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21. 发明授权

US5750521A Mercaptoacetylamide disulfide derivatives useful as inhibitors of enkephalinase and ACE 失效
标题翻译：巯基乙酰胺二硫化物衍生物可用作脑啡肽酶和ACE的抑制剂
公开(公告)号：US5750521A
公开(公告)日：1998-05-12
申请号：US669521
申请日：1996-11-04
申请人： Gary A. Flynn , Douglas W. Beight , Shujaath Mehdi , Alan M. Warshawsky , John F. French , John H. Kehne
发明人： Gary A. Flynn , Douglas W. Beight , Shujaath Mehdi , Alan M. Warshawsky , John F. French , John H. Kehne
IPC分类号： C07D487/04 , A61K31/55 , A61K38/00 , A61P1/00 , A61P1/12 , A61P5/38 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P25/04 , A61P25/24 , A61P25/28 , A61P27/02 , A61P27/06 , A61P39/02 , A61P43/00 , C07D471/04 , C07D491/052 , C07D498/04 , C07D513/04 , C07K5/078
CPC分类号： C07D471/04 , A61K31/55 , C07K5/06139 , A61K38/00
摘要： The present invention relates to certain mercaptoacetylamide disulfide derivatives of Formula (I) ##STR1## useful as inhibitors of enkephalinase and ACE.
摘要翻译： PCT No.PCT / US94 / 14235 Sec。 371日期：1996年11月4日 102（e）日期1996年11月4日PCT 1994年12月13日PCT PCT。公开号WO95 / 21839 日期：1995年8月17日本发明涉及可用作脑啡肽酶和ACE抑制剂的式（I）的式（I）的某些巯基乙酰胺二硫化物衍生物。

22. 发明授权

US5747708A Retractable batch reactor sampler 失效
标题翻译：伸缩式间歇式反应器取样器
公开(公告)号：US5747708A
公开(公告)日：1998-05-05
申请号：US745765
申请日：1996-11-08
申请人： Franz Josef Weiberth
发明人： Franz Josef Weiberth
IPC分类号： G01N1/20 , G01N1/12
CPC分类号： G01N1/2035
摘要： This application relates to a retractable batch reactor sampler that is temporarily attached to a reactor, for use in sampling small volumes of a reaction mixture within a reactor on single or multiple occasions, and then detached from the reactor, all without affecting an inert gas blanket already existing within the reactor.
摘要翻译：本申请涉及一种可伸缩的间歇式反应器取样器，其暂时连接到反应器，用于在单个或多个场合对反应器内的小体积反应混合物进行取样，然后从反应器中分离，全部不影响惰性气体层已经存在于反应堆内。

23. 发明授权

US5739354A Process for the preparation of N-methyl-D-phenylalanyl-N-�1-�3-�(aminoiminomethyl)amino!propyl!-3,3-dif luoro-2-oxohexyl!-L-prolinamide 失效
标题翻译：制备N-甲基-D-苯丙氨酰-N- [1- [3 - [（氨基亚氨基甲基）氨基]丙基] -3,3-二氟-2-氧代己基] -L-脯氨酰胺的方法
公开(公告)号：US5739354A
公开(公告)日：1998-04-14
申请号：US786997
申请日：1997-01-23
申请人： Duane E. Rudisill
发明人： Duane E. Rudisill
IPC分类号： C07D207/16 , C07D207/08 , C07C215/06
CPC分类号： C07D207/16
摘要： The present invention relates to a novel process for preparing preparing N-methyl-D-phenylalanyl-N-�1-�3-�(aminoiminomethyl)amino!propyl!-3,3-difluoro-2-oxohexyl!-L-prolinamide or a pharmaceutically acceptable salt thereof and to a key intermediate by directly guanylating Dakin-West intermediates.
摘要翻译：本发明涉及制备N-甲基-D-苯丙氨酰-N- [1- [3 - [（氨基亚氨基甲基）氨基]丙基] -3,3-二氟-2-氧己基] -L-脯氨酰胺的新方法或其药学上可接受的盐，并通过直接脯氨酸化Dakin-West中间体与关键中间体反应。

24. 发明授权

US5734062A Method of preparation of physostigmine carbamate derivatives from eseretholes 失效
标题翻译：从eseretholes制备毒扁豆碱氨基甲酸酯衍生物的方法
公开(公告)号：US5734062A
公开(公告)日：1998-03-31
申请号：US858987
申请日：1997-05-20
申请人： Thomas B. K. Lee , Zhongli Gao
发明人： Thomas B. K. Lee , Zhongli Gao
IPC分类号： C07D487/04 , C07D471/02
CPC分类号： C07D487/04
摘要： This invention relates to a process for the preparation of a product of the formula ##STR1## wherein R is loweralkyl; R.sub.1 is hydrogen, loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; Rs is loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; or R.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are attached form a group of the formula (Ia) ##STR2## wherein Y is hydrogen or loweralkyl and Z is hydrogen, loweralkyl, halogen, loweralkoxy or hydroxy; X is loweralkyl, loweralkoxy, halogen or trifluoromethyl; and m is 0, 1 or 2; or a pharmaceutically acceptable salt thereof; which process comprises(a) contacting a compound of formula (II) as defined herein with fortified hydrogen bromide to afford a compound of formula (III) as defined herein; contacting the reaction mixture containing a compound of formula (III) with either (1) an isocyanate of formula R.sub.1 NCO or (2) with a compound of formula (IV) as defined to afford a compound of formula (V) as defined herein and contacting the reaction mixture containing the compound of formula (V) with an amine of the formula R.sub.1 R.sub.2 NH herein in the presence of a carboxylic acid of the formula R.sub.5 COOH and forming and isolating the product of Formula (I).
摘要翻译：本发明涉及一种制备式（I）的产物的方法，其中R是低级烷基; R 1是氢，低级烷基，低级环烷基，低级环烷基低级烷基，低级双环烷基，芳基或芳基低级烷基; 低级烷基，低级环烷基，低级环烷基低级烷基，低级二环烷基，芳基或芳基低级烷基; 或者R 1和R 2与它们所连接的氮原子一起形成式（Ia）的基团，其中Y是氢或低级烷基，Z是氢，低级烷基，卤素，低级烷氧基或羟基; X是低级烷基，低级烷氧基，卤素或三氟甲基; m为0,1或2; 或其药学上可接受的盐; 该方法包括（a）使本文定义的式（II）化合物与强化溴化氢接触，得到本文定义的式（III）化合物; 使含有式（III）化合物的反应混合物与（1）式R1NCO或（2）的异氰酸酯与式（IV）化合物的定义相接触，得到如本文所定义的式（V）化合物和接触本文在式R 5 COOH的羧酸存在下将含有式（Ⅴ）化合物的反应混合物与式R 1 R 2 NH的胺反应，并形成并分离式（I）的产物。

25. 发明授权

US5728717A Pyridiniminyl-1,2-benzisothiazoles 失效
标题翻译：吡啶亚甲基-1,2-苯并异噻唑
公开(公告)号：US5728717A
公开(公告)日：1998-03-17
申请号：US806981
申请日：1997-02-26
申请人： David M. Fink , Barbara E. Kurys , Gregory M. Shutske , John D. Tomer, IV
发明人： David M. Fink , Barbara E. Kurys , Gregory M. Shutske , John D. Tomer, IV
IPC分类号： A61K31/44 , A61K31/4439 , A61K31/495 , A61K31/496 , A61K31/55 , A61K31/551 , A61P25/00 , A61P25/18 , A61P25/24 , A61P25/28 , C07D231/56 , C07D261/20 , C07D275/04 , C07D403/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D401/12
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12
摘要： Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermediates, or compositions thereof are disclosed.
摘要翻译：公开了新的吡啶亚甲基-1,2-苯并异恶唑和 - 苯并异噻唑，其制备方法和方法，以及利用1,2-苯并异恶唑和 - 苯并异噻唑及其中间体缓解记忆功能障碍和治疗抑郁症的方法或其组合物。

26. 发明授权

US5672602A Substituted piperazine derivatives 失效
标题翻译：取代的哌嗪衍生物
公开(公告)号：US5672602A
公开(公告)日：1997-09-30
申请号：US640121
申请日：1996-04-30
申请人： Timothy P. Burkholder , Tieu-Binh Le , Elizabeth M. Kudlacz
发明人： Timothy P. Burkholder , Tieu-Binh Le , Elizabeth M. Kudlacz
IPC分类号： C07D241/04 , A61K31/50 , A61P1/00 , A61P1/08 , A61P11/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P27/02 , A61P27/14 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D241/08 , C07D309/12 , C07D403/06 , A61K31/495 , C07D403/04
CPC分类号： C07D403/06 , C07D241/08 , C07D309/12
摘要： The present invention relates to substituted piperazine derivatives (herein referred to as compounds or compounds of formula (1)) or stereoisomers, or pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, cough, and bronchitis.
摘要翻译：本发明涉及取代的哌嗪衍生物（本文中称为化合物或式（1）的化合物）或其立体异构体或其药学上可接受的盐及其作为速激肽受体拮抗剂的用途。这样的拮抗剂可用于治疗速激肽介导的疾病和本文公开的病症，包括：哮喘，咳嗽和支气管炎。

27. 发明授权

US5665880A Method of preparation of physostigmine carbamate derivatives from eseretholes 失效
标题翻译：从eseretholes制备毒扁豆碱氨基甲酸酯衍生物的方法
公开(公告)号：US5665880A
公开(公告)日：1997-09-09
申请号：US739402
申请日：1996-10-31
申请人： Thomas B. K. Lee , Zhongli Gao
发明人： Thomas B. K. Lee , Zhongli Gao
IPC分类号： C07D487/04 , C07D471/02
CPC分类号： C07D487/04
摘要： This invention relates to a process for the preparation of a product of the formula ##STR1## wherein R is loweralkyl; R.sub.1, is hydrogen, loweralkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralyl; R.sub.2 is lower alkyl, lowercycloalkyl, lowercycloalkylloweralkyl, lowerbicycloalkyl, aryl or arylloweralkyl; or R.sub.1 and R.sub.2 taken together with the nitrogen atom to which they are attached form a group of the formula (Ia) ##STR2## wherein Y is hydrogen or loweralkyl and Z is hydrogen, loweralkyl, halogen, loweralkoxy or hydroxy; X is loweralkyl, loweralkoxy, halogen or trifluoromethyl; and m is 0, 1 or 2; or a pharmaceutically acceptable salt thereof; which process comprises(a) contacting a compound of formula (II) as defined herein with fortified hydrogen bromide to afford a compound of formula (III) as defined herein; contacting the reaction mixture containing a compound of formula (III) with either (1) an isocyanate of formula R.sub.1 NCO or (2) with a compound of formula (IV) as defined to afford a compound of formula (V) as defined herein and contacting the reaction mixture containing the compound of formula (V) with an amine of the formula R.sub.1 R.sub.2 NH herein in the presence of a carboxylic acid of the formula R.sub.5 COOH and forming and isolating the product of Formula (I).
摘要翻译：本发明涉及一种制备式（I）的产物的方法，其中R是低级烷基; R1，是氢，低级烷基，低级环烷基，低级环烷基低级烷基，低级双环烷基，芳基或芳基甲酰基; R2是低级烷基，低级环烷基，低级环烷基低级烷基，低级二环烷基，芳基或芳基低级烷基; 或者R 1和R 2与它们所连接的氮原子一起形成式（Ia）的基团，其中Y是氢或低级烷基，Z是氢，低级烷基，卤素，低级烷氧基或羟基; X是低级烷基，低级烷氧基，卤素或三氟甲基; m为0,1或2; 或其药学上可接受的盐; 该方法包括（a）使本文定义的式（II）化合物与强化溴化氢接触，得到本文定义的式（III）化合物; 使含有式（III）化合物的反应混合物与（1）式R1NCO或（2）的异氰酸酯与式（IV）化合物的定义相接触，得到如本文所定义的式（V）化合物和接触本文在式R 5 COOH的羧酸存在下将含有式（Ⅴ）化合物的反应混合物与式R 1 R 2 NH的胺反应，并形成并分离式（I）的产物。

28. 发明授权

US5665756A Aminoalkyloximes useful in the treatment of depression and obsessive compulsive disorders 失效
标题翻译：可用于治疗抑郁症和强迫症的氨基肟
公开(公告)号：US5665756A
公开(公告)日：1997-09-09
申请号：US285668
申请日：1994-08-03
申请人： Gregory M. Shutske , Brian S. Freed , John D. Tomer, IV , R. Richard L. Hamer
发明人： Gregory M. Shutske , Brian S. Freed , John D. Tomer, IV , R. Richard L. Hamer
IPC分类号： C07D233/60 , A61K31/415 , A61K31/4184 , A61K31/4427 , A61K31/445 , A61K31/454 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , C07D211/14 , C07D211/32 , C07D233/54 , C07D233/61 , C07D235/26 , C07D401/04 , C07D401/12 , C07D521/00 , C07C251/58 , A61K31/15 , C07C233/61
CPC分类号： C07D233/64 , C07D211/14 , C07D211/32 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/04
摘要： Novel aminoalkyloximes of the formula ##STR1## wherein: a. X is hydrogen, loweralkyl, loweralkoxy, halogen, trifluoromethyl, or a group of the formula ##STR2## wherein Y is hydrogen or loweralkyl, and p is 1 or 2; b. A is a group of the formula ##STR3## c. R.sup.1 and R.sup.2 are independently hydrogen or lowerakyl; and d. m is 2 to 6 and n is 0, or 2 to 6, inclusive, serotonin reuptake inhibitors, useful for treating depression and obsessive compulsive disorders are described. Also described are precursors of and processes for the preparation of such aminoakyloximes.
摘要翻译：新颖的式（Ia）的氨基肟类化合物其中：a。 X是氢，低级烷基，低级烷氧基，卤素，三氟甲基或下式的基团，其中Y是氢或低级烷基，p是1或2; b。 A是一个组织或低分子基团; 和d。 m为2〜6，n为0或2〜6，含有用于治疗抑郁症和强迫症的5-羟色胺再摄取抑制剂。还描述了制备这种氨基肟基的前体和方法。

29. 发明授权

US5658911A Heteroarylpiperidines, and their use as antipsychotics and analgetics 失效
标题翻译：杂芳基哌啶，以及它们作为抗精神病药和止痛剂的用途
公开(公告)号：US5658911A
公开(公告)日：1997-08-19
申请号：US309395
申请日：1994-09-20
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： A61K31/09 , A61K31/00 , A61K31/12 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/4162 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/55 , A61P25/04 , A61P25/18 , A61P29/00 , C07C45/45 , C07C45/67 , C07C45/71 , C07C47/277 , C07C47/575 , C07C49/84 , C07C233/25 , C07C233/33 , C07C255/54 , C07C323/22 , C07D20060101 , C07D207/08 , C07D221/04 , C07D231/56 , C07D239/02 , C07D261/20 , C07D275/04 , C07D275/06 , C07D277/82 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D419/04 , 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 , C07D413/10 , 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. 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。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。

30. 发明授权

US5652241A 4-(heteroaryl)-1-[(2,3-dihydro-1-indol-1-yl)alkyl]piperadines and related compounds and their therapeutic utility 失效
标题翻译： 4-（杂芳基）-1-Ä（2,3-二氢-1h-吲哚-1-基）烷基哌嗪及其相关化合物及其治疗效用
公开(公告)号：US5652241A
公开(公告)日：1997-07-29
申请号：US468344
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
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。

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