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1. 发明授权

US5571828A N-[(3-heteroaryl-1-pyrrolidinyl)alkyl]-2,3-napthalimides and related compounds and their therapeutic utility 失效
标题翻译： N - [（3-杂芳基-1-吡咯烷基）烷基] -2,3-萘二酰亚胺及其相关化合物及其治疗用途
公开(公告)号：US5571828A
公开(公告)日：1996-11-05
申请号：US469361
申请日：1995-06-06
申请人： Joseph T. Strupczewski , Grover C. Helsley , Edward J. Glamkowski , Yulin Chiang , Kenneth J. Bordeau , Peter A. Nemoto , John J. Tegeler
发明人： Joseph T. Strupczewski , Grover C. Helsley , Edward J. Glamkowski , Yulin Chiang , Kenneth J. Bordeau , Peter A. Nemoto , John J. Tegeler
IPC分类号： A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/55 , A61P23/00 , A61P25/00 , A61P25/04 , A61P25/18 , C07C45/45 , C07C45/67 , C07C45/71 , C07C49/84 , C07C233/25 , C07C233/33 , C07C255/54 , C07C323/22 , C07D207/08 , C07D221/04 , C07D231/56 , C07D239/02 , C07D261/20 , C07D275/04 , C07D275/06 , C07D277/82 , C07D401/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/00 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/00 , C07D417/04 , C07D417/14 , C07D419/00 , C07D471/04 , C07F7/18
CPC分类号： C07D231/56 , C07C233/25 , C07C233/33 , C07C255/54 , C07C323/22 , C07C45/45 , C07C45/673 , C07C45/71 , C07D207/08 , C07D261/20 , C07D275/04 , C07D275/06 , C07D277/82 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07F7/1856
摘要： Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
摘要翻译：杂芳基哌啶，吡咯烷酮和哌嗪可用作抗精神病药和镇痛药。该化合物特别可用于通过向哺乳动物施用精神病治疗有效量的一种化合物来治疗精神病。化合物的储备衍生物可用于提供化合物的长效作用。通过向哺乳动物施用减轻疼痛的有效量的一种化合物，化合物也可用作镇痛药。

2. 发明授权

US5571803A Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgetics 失效
标题翻译：杂芳基哌啶，吡咯烷酮和哌嗪以及它们作为抗精神病药和止痛药的用途
公开(公告)号：US5571803A
公开(公告)日：1996-11-05
申请号：US577325
申请日：1995-12-22
申请人： Joseph T. Strupczewski , Grover C. Helsley , Edward J. Glamkowski , Yulin Chiang , Kenneth J. Bordeau , Peter A. Nemoto , John J. Tegeler
发明人： Joseph T. Strupczewski , Grover C. Helsley , Edward J. Glamkowski , Yulin Chiang , Kenneth J. Bordeau , Peter A. Nemoto , John J. Tegeler
IPC分类号： A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/55 , A61P23/00 , A61P25/00 , A61P25/04 , A61P25/18 , C07C45/45 , C07C45/67 , C07C45/71 , C07C49/84 , C07C233/25 , C07C233/33 , C07C255/54 , C07C323/22 , C07D207/08 , C07D221/04 , C07D231/56 , C07D239/02 , C07D261/20 , C07D275/04 , C07D275/06 , C07D277/82 , C07D401/00 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/00 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/00 , C07D417/04 , C07D417/14 , C07D419/00 , C07D471/04 , C07F7/18
CPC分类号： C07D231/56 , C07C233/25 , C07C233/33 , C07C255/54 , C07C323/22 , C07C45/45 , C07C45/673 , C07C45/71 , C07D207/08 , C07D261/20 , C07D275/04 , C07D275/06 , C07D277/82 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07F7/1856
摘要： Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.
摘要翻译：杂芳基哌啶，吡咯烷酮和哌嗪可用作抗精神病药和止痛剂，该化合物特别可用于通过向哺乳动物施用精神病治疗有效量的一种化合物来治疗精神病。化合物的储备衍生物可用于提供化合物的长效作用。通过向哺乳动物施用减轻疼痛的有效量的一种化合物，化合物也可用作镇痛药。

3. 发明授权

US5557006A 1-Alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols and related compounds 失效
标题翻译： 1-烷基 - ，1-烯基 - 和1-炔基芳基-2-氨基-1,3-丙二醇及相关化合物
公开(公告)号：US5557006A
公开(公告)日：1996-09-17
申请号：US425529
申请日：1995-04-20
申请人： John J. Tegeler , Barbara S. Rauckman , Russell R. L. Hamer , Brian S. Freed , Gregory H. Merriman
发明人： John J. Tegeler , Barbara S. Rauckman , Russell R. L. Hamer , Brian S. Freed , Gregory H. Merriman
IPC分类号： A61K31/44 , C07C45/68 , C07C47/542 , C07C215/36 , C07C219/22 , C07C233/18 , C07D213/38 , C07D213/40 , C07D213/48 , C07D213/61 , C07D213/80 , C07D261/08 , C07D333/20 , C07D333/22 , C07D333/24 , C07D405/04 , C07D409/04 , C07C69/76 , C07C33/28 , C07D211/70
CPC分类号： C07D213/40 , C07C215/36 , C07C219/22 , C07C233/18 , C07C45/68 , C07C47/542 , C07D213/38 , C07D213/48 , C07D213/61 , C07D213/80 , C07D261/08 , C07D333/20 , C07D333/22 , C07D333/24 , C07D405/04 , C07D409/04
摘要： Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth fire disclosed.
摘要翻译：新型1-烷基 - ，1-烯基 - 和1-炔基芳基-2-氨基-1,3-丙二醇，其制备方法及其制备方法，减轻炎症和细胞增殖，缓解记忆功能障碍，抑制细菌和真菌生长火灾披露。

4. 发明授权

US5488063A 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols and related compounds 失效
标题翻译： 1-烷基 - ，1-烯基 - 和1-炔基芳基-2-氨基-1,3-丙二醇及相关化合物
公开(公告)号：US5488063A
公开(公告)日：1996-01-30
申请号：US247368
申请日：1994-05-23
申请人： John J. Tegeler , Barbara S. Rauckman , Russell R. L. Harmer , Brian S. Freed , Gregory H. Merriman
发明人： John J. Tegeler , Barbara S. Rauckman , Russell R. L. Harmer , Brian S. Freed , Gregory H. Merriman
IPC分类号： A61K31/44 , C07C45/68 , C07C47/542 , C07C215/36 , C07C219/22 , C07C233/18 , C07D213/38 , C07D213/40 , C07D213/48 , C07D213/61 , C07D213/80 , C07D261/08 , C07D333/20 , C07D333/22 , C07D333/24 , C07D405/04 , C07D409/04 , A61K31/38
CPC分类号： C07D213/40 , C07C215/36 , C07C219/22 , C07C233/18 , C07C45/68 , C07C47/542 , C07D213/38 , C07D213/48 , C07D213/61 , C07D213/80 , C07D261/08 , C07D333/20 , C07D333/22 , C07D333/24 , C07D405/04 , C07D409/04
摘要： Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
摘要翻译：新型1-烷基 - ，1-烯基 - 和1-炔基芳基-2-氨基-1,3-丙二醇，其制备方法及其制备方法，减轻炎症和细胞增殖，缓解记忆功能障碍，抑制公开了细菌和真菌生长。

5. 发明授权

US5360811A 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols and related compounds as anti-inflammatory agents 失效
标题翻译： 1-烷基 - ，1-烯基 - 和1-炔基芳基-2-氨基-1,3-丙二醇和相关化合物作为抗炎剂
公开(公告)号：US5360811A
公开(公告)日：1994-11-01
申请号：US942908
申请日：1992-09-10
申请人： John J. Tegeler , Barbara S. Rauckman , Russell R. L. Hamer , Brian S. Freed , Gregory H. Merriman
发明人： John J. Tegeler , Barbara S. Rauckman , Russell R. L. Hamer , Brian S. Freed , Gregory H. Merriman
IPC分类号： A61K31/44 , C07C45/68 , C07C47/542 , C07C215/36 , C07C219/22 , C07C233/18 , C07D213/38 , C07D213/40 , C07D213/48 , C07D213/61 , C07D213/80 , C07D261/08 , C07D333/20 , C07D333/22 , C07D333/24 , C07D405/04 , C07D409/04 , C07D213/46 , C07D213/56
CPC分类号： C07D213/40 , C07C215/36 , C07C219/22 , C07C233/18 , C07C45/68 , C07C47/542 , C07D213/38 , C07D213/48 , C07D213/61 , C07D213/80 , C07D261/08 , C07D333/20 , C07D333/22 , C07D333/24 , C07D405/04 , C07D409/04
摘要： Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols of the formulaRCH(OR.sup.1)CH(NR.sup.2 R.sup.3)R.sup.4 or RCH.sub.2 CR.sup.35 (NR.sup.2 R.sup.3)R.sup.4wherein R is ##STR1## wherein R.sup.5 is CH.sub.3 (CH.sub.2).sub.m C.tbd.C, CH.sub.3 (CH.sub.2).sub.m CH.dbd.CH,CH.sub.3 (CH.sub.2).sub.m CH.sub.2 CH.sub.2, ##STR2## wherein m is 3 to 15, n is 0 to 12, and W and X are independently hydrogen, hydroxy, alkyl, alkoxy, halogen, or trifluoromethyl, ##STR3## wherein R.sup.23 loweralkyl; Z is S, O, or C.dbd.O; and A is S or O; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.35 and R.sup.40 are as defined in the specification, the optical isomers thereof, or the pharmaceutically acceptable salts thereof, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.
摘要翻译：式RCH（OR1）CH（NR2R3）R4或RCH2CR35（NR2R3）R4的新型1-烷基 - ，1-烯基 - 和1-炔基芳基-2-氨基-1,3-丙二醇，其中R是CH3 （CH2）mC 3BOND C，CH3（CH2）mCH = CH，CH3（CH2）mCH2CH2，其中m为3至15，n为0至12，W和X 独立地是氢，羟基，烷基，烷氧基，卤素或三氟甲基，其中R 23是低级烷基; Z是S，O或C = O; A为S或O; R1，R2，R3，R4，R35和R40如说明书中所定义，其光学异构体或其药学上可接受的盐，其中间体及其制备方法，以及减少炎症和细胞增殖以及缓解记忆的方法公开了功能障碍和抑制细菌和真菌生长。

6. 发明授权

US5214059A 2-(aminoaryl) indoles and indolines as topical antiinflammatory agents for the treatment of skin disorders 失效
标题翻译： 2-（氨基芳基）吲哚和吲哚啉作为治疗皮肤病的局部抗炎药
公开(公告)号：US5214059A
公开(公告)日：1993-05-25
申请号：US927050
申请日：1992-08-10
申请人： John J. Tegeler , Eileen M. Gardenhire , Grover C. Helsley
发明人： John J. Tegeler , Eileen M. Gardenhire , Grover C. Helsley
IPC分类号： C07D209/14 , C07D401/04
CPC分类号： C07D401/04 , C07D209/14
摘要： There are described compounds of the formula ##STR1## where A is CH or N;X is hydrogen, loweralkyl, halogen, trifluromethyl, loweralkoxy, arylloweralkoxy, hydroxy or phenylamino;Y is hydrogen, loweralkyl, halogen, loweralkoxy, arylloweralkoxy or hydroxy;R.sub.1 is hydrogen or loweralkyl;R.sub.2 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkylcarbonyl, arylcarbonyl, alkoxycarbonyl, arylloweralkoxycarbonyl or aryloxycarbonyl;R.sub.3 is hydrogen, alkyl, alkylcarbonyl, arylloweralkylcarbonyl, arylcarbonyl, alkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl or --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5 ;which compounds are useful as topical antiinflammatory agents for the treatment of skin disorders.
摘要翻译：描述式为“IMAGE”的化合物，其中A为CH或N; X是氢，低级烷基，卤素，三氟甲基，低级烷氧基，芳基低级烷氧基，羟基或苯基氨基; Y是氢，低级烷基，卤素，低级烷氧基，芳基低级烷氧基或羟基; R1是氢或低级烷基; R2是氢，低级烷基，甲酰基，烷基羰基，芳基低级烷基羰基，芳基羰基，烷氧基羰基，芳基低级烷氧基羰基或芳氧基羰基; R3是氢，烷基，烷基羰基，芳基低级烷基羰基，芳基羰基，烷氧基羰基，芳基低级烷氧基羰基，芳氧基羰基或-CH2CO2C2H5; 哪些化合物可用作治疗皮肤病症的局部抗炎药。

7. 发明授权

US5045539A 1H-indolo[3,2-c]quinoline-derivatives, compositions containing same, useful for treating pain, psychosis or convulsions 失效
标题翻译： 1H-吲哚并[3,2-c]喹啉衍生物，含有它们的组合物，可用于治疗疼痛，精神病或抽搐
公开(公告)号：US5045539A
公开(公告)日：1991-09-03
申请号：US654113
申请日：1991-02-06
申请人： Grover C. Helsley , John J. Tegeler , Kirk D. Shoger
发明人： Grover C. Helsley , John J. Tegeler , Kirk D. Shoger
IPC分类号： C07D471/20
CPC分类号： C07D471/20
摘要： There are disclosed compounds having the formula ##STR1## where n is 0, 1, or 2;p and q are each independently 1, 2 or 3;each X and each Y are independently hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro, amino, loweralkylamino, diloweralkylamino, trifluoromethyl or loweralkylthio;R.sub.1 and R.sub.2 are each independently hydrogen or loweralkyl; andR.sub.3 is hydrogen, loweralkyl, loweralkylcarbonyl, arylloweralkyl or aminocarbonyl;which are useful as analgesic, antipsychotic and anticonvulsant agents.
摘要翻译：公开了具有式（I）的化合物，其中n为0,1或2; p和q各自独立地为1,2或3; 每个X和每个Y独立地是氢，低级烷基，低级烷氧基，卤素，羟基，硝基，氨基，低级烷基氨基，二低级烷基氨基，三氟甲基或低级烷硫基。 R1和R2各自独立地为氢或低级烷基; 并且R 3是氢，低级烷基，低级烷基羰基，芳基低级烷基或氨基羰基; 其可用作止痛剂，抗精神病药和抗惊厥剂。

8. 发明授权

US4985450A Arylthiadiazolylsulfonamides and derivatives 失效
标题翻译：芳基噻二唑磺酰胺及其衍生物
公开(公告)号：US4985450A
公开(公告)日：1991-01-15
申请号：US393494
申请日：1989-08-14
申请人： John J. Tegeler , Kirk D. Shoger
发明人： John J. Tegeler , Kirk D. Shoger
IPC分类号： C07D285/08
CPC分类号： C07D285/08
摘要： There are described compounds of the formula ##STR1## where n is 0, 1 or 2; x and y are independently hydrogen, loweralkyl, loweralkoxy, arylloweralkyl, aryloxy, halogen, --CF.sub.3, --NO.sub.2, --OH, --OCOR.sub.1, ##STR2## where R.sub.1 is loweralkyl, arylloweralkyl, aryl or loweralkoxy, R.sub.2 is hydrogen, loweralkyl or loweralkylcarbonyl, R.sub.3 is hydrogen or loweralkyl, or the group --NR.sub.2 R.sub.3 whole is ##STR3## m is 0, 1 or 2, and R.sub.4 is hydrogen, loweralkyl or aryl; and Z is (R.sub.5, R.sub.6), ##STR4## where R.sub.5 and R.sub.6 are each independently hydrogen or loweralkyl, R.sub.7 loweralkyl, R.sub.8 is hydrogen, loweralkyl or aryl, R.sub.9 and R.sub.10 are each independently loweralkyl or the group --NR.sub.9 R.sub.10 as a whole is ##STR5## R.sub.12 being hydrogen, loweralkyl or aryl, and R.sub.11 is hydrogen, loweralkyl or aryl; which are useful for the treatment of glaucoma.
摘要翻译：描述了式为“IMAGE”的化合物，其中n为0,1或2; x和y独立地是氢，低级烷基，低级烷氧基，芳基低级烷基，芳氧基，卤素，-CF 3，-NO 2，-OH，-OCOR 1，其中R 1是低级烷基，芳基低级烷基，芳基或低级烷氧基，R 2是氢，低级烷基或低级烷基羰基，R 3为氢或低级烷基，或基团-NR 2 R 3全部为0,1或2，R 4为氢，低级烷基或芳基; 其中R 5和R 6各自独立地为氢或低级烷基，R 7为低级烷基，R 8为氢，低级烷基或芳基，R 9和R 10各自为低级烷基或基团-NR 9 R 10为整体。 R12为氢，低级烷基或芳基，R11为氢，低级烷基或芳基; 其可用于治疗青光眼。

9. 发明授权

US4897392A 4H-indolo(1,2-d)(1,2,4)triazolo(4,3-A)(1,4)benzodiazepines 失效
标题翻译： 4H-吲哚（1,2-d）（1,2,4）三唑并（4,3-A）（1,4）苯并二氮杂卓
公开(公告)号：US4897392A
公开(公告)日：1990-01-30
申请号：US375444
申请日：1989-07-03
申请人： John J. Tegeler , Eileen M. Gardenhire , Grover C. Helsley
发明人： John J. Tegeler , Eileen M. Gardenhire , Grover C. Helsley
IPC分类号： A61K31/55 , A61P25/04 , C07D487/14
CPC分类号： C07D487/14
摘要： There are disclosed compounds having the formula ##STR1## where X is H, halogen, --OH,--OCH.sub.3,--NO.sub.2 or --CF.sub.3 ; Y is H, Cl or Br; Z is H, halogen, --OH or --OCH.sub.3 ; and R is H, loweralkyl, --CH.sub.2 OH or diloweralkylaminomethyl, which compounds are useful as analgesic agents.

10. 发明授权

US4873239A Arylthiadiazolylsulfonamides and derivatives 失效
标题翻译：芳基噻二唑磺酰胺及其衍生物
公开(公告)号：US4873239A
公开(公告)日：1989-10-10
申请号：US189919
申请日：1988-05-03
申请人： John J. Tegeler , Kirk D. Shoger
发明人： John J. Tegeler , Kirk D. Shoger
IPC分类号： C07D285/08
CPC分类号： C07D285/08
摘要： There are described compounds of the formula ##STR1## where n is 0, 1 or 2; X and Y are independently hydrogen, loweralkyl, loweralkoxy, arylloweralkyl, aryloxy, halogen, --CF.sub.3, --NO.sub.2, --OH, --OCOR.sub.1, ##STR2## where R.sub.1 is loweralkyl, arylloweralkyl, aryl or loweralkoxy, R.sub.2 is hydrogen, loweralkyl or loweralkylcarbonyl, R.sub.3 is hydrogen or loweralkyl, or the group --NR.sub.2 R.sub.3 as a whole is ##STR3## m is 0, 1 or 2, and R.sub.4 is hydrogen, loweralkyl or aryl; and Z is (R.sub.5,R.sub.6), ##STR4## where R.sub.5 and R.sub.6 are each independently hydrogen or loweralkyl, R.sub.7 is loweralkyl, R.sub.8 is hydrogen, loweralkyl or aryl, R.sub.9 and R.sub.10 are each independently loweralkyl or the group --NR.sub.9 R.sub.10 as a whole is ##STR5## R.sub.12 being hydrogen, loweralkyl or aryl, and R.sub.11 is hydrogen, loweralkyl or aryl; which are useful for the treatment of glaucoma.
摘要翻译：描述了式为“IMAGE”的化合物，其中n为0,1或2; X和Y独立地是氢，低级烷基，低级烷氧基，芳基低级烷基，芳氧基，卤素，-CF 3，-NO 2，-OH，-OCOR 1，其中R 1是低级烷基，芳基低级烷基，芳基或低级烷氧基，R 2是氢，低级烷基或低级烷基羰基 R 3是氢或低级烷基，或者基团-NR 2 R 3整体上是0,1或2，R 4是氢，低级烷基或芳基; 其中R 5和R 6各自独立地为氢或低级烷基，R 7为低级烷基，R 8为氢，低级烷基或芳基，R 9和R 10各自独立地为低级烷基或-NR 9 R 10基团 R12为氢，低级烷基或芳基，R11为氢，低级烷基或芳基; 其可用于治疗青光眼。

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