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1. 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。

2. 发明授权

US5424322A A personality disorder treatment method and composition 失效
标题翻译：人格障碍治疗方法及组成
公开(公告)号：US5424322A
公开(公告)日：1995-06-13
申请号：US38427
申请日：1993-03-25
申请人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
发明人： Richard C. Effland , Joseph T. Klein , Lawrence L. Martin
IPC分类号： C07D401/12 , C07D409/12 , C07D417/12 , A61K31/44
CPC分类号： C07D401/12 , C07D409/12 , C07D417/12
摘要： This invention relates to compositions of substituted pyridinylamino-1H-indoles of the formula ##STR1## wherein Q is N or NR.sub.2 ;Y is CHR.sub.1 is hydrogen, loweralkyl, loweralkynyl, loweralkenyl, arylloweralkyl, loweralkoxycarbonylaminoloweralkylcarbonyl, arylloweralkoxycarbonylaminoloweralkylcarbonyl, aminoloweralkylcarbonyl, loweralkoxycarbonyl or acyl;R.sub.2 is hydrogen or loweralkyl;R.sub.3 is hydrogen or loweralkyl;X is hydrogen, loweralkyl, halogen; andn is 0 or 1 with utility in the treatment of personality disorders as obsessive compulsive disorders.
摘要翻译：本发明涉及式（I）的取代吡啶基氨基-1H-吲哚的组合物，其中Q是N或NR2; Y是CHR 1是氢，低级烷基，低级炔基，低级烯基，芳基低级烷基，低级烷氧基羰基氨基低级烷基羰基，芳基低级烷基羰基，低级烷氧基羰基或酰基。 R2是氢或低级烷基; R3是氢或低级烷基; X是氢，低级烷基，卤素; n为0或1，可用于治疗人格障碍作为强迫症。

3. 发明授权

US5229417A 2-(3-phenylpropyl)hydrazines and method of treating personality disorders 失效
标题翻译： 2-（3-苯丙氨酸）水解剂和治疗个体病症的方法
公开(公告)号：US5229417A
公开(公告)日：1993-07-20
申请号：US802599
申请日：1991-12-05
申请人： Richard C. Effland , Joseph T. Klein
发明人： Richard C. Effland , Joseph T. Klein
IPC分类号： A61K31/15 , A61K31/16 , A61K31/165 , A61K31/27 , A61P25/00 , A61P25/18 , A61P25/20 , A61P43/00 , C07C241/02 , C07C243/06 , C07C243/10 , C07C243/18 , C07C243/24 , C07C243/28 , C07C243/30 , C07C243/32 , C07C271/60 , C07C281/02
CPC分类号： C07C243/28 , C07C243/06 , C07C243/18 , C07C243/32 , C07C281/02
摘要： Novel 2-(3-phenylpropyl)hydrazines, intermediates in and processes for the preparation thereof, and a method of treating personality disorders utilizing compounds or compositions thereof are disclosed.

4. 发明授权

US5221682A Heteroarylamino- and heteroaryloxypyridinamines and related compounds 失效
标题翻译：杂芳基氨基和杂芳氧基吡啶胺及相关化合物
公开(公告)号：US5221682A
公开(公告)日：1993-06-22
申请号：US695156
申请日：1991-05-03
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： C07D213/74 , C07D213/89 , C07D401/12 , C07D403/12
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 dematoses.
摘要翻译：描述式为“IMAGE”的化合物，其中n为0或1; X是O或NR 2，R 2是氢，低级烷基或低级烷基羰基; R是氢，低级烷基，芳基低级烷基或低级烷基羰基; R1是其中R3是氢，低级烷基或低级烷基羰基; m为1或2; 每个R 4独立地是氢或低级烷基; Y为氢，卤素，低级烷基，低级烷氧基或三氟甲基; 哪些化合物可用作治疗各种甲状腺炎的局部抗炎药。

5. 发明授权

US5179099A 2,3-dihydro-1-(pyridinylamino)-indoles 失效
标题翻译： 2,3-二氢-1-（吡啶基氨基） - 吲哚
公开(公告)号：US5179099A
公开(公告)日：1993-01-12
申请号：US705220
申请日：1991-05-24
申请人： Richard C. Effland , David G. Wettlaufer , Joseph T. Klein
发明人： Richard C. Effland , David G. Wettlaufer , Joseph T. Klein
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： This invention relates to 2,3-dihydro-1-(pyridinylamino)-indoles of the formula ##STR1## wherein R.sub.1 is hydrogen, loweralkyl, aryl, arylloweralkyl, alkenyl, alkynyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; R.sub.2 and R.sub.3 and independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl; or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl or heteroaryl; the term heteroaryl signifying a group selected from pyridine or thiophene; X and Y are independently hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m and n are independently integers of 1 to 3, or a pharmaceutically acceptable acid addition salt thereof or where appropriate, an optical, geometrical or stereoisomer or racemic mixture thereof. The compounds of this invention are useful as analgesics, anticonvulsants, and for the treatment of memory dysfunctions characterized by a cholinergic deficit.
摘要翻译：本发明涉及式IMA的2,3-二氢-1-（吡啶基氨基） - 吲哚，其中R 1是氢，低级烷基，芳基，芳基低级烷基，烯基，炔基或杂芳基低级烷基，其选自吡啶基甲基，吡啶基乙基，噻吩基甲基，噻吩乙基; R2和R3独立地是氢，低级烷基，芳基，芳基低级烷基或杂芳基低级烷基，选自吡啶基甲基，吡啶基乙基，噻吩基甲基，噻吩基乙基; 或R 2和R 3一起形成4至6个碳的环烷烃环或螺稠合的芳基或杂芳基; 表示选自吡啶或噻吩的基团的术语杂芳基; X和Y独立地是氢，卤素，羟基，低级烷基，低级烷氧基，硝基，氨基或三氟甲基; m和n独立地为1至3的整数，或其药学上可接受的酸加成盐，或适当时为其光学，几何或立体异构体或外消旋混合物。本发明的化合物可用作镇痛药，抗惊厥药，并用于治疗以胆碱能缺乏为特征的记忆功能障碍。

6. 发明授权

US5037835A Benzocycloalkylaminopyridinamines and related compounds as topical antiinflammatory agents for the treatment of skin disorders 失效
标题翻译：苯并环烷基氨基吡啶胺和相关化合物作为治疗皮肤病症的局部抗炎药
公开(公告)号：US5037835A
公开(公告)日：1991-08-06
申请号：US588789
申请日：1990-09-27
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： C07D401/04
CPC分类号： C07D401/04
摘要： There are described compounds of the formula, ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;k is 0 or 1;m is 1, 2 or 3;k+m is 2 or 3; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.
摘要翻译：描述了下式的化合物，其中R是氢，低级烷基，芳基低级烷基或低级烷基羰基; k为0或1; m为1,2或3; k + m为2或3; 并且n为0或1; 哪些化合物可用作治疗各种皮肤病的局部抗炎剂。

7. 发明授权

US5032599A N-(pyrrol-l-yl)pyridinamines 失效
标题翻译： N-（吡咯-1-基）吡啶胺
公开(公告)号：US5032599A
公开(公告)日：1991-07-16
申请号：US245252
申请日：1988-09-16
申请人： Richard C. Effland , Joseph T. Klein , Kevin J. Kapples
发明人： Richard C. Effland , Joseph T. Klein , Kevin J. Kapples
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： There are disclosed novel compounds of the formula ##STR1## where n is 0 or 1; R is hydrogen or loweralkyl; R.sub.1 is hydrogen, loweralkyl, halogen, cyano, loweralkanoyl, arylloweralkanoyl, aroyl, --CH(OH)R.sub.4, --C(OH)R.sub.4 R.sub.5 or --CH.sub.2 OR.sub.5, --CH.dbd.CR.sub.6 R.sub.7, --CH.dbd.CHCN, --CH.dbd.CHOCH.sub.3, --CH.dbd.CHCO.sub.2 C.sub.2 H.sub.5, ##STR2## R.sub.4 being hydrogen, loweralkyl, arylloweralkyl or aryl, R.sub.5 being loweralkyl, aryl or arylloweralkyl, R.sub.6 being hydrogen or loweralkyl and R.sub.7 being hydrogen, loweralkyl or aryl; R.sub.2 is hydrogen, loweralkyl, loweralkenyl, loweralkynyl, --CH.sub.2 CO.sub.2 C.sub.2 H.sub.5, arylloweralkyl, phenyl, nitrophenyl, cyanophenyl, trifluoromethylphenyl, aminophenyl, loweralkanoylaminophenyl, loweralkoxycarbonyl, arylloweralkoxycarbonyl, aryloxycarbonyl, loweralkylaminocarbonyl, arylloweralkylaminocarbonyl, arylaminocarbonyl, alkanoyl, arylloweralkanoyl, aroyl, alkenoyl, alkynoyl, --CH.sub.2 C.tbd.CCH.sub.2 --NR'R", --CH.sub.2 CH.dbd.CHCH.sub.2 --NR'R" or --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 --NR'R", R' and R" being independently loweralkyl or --NR'R" taken as a whole being ##STR3## and R.sub.3 is hydrogen, NO.sub.2, NH.sub.2, halogen, loweralkanoylamino, arylloweralkanoylamino, aroylamino or loweralkyl; with the proviso that when n is 0, R.sub.2 is phenyl, R.sub.3 is hydrogen and the pyridine moiety is 2-pyridinyl, R and R.sub.1 may not be 2-methyl and 5-methyl; or pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory, methods for synthesizing them, pharmaceutical compositions comprising an effective memory enhancing amount of such a compound and a method of treating a patient in need of memory enhancement which comprises administering such a compound to the patient.
摘要翻译：公开了新颖的化合物，其中n为0或1; R是氢或低级烷基; R 1是氢，低级烷基，卤素，氰基，低级烷酰基，芳基低级烷酰基，芳酰基，-CH（OH）R 4，-C（OH）R 4 R 5或-CH 2 OR 5，-CH = CR 6 R 7，-CH = CHCN，-CH = CHOCH 3，-CH R 2是氢，低级烷基，芳基低级烷基或芳基，R 5是低级烷基，芳基或芳基低级烷基，R 6是氢或低级烷基，R 7是氢或低级烷基，R 7是氢，是氢，低级烷基或芳基; R2是氢，低级烷基，低级烯基，低级炔基，-CH2CO2C2H5，芳基低级烷基，苯基，硝基苯基，氰基苯基，三氟甲基苯基，氨基苯基，低级烷酰基氨基苯基，低级烷氧基羰基，芳基低级烷氧基羰基，芳氧基羰基，低级烷基氨基羰基，芳基低级烷基氨基羰基，芳基氨基羰基，烷酰基，芳基低级烷酰基，芳酰基，烯酰基， CH2C 3BOND CCH2-NR'R“，-CH2CH = CHCH2-NR'R”或-CH2CH2CH2CH2-NR'R“，R'和R”独立地为低级烷基或-NR'R“ 并且R 3是氢，NO 2，NH 2，卤素，低级烷酰基氨基，芳基低级烷酰基氨基，芳酰基氨基或低级烷基; 条件是当n是0时，R2是苯基，R3是氢，吡啶部分是2-吡啶基，R和R1可以不是2-甲基和5-甲基; 其可用于增强记忆，其合成方法，包含有效记忆增加量的这种化合物的药物组合物和治疗需要记忆增强的患者的方法，其包括给予这种化合物给病人

8. 发明授权

US5017578A N-heteroaryl-purin-6-amines useful as analgesic and anticonvulsant agents 失效
标题翻译： N-杂芳基 - 嘌呤-6-胺可用作止痛剂和抗惊厥剂
公开(公告)号：US5017578A
公开(公告)日：1991-05-21
申请号：US363837
申请日：1989-06-09
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： A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7076 , A61P25/04 , C07D403/12 , C07D403/14 , C07D473/34 , C07H19/16 , C07H19/167
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 anticonvulsant agents.

9. 发明授权

US4992448A Benzocycloalkylaminopyridinamines and related compounds as topical antiinflammatory agents for the treatment of skin disorders 失效
标题翻译：苯并环烷基氨基吡啶胺和相关化合物作为治疗皮肤病症的局部抗炎药
公开(公告)号：US4992448A
公开(公告)日：1991-02-12
申请号：US425712
申请日：1989-10-24
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 , A61K31/4427 , A61K31/47 , A61P17/00 , A61P29/00 , C07D401/04
CPC分类号： C07D401/04
摘要： There are described compounds of the formula, ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;k is 0 or 1;m is 1,2 or 3;k+m is 2 or 3; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.

10. 发明授权

US4988690A 1-aryloxy-2,3,4,5-tetrahydro-3-benzazepines and anti-depressant use thereof 失效
标题翻译： 1-芳氧基-2,3,4,5-四氢-3-苯并氮杂及其抗抑郁剂
公开(公告)号：US4988690A
公开(公告)日：1991-01-29
申请号：US387916
申请日：1982-06-14
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： A61K31/55 , A61P9/12 , A61P25/04 , A61P25/24 , A61P25/26 , C07D223/16 , C07D233/16
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 or 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 -alkylene ##STR3## where Z is hydrogen, lower alkyl, lower alkoxy, halogen, CF.sub.3, NO.sub.2 and NH.sub.2 ; and an alkylene amine of the formula ##STR4## where R.sub.1 and R.sub.2 are the same of different and are hydrogen and lower alkyl, 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相同或不同，为氢和低级烷氧基; 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的式 - 亚烷基的低级烷基; 和其中R 1和R 2相同且为氢和低级烷基的式“IMAGE”的亚烷基胺及其药学上可接受的酸加成盐。

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