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41. 发明授权

US5155098A N-heteroaryl-purin-6-amines, and pharmaceutical compositions and methods employing them 失效
标题翻译： N-杂芳基 - 嘌呤-6-胺，以及使用它们的药物组合物和方法
公开(公告)号：US5155098A
公开(公告)日：1992-10-13
申请号：US696472
申请日：1991-05-06
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olson
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olson
IPC分类号： C07D473/34 , C07H19/16
CPC分类号： C07H19/16 , C07D473/34
摘要： This invention relates to a N-heteroaryl-purin-6-amine of the formula ##STR1## where R.sub.1 is hydrogen, lower alkyl, and arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen, lower alkyl, or R.sub.4 and R.sub.5 taken together are aryl; R.sub.6 is hydrogen, lower alkyl, aryl, arylloweralkyl, ##STR2## where R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, 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 and anitconvulsant agents.
摘要翻译：本发明涉及下式的N-杂芳基 - 嘌呤-6-胺：其中R 1是氢，低级烷基和芳基低级烷基; R2和R3独立地是氢，低级烷基或R2和R3一起是芳基; R4和R5独立地是氢，低级烷基或R4和R5一起是芳基; R 6是氢，低级烷基，芳基，芳基低级烷基，其中R 2，R 3，R 4和R 5如上定义，其药学上可接受的酸加成盐，以及适用的几何和旋光异构体及其外消旋混合物。本发明化合物显示出作为止痛剂和抗惊厥剂的用途。

42. 发明授权

US5059602A 4-substituted dihydropyrido(4,3-d)pyrimidines as analgesics and topical antiinflammatory agents for the treatment of skin disorders 失效
标题翻译： 4-取代二氢吡啶（4,3-d）嘧啶作为止痛剂和局部用于治疗皮肤病的抗炎药
公开(公告)号：US5059602A
公开(公告)日：1991-10-22
申请号：US573414
申请日：1990-08-27
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： A61K31/505 , A61K31/485 , A61K31/519 , A61P17/00 , A61P25/04 , A61P29/00 , C07D213/16 , C07D239/20 , C07D471/04
CPC分类号： C07D471/04
摘要： There are described compounds of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylloweralkyl or aryl;R.sub.2 when present is hydrogen, loweralkyl, arylloweralkyl; andR.sub.3 is hydrogen, loweralkyl, cycloalkyl or aryl;which compounds are useful as analgesics and topical antiinflammatory agents for the treatment of skin disorders.

43. 发明授权

US5051430A 3-(1H-indazol-3-yl)-4-pyridinamines 失效
标题翻译： 3-（1H-吲唑-3-基）-4-吡啶胺
公开(公告)号：US5051430A
公开(公告)日：1991-09-24
申请号：US579751
申请日：1990-09-10
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： A61K31/40 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/4439 , A61P17/00 , A61P25/04 , A61P29/00 , C07D213/73 , C07D213/74 , C07D213/75 , C07D401/04
CPC分类号： C07D213/73 , C07D213/75 , C07D401/04
摘要： This invention relates to 3-(1H-indazol-3-yl)-4-pyridinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, arylalkyl or acyl; R.sub.2 is hydrogen, loweralkyl or arylalkyl; R.sub.3 is hydrogen, loweralkyl or aryl and X is hydrogen, halogen, nitro or amino or the pharmaceutically acceptable addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention are useful as analgesics and as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：本发明涉及式（Ia）的3-（1H-吲唑-3-基）-4-吡啶胺，其中R 1是氢，低级烷基，芳烷基或酰基; R2是氢，低级烷基或芳基烷基; R 3是氢，低级烷基或芳基，X是氢，卤素，硝基或氨基或其药学上可接受的加成盐，并且在适用的情况下，其几何和旋光异构体及其外消旋混合物。本发明的化合物可用作止痛剂和用作治疗各种皮肤病的局部抗炎剂。

44. 发明授权

US4983615A Heteroarylamino- and heteroaryloxypyridinamine compounds which are useful in treating skin disorders 失效
标题翻译：可用于治疗皮肤病症的杂芳基氨基和杂芳基嘧啶胺化合物
公开(公告)号：US4983615A
公开(公告)日：1991-01-08
申请号：US496723
申请日：1990-03-21
申请人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis , Russell R. L. Hamer , Brian S. Freed
发明人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis , Russell R. L. Hamer , Brian S. Freed
IPC分类号： C07D213/63 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4427 , A61P17/00 , C07D213/74 , C07D213/75 , C07D213/89 , C07D401/12 , C07D403/12 , C07D417/12
CPC分类号： C07D213/74 , C07D213/89 , C07D401/12 , C07D403/12
摘要： There are described compounds of the formula ##STR1## where n is 0 or 1;X is O or NR.sub.2, R.sub.2 being hydrogen, loweralkyl or loweralkylcarbonyl;R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl; andR.sub.1 is ##STR2## wherein R.sub.3 is hydrogen, loweralkyl or loweralkylcarbonyl; m is 1 or 2; each R.sub.4 is independently hydrogen or loweralkyl; and Y is hydrogen, halogen, loweralkyl, loweralkoxy or trifluoromethyl;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.

45. 发明授权

US4983608A N-substituted-4-pyrimidinamines and pyrimidinediamines 失效
标题翻译： N-取代-4-嘧啶胺和嘧啶二胺
公开(公告)号：US4983608A
公开(公告)日：1991-01-08
申请号：US402415
申请日：1989-09-05
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis , Gordon E. Olsen
IPC分类号： A61K31/505 , A61P25/04 , A61P25/28 , C07D403/12 , C07D403/14
CPC分类号： C07D403/12 , C07D403/14
摘要： This invention relates to N-heteroaryl-4-pyrimidinamines of the formula ##STR1## where R.sub.1 is hydrogen, loweralkyl, aryl, or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen or loweralkyl, or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen or lowealkyl, or R.sub.4 and R.sub.5 taken together are aryl; X is hydrogen, halogen, cyano, nitro, amino, loweralkyl, loweralkoxy, trifluoromethyl or ##STR2## where Y is hydrogen, halogen or loweralkyl; m is an integer of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometrical and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as memory enhancing agents and as analgesic agents.

46. 发明授权

US4959377A Phenoxypyridinamine compounds which are use as a dermatological composition 失效
标题翻译：用作皮肤病学组合物的苯氧吡啶胺化合物
公开(公告)号：US4959377A
公开(公告)日：1990-09-25
申请号：US372970
申请日：1989-06-29
申请人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis
发明人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61P17/00 , A61P29/00 , A61P37/08 , C07B41/04 , C07C39/02 , C07D213/68 , C07D213/73 , C07D213/75 , C07D213/89
CPC分类号： C07D213/73 , C07D213/68 , C07D213/75 , C07D213/89
摘要： There are described compounds of the formula ##STR1## where n is 0 or 1;X is hydrogen, loweralkyl, loweralkoxy, halogen, formyl, loweralkylcarbonyl, loweralkyoxycarbonyl, loweralkoxycarbonylloweralkyl or hydroxymethyl;Y is hydrogen or halogen;andR is hydrogen, loweralkyl arylloweralkyl or loweralkylcarbonyl,which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：描述式为“IMAGE”的化合物，其中n为0或1; X是氢，低级烷基，低级烷氧基，卤素，甲酰基，低级烷基羰基，低级烷氧基羰基，低级烷氧基羰基低级烷基或羟甲基; Y是氢或卤素; R是氢，低级烷基芳基低级烷基或低级烷基羰基，该化合物可用作治疗各种皮肤病的局部抗炎剂。

47. 发明授权

US4931457A Naphthylamino-and naphthyloxy-pyridinamine comounds useful as topical antiinflammatory agents for the treatment of skin disorders 失效
标题翻译：可用作治疗皮肤疾病的局部抗炎剂的萘基氨基 - 和萘氧基 - 吡啶胺化合物
公开(公告)号：US4931457A
公开(公告)日：1990-06-05
申请号：US372508
申请日：1989-06-28
申请人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis
发明人： Richard C. Effland , Joseph T. Klein , Gordon E. Olsen , Larry Davis
IPC分类号： A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61P17/00 , A61P29/00 , A61P37/08 , C07D213/68 , C07D213/73 , C07D213/74 , C07D213/89
CPC分类号： C07D213/89 , C07D213/68 , C07D213/73
摘要： There are described compounds of the formula ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;X is O or NR.sub.1, R.sub.1 being hydrogen, loweralkyl or loweralkylcarbonyl; andY is hydrogen, loweralkyl, loweralkoxy, halogen or trifluoromethyl;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R是氢，低级烷基，芳基低级烷基或低级烷基羰基; X是O或NR 1，R 1是氢，低级烷基或低级烷基羰基; Y为氢，低级烷基，低级烷氧基，卤素或三氟甲基; 哪些化合物可用作治疗皮肤病症的局部抗炎药。

48. 发明授权

US4883794A Pyrrolo(1,2-b)cinnolines 失效
标题翻译：吡咯（1,2-b）噌啉
公开(公告)号：US4883794A
公开(公告)日：1989-11-28
申请号：US286396
申请日：1988-12-19
申请人： R. Russell L. Hamer , Richard C. Effland , Joseph T. Klein
发明人： R. Russell L. Hamer , Richard C. Effland , Joseph T. Klein
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： There are described pyrrolo[1,2-b] cinnolines having formula ##STR1## where R.sub.1 when present is hydrogen, loweralky, arylloweralkyl or --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5 ; is hydrogen, loweralkyl, arylloweralkyl, chlorine, bromine, iodine, formyl, nitro, --CH.dbd.CR.sub.3 R.sub.4 or --CH.sub.2 CHR.sub.3 R.sub.4, R.sub.3 and R.sub.4 being independently hydrogen, loweralkyl, aryl or arylloweralkyl; X is oxygen, amino, loweralkylamino, arylloweralkylamino or methoxy; and Y is hydrogen, flourine, chlorine, bromine, iodine, trifluoromethyl or nitro, and pharmaceutically acceptable acid addition salts thereof which are useful as analgesic agents and as enhancers of cholinergic function and hence for the treatment of memory dysfunctions and senile demetia's such as Alzheimer's disease characterized by diminished cholinergic function.
摘要翻译：描述了具有式“IMAGE”的吡咯并[1,2-b]噌啉，其中R 1当存在时是氢，低级烷基，芳基低级烷基或-CH 2 CO 2 C 2 H 5; 芳基低级烷基，氯，溴，碘，甲酰基，硝基，-CH = CR 3 R 4或-CH 2 CHR 3 R 4，R 3和R 4独立地是氢，低级烷基，芳基或芳基低级烷基; X是氧，氨基，低级烷基氨基，芳基低级烷基氨基或甲氧基; 和Y是氢，氟，氯，溴，碘，三氟甲基或硝基，以及其药学上可接受的酸加成盐，其可用作止痛剂和作为胆碱能功能的增强剂，因此用于治疗记忆功能障碍和老年脱氨如阿尔茨海默病以胆碱能功能下降为特征的疾病。

49. 发明授权

US4794181A 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines 失效
标题翻译： 1-芳氧基-2,3,4,5-四氢-3-苯并吖庚因
公开(公告)号：US4794181A
公开(公告)日：1988-12-27
申请号：US819439
申请日：1986-01-16
申请人： Richard C. Effland , Joseph T. Klein , Larry Davis
发明人： Richard C. Effland , Joseph T. Klein , Larry Davis
IPC分类号： C07D223/16
CPC分类号： C07D223/16
摘要： The invention relates to 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines of the formula ##STR1## wherein Y is the same of different and is hydrogen and lower alkoxy; X is hydrogen, halogen, lower alkyl, lower alkoxy, CF.sub.3, NO.sub.2, CN and NH.sub.2 ; R is hydrogen, lower alkyl, cycloalkyllower alkyl, ##STR2## Ar lower alkyl of the formula ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen CF.sub.3, NO.sub.2 and NH.sub.2 ; Aryloxy lower alkyl of the formula ##STR4## where Z is as previously defined; and an alkylene amine of the formula ##STR5## where R.sub.1 and R.sub.2 are the same or different and are hydrogen and lower alkyl, n is an integer of 1 or 2; and the pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及式（I）的1-芳氧基-2,3,4,5-四氢-3-苯并吖庚因，其中Y是不同的并且是氢和低级烷氧基; X是氢，卤素，低级烷基，低级烷氧基，CF 3，NO 2，CN和NH 2; R是氢，低级烷基，环烷基低级烷基，其中Z是氢，低级烷基，低级烷氧基，卤素，CF 3，NO 2和NH 2; 其中Z如前所定义的式“IMAGE”的芳氧基低级烷基; 和式“IMAGE”的亚烷基胺，其中R 1和R 2相同或不同，为氢和低级烷基，n为1或2的整数; 及其药学上可接受的酸加成盐。

50. 发明授权

US4546105A Pyrrolylaminopiperidines, compositions thereof and methods of use 失效
标题翻译：吡咯基氨基哌啶，其组合物和使用方法
公开(公告)号：US4546105A
公开(公告)日：1985-10-08
申请号：US647309
申请日：1984-09-04
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： C07D401/12 , C07D409/14 , A61K31/445
CPC分类号： C07D401/12 , C07D409/14
摘要： This invention relates to pyrrolylaminopiperidines and related compounds of the formula ##STR1## where R is hydrogen, loweralkyl, Arloweralkyl, cycloalkylloweralkyl, loweralkenyl and thienylloweralkyl; R.sub.1 loweralkyl, hydrogen, loweralkylcarbonyl, loweralkoxycarbonyl, loweralkylthiocarbonyl of the formula ##STR2## cyano, loweralkylaminocarbonyl, diloweralkylaminocarbonyl, cycloalkylcarbonyl, cycloalkylloweralkylcarbonyl and loweralkenylcarbonyl; R.sub.2 is hydrogen, halogen and methyl; and the pharmaceutically acceptable acid addition salts thereof.
摘要翻译：本发明涉及吡咯并氨基哌啶及其相关化合物，其中R是氢，低级烷基，低级烷基，环烷基低级烷基，低级烯基和噻吩基低级烷基; R 1低级烷基，氢，低级烷基羰基，低级烷氧基羰基，低级烷硫基羰基，氰基，低级烷基氨基羰基，二低级烷基氨基羰基，环烷基羰基，环烷基低级烷基羰基和低级烯基羰基。 R2是氢，卤素和甲基; 及其药学上可接受的酸加成盐。

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