷基，低级烷氧基羰基，低级烷基羰基，芳基羰基或芳基低级烷基羰基; m为0或1，n为0〜4的整数或其药学上可接受的盐。本发明的化合物可用作用于治疗各种皮肤病的止痛剂和局部抗炎剂和用于治疗环氧合酶和/或脂氧合酶代谢物积累是致病因素的病症的药剂。

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