公开(公告)号：US5102891A

公开(公告)日：1992-04-07

申请号：US555890

申请日：1990-07-23

申请人： Richard C. Effland ,  Larry Davis ,  Gordon E. Olsen ,  Joseph T. Klein ,  David G. Wettlaufer ,  Peter A. Nemoto

发明人： Richard C. Effland ,  Larry Davis ,  Gordon E. Olsen ,  Joseph T. Klein ,  David G. Wettlaufer ,  Peter A. Nemoto

IPC分类号： A61K31/44 ,  A61K31/4427 ,  A61K31/535 ,  A61K31/55 ,  A61P25/28 ,  A61P43/00 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C12N9/99

CPC分类号： C07D401/12 ,  C07D401/14

摘要： There are disclosed various compounds of the formula below, ##STR1## where n is 0 or 1;X is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;Y is hydrogen, halogen, nitro, amino, trifluoromethyl, loweralkyl, or loweralkoxy;R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkynyl, loweralkanoyl, arylloweralkanoyl, heteroarylloweralkyl or heteroarylloweralkanoyl;R.sub.2 is hydrogen, loweralkyl, formyl or cyano;R.sub.3 is hydrogen or loweralkyl;R.sub.4 is loweralkyl, arylloweralkyl, cycloalkyl, aryl or heteroaryl; or alternatively, --NR.sub.3 R.sub.4 taken together constitutes ##STR2## R.sub.5 being hydrogen, loweralkyl, aryl, arylloweralkyl, heteroaryl or heteroarylloweralkyl,which compounds are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.

摘要翻译： 公开了下式的各种化合物，其中n为0或1; X是氢，卤素，硝基，氨基，三氟甲基，低级烷基或低级烷氧基; Y是氢，卤素，硝基，氨基，三氟甲基，低级烷基或低级烷氧基; R 1是氢，低级烷基，芳基低级烷基，低级烯基，低级炔基，低级烷酰基，芳基低级烷酰基，杂芳基低级烷基或杂芳基低级烷酰基。 R2是氢，低级烷基，甲酰基或氰基; R3是氢或低级烷基; R4是低级烷基，芳基低级烷基，环烷基，芳基或杂芳基; 或者可选地，-NR 3 R 4一起构成R 5为氢，低级烷基，芳基，芳基低级烷基，杂芳基或杂芳基低级烷基，该化合物可用于治疗以胆碱能缺乏为特征的各种记忆功能障碍如阿尔茨海默氏病。

公开(公告)号：US5097033A

公开(公告)日：1992-03-17

申请号：US638933

申请日：1991-01-09

申请人： Richard C. Allen ,  Marc N. Agnew ,  David M. Fink

发明人： Richard C. Allen ,  Marc N. Agnew ,  David M. Fink

IPC分类号： C07D471/08

CPC分类号： C07D471/08

摘要： Novel 2,6-methano-1,3-benzodiazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain and for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease, utilizing compounds or compositions thereof are disclosed.

摘要翻译： 新颖的2,6-亚甲基-1,3-苯并二氮杂环丁烷，中间体，其制备方法，利用化合物或组合物，减轻疼痛和减轻胆碱能功能降低的各种记忆障碍功能如阿尔茨海默病的方法， 披露

公开(公告)号：US5096906A

公开(公告)日：1992-03-17

申请号：US622138

申请日：1990-12-05

申请人： Gerald L. Mandell ,  Gail W. Sullivan ,  William J. Novick

发明人： Gerald L. Mandell ,  Gail W. Sullivan ,  William J. Novick

IPC分类号： A61K31/52

CPC分类号： A61K31/52 ,  Y10S514/929

摘要： A family of compounds effective in inhibiting interleukin-1 (IL-1) activity, tumor necrosis factor (TNF) activity, and the activity of other leukocyte derived cytokines is comprised of 7-(oxoalkyl) 1,3-dialkyl xanthines of the formula ##STR1## in which R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of straight-chain or branched alkyl radicals with 2 to 6 carbon atoms, cyclohexyl, alkoxyalkyl and hydroxyalkyl radicals, and A represents a hydrocarbon radical with up to 4 carbon atoms which can be substituted by a methyl group. Another family of effective compounds is identified as ##STR2## The inhibition of IL-1, TNF, and other cytokines in mammals is implicated in alleviation of a wide variety of disease conditions.

摘要翻译： 有效抑制白细胞介素-1（IL-1）活性，肿瘤坏死因子（TNF）活性和其他白细胞衍生细胞因子活性的化合物家族由式（VII）的7-（氧代烷基）1,3-二烷基黄嘌呤组成 其中R1和R2相同或不同并且选自具有2至6个碳原子的直链或支链烷基，环己基，烷氧基烷基和羟烷基，并且A表示烃 具有多达4个可被甲基取代的碳原子的基团。 （II）哺乳动物中IL-1，TNF和其他细胞因子的抑制涉及缓解各种疾病状况。

公开(公告)号：US5089615A

公开(公告)日：1992-02-18

申请号：US640348

申请日：1991-01-11

申请人： Lawrence L. Martin ,  Joseph F. Payack ,  Helen H. Ong

发明人： Lawrence L. Martin ,  Joseph F. Payack ,  Helen H. Ong

IPC分类号： C07D219/10 ,  C07D413/04

CPC分类号： C07D413/04 ,  C07D219/10

摘要： There are described compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy or halogen;R when present is hydrogen, loweralkyl or aryloweralkyl;R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; andR.sub.2 when present is hydrogen or loweralkyl;which compounds are useful for alleviating various memory dysfunctions characterized by a decreased cholinergic function such Alzheimer's disease.

摘要翻译： 描述了式（I）的化合物，其中X是氢，低级烷基，低级烷氧基或卤素; 存在时R为氢，低级烷基或芳基烷基; R1是氢，低级烷基或芳基低级烷基; 当R 2为氢或低级烷基时; 哪些化合物可用于缓解以胆碱能功能降低为特征的各种记忆功能障碍，如阿尔茨海默氏病。

公开(公告)号：US5045546A

公开(公告)日：1991-09-03

申请号：US603491

申请日：1990-10-26

申请人： Nicholas J. Hrib ,  John G. Jurcak

发明人： Nicholas J. Hrib ,  John G. Jurcak

IPC分类号： A61K31/46 ,  A61P25/18 ,  C07D451/08

CPC分类号： C07D451/08

摘要： Novel 8-azabicyclo[3.2.1]octylalkylthiazolidinones of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, m, x and y are defined herein, process for the preparation thereof, and methods of treating psychoses and alleviating pain employing compounds and compositions thereof are disclosed.

摘要翻译： 其中R 1，R 2，R 3，R 4，m，x和y在本文中定义的式IMAGE的新型8-氮杂双环[3.2.1]辛基烷基噻唑烷酮，其制备方法，以及使用化合物治疗精神病和缓解疼痛的方法 并且其组合物被公开。

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。

公开(公告)号：US5039809A

公开(公告)日：1991-08-13

申请号：US594496

申请日：1990-10-09

申请人： Richard C. Effland ,  David M. Fink

发明人： Richard C. Effland ,  David M. Fink

IPC分类号： C07D213/64

CPC分类号： C07D213/64

摘要： A compound of the formula: ##STR1## where n is 1, 2, or 3;R.sub.3 is hydrogen or loweralkyl;R.sub.4 is hydrogen or loweralkyl; andAr is a phenyl group optionally mono-substituted with a loweralkoxy, halogen or trifluoromethyl group which are useful as intermediates.

摘要翻译： 下式的化合物：其中n为1,2或3; R3是氢或低级烷基; R4是氢或低级烷基; 并且Ar是任选被用作中间体的低级烷氧基，卤素或三氟甲基单取代的苯基。

公开(公告)号：US5037984A

公开(公告)日：1991-08-06

申请号：US487328

申请日：1990-03-02

申请人： Nicholas J. Hrib ,  John G. Jurcak

发明人： Nicholas J. Hrib ,  John G. Jurcak

IPC分类号： A61K31/425 ,  A61K31/44 ,  A61K31/47 ,  A61K31/495 ,  A61K31/505 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D277/14 ,  C07D277/60 ,  C07D277/82 ,  C07D417/12 ,  C07D417/14 ,  C07D513/10

CPC分类号： C07D277/60 ,  C07D277/14 ,  C07D277/82 ,  C07D417/12 ,  C07D417/14

摘要： There are disclosed compounds of the formula ##STR1## where n is 0 or 1; A is ##STR2## where X in each occurrence is independently hydrogen, halogen, loweralkyl hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R.sub.1 and R.sub.2 are independently hydrogen, loweralkyl, ##STR3## or aryl except that when R.sub.1 is ##STR4## or aryl, R.sub.2 is hydrogen, or alternatively R.sub.1 +R.sub.2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl, or alternatively R.sub.3 +R.sub.4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkythio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

摘要翻译： 公开了下式的化合物，其中n为0或1; A是每一次出现的X独立地是氢，卤素，低级烷基羟基，硝基，低级烷氧基，氨基，氰基，三氟甲基或甲硫基; Y在每次出现时独立地是氢，卤素，低级烷基，羟基，硝基，低级烷氧基，氨基，氰基，三氟甲基或甲硫基; m为1或2; k为1或2; R1和R2独立地是氢，低级烷基，低级或芳基，除了当R 1是芳基或芳基时，R 2是氢，或者R 1 + R 2与它们所连接的碳原子一起形成环戊烷，环己烷 ，环庚烷，吡喃，噻喃，茚满或哌啶环; R3和R4独立地是氢或低级烷基，或者R3 + R4与它们所连接的碳原子一起形成环戊烷，环己烷，环庚烷，吡喃，噻喃，吡咯烷或哌啶环，术语表示未取代的苯基的芳基 或被1,2或3个取代基取代的苯基，其各自独立地为低级烷基，低级烷氧基，羟基，卤素，低级链段，氰基，氨基或三氟甲基，其可用作抗精神病药，镇痛药，抗惊厥药和抗焦虑剂。

公开(公告)号：US5006536A

公开(公告)日：1991-04-09

申请号：US457132

申请日：1989-12-26

申请人： Richard C. Effland ,  David G. Wettlaufer

发明人： Richard C. Effland ,  David G. Wettlaufer

IPC分类号： A61K31/38 ,  A61K31/381 ,  A61P25/04 ,  C07D333/16 ,  C07D333/74 ,  C07D409/04 ,  C07D409/06 ,  C07D495/04

CPC分类号： C07D409/04 ,  C07D409/06 ,  C07D495/04

摘要： Novel thienobenzoxepins and naphthothiophenes, intermediates and processes for the preparation thereof, and methods of alleviating pain utilizing compounds or compositions thereof are disclosed.

公开(公告)号：US4999351A

公开(公告)日：1991-03-12

申请号：US295840

申请日：1989-01-11

申请人： Raymond W. Kosley, Jr. ,  Gerard O'Malley ,  Bettina Spahl

发明人： Raymond W. Kosley, Jr. ,  Gerard O'Malley ,  Bettina Spahl

IPC分类号： C07D311/92 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D473/00 ,  C07D493/06 ,  C07D493/10

CPC分类号： C07D405/12 ,  C07D311/92 ,  C07D473/00 ,  C07D493/10

摘要： Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.