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81. 发明申请

US20070082913A1 Substituted heterocyclic compounds with CXCR3 antagonist activity 有权
标题翻译：取代的具有CXCR3拮抗剂活性的杂环化合物
公开(公告)号：US20070082913A1
公开(公告)日：2007-04-12
申请号：US11545201
申请日：2006-10-10
申请人： Seong Kim , Bandarpalle Shankar , Joseph Kozlowski , Stuart Rosenblum , Neng-Yang Shih
发明人： Seong Kim , Bandarpalle Shankar , Joseph Kozlowski , Stuart Rosenblum , Neng-Yang Shih
IPC分类号： A61K31/497 , A61K31/496 , C07D403/14
CPC分类号： C07D401/14 , C07D401/08 , C07D413/14
摘要： The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, type I diabetes, viral meningitis and tumors using a compound of Formula 1.
摘要翻译：本申请公开了所述化合物或所述前体药物的所述化合物或其药学上可接受的盐，溶剂合物或酯的化合物或对映异构体，立体异构体，旋转异构体，互变异构体或前药，所述化合物具有式1所示的一般结构：或其药学上可接受的盐，溶剂合物或酯，其中各种部分在本文中定义。还公开了治疗趋化因子介导的疾病的方法，例如姑息治疗，疗效治疗，某些疾病和疾病如炎性疾病的预防性治疗（非限制性实例，牛皮癣），自身免疫性疾病（非限制性的例如，类风湿性关节炎，多发性硬化症），移植排斥反应（非限制性实例包括，同种异体移植排斥反应，异种移植物排斥），感染性疾病（例如结核性麻风病），固定药物爆发，皮肤迟发型超敏反应应答，I型糖尿病，病毒性脑膜炎和使用式1的化合物的肿瘤。

82. 发明申请

US20060281778A1 Compounds for inhibiting KSP Kinesin activity 审中-公开
标题翻译：用于抑制KSP驱动蛋白活性的化合物
公开(公告)号：US20060281778A1
公开(公告)日：2006-12-14
申请号：US11369625
申请日：2006-03-07
申请人： Jayaram Tagat , Timothy Guzi , Marc Labroli , Cory Poker , Angela Kerekes , Tao Yu , Hon-Chung Tsui , Neng-Yang Shih , Yushi Xiao , Sunil Paliwal
发明人： Jayaram Tagat , Timothy Guzi , Marc Labroli , Cory Poker , Angela Kerekes , Tao Yu , Hon-Chung Tsui , Neng-Yang Shih , Yushi Xiao , Sunil Paliwal
IPC分类号： A61K31/4745 , C07D498/02
CPC分类号： C07D495/04
摘要： The present invention provides compounds of Formula I (wherein R1, R3, X, W, Z and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.
摘要翻译：本发明提供式I化合物（其中R 1，R 3，X，W，Z和环Y如本文所定义）。本发明还提供了包含这些化合物的组合物，其可用于治疗与KSP驱动蛋白活性相关的细胞增殖性疾病或病症并抑制KSP驱动蛋白活性。

83. 发明申请

US20060199815A1 NK1 antagonists 有权
标题翻译： NK1拮抗剂
公开(公告)号：US20060199815A1
公开(公告)日：2006-09-07
申请号：US11358827
申请日：2006-02-21
申请人： Sunil Paliwal , Gregory Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan Arredondo , Michelle Wrobleski , Anandan Palani
发明人： Sunil Paliwal , Gregory Reichard , Cheng Wang , Dong Xiao , Hon-Chung Tsui , Neng-Yang Shih , Juan Arredondo , Michelle Wrobleski , Anandan Palani
IPC分类号： A61K31/538 , A61K31/498 , A61K31/4747
CPC分类号： C07D498/10 , A61K31/166 , A61K31/40 , A61K31/4025 , A61K31/437 , A61K31/4375 , A61K31/438 , A61K31/451 , A61K31/454 , A61K31/4545 , A61K31/537 , A61K31/5377 , A61K31/573 , A61K45/06 , C07D207/14 , C07D207/50 , C07D211/28 , C07D211/32 , C07D211/42 , C07D211/56 , C07D211/60 , C07D211/72 , C07D211/76 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D413/10 , C07D413/12 , C07D471/10 , C07D487/10 , C07D491/10 , C07D513/10
摘要： A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
摘要翻译：具有式（I）的NK 1拮抗剂，其中Ar 1和Ar 2是任选取代的苯基或杂芳基，X 1 硫醚或亚氨基键，R 4和R 5不都是H或烷基，其余的变量如说明书中所定义，可用于治疗许多障碍，包括呕吐，抑郁，焦虑和咳嗽。药物组合物。还公开了治疗方法和与其它药剂的组合。

84. 发明授权

US07034057B2 Compounds for the treatment of inflammatory disorders 失效
公开(公告)号：US07034057B2
公开(公告)日：2006-04-25
申请号：US10716890
申请日：2003-11-19
申请人： Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian J. Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
发明人： Zhaoning Zhu , Robert Mazzola , Zhuyan Guo , Brian J. Lavey , Lisa Sinning , Joseph Kozlowski , Brian McKittrick , Neng-Yang Shih
IPC分类号： A61K31/165 , A61K31/18 , A61K31/21 , A61K31/27
CPC分类号： C07D213/30 , C07C62/34 , C07C69/757 , C07C235/40 , C07C255/54 , C07C259/08 , C07C279/08 , C07C311/29 , C07C317/22 , C07C323/19 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D213/40 , C07D213/73 , C07D213/74 , C07D215/06 , C07D215/14 , C07D215/18 , C07D215/233 , C07D215/26 , C07D215/38 , C07D219/02 , C07D221/16 , C07D233/60 , C07D233/64 , C07D251/10 , C07D277/24 , C07D277/64 , C07D311/04 , C07D311/58 , C07D317/08 , C07D317/64 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/04 , C07D413/12 , C07D417/12 , Y02P20/582
摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-α or combinations thereof.

85. 发明申请

US20060009528A1 Cannabinoid receptor ligands 有权
公开(公告)号：US20060009528A1
公开(公告)日：2006-01-12
申请号：US11203946
申请日：2005-08-15
申请人： Joseph Kozlowski , Neng-Yang Shih , Brian Lavey , Razia Rizvi , Bandarpalle Shankar , James Spitler , Ling Tong , Ronald Wolin , Michael Wong
发明人： Joseph Kozlowski , Neng-Yang Shih , Brian Lavey , Razia Rizvi , Bandarpalle Shankar , James Spitler , Ling Tong , Ronald Wolin , Michael Wong
IPC分类号： A61K31/18
CPC分类号： C07D213/70 , C07C31/24 , C07C317/22 , C07C317/32 , C07C317/36 , C07C317/44 , C07C323/41 , C07C323/65 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07C2603/74 , C07D213/71 , C07D213/74 , C07D213/89 , C07D215/36 , C07D233/42 , C07D233/84 , C07D239/38 , C07D307/64 , C07D333/20 , C07D333/34 , C07D333/38
摘要： There are disclosed compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.

87. 发明授权

US06635630B2 Selective neurokinin antagonists 失效
标题翻译：选择性神经激肽拮抗剂
公开(公告)号：US06635630B2
公开(公告)日：2003-10-21
申请号：US10163663
申请日：2002-06-06
申请人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
发明人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
IPC分类号： A61K31330
CPC分类号： C07D239/10 , C07C45/71 , C07C217/48 , C07D211/58 , C07D233/14 , C07D233/16 , C07D233/22 , C07D233/30 , C07D233/32 , C07D233/42 , C07D233/46 , C07D233/48 , C07D233/78 , C07D285/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07F9/6506 , C07C47/575
摘要： Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —S—, —SO—, —SO2—, —NR12—, —NCOR12— or —NR12SO2R15; is selected from the group consisting of X2 is —O—, —S— or —NR5—; Y is ═O, ═S or ═NR11; Y1 is H, C1-C6 alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6—heterocycloalkyl, —(C1-C3)alkyl-NH—C(O)O(C1-C6)alkyl or —NHC(O)R15; R5 is H or —(CH2)n1—G, wherein n1 is 0-5, G is H, —CF3, —CHF2, —CH2F, —OH, —O—(C1-C6 alkyl), —SO2R13, —O—(C3-C8 cycloalkyl), —NR13R14, —SO2NR13R14, —NR13SO2R15, —NR13COR12, —NR12(CONR13R14), —CONR13R14, —COOR12, C3-C8 cycloalkyl, R19-aryl, R19-heteroaryl, and provided when n1=0, G is not H; R1, R2, R3 and R7 are H, alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2, together with the carbon to which they are attached, form an alkylene ring; or R1 and R2 together are ═O; R6 is R7 or —OH; and the remaining variables are as defined in the specification, methods of treating diseases susceptible to treatment with neurokinin antagonists with said compounds, and pharmaceutical compositions comprising said compounds are disclosed. Also disclosed are pharmaceutical compositions comprising an effective amount of a compound of claim 1, at least one pharmaceutically acceptable carrier, and in combination with an effective amount of a selective serotonin reuptake inhibitor.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O - ， - S - ， - SO-，-SO 2 - ，-NR 12 - ， - NR C 12 - 或-NR 12 SO 2 R 15选自X 2是-O - ， - S-或-NR 5 - ; Y是= O，= S或= NR 11; Y 1是H，C 1 -C 6烷基，-NR 17 R 13，-SCH 3，R 19 - 芳基（CH 2）n6 - （CH 2）n6 - ， - （CH 2）n 6-杂环烷基， - （C 1 -C 3）烷基-NH-C（O）O（C 1 -C 6）烷基或-NHC（O） R 15; R 5是H或 - （CH 2）n1-G，其中n1是0-5，G是H，-CF 3，-CHF 2，-CH 2 F，-OH，-O-（C 1 -C 6 烷基），-SO 2 R 13，-O-（C 3 -C 8环烷基），-NR 13 R 14，-SO 2 NR 13 R 14，-NR 13 SO 2 R 15， NR 13 R 12，-NR 12（CONR 13 R 14），-CONR 13 R 14，-COOR 12，C 3 -C 8环烷基，R 19 芳基，R 19 - 杂芳基，并且当n 1 = 0时，G不为H; R 1，R 2，R 3和R 7为H，烷基，环烷基，-CHF 2 ，-CH2F或-CF3; 或R 1和R 2与它们所连接的碳一起形成亚烷基环; 或R 1和R 2一起为= O; R 6为R 7或-OH;其余变量如本说明书中所定义，治疗易受神经激肽拮抗剂治疗的疾病的方法，所述化合物和包含所述化合物的药物组合物。还公开了药物组合物，其包含有效量的权利要求1的化合物，至少一种药学上可接受的载体，并与有效量的选择性5-羟色胺再摄取抑制剂组合。

88. 发明授权

US06436928B1 Selective neurokinin antagonists 失效
标题翻译：选择性神经激肽拮抗剂
公开(公告)号：US06436928B1
公开(公告)日：2002-08-20
申请号：US09737036
申请日：2000-12-14
申请人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
发明人： Neng-Yang Shih , Ho-Jane Shue , Gregory A. Reichard , Sunil Paliwal , David J. Blythin , John J. Piwinski , Dong Xiao , Xiao Chen
IPC分类号： A61K314166
CPC分类号： C07D239/10 , C07C45/71 , C07C217/48 , C07D211/58 , C07D233/14 , C07D233/16 , C07D233/22 , C07D233/30 , C07D233/32 , C07D233/42 , C07D233/46 , C07D233/48 , C07D233/78 , C07D285/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/10 , C07F9/6506 , C07C47/575
摘要： A compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted phenyl; X1 is —O—, —SO0-2—, —NR12—, —NCOR12— or —NR12SO2R15; is X2 is —O—, —S— or optionally substituted nitrogen; Y is ═O, ═S or ═NR11; Y1 is H, alkyl, —NR17R13, —SCH3, R19-aryl(CH2)n6—, R19-heteroaryl-(CH2)n6—, —(CH2)n6-heterocycloalkyl, -alkyl-NH—C(O)O-alkyl or —NHC(O)R15; R1, R2, R3 and R7 are H, alkyl, OH-alkyl, cycloalkyl, —CHF2, —CH2F or —CF3; or R1 and R2 form an alkylene ring; or R1 and R2 together are ═O; R6 is H, alkyl, —OR13 or —SR12; and the remaining variables are as defined in the specification, is disclosed, as well as a pharmaceutical compositions comprising said compound, methods of using said compound as a neurokinin antagonist, and the combination of said compounds with a selective serotonin reuptake inhibitor.
摘要翻译：由结构式表示的化合物或其药学上可接受的盐，其中Ar 1和Ar 2是任选取代的杂芳基或任选取代的苯基; X 1是-O-，-SOO 2 - ， - NR 12 - ， - NRCOR 12 - 或-NR 12 SO 2 R 15; isX2是-O - ， - S-或任选取代的氮; Y是= O，= S或= NR 11; Y 1是H，烷基，-NR 17 R 13，-SCH 3，R 19 - 芳基（CH 2）n6 - ，R 19 - （CH2）n6-， - （CH2）n6-杂环烷基， - 烷基-NH-C（O）O-烷基或-NHC（O）R15; R1，R2，R3和R7是H，烷基，环烷基，-CHF 2，-CH 2 F或-CF 3; 或R 1和R 2形成亚烷基环; 或R 1和R 2一起为= O; R 6为H，烷基，-OR 13或-SR 12;其余变量如本说明书中所定义，以及包含所述化合物的药物组合物，使用所述化合物的方法作为神经激肽拮抗剂，以及所述化合物与选择性5-羟色胺再摄取抑制剂的组合。

89. 发明授权

US6063926A Substituted oximes as neurokinin antagonists 失效
标题翻译：取代肟作为神经激肽拮抗剂
公开(公告)号：US6063926A
公开(公告)日：2000-05-16
申请号：US195429
申请日：1998-11-18
申请人： Gregory A. Reichard , Cheryl A. Alaimo , Neng-Yang Shih , Pauline C. Ting , Nicholas I. Carruthers , Brian J. Lavey
发明人： Gregory A. Reichard , Cheryl A. Alaimo , Neng-Yang Shih , Pauline C. Ting , Nicholas I. Carruthers , Brian J. Lavey
IPC分类号： C07D211/24 , C07D211/52 , C07D211/58 , C07D211/62 , C07D211/76 , C07D211/94 , C07D401/12 , C07D401/14 , C07D417/14 , C07D401/00 , C07D211/26 , C07D211/44 , C07D211/68
CPC分类号： C07D401/12 , C07D211/24 , C07D211/52 , C07D211/58 , C07D211/62 , C07D211/76 , C07D211/94 , C07D401/14 , C07D417/14
摘要： Compounds within the genus represented by the structural formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein: T is substituted phenyl or substituted pyridyl; ##STR2## R.sup.4 is methyl or ethyl; and Z is substituted piperidinyl.
摘要翻译：由结构式I表示的属的化合物或其药学上可接受的盐，其中：T是取代的苯基或取代的吡啶基; R4是甲基或乙基; Z是取代的哌啶基。

90. 发明授权

US5892039A Piperazino derivatives as neurokinin antagonists 失效
标题翻译：哌嗪衍生物作为神经激肽拮抗剂
公开(公告)号：US5892039A
公开(公告)日：1999-04-06
申请号：US706016
申请日：1996-08-30
申请人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , John J. Piwinski , Kevin D. McCormick
发明人： Ho-Jane Shue , Neng-Yang Shih , David J. Blythin , Xiao Chen , John J. Piwinski , Kevin D. McCormick
IPC分类号： C07D487/08 , A61K31/40 , A61K31/439 , A61K31/46 , A61K31/495 , A61K31/496 , A61K31/497 , A61K31/498 , A61K31/4995 , A61K31/50 , A61K31/501 , A61K31/505 , A61P1/00 , A61P9/00 , A61P11/00 , A61P11/06 , A61P11/14 , A61P13/02 , A61P15/00 , A61P25/00 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/02 , A61P29/00 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07D241/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D453/02 , C07D453/06 , C07D471/08 , C07D487/04 , C07D487/18 , C07D401/02
CPC分类号： C07D401/06 , C07D241/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D453/02 , C07D487/04
摘要： The invention relates to compounds of the formula ##STR1## These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
摘要翻译：本发明涉及下式的化合物这些化合物是神经激肽拮抗剂。这些化合物可用于治疗慢性气道疾病如哮喘。

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