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101. 发明授权

US5663449A Intermediate compounds in the synthesis of heteroarylpiperidines, pyrrolidines and piperazines 失效
标题翻译：杂芳基哌啶，吡咯烷和哌嗪的合成中的中间体化合物
公开(公告)号：US5663449A
公开(公告)日：1997-09-02
申请号：US470059
申请日：1995-06-06
申请人： Joseph T. Strupczewski
发明人： Joseph T. Strupczewski
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 , C07D239/04 , C07D419/04
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。

102. 发明授权

US5646300A (1H-indol-1-yl)-2-(amino)acetamides and related (1H-indol-1-yl)-(aminoalkyl)amides, pharmaceutical composition and use 失效
标题翻译：（1H-吲哚-1-基）-2-（氨基）乙酰胺和相关的（1H-吲哚-1-基） - （氨基烷基）酰胺，药物组合物和用途
公开(公告)号：US5646300A
公开(公告)日：1997-07-08
申请号：US457649
申请日：1995-06-01
申请人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
发明人： Raymond W. Kosley, Jr. , Denise M. Flanagan , Lawrence L. Martin , Peter A. Nemoto
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61P25/00 , C07D209/08 , C07D209/12 , C07D209/30 , C07D209/10 , C07D493/04
CPC分类号： C07D209/08 , A61K31/40 , C07D209/12 , C07D209/30
摘要： There are disclosed neuroprotective compounds having the formula ##STR1## wherein the moieties are defined in the specification, and processes for making them.
摘要翻译：公开了具有式“IMAGE”的神经保护性化合物，其中部分在说明书中定义，以及制备它们的方法。

103. 发明授权

US5621114A Method for preparing 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：制备1,2,3,3,8,8a-六氢-3A，8（和1,3A，8）-DI（和TRI）甲基吡咯并[2,3-B]吲哚的方法
公开(公告)号：US5621114A
公开(公告)日：1997-04-15
申请号：US479197
申请日：1995-06-07
申请人： Richard L. Hamer , Grover C. Helsley , Edward J. Glamkowski , Yulin Chiang
发明人： 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。

104. 发明授权

US5614543A 1-(aryloxyalkyl)-3- (heteroaryl) pyrrolidines and related compounds useful as antipsychotics and analgesics 失效
标题翻译： 1-（芳氧基烷基）-3-（杂芳基）吡咯烷酮和可用作抗精神病药和镇痛药的相关化合物
公开(公告)号：US5614543A
公开(公告)日：1997-03-25
申请号：US469000
申请日：1995-06-06
申请人： Joseph T. Strupczewski , Kenneth J. Bordeau , Edward J. Glamkowski , Yulin Chiang , Grover C. Helsley
发明人： Joseph T. Strupczewski , Kenneth J. Bordeau , Edward J. Glamkowski , Yulin Chiang , Grover C. Helsley
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。通过向哺乳动物施用精神病治疗有效量的一种化合物，该化合物特别可用于治疗精神病。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。

105. 发明授权

US5608095A Alkyl-4-silyl-phenols and esters thereof as antiatherosclerotic agents 失效
标题翻译：烷基-4-甲硅烷基 - 苯酚及其酯作为抗动脉粥样硬化剂
公开(公告)号：US5608095A
公开(公告)日：1997-03-04
申请号：US637968
申请日：1996-04-30
申请人： Roger A. Parker , Michael L. Edwards , Mark J. Vaal , James E. Matt, Jr. , Kim S. Chen , Mark T. Yates , Paul S. Wright , Steven J. Busch
发明人： Roger A. Parker , Michael L. Edwards , Mark J. Vaal , James E. Matt, Jr. , Kim S. Chen , Mark T. Yates , Paul S. Wright , Steven J. Busch
IPC分类号： A61K31/695 , A61P3/06 , A61P11/06 , A61P19/02 , A61P29/00 , A61P37/00 , A61P43/00 , C07F7/08 , C07F7/10 , C07F7/12 , C07F7/18
CPC分类号： C07F7/0818
摘要： This invention relates to compounds of the formula ##STR1## wherein R.sub.1 and R.sub.6 are each independently C.sub.1 -C.sub.6 alkyl;R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl;R is hydrogen or --C(O)--(CH.sub.2).sub.m --Q wherein Q is hydrogen or --COOH and m is an integer 1, 2, 3 or 4;Z is a thio, oxy or methylene group;A is a C.sub.1 -C.sub.4 alkylene group;R.sub.5 and R.sub.7 are each independently a C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.n --(Ar) wherein n is an integer 0, 1, 2 or 3; and Ar is phenyl or naphthyl unsubstituted or substituted with one to three substituents selected from the group consisting of hydroxy, methoxy, ethoxy, halogen, trifluoromethyl, C.sub.1 -C.sub.6 alkyl, or --NR.sub.8 R.sub.9, wherein R.sub.8 and R.sub.9 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl; with the proviso that when R.sub.2 and at least one of R.sub.5 or R.sub.7 is C.sub.1 -C.sub.6 alkyl, and Ar is not substituted with trifluoromethyl or --NR.sub.8 R.sub.9, then R is --C(O)--(CH.sub.2).sub.m --Q; or a pharmaceutically acceptable salt thereof; useful for the treatment of atherosclerosis and chronic inflammatory disorders; for inhibiting cytokine-induced expression of VCAM-1 and/or ICAM-1; for inhibiting the peroxidation of LDL lipid; for lowering plasma cholesterol; and as antioxidant chemical additives useful for preventing oxidative deterioration in organic materials.
摘要翻译：本发明涉及式（1）的化合物，其中R 1和R 6各自独立地为C 1 -C 6烷基; R2，R3和R4各自独立地为氢或C1-C6烷基; R是氢或-C（O） - （CH 2）m-Q其中Q是氢或-COOH，m是整数1,2,3或4; Z是硫基，氧基或亚甲基; A是C1-C4亚烷基; R 5和R 7各自独立地为C 1 -C 6烷基或 - （CH 2）n - （Ar），其中n为整数0,1,2或3; 并且Ar是未取代的或被一至三个选自羟基，甲氧基，乙氧基，卤素，三氟甲基，C 1 -C 6烷基或-NR 8 R 9的取代基取代的苯基或萘基，其中R 8和R 9各自独立地为氢或C1- C6烷基; 条件是当R 2和R 5或R 7中的至少一个是C 1 -C 6烷基，并且Ar不被三氟甲基或-NR 8 R 9取代时，则R是-C（O） - （CH 2）m -Q; 或其药学上可接受的盐; 可用于治疗动脉粥样硬化和慢性炎症性疾病; 用于抑制VCAM-1和/或ICAM-1的细胞因子诱导的表达; 用于抑制LDL脂质的过氧化; 用于降低血浆胆固醇; 以及用作防止有机材料氧化变质的抗氧化剂添加剂。

106. 发明授权

US5589495A 2-[(3-heteroaryl-1-pyrrolidinyl)alkyl]-1,3- indandiones and related compounds and their therapeutic utility 失效
标题翻译： 2 - [（3-杂芳基-1-吡咯烷基）烷基] -1,3-茚二酮和相关化合物及其治疗用途
公开(公告)号：US5589495A
公开(公告)日：1996-12-31
申请号：US471515
申请日：1995-06-06
申请人： Edward J. Glamkowski , Yulin Chiang
发明人： Edward J. Glamkowski , Yulin Chiang
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 , C07D407/04 , C07D419/04
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。

107. 发明授权

US5567718A 2,3-dihydro-1h-isoindole derivatives and their use as serotonin reuptake inhibitors 失效
标题翻译： 2,3-二氢-1h异吲哚衍生物及其作为5-羟色胺再摄取抑制剂的用途
公开(公告)号：US5567718A
公开(公告)日：1996-10-22
申请号：US288844
申请日：1994-08-11
申请人： Gregory M. Shutske , Kevin J. Kapples
发明人： Gregory M. Shutske , Kevin J. Kapples
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/454 , A61P25/00 , A61P25/24 , A61P25/26 , A61P43/00 , C07D401/04
CPC分类号： C07D401/04
摘要： 2,3-dihydro-1H-isoindole derivatives of the formula ##STR1## where R.sub.1 -R.sub.5 and X are defined herein which are useful as serotonin reuptake inhibitors are disclosed. As such, these compounds may be useful for the treatment of depression, obsessive-compulsive disorders, stuttering and trichotillomania.
摘要翻译：公开了其中R1-R5和X定义为5-羟色胺再摄取抑制剂的式“IMAGE”的2,3-二氢-1H-异吲哚衍生物。因此，这些化合物可用于治疗抑郁症，强迫症，口吃和头发性痉挛症。

108. 发明授权

US5534551A Aminoguanidine spray drying process 失效
标题翻译：氨基胍喷雾干燥过程
公开(公告)号：US5534551A
公开(公告)日：1996-07-09
申请号：US318754
申请日：1994-12-22
申请人： Phillip E. Page , Jonathan Berman , Janet M. Pence , Sharon K. Minish
发明人： Phillip E. Page , Jonathan Berman , Janet M. Pence , Sharon K. Minish
IPC分类号： A61K9/14 , A61K20060101 , A61K9/20 , A61K31/155 , A61K47/38 , A61P3/00
CPC分类号： A61K31/155 , A61K9/2095
摘要： A compressed tablet comprising aminoguanidine or a pharmaceutically acceptable salt thereof and a suitably compatible binder prepared by spray drying techniques from an aminoguanidine solution, and methods of making same.
摘要翻译： PCT No.PCT / US93 / 02714 Sec。 371日期1994年12月22日第 102（e）日期1994年12月22日PCT 1993年3月24日PCT公布。公开号WO93 / 20808 日期：1993年10月28日。包含氨基胍或其药学上可接受的盐和通过氨基胍溶液的喷雾干燥技术制备的适当相容的粘合剂的压片，及其制备方法。

109. 发明授权

US5522625A Coupling device 失效
标题翻译：耦合装置
公开(公告)号：US5522625A
公开(公告)日：1996-06-04
申请号：US346378
申请日：1994-11-29
申请人： David L. Flick , Perry J. Parkhurst , Lauren W. Burnett
发明人： David L. Flick , Perry J. Parkhurst , Lauren W. Burnett
IPC分类号： F16L23/00
CPC分类号： F16L23/10 , Y10T24/1441
摘要： A coupling device is provided for coupling peripheral flanges of first and second pipes. The device comprises first and second arcuate retaining members, coupling structure and a latching mechanism. The coupling device is capable of being initially set via the latching mechanism so as to permit the coupling device to securely couple two pipe flanges of a given diameter. After being initially set, the device is capable of being easily and quickly disassembled and reassembled about the peripheral flanges of the two pipes.
摘要翻译：提供联接装置用于联接第一和第二管道的周边凸缘。该装置包括第一和第二弓形保持构件，联接结构和闩锁机构。联接装置能够经由闩锁机构初始设定，以便允许联接装置可靠地连接给定直径的两个管子凸缘。在初始设定之后，该装置能够容易且快速地拆卸和重新组装在两个管道的周边法兰上。

110. 发明授权

US6075144A 9-hydroxyamino tetrahydroacridine and related compounds 失效
标题翻译： 9-羟基氨基四氢吖啶及相关化合物
公开(公告)号：US6075144A
公开(公告)日：2000-06-13
申请号：US259739
申请日：1994-06-13
申请人： Gregory Michael Shutske , Kevin James Kapples
发明人： Gregory Michael Shutske , Kevin James Kapples
IPC分类号： C07D219/10 , C07D221/16 , C07D405/12 , C07D409/12 , C07D219/12 , C07D221/06
CPC分类号： C07D409/12 , C07D219/10 , C07D221/16 , C07D405/12
摘要： There are disclosed compounds having the formula ##STR1## wherein n is 1-4; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; R is hydrogen, loweralkyl or loweralkylcarbonyl; and R.sub.1 is hydrogen, loweralkyl, aryl, diloweralkylaminoloweralkyl, arylloweralkyl, furylloweralkyl, thienylloweralkyl, pyridinylloweralkyl, diarylloweralkyl, oxygen-bridged arylloweralkyl or oxygen-bridged diarylloweralkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof which are useful for enhancing memory.
摘要翻译：公开了具有下式的化合物，其中n为1-4; X是氢，低级烷基，环烷基，低级烷氧基，卤素，羟基，硝基，三氟甲基，甲酰基，低级烷基羰基，芳基羰基，-SH，低级烷硫基，-NHCOR2或-NR3R4，其中R2是氢或低级烷基，R3和R4独立地是氢，或环烷基; R是氢，低级烷基或低级烷基羰基; 芳基，低级烷基氨基低级烷基，芳基低级烷基，呋喃基低级烷基，噻吩基低级烷基，吡啶基低级烷基，二芳基低级烷基，氧桥连的芳基低级烷基或氧桥连的二芳基低级烷基。立体，光学和几何异构体及其药学上可接受的酸加成盐，其可用于增强记忆力。

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