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公开(公告)号:US06333336B1
公开(公告)日:2001-12-25
申请号:US09622878
申请日:2000-08-23
申请人: Wesley Peter Blackaby , Jose Luis Castro Pineiro , Richard Thomas Lewis , Michael Geoffrey Neil Russell , Leslie Joseph Street
发明人: Wesley Peter Blackaby , Jose Luis Castro Pineiro , Richard Thomas Lewis , Michael Geoffrey Neil Russell , Leslie Joseph Street
IPC分类号: A61K31435
CPC分类号: C07D471/04
摘要: Pyrazolo[4,3-c]pyridin-3-one derivatives substituted at the 2-position by an optionally substituted aryl or heteroaryl moiety, and having pendant substituents at the 7-position and optionally also at the 6-position, are selective ligands for GABAA receptors, particularly having high affinity for the &agr;2 and/or &agr;3 subunit, and are useful in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
摘要翻译: 在2-位被任选取代的芳基或杂芳基部分取代的吡唑并[4,3-c]吡啶-3-酮衍生物在7-位和任选也在6-位上具有侧取代基是选择性配体 对于具有对α2和/或α3亚基具有高亲和力的GABA A受体,并且可用于治疗和/或预防中枢神经系统疾病,包括焦虑和抽搐。
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公开(公告)号:US20100222317A1
公开(公告)日:2010-09-02
申请号:US12085340
申请日:2006-11-23
IPC分类号: A61K31/4427 , C07D213/56 , A61K31/4418 , A61P25/18 , C07D401/12 , C07C311/07 , A61K31/18 , C07D231/18 , A61K31/415 , C07C307/08 , C07C233/31 , A61K31/166 , C07D239/28 , A61K31/505
CPC分类号: C07D213/24 , C07C307/08 , C07C309/66 , C07C311/07 , C07C317/28 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D231/24 , C07D239/30 , C07D403/12
摘要: The present invention relates to compounds of formula (I); and pharmaceutically acceptable salts thereof and individual enantiomers and diastereomers thereof, as GIyT1 inhibitors for treating neurological and psychiatric disorders.
摘要翻译: 本发明涉及式(I)化合物; 及其药学上可接受的盐及其单独的对映异构体和非对映异构体,作为用于治疗神经和精神障碍的GIyT1抑制剂。
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公开(公告)号:US06900215B2
公开(公告)日:2005-05-31
申请号:US10100797
申请日:2002-03-19
申请人: Mark Stuart Chambers , Simon Charles Goodacre , David James Hallett , Andrew Jennings , Philip Jones , Richard Thomas Lewis , Kevin William Moore , Michael Geoffrey Neil Russell , Leslie Joseph Street , Helen Jane Szekeres
发明人: Mark Stuart Chambers , Simon Charles Goodacre , David James Hallett , Andrew Jennings , Philip Jones , Richard Thomas Lewis , Kevin William Moore , Michael Geoffrey Neil Russell , Leslie Joseph Street , Helen Jane Szekeres
IPC分类号: C07D487/04 , A61K31/519 , A61P25/22
CPC分类号: C07D487/04
摘要: A class of 3-phenylimidazo[1,2-α]pyrimidine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and further substituted on the phenyl ring by alkyl, trifluoromethyl, alkoxy or one or two halogen atoms, especially fluoro, are selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译: 一类3-苯基咪唑并[1,2-a]嘧啶衍生物,其在苯环的间位被被氧原子或-NH-键直接连接或桥连的任选取代的芳基或杂芳基取代, 并且在苯环上被烷基,三氟甲基,烷氧基或一个或两个卤原子,特别是氟取代,是GABA A A受体的选择性配体,特别是对α2和/或α3具有良好的亲和力 和/或其α5亚基,因此有益于治疗和/或预防中枢神经系统的不良状况,包括焦虑,抽搐和认知障碍。
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公开(公告)号:US06936608B2
公开(公告)日:2005-08-30
申请号:US10416318
申请日:2001-11-08
申请人: Michela Bettati , Peter Blurton , William Robert Carling , Mark Stuart Chambers , David James Hallett , Andrew Jennings , Richard Thomas Lewis , Michael Geoffrey Neil Russell , Leslie Joseph Street , Helen Jane Szekeres , Monique Bodil Van Neil
发明人: Michela Bettati , Peter Blurton , William Robert Carling , Mark Stuart Chambers , David James Hallett , Andrew Jennings , Richard Thomas Lewis , Michael Geoffrey Neil Russell , Leslie Joseph Street , Helen Jane Szekeres , Monique Bodil Van Neil
CPC分类号: C07D487/04
摘要: A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译: 一类7-苯基咪唑并[1,2-b] [1,2,4]三嗪衍生物,其在苯环的间位被任选取代的被氧原子连接或桥连的芳基或杂芳基取代 或-NH-连接,作为GABA A受体的选择性配体,特别是对α2和/或α3和/或α5亚基具有良好的亲和力,因此在治疗和/ 或预防中枢神经系统的不良状况,包括焦虑,抽搐和认知障碍。
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公开(公告)号:US06500828B1
公开(公告)日:2002-12-31
申请号:US09890000
申请日:2001-07-23
申请人: William Robert Carling , Jose Luis Castro Pineiro , Richard Thomas Lewis , Kevin William Moore , Leslie Joseph Street
发明人: William Robert Carling , Jose Luis Castro Pineiro , Richard Thomas Lewis , Kevin William Moore , Leslie Joseph Street
IPC分类号: A61K315025
CPC分类号: C07D487/04
摘要: 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a difluoro-or tri-fluoro-substituted phenyl ring at the 3-position, a triazolyl moiety at the 6-position, and a tert-butyl group at the 7-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are useful in the treatment of anxiety and convulsions.
摘要翻译: 在3位具有二氟或三氟取代的苯环,6位的三唑基部分和叔丁基的1,2,4-三唑并[4,3-b]哒嗪衍生物 在7位是GABA A受体的选择性配体,特别是对其α2和/或α3亚基具有高亲和力,并且可用于治疗焦虑和抽搐。
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公开(公告)号:US06916435B2
公开(公告)日:2005-07-12
申请号:US10649359
申请日:2003-08-27
申请人: James William Kortovich , Richard Liichang Shao , Dai Huang , Irwin Charles Lewis , Richard Thomas Lewis
发明人: James William Kortovich , Richard Liichang Shao , Dai Huang , Irwin Charles Lewis , Richard Thomas Lewis
IPC分类号: C01B31/04 , B29C47/36 , B29C47/78 , B32B20060101 , C01B31/00 , C04B35/52 , C04B35/532 , C04B35/83 , C25B11/12 , H05B7/085
CPC分类号: C04B35/532 , C04B35/522 , C04B35/63496 , C04B35/83 , C04B2235/422 , C04B2235/526 , C04B2235/5264 , C04B2235/6021 , C04B2235/77 , C04B2235/96 , C04B2235/9607
摘要: A process for preparing graphite articles is presented. In particular, the process includes employing a particulate fraction comprising at least about 35 weight percent coke, coal or combinations thereof having a diameter such that a major fraction of it passes through a 0.25 mm to 25 mm mesh screen. The particulate fraction is mixed with a liquid or solid pitch binder, to form a stock blend; the stock blend is extruded to form a green stock; the green stock is baked to form a carbonized stock; and the carbonized stock is graphitized. The stock blend further comprises one or both of carbon fibers (advantageously added after mixing of the particulate fraction and pitch has begun) and small particle size filler (advantageously added as part of the particulate fraction).
摘要翻译: 介绍了制备石墨制品的方法。 特别地,该方法包括采用包含至少约35重量%的焦炭,煤或其组合的颗粒部分,其直径使得其主要部分通过0.25mm至25mm的筛网。 将颗粒级分与液体或固体沥青粘合剂混合以形成原料共混物; 将原料混合物挤出以形成绿色原料; 将绿色坯料烘烤以形成碳化原料; 碳化原料被石墨化。 原料混合物还包含一种或两种碳纤维(有利地在混合颗粒馏分和沥青已经开始后加入)和小颗粒填料(有利地作为颗粒馏分的一部分加入)。
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公开(公告)号:US09777221B2
公开(公告)日:2017-10-03
申请号:US11427786
申请日:2006-06-29
IPC分类号: C10B55/00 , C04B35/52 , C04B35/532 , C04B35/626 , C04B35/83 , C10B57/04 , C10C1/04 , C10L9/08 , F27D11/08
CPC分类号: C10B55/00 , C04B35/522 , C04B35/532 , C04B35/6267 , C04B35/83 , C04B2235/5248 , C04B2235/5276 , C04B2235/6021 , C04B2235/656 , C04B2235/722 , C04B2235/726 , C04B2235/9607 , C10B57/045 , C10C1/04 , C10L9/08 , F27D11/08
摘要: A method of producing low CTE graphite electrodes from needle coke formed from a coal tar distillate material having a relatively high initial boiling point.
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公开(公告)号:US20120190666A1
公开(公告)日:2012-07-26
申请号:US13319683
申请日:2010-05-12
申请人: Christiane Bode , Alessandro Boezio , Alan C. Cheng , Deborah Choquette , James Robert Coats , Katrina Woodin Copeland , Hongbing Huang , Daniel La , Richard Thomas Lewis , Hongyu Liao , Michele Potashman , John Stellwagen , Shuyan Yi , Mark H. Norman , Markian M. Stec , Emily Anne Peterson , Russell Graceffa
发明人: Christiane Bode , Alessandro Boezio , Alan C. Cheng , Deborah Choquette , James Robert Coats , Katrina Woodin Copeland , Hongbing Huang , Daniel La , Richard Thomas Lewis , Hongyu Liao , Michele Potashman , John Stellwagen , Shuyan Yi , Mark H. Norman , Markian M. Stec , Emily Anne Peterson , Russell Graceffa
IPC分类号: A61K31/52 , C07D401/14 , A61K31/506 , A61P35/02 , A61K31/53 , C07D487/04 , A61K31/5377 , A61P35/00 , C07D473/40 , C07D471/04
CPC分类号: C07D401/14 , C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04 , C07D519/00
摘要: The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3Kα kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3Kα, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
摘要翻译: 本发明提供了PIKK抑制剂,更具体地,mTOR和/或PI3Kα激酶抑制剂的化合物,因此可用于治疗通过抑制激酶可治疗的疾病,特别是PI3激酶,更具体地,mTOR和/或PI3Kα,例如 癌症。 还提供含有这些化合物的药物组合物和制备这些化合物的方法。
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公开(公告)号:US6133255A
公开(公告)日:2000-10-17
申请号:US381988
申请日:1999-09-27
申请人: Timothy Harrison , Richard Thomas Lewis , Christopher Richard Moyes , Alan Nadin , Andrew Pate Owens
发明人: Timothy Harrison , Richard Thomas Lewis , Christopher Richard Moyes , Alan Nadin , Andrew Pate Owens
IPC分类号: A61K31/4375 , A61K31/4745 , A61K31/55 , A61P25/00 , A61P25/08 , A61P25/22 , A61P43/00 , C07D471/04 , C07D471/14 , A61K31/435
CPC分类号: C07D471/04 , C07D471/14
摘要: Tricyclic pyridin-2-one analogues which are ligands for GABA.sub.A receptors, are useful in the therapy of deleterious mendtal states, and are represented by the formula: ##STR1##
摘要翻译: PCT No.PCT / GB98 / 01167 371 1999年9月27日第 102(e)1999年9月27日PCT提交1998年4月22日PCT公布。 出版物WO98 / 50384 日期1998年11月12日作为GABA A受体的配体的三环吡啶-2-酮类似物可用于治疗有害的门塔状态,并由下式表示:
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公开(公告)号:US06440563B2
公开(公告)日:2002-08-27
申请号:US09837841
申请日:2001-04-18
IPC分类号: B32B900
CPC分类号: C04B35/532 , H01M4/583 , H01M4/96 , Y10T428/249928 , Y10T428/30
摘要: A process for preparing pins for connecting carbon electrodes is presented. In particular, a process for preparing pins for connecting carbon electrodes including the steps of combining calcined coke, a liquid pitch binder and carbon fibers derived from mesophase pitch to form a pinstock blend; extruding the pinstock blend to form a green pinstock; baking the green pinstock to form a carbonized pinstock; and graphitizing the carbonized pinstock by maintaining the carbonized pinstock at a temperature of at least about 2500° C. for no more than about 18 hours is presented. The pins prepared by the inventive process are also presented.
摘要翻译: 提出了一种制备用于连接碳电极的引脚的工艺。 具体地说,一种制备用于连接碳电极的引脚的方法,包括以下步骤:将煅烧焦炭,液体沥青粘合剂和衍生自中间相间距的碳纤维组合以形成母料共混物; 挤压坯料混合物以形成绿色的坯料; 烘烤绿色的脚骨以形成碳化的脚钉; 并且通过将碳化的母料保持在至少约2500℃的温度下不超过约18小时来呈现碳化的母料的石墨化。 还提出了由本发明方法制备的针。
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