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1. 发明授权

US06600052B1 Regioselective synthesis of 3,4-di(carbocyclyl or heterocyclyl)thiophenes 失效
标题翻译： 3,4-二（碳环基或杂环基）噻吩的区域选择性合成
公开(公告)号：US06600052B1
公开(公告)日：2003-07-29
申请号：US09838986
申请日：2001-04-20
申请人： David L. Brown , Cindy L. Ludwig
发明人： David L. Brown , Cindy L. Ludwig
IPC分类号： C07D33310
CPC分类号： C07D231/12 , C07D231/16 , C07D261/08 , C07D307/46 , C07D333/18 , C07D333/38
摘要： A novel process for preparing 3,4-di(carbocyclyl or heterocyclyl)thiophenes comprising reacting a compound of Formula IV: with a ring cyclizing reagent to form the compound of Formula V to yield a compound of Formula V: wherein R1, R2 and R3 are as defined in the specification.
摘要翻译：一种制备3,4-二（碳环基或杂环基）噻吩的新方法，包括使式IV化合物与环环化试剂反应以形成式V化合物，得到式V化合物：其中R1，R2和R3 如说明书中所定义。

2. 发明授权

US06833385B2 3-heteroarylalkyl substituted GABA analogs 失效
标题翻译： 3-杂芳基烷基取代的GABA类似物
公开(公告)号：US06833385B2
公开(公告)日：2004-12-21
申请号：US10741116
申请日：2003-12-19
申请人： Po-Wai Yuen
发明人： Po-Wai Yuen
IPC分类号： C07D33310
CPC分类号： C07D307/54 , C07D333/24
摘要： The invention is a novel series of compounds which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
摘要翻译：本发明是可用于治疗癫痫，微弱发作，神经退行性疾病，抑郁症，焦虑症，恐慌症，疼痛，神经病理学障碍，胃肠道疾病如肠易激综合征（IBS）和炎症，特别是关节炎的新一系列化合物。包括含有本发明化合物的药物组合物以及制备化合物的方法和用于制备最终化合物的新中间体。

3. 发明授权

US06211373B1 Phenyl urea antagonists of the IL-8 receptor 失效
标题翻译：苯基脲拮抗剂的IL-8受体
公开(公告)号：US06211373B1
公开(公告)日：2001-04-03
申请号：US09111663
申请日：1998-07-08
申请人： Katherine Louisa Widdowson , Daniel Frank Veber , Anthony Joseph Jurewicz , Robert Philip Hertzberg , Melvin Clarence Rutledge, Jr.
发明人： Katherine Louisa Widdowson , Daniel Frank Veber , Anthony Joseph Jurewicz , Robert Philip Hertzberg , Melvin Clarence Rutledge, Jr.
IPC分类号： C07D33310
CPC分类号： A61K31/426 , A61K31/18 , A61K31/277 , A61K31/381 , A61K31/47 , Y02A50/411
摘要： This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor. Compounds of Formula (1) are represented by the structure: wherein interalia, X is oxygen or sulfur; R is any functional moiety having an ionizable hydrogen and a pKa of 10 or less; R1 is independently selected from hydrogen; halogen; nitro; cyano; C1-C10 alkyl; halosubstituted C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; halosubstituted C1-10 alkoxy; azide; (CR8R8)qS(O)tR4; hydroxy; hydroxy substituted C1-4 alkyl; aryl; aryl C1-4 alkyl; aryl C2-10 alkenyl; aryloxy; aryl C1-4 alkyloxy; heteroaryl; heteroarylalkyl; heteroaryl C2-10 alkenyl; heteroaryl C1-4 alkyloxy; heterocyclic, heterocyclic C1-4 alkyl; heterocyclic C1-4 alkyloxy; heterocyclic C2-10 alkenyl; q is 0 or an integer having a value of 1 to 10; n is an integer having a value of 1 to 3; m is an integer having a value of 1 to 3; n is an integer having a value of 1 to 3; Y is hydrogen; halogen; nitro; cyano; halosubstituted C1-10 alkyl; C1-10 alkyl; C2-10 alkenyl; C1-10 alkoxy; halosubstituted C1-1- alkoxy; azide; (CR8R8)qS(O)tR4, (CR8R8)qOR4; hydroxy; hydroxy substituted C1-4 alkyl; aryl; aryl C1-4 alkyl; aryloxy; aryC1-4 alkyloxy; aryl C2-10 alkenyl; heteroaryl; heteroarylalkyl; heteroaryl C1-4 alkyloxy; heteroaryl C2-10 alkenyl; heterocyclic, heterocyclic C1-4 alkyl; heterocyclic C2-10 alkenyl; or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及式（I）的新型化合物，以及这些化合物在治疗趋化因子介导的疾病中的新用途，其中趋化因子与IL-8α或b受体结合。式（1）的化合物由以下结构表示：其中间隔，X是氧或硫; R是具有可电离的氢和pKa为10或更小的任何官能部分; R 1独立地选自氢; 卤素; 硝基氰基; C1-C10烷基; 卤代C 1-10烷基; C 2-10烯基; C 1-10烷氧基; 卤代C 1-10烷氧基; 叠氮化物（CR8R8）qS（O）tR4; 羟基; 羟基取代的C 1-4烷基; 芳基; 芳基C 1-4烷基; 芳基C2-10烯基; 芳氧基芳基C 1-4烷氧基; 杂芳基; 杂芳基烷基; 杂芳基C2-10烯基; 杂芳基C 1-4烷氧基; 杂环，杂环C 1-4烷基; 杂环C 1-4烷氧基; 杂环C 2-10烯基; q为0或值为1至10的整数; n为1〜3的整数，m为1〜3的整数，n为1〜3的整数，Y为氢; 卤素; 硝基氰基; 卤代C 1-10烷基; C 1-10烷基; C 2-10烯基; C 1-10烷氧基; 卤代C 1-1烷氧基; 叠氮化物（CR8R8）qS（O）tR4，（CR8R8）qOR4; 羟基; 羟基取代的C 1-4烷基; 芳基; 芳基C 1-4烷基; 芳氧基 aryC1-4烷氧基; 芳基C2-10烯基; 杂芳基; 杂芳基烷基; 杂芳基C 1-4烷氧基; 杂芳基C2-10烯基; 杂环，杂环C 1-4烷基; 杂环C 2-10烯基;或其药学上可接受的盐。

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