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31. 发明申请

US20120220596A1 CYSTEINE AND CYSTINE PRODRUGS TO TREAT SCHIZOPHRENIA AND REDUCE DRUG CRAVINGS 审中-公开
标题翻译： CYSTININE和CYSTINE PRODRUGS TREAT SCHIZOPHRENIA并减少药物伤口
公开(公告)号：US20120220596A1
公开(公告)日：2012-08-30
申请号：US13465383
申请日：2012-05-07
申请人： James M. Cook , David A. Baker , Wenyuan Yin , Edward Merle Johnson, II
发明人： James M. Cook , David A. Baker , Wenyuan Yin , Edward Merle Johnson, II
IPC分类号： A61K31/495 , C07D211/86 , A61K31/45 , C07D487/04 , A61K31/4985 , A61K31/4965 , C07D403/12 , A61K31/497 , C07C327/34 , A61K31/21 , C07C323/60 , A61K31/24 , A61K31/225 , A61P25/30 , A61P25/18 , C07D241/08
CPC分类号： C07D241/08 , A61K9/0053 , C07C323/60 , C07C327/34 , C07D211/86 , C07D487/04 , C07K5/0606
摘要： The present invention provides cysteine and cystine prodrugs for the treatment of schizophrenia and drug addiction. The invention further encompasses pharmaceutical compositions containing prodrugs and methods of using the prodrugs and compositions for treatment of schizophrenia and drug addiction.
摘要翻译：本发明提供了用于治疗精神分裂症和药物成瘾的半胱氨酸和胱氨酸前药。本发明还包括含有药物组合物的药物组合物和使用前药和组合物治疗精神分裂症和药物成瘾的方法。

32. 发明申请

US20090203739A1 Anti-Inflammatory Agents 审中-公开
标题翻译：抗炎药
公开(公告)号：US20090203739A1
公开(公告)日：2009-08-13
申请号：US11922283
申请日：2006-06-14
申请人： David J. Grainger , David John Fox
发明人： David J. Grainger , David John Fox
IPC分类号： A61K31/45 , A61K31/395 , C07D207/36 , C07D211/86 , C07D225/02 , A61K31/4015 , A61P35/00 , A61P19/02 , A61P11/06 , A61P19/10 , A61P9/00 , A61P17/06 , A61P17/02 , A61P31/12 , A61P29/00 , A61P37/06
CPC分类号： C07D213/76 , A61K31/4015 , A61K31/45 , C07D207/267 , C07D207/50 , C07D211/76 , C07D225/02
摘要： The invention provides compounds, pharmaceutical compositions and uses of compounds of general formula (I) or a pharmaceutically acceptable salt thereof, for the preparation of a medicament intended to treat an inflammatory disorder; wherein z X is 1, 2 or 4; X is —CO—Yk—(R1)n or SO2—Yk—(R1)n; k is 0 or 1; Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group; each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms (for example of 5 to 20 carbon atoms, of 8 to 20 carbon atoms, of 9 to 20 carbon atoms, of 10 to 18 carbon atoms, of 12 to 18 carbon atoms, of 13 to 18 carbon atoms, of 14 to 18 carbon atoms, of 13 to 17 carbon atoms); or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radical; and n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y (such that n=1 if k=0, such that the R1 group is bonded directly to the carbonyl or sulfonyl group); provided that simultaneously X cannot be an undec-10-en-1-oyl group and z be equal to 1 or 2; or alternatively R1 is selected from a peptido radical having from 1 to 4 peptidic moieties linked together by peptide bonds.
摘要翻译：本发明提供化合物，药物组合物和通式（I）化合物或其药学上可接受的盐在制备用于治疗炎症性疾病的药物中的应用; 其中z X为1,2或4; X是-CO-Yk-（R1）n或SO2-Yk-（R1）n; k为0或1; Y是环烷基或聚环烷基（例如金刚烷基，金刚烷甲基，双环辛基，环己基，环丙基）; 或者是环烯基或多环烯基; 每个R 1独立地选自氢或具有1至20个碳原子的烷基，卤代烷基，烷氧基，卤代烷氧基，烯基，炔基或烷基氨基（例如5至20个碳原子，8至20个碳原子，9至20个碳原子数10〜18，碳原子数12〜18，碳原子数13〜18，碳原子数14〜18，碳原子数13〜17的碳原子数）。或每个R 1独立地选自氟，氯，溴，碘，羟基，氧烷基，氨基，氨基烷基或氨基二烷基; 并且n是从1到m的任何整数，其中m是环组Y上允许的最大取代数（如果k = 0，则n = 1，使得R1基团直接键合到羰基或磺酰基上）; 条件是同时X不能是十一碳-1-烯-1-基，z等于1或2; 或者R1选自具有通过肽键连接在一起的1至4个肽部分的肽基。

33. 发明授权

US07517994B2 Heterocyclic inhibitors of MEK and methods of use thereof 有权
标题翻译： MEK的杂环抑制剂及其使用方法
公开(公告)号：US07517994B2
公开(公告)日：2009-04-14
申请号：US11132164
申请日：2005-05-18
申请人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
发明人： Allison L. Marlow , Eli Wallace , Jeongbeob Seo , Joseph P. Lyssikatos , Hong Woon Yang , James Blake
IPC分类号： C07D211/76 , C07D211/86 , C07D213/74 , C07D213/75 , C07D237/04 , C07D413/06 , C07D413/14 , C07D237/12 , C07D487/06 , C07D401/06 , C07D401/14 , C07D403/06 , C07D405/06 , C07D409/06 , C07D411/06 , C07D419/06 , C07D221/04 , C07D213/22 , C07D213/26 , A61K31/501 , A61K31/4412 , A61P35/00 , C07D417/06
CPC分类号： C07D213/80 , A61K31/437 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/497 , A61K31/50 , A61K31/501 , A61K31/5025 , A61K31/5377 , A61K45/06 , C07D209/46 , C07D213/82 , C07D215/48 , C07D231/56 , C07D237/24 , C07D237/28 , C07D237/32 , C07D239/74 , C07D401/04 , C07D401/06 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , A61K2300/00
摘要： Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
摘要翻译：公开了式I化合物及其药学上可接受的盐和前药，其中R1，R2，R7，R8和R9，W，X和Y如说明书中所定义。这些化合物是MEK抑制剂，可用于治疗哺乳动物和炎性病症中的过度增殖性疾病，例如癌症和炎症。还公开了使用这些化合物治疗哺乳动物中过度增殖性疾病的方法和含有这些化合物的药物组合物。

34. 发明授权

US07371753B2 Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions 有权
标题翻译：二氢蝶啶酮，其制备方法及其作为药物组合物的用途
公开(公告)号：US07371753B2
公开(公告)日：2008-05-13
申请号：US11211783
申请日：2005-08-25
申请人： Heinz Stadtmueller , Harald Engelhardt , Andreas Schoop , Martin Steegmaier , Matthias Hoffmann , Matthias Grauert
发明人： Heinz Stadtmueller , Harald Engelhardt , Andreas Schoop , Martin Steegmaier , Matthias Hoffmann , Matthias Grauert
IPC分类号： A61K31/5025 , A61K31/496 , A61K31/551 , A61K31/5355 , C07D237/20 , C07D237/22 , C07D239/10 , C07D241/18 , C07D243/08 , C07D413/12 , A61P35/00 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D211/74 , C07D211/72 , C07D211/84 , C07D211/86 , C07D213/73 , C07D213/76 , C07D213/22
CPC分类号： C07D475/04
摘要： Disclosed are new dihydropteridinones of general formula (I) wherein the groups R1 to R5, Ra to Rc, W, Q1 and Q2 have the meanings given in the claims and specification, the isomers thereof and the use thereof for preparing a pharmaceutical composition for the treatment of diseases characterised by excessive or abnormal cell proliferation.
摘要翻译：公开了通式（I）的新的二氢蝶啶酮，其中基团R 1至R 5，R a至R c， SUP，W，Q 1和Q 2具有权利要求书和说明书中给出的含义，其异构体及其用于制备治疗药物组合物的用途以细胞增殖过度或异常为特征的疾病。

35. 发明申请

US20070249838A1 USING ALKYLMETAL REAGENTS FOR DIRECTED METALATION OF AZAAROMATICS 失效
标题翻译：使用碱性试剂对AZAAROMATICS的指导金属化
公开(公告)号：US20070249838A1
公开(公告)日：2007-10-25
申请号：US11539940
申请日：2006-10-10
申请人： Christopher Woltermann , Douglas Sutton
发明人： Christopher Woltermann , Douglas Sutton
IPC分类号： C07D211/86
CPC分类号： C07D213/68 , C07F7/0803
摘要： Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with pyridinic compounds to produce functionalized pyridinic compounds.
摘要翻译：将取代的烷基金属试剂如（三甲基甲硅烷基甲基）锂与吡啶化合物反应以产生官能化的吡啶化合物。

36. 发明授权

US06974827B2 Phenyl substituted 4-hydroxy tetrahydroxypyridone 失效
标题翻译：苯基取代的4-羟基四羟基吡啶酮
公开(公告)号：US06974827B2
公开(公告)日：2005-12-13
申请号：US10257237
申请日：2001-04-05
申请人： Reiner Fischer , Alan Graff , Axel Trautwein , Astrid Ullmann , Udo Schneider , Ralf Wischnat , Mark Wilhelm Drewes , Christoph Erdelen , Dieter Feucht
发明人： Reiner Fischer , Alan Graff , Axel Trautwein , Astrid Ullmann , Udo Schneider , Ralf Wischnat , Mark Wilhelm Drewes , Christoph Erdelen , Dieter Feucht
IPC分类号： A01M21/04 , A01N43/40 , A01N43/42 , A01N43/56 , A01N43/90 , B27K3/34 , B27K3/40 , C07C233/51 , C07C233/52 , C07D211/34 , C07D211/66 , C07D211/86 , C07D221/20 , C07D309/08 , C07D309/14 , C07D401/12 , C07D409/06 , C07D409/10 , C07D455/02 , C07D491/10 , C07D491/107 , C07D211/74
CPC分类号： C07D221/20 , A01N43/40 , A01N43/42 , A01N43/56 , A01N43/90 , C07C233/51 , C07C233/52 , C07C2601/02 , C07C2601/14 , C07D211/34 , C07D211/66 , C07D401/12 , C07D409/06 , C07D409/10 , C07D455/02 , C07D491/10
摘要： The present invention relates to novel compounds of the formula (I) in which W, X, Y, Z, G, A, B, Q1, Q2 and D are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.
摘要翻译：本发明涉及新的式（I）化合物，其中W，X，Y，Z，G，A，B，Q 1，Q 2和D 各自如说明书中所定义，涉及它们的制备和用作农药和除草剂的多种方法。

37. 发明申请

US20050261342A1 Metabolites of (+)-(2S,3S)-3(2-methoxy-5- trifluoromethoxybenzylamino)-2-phenyl-piperidine 审中-公开
标题翻译：（+） - （2S，3S）-3（2-甲氧基-5-三氟甲氧基苄基氨基）-2-苯基 - 哌啶的代谢物
公开(公告)号：US20050261342A1
公开(公告)日：2005-11-24
申请号：US11131733
申请日：2005-05-17
申请人： Amin Kamel , Kevin Colizza , John Davis
发明人： Amin Kamel , Kevin Colizza , John Davis
IPC分类号： A61K31/40 , A61K31/445 , C07D207/10 , C07D211/56 , C07D211/74 , C07D211/86 , C07D211/92
CPC分类号： C07D211/74 , C07D211/56 , C07D211/86
摘要： Metabolites of (+)-(2S, 3S)-3-(2-methoxy-5-trifluoromethoxybenzylamino)-2-phenyl-piperidine, and use of same.
摘要翻译：（+） - （2S，3S）-3-（2-甲氧基-5-三氟甲氧基苄基氨基）-2-苯基 - 哌啶的代谢物及其用途。

38. 发明申请

US20050245566A1 Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones 失效
公开(公告)号：US20050245566A1
公开(公告)日：2005-11-03
申请号：US11147634
申请日：2005-06-08
申请人： Jiacheng Zhou , Lynette Oh , Philip Ma , Hui-Yin Li , Pasquale Confalone
发明人： Jiacheng Zhou , Lynette Oh , Philip Ma , Hui-Yin Li , Pasquale Confalone
IPC分类号： C07D211/76 , C07B53/00 , C07D211/86 , C07D211/88 , C07D471/04 , A61K31/4745 , C07D471/02
CPC分类号： C07D211/88 , C07D211/86 , C07D471/04
摘要： A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.

39. 发明授权

US06924289B2 Benzyl(Idene)-lactam derivatives, their preparation and their use as selective (ANT) agonists of 5-HT1A- and/or 5-HT1D receptors 失效
标题翻译：苄基（Idene） - 内酰胺衍生物，它们的制备及其作为5-HT1A和/或5-HT1D受体的选择性（ANT）激动剂的用途
公开(公告)号：US06924289B2
公开(公告)日：2005-08-02
申请号：US10219692
申请日：2002-08-15
申请人： Harry R. Howard
发明人： Harry R. Howard
IPC分类号： C07D215/22 , A61K31/395 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/403 , A61K31/404 , A61K31/445 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/55 , A61P1/00 , A61P3/04 , A61P9/00 , A61P9/12 , A61P25/00 , A61P43/00 , C07D205/08 , C07D207/26 , C07D207/36 , C07D207/38 , C07D209/34 , C07D211/76 , C07D211/86 , C07D217/24 , C07D223/10 , C07D401/10 , C07D403/00 , C07D403/10
CPC分类号： C07D207/26 , C07D207/38 , C07D209/34 , C07D211/76 , C07D211/86
摘要： The present invention relates to lactam derivatives of the formula wherein R1, R2, R3, A, X, Z, n and the dashed line are defined herein, and pharmaceutical compositions thereof, to processes and intermediates for their preparation, and to their medicinal use as selective agonists and antagonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1D receptors. These compounds are useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.
摘要翻译：本发明涉及下式的内酰胺衍生物：其中R 1，R 2，R 3，A，X，Z，n和虚线在本文中定义，其药物组合物，其制备方法和中间体及其作为5-羟色胺1（5-HT 1 H 2）受体的选择性激动剂和拮抗剂的药物用途，特别是一个或两个5-HT 1A和5-HT 1D受体。这些化合物可用于治疗或预防偏头痛，抑郁症和其它指示5-HT 1激动剂或拮抗剂的疾病。

40. 发明授权

US06846931B2 Organic acid salt of amlodipine 失效
标题翻译：氨氯地平的有机酸盐
公开(公告)号：US06846931B2
公开(公告)日：2005-01-25
申请号：US10642754
申请日：2003-08-19
申请人： Yong Sik Youn , Seong Hwan Cho , Choong Sil Park , Yun Cheul Kim , Dong Kwon Lim , Sung Hak Jung , Sung Hak Lee , Hyun Suk Kang , Kyung Mi Park , Yun Taek Jung , Young Hoon Kim , Kyu Jeong Yeon , Myeong Yun Chae , Hae Tak Jin , Hea Ran Suh , Kwang Hyeg Lee , Hyuk Koo Lee
发明人： Yong Sik Youn , Seong Hwan Cho , Choong Sil Park , Yun Cheul Kim , Dong Kwon Lim , Sung Hak Jung , Sung Hak Lee , Hyun Suk Kang , Kyung Mi Park , Yun Taek Jung , Young Hoon Kim , Kyu Jeong Yeon , Myeong Yun Chae , Hae Tak Jin , Hea Ran Suh , Kwang Hyeg Lee , Hyuk Koo Lee
IPC分类号： A61K31/4015 , A61K31/4422 , A61P9/10 , A61P9/12 , A61P43/00 , C07D207/28 , C07D211/90 , C07D211/86
CPC分类号： C07D211/90
摘要： Disclosed are a novel organic acid salt of amlodipine, its preparation method, and a pharmaceutical composition containing the same as a therapeutically active ingredient.
摘要翻译：公开了一种新型的氨氯地平有机酸盐及其制备方法和含有其作为治疗活性成分的药物组合物。

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