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31. 发明申请

US20040253277A1 Anaesthetic formulations of propofol 审中-公开
标题翻译：异丙酚麻醉剂
公开(公告)号：US20040253277A1
公开(公告)日：2004-12-16
申请号：US10487617
申请日：2004-08-12
发明人： John Meadows , Simon Higginbottom
IPC分类号： A61K031/24 , A61K031/05 , A61K009/00
CPC分类号： A61K9/0019 , A61K9/1075 , A61K31/05 , A61K31/445 , A61K47/10 , A61K47/34 , A61K2300/00
摘要： Propofol solubilised in aqucous micellar preparations of poloxamers and containing local anaesthctic is associated with reduced levels of pain on injection.
摘要翻译：溶解在泊洛沙姆的含水胶束制剂中并含有局部麻醉的异丙酚与注射时疼痛水平降低有关。

32. 发明申请

US20040242685A1 N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives 失效
标题翻译： N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺衍生物
公开(公告)号：US20040242685A1
公开(公告)日：2004-12-02
申请号：US10484410
申请日：2004-07-19
发明人： John Richard Morphy , Zoran Rankovoc
IPC分类号： C07C233/67 , A61K031/165 , A61K031/24
CPC分类号： C07D333/16 , C07C235/50 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2601/18
摘要： The present invention relates to N-null(1-dimethylaminocycloalkyl)methylnullbenzamide derivatives having the general formula I 1 wherein n is 0, 1, 2 or 3; R1 and R2 are independently H, (C1-4)alkyl or (C1-4)alkyloxy; R3 is (C3-8)alkyl, (C4-7)cycloalkyl, (C4-7)cycloalkyl (C1-3)alkyl, (C6-12)aryl(C1-3)alkyl (wherein the aryl moiety is optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, halogen, trifluoromethyl and methoxycarbonyl), or (C4-9)heteroaryl(C1-3)alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these N-null(1-dimethylaminocycloalkyl)methylnullbenzamide derivatives in the treatment of disorders or conditions which are responsive to inhibition of the GlyT-2 transporter, such as muscle spasticity, epilepsy and, particularly, acute, chronic and neuropathic pain.
摘要翻译：本发明涉及具有通式I的N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺衍生物，其中n为0,1,2或3; R1和R2独立地为H，（C1-4）烷基或（C1-4）烷氧基; R3为（C3-8）烷基，（C4-7）环烷基，（C4-7）环烷基（C1-3）烷基，（C6-12）芳基（C1-3）烷基（其中芳基部分任选被 1-3个选自（C 1-4）烷基，（C 1-4）烷氧基，卤素，三氟甲基和甲氧基羰基的取代基）或（C 4-9）杂芳基（C 1-3）烷基; 或其药学上可接受的盐。本发明还涉及包含所述衍生物的药物组合物，以及这些N - [（1-二甲基氨基环烷基）甲基]苯甲酰胺衍生物用于治疗对抑制GlyT-2转运蛋白有反应的病症或病症的用途，例如肌肉痉挛，癫痫，特别是急性，慢性和神经性疼痛。

33. 发明申请

US20040198833A1 Acetylenic sulfonamide derivatives 审中-公开
标题翻译：乙酰磺酰胺衍生物
公开(公告)号：US20040198833A1
公开(公告)日：2004-10-07
申请号：US10343732
申请日：2003-01-30
发明人： David Michael Bender , Scott Louis Forman , Winton Dennis Jones , Daryl Lynn Smith , Dennis Michael Zimmermann
IPC分类号： A61K031/18 , A61K031/24 , C07C39/41
CPC分类号： C07C311/05 , C07C311/04
摘要： The present invention provides compounds of formula (I), useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
摘要翻译：本发明提供了可用于增强哺乳动物中谷氨酸受体功能的式（I）化合物，因此可用于治疗各种各样的病症如精神病和神经障碍。

34. 发明申请

US20040198816A1 Local anesthetic methods and kits 审中-公开
公开(公告)号：US20040198816A1
公开(公告)日：2004-10-07
申请号：US10816900
申请日：2004-04-05
申请人： Novalar Pharmaceuticals, Inc.
发明人： Eckard Weber , Howard I. Katz
IPC分类号： A61K031/137 , A61K031/24
CPC分类号： A61K31/135 , A61K31/165 , A61K31/24 , A61K31/415 , A61K31/44 , A61K31/445 , A61K31/505 , Y10S435/81 , Y10S514/816 , Y10S514/818
摘要： Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.

35. 发明申请

US20040176445A1 Propionic acid derivatives 审中-公开
标题翻译：丙酸衍生物
公开(公告)号：US20040176445A1
公开(公告)日：2004-09-09
申请号：US10797311
申请日：2004-03-09
申请人： Bayer Pharmaceuticals Corporation
发明人： Klaus Urbahns , Michael Woltering , Susanne Nikolic , Josef Pernerstorfer , Berthold Hinzen , Elke Dittrich-Wengenroth , Hilmar Bischoff , Claudia Hirth-Dietrich , Klemens Lustig
IPC分类号： A61K031/277 , A61K031/195 , A61K031/24
CPC分类号： C07D307/52 , C07C229/18 , C07C229/34 , C07C237/04 , C07C317/28 , C07C323/52 , C07C2601/14 , C07D263/32 , C07D333/20
摘要： The present application relates to novel potent PPAR-alpha-activating compounds for treating, for example, coronary heart disease, and to their preparation.
摘要翻译：本申请涉及用于治疗例如冠心病的新型有效的PPAR-α活化化合物及其制备。

36. 发明申请

US20040167216A1 Carbidopa prodrugs and derivatives, and compositions and uses thereof 失效
标题翻译：卡比多巴前药及其衍生物及其组合物和用途
公开(公告)号：US20040167216A1
公开(公告)日：2004-08-26
申请号：US10728942
申请日：2003-12-08
发明人： Jia-Ning Xiang , Mark A. Gallop , Kenneth C. Cundy , Jianhua Li , Feng Xu , Cindy X. Zhou , Laxminarayan Bhat
IPC分类号： A61K031/24
CPC分类号： C07D213/30 , C07C243/18 , C07C281/02 , C07D295/088 , C07D307/89
摘要： Prodrugs of carbidopa, derivatives of carbidopa prodrugs, methods of making prodrugs of carbidopa and derivatives thereof, methods of using prodrugs of carbidopa and derivatives thereof, and compositions of prodrugs of carbidopa and derivatives thereof are disclosed.
摘要翻译：卡比多巴的前药，卡比多前药的衍生物，卡比多巴的前药及其衍生物的制备方法，卡比多巴的前药及其衍生物的使用方法，卡比多巴及其衍生物的前药组合物。

37. 发明申请

US20040167185A1 Methods of treating conditions associated with an Edg-3 receptor 审中-公开
公开(公告)号：US20040167185A1
公开(公告)日：2004-08-26
申请号：US10760064
申请日：2004-01-16
发明人： Geetha Shankar , David Solow-Cordero , Juliet V. Spencer , Charles Gluchowski
IPC分类号： A61K031/44 , A61K031/40 , A61K031/275 , A61K031/24
CPC分类号： A61K31/275 , A61K31/24 , A61K31/40 , A61K31/44
摘要： In one aspect, the present invention provides a method of inhibiting an Edg-3 receptor mediated biological activity in a cell. A cell expressing the Edg-3 receptor is contacted with an amount of an Edg-3 receptor inhibitor sufficient to inhibit the Edg-3 receptor mediated biological activity. Preferably, the inhibitor is not a phospholipid. In a second aspect, the present invention provides a method where an Edg-3 receptor mediated biological activity is inhibited in a subject. A therapeutically effective amount of an inhibitor of the Edg-3 receptor is administered to the subject. Preferably, the inhibitor is not a phospholipid.

38. 发明申请

US20040110830A1 20-HETE synthase inhibitor 失效
标题翻译： 20-HETE合酶抑制剂
公开(公告)号：US20040110830A1
公开(公告)日：2004-06-10
申请号：US10609547
申请日：2003-07-01
申请人： TAISHO PHARMACEUTICAL CO., LTD.
发明人： Masakazu Sato , Noriyuki Miyata , Takaaki Ishii , Yuko Kobayashi , Hideaki Amada
IPC分类号： A61K031/325 , A61K031/277 , A61K031/155 , A61K031/24
CPC分类号： A61K31/155 , A61K31/166 , A61K31/18 , A61K31/245 , A61K31/275 , A61K31/341 , A61K31/343 , A61K31/351 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/4192 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/44 , A61K31/4402 , A61K31/445 , A61K31/4453 , A61K31/45 , A61K31/472 , A61K31/502 , A61K31/505 , A61K31/522 , A61K31/5375 , C07C311/21 , C07C311/46 , C07C317/40 , C07C323/12 , C07C323/19 , C07C323/41 , C07C323/52 , C07C323/65 , C07C335/26 , C07C2601/08 , C07C2601/14
摘要： The present invention relates to an inhibitor for production of 20-hydroxyeicosatetraenoic acid, comprising, as an effective ingredient, specific hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof. The inhibitors according to the present invention are useful as therapeutic agents for kidney diseases, cerebrovascular diseases, or circulatory diseases. In addition, the present invention also provides novel hydroxyformamidine derivatives or pharmaceutically-acceptable salts thereof.
摘要翻译：本发明涉及一种用于制备20-羟基二十碳烯四烯酸的抑制剂，其包含作为有效成分的特定羟基甲脒衍生物或其药学上可接受的盐。根据本发明的抑制剂可用作肾脏疾病，脑血管疾病或循环系统疾病的治疗剂。此外，本发明还提供新的羟基甲脒衍生物或其药学上可接受的盐。

39. 发明申请

US20040102652A1 Optically active2-aminotetralin derivatives, the processes for the preparation thereof and the therapeutical use of pharmaceutical compositions containing them 审中-公开
标题翻译：光学活性2-氨基四氢萘衍生物，其制备方法和含有它们的药物组合物的治疗用途
公开(公告)号：US20040102652A1
公开(公告)日：2004-05-27
申请号：US10275894
申请日：2003-06-09
发明人： Gabriele Amari , Maurizio Del Canale , Roberta Razzetti , Pier Alessandro Monici Preti , Ivano Rondelli
IPC分类号： A61K031/135 , A61K031/24 , C07C215/86
CPC分类号： C07C219/26 , C07C215/64 , C07C2602/10
摘要： The use of the optically active forms of 5,6-dihydroxy-2-methylaminotetralin and acyl esters thereof as medicaments for cardiovascular diseases a process for the preparation thereof and their use in pharmaceutical compositions.
摘要翻译：光学活性形式的5,6-二羟基-2-甲基氨基四氢萘及其酰基酯用作心血管疾病的药物，其制备方法及其在药物组合物中的应用。

40. 发明申请

US20040097572A1 Antiamyloid phenylsulfonamides: N-alkanol derivatives 有权
标题翻译：抗氨基苯基磺酰胺：N-烷醇衍生物
公开(公告)号：US20040097572A1
公开(公告)日：2004-05-20
申请号：US10626299
申请日：2003-07-24
发明人： David W. Smith , Michael F. Parker
IPC分类号： A61K031/4172 , A61K031/195 , A61K031/24 , A61K031/18
CPC分类号： C07C311/21 , C07C2601/08 , C07C2601/14
摘要： A series of N-alkanol-N-phenyl benzenesulfonamide and related derivatives of the Formula I are disclosed, 1 wherein R1, R2, R3, X, and Y are defined herein. The compounds are inhibitors of null-amyloid peptide (null-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions characterized by aberrant extracellular deposition of amyloid. Pharmaceutical compositions and methods of treatment are also disclosed.
摘要翻译：公开了一系列N-烷醇-N-苯基苯磺酰胺和式I的相关衍生物，其中R 1，R 2，R 3，X和Y在本文中定义。这些化合物是β-淀粉样蛋白肽（β-AP）产生的抑制剂，并且可用于治疗阿尔茨海默氏病和以淀粉样蛋白异常细胞外沉积为特征的其它病症。还公开了药物组合物和治疗方法。

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