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1. 发明授权

US06451804B1 Heteroalkylamino-substituted bicyclic nitrogen heterocycles 失效
标题翻译：杂芳基氨基取代的双环氮杂环
公开(公告)号：US06451804B1
公开(公告)日：2002-09-17
申请号：US09693337
申请日：2000-10-20
申请人： James Patrick Dunn , Lawrence Emerson Fisher , David Michael Goldstein , William Harris , Christopher Huw Hill , Ian Edward David Smith , Teresa Rosanne Welch
发明人： James Patrick Dunn , Lawrence Emerson Fisher , David Michael Goldstein , William Harris , Christopher Huw Hill , Ian Edward David Smith , Teresa Rosanne Welch
IPC分类号： A61K31505
CPC分类号： C07D487/04
摘要： The invention provides compounds represented by the formula: wherein R1, R2, R3, R4, and n are as defined in the Summary of the Invention; and individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.
摘要翻译：本发明提供由下式表示的化合物：其中R1，R2，R3，R4和n如发明概述中所定义; 和各异构体，异构体的外消旋或非外消旋混合物及其药学上可接受的盐。本发明还涉及含有这些化合物的药物组合物，其用作治疗剂的方法及其制备方法。

2. 发明授权

US06642241B1 Alkylamino-substituted bicyclic nitrogen heterocycles 失效
标题翻译：烷基氨基取代的双环氮杂环
公开(公告)号：US06642241B1
公开(公告)日：2003-11-04
申请号：US09693364
申请日：2000-10-20
申请人： James Patrick Dunn , David Michael Goldstein , William Harris , Ian Edward David Smith , Teresa Rosanne Welch
发明人： James Patrick Dunn , David Michael Goldstein , William Harris , Ian Edward David Smith , Teresa Rosanne Welch
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： Alkylamino-substituted dihydropyrimido[4,5-d]pyrimidinone derivatives are provided which are useful as inhibitors of p38, along with a process for their manufacture and pharmaceutical preparations containing them.
摘要翻译：提供了可用作p38抑制剂的烷基氨基取代的二氢嘧啶并[4,5-d]嘧啶酮衍生物及其制备方法和含有它们的药物制剂。

3. 发明授权

US6150373A Bicyclic nitrogen heterocycles 失效
标题翻译：双环氮杂环
公开(公告)号：US6150373A
公开(公告)日：2000-11-21
申请号：US422451
申请日：1999-10-21
申请人： William Harris , Christopher Huw Hill , Ian Edward David Smith
发明人： William Harris , Christopher Huw Hill , Ian Edward David Smith
IPC分类号： A61K31/505 , A61K31/519 , A61P3/10 , A61P9/00 , A61P11/06 , A61P17/00 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07D487/04 , A01N43/54 , C07D487/00
CPC分类号： C07D487/04
摘要： Amino-substituted dihydropyrimido[4,5-d]pyrimidinones of the formula in which R.sup.1 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl, R.sup.2 represents lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl or lower cycloalkyl-lower alkyl, and R.sup.3 represents hydrogen, lower alkyl, aryl, aryl-lower alkyl, heteroaryl, heteroaryl-lower alkyl, lower cycloalkyl, lower cycloalkenyl or lower cycloalkyl-lower alkyl, and pharmaceutically acceptable salts thereof are protein kinase inhibitors. They can be used in the treatment or prophylaxis of inflammatory, immunological, oncological, bronchopulmonary, dermatological and cardiovascular disorders, in the treatment of asthma, central nervous system disorders or diabetic complications or for the prevention of graft rejection following transplant surgery.
摘要翻译：其中R 1表示氢，低级烷基，芳基，芳基 - 低级烷基，杂芳基，杂芳基 - 低级烷基，低级环烷基或低级环烷基 - 低级烷基的下式的氨基取代二氢嘧啶并[4,5-d] 烷基，芳基，芳基 - 低级烷基，杂芳基，杂芳基 - 低级烷基，低级环烷基或低级环烷基 - 低级烷基，R3代表氢，低级烷基，芳基，芳基 - 低级烷基，杂芳基，杂芳基 - 低级烷基，低级环烷基，低级环烯基或低级环烷基 - 低级烷基及其药学上可接受的盐是蛋白激酶抑制剂。它们可用于治疗或预防炎症，免疫学，肿瘤学，支气管肺，皮肤病和心血管疾病，用于治疗哮喘，中枢神经系统疾病或糖尿病并发症，或用于预防移植手术后的移植排斥反应。

4. 发明申请

US20100099690A1 XANTHINE DERIVATIVES AS SELECTIVE HM74A AGONISTS 审中-公开
标题翻译： XANTHINE衍生物作为选择性HM74A激动剂
公开(公告)号：US20100099690A1
公开(公告)日：2010-04-22
申请号：US12063433
申请日：2006-08-08
申请人： Jag Paul Heer , Ian Edward David Smith
发明人： Jag Paul Heer , Ian Edward David Smith
IPC分类号： A61K31/522 , C07D473/04 , A61P3/00 , A61P9/00
CPC分类号： C07D473/06 , C07D473/04
摘要： The present invention relates to compounds which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
摘要翻译：本发明涉及作为黄嘌呤衍生物的化合物，用于制备所述衍生物的方法，含有活性化合物的药物制剂以及该化合物在治疗中的用途，例如用于治疗HM74A受体活化不足的疾病有助于疾病或受体激活将是有益的。

5. 发明申请

US20080139565A1 Anthranilic Acid Derivatives and Their Use in Treatment of Diseases of Lipid Metabolism, in Particular Dyslipidaemia 审中-公开
标题翻译：邻氨基苯甲酸衍生物及其在治疗脂质代谢疾病中的应用，特别是血脂异常
公开(公告)号：US20080139565A1
公开(公告)日：2008-06-12
申请号：US11815349
申请日：2006-02-14
申请人： Matthew Campbell , Andrew McMurtrie Mason , Ivan Leo Pinto , Ian Edward David Smith
发明人： Matthew Campbell , Andrew McMurtrie Mason , Ivan Leo Pinto , Ian Edward David Smith
IPC分类号： A61K31/4965 , C07D241/04 , C07D403/04 , A61K31/53 , A61P9/10 , C07D253/10 , A61K31/497
CPC分类号： C07D241/44 , C07D215/12 , C07D217/22 , C07D253/10 , C07D277/82 , C07D285/08 , C07D295/215 , C07D333/66
摘要： Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2, W, Y and Z are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
摘要翻译：式（I）的其中R 1，R 2，W，Y和Z的治疗活性的邻氨基苯甲酸衍生物如说明书中所定义，用于制备所述衍生物的方法公开了含有活性化合物的药物制剂和该药物在治疗中的用途，特别是用于治疗其中HM74A受体的未激活有助于疾病或受体活化将是有益的疾病。

6. 发明申请

US20080242666A1 1-6-Substituted (3R,6R)-3-(2,3-Dihydro-1H-Inden-2-Yl)-2,5-Piperazinedione Derivatives as Oxytocin Receptor Antagonists For the Treatment of Preterm Labour, Dysmenorrhea and Endometriosis 审中-公开
标题翻译：取代（3R，6R）-3-（2,3-二氢-1H-茚-2-基）-2,5-哌嗪二酮衍生物作为催产素受体拮抗剂治疗早产，痛经和子宫内膜异位症
公开(公告)号：US20080242666A1
公开(公告)日：2008-10-02
申请号：US11722732
申请日：2005-12-22
申请人： Colin Andrew Leach , John Liddle , Simon Peace , Joanne Philp , Ian Edward David Smith , Lamont Roscoe Terrell , Jing Zhang
发明人： Colin Andrew Leach , John Liddle , Simon Peace , Joanne Philp , Ian Edward David Smith , Lamont Roscoe Terrell , Jing Zhang
IPC分类号： C07D241/08 , A61K31/496 , A61K31/5377 , C07D413/12 , C07D401/12 , A61K31/495 , C07D403/12 , A61K31/551 , A61P5/00 , A61P43/00
CPC分类号： C07D241/08 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D417/12
摘要： The present invention relates to Compound S of Formula (I).
摘要翻译：本发明涉及式（I）的化合物S。

7. 发明申请

US20120058984A1 PYRIMIDINE DERIVATIVES USED AS ITK INHIBITORS 审中-公开
标题翻译：用作ITK抑制剂的吡咯烷酮衍生物
公开(公告)号：US20120058984A1
公开(公告)日：2012-03-08
申请号：US13257098
申请日：2010-03-15
申请人： Catherine Mary Alder , Ian Robert Baldwin , Nicholas Paul Barton , Amanda Jennifer Campbell , Aurelie Cecile Champigny , John David Harling , Aoife Caitriona Maxwell , Juliet Kay Simpson , Ian Edward David Smith , Christopher John Tame , Caroline Wilson , James Michael Woolven
发明人： Catherine Mary Alder , Ian Robert Baldwin , Nicholas Paul Barton , Amanda Jennifer Campbell , Aurelie Cecile Champigny , John David Harling , Aoife Caitriona Maxwell , Juliet Kay Simpson , Ian Edward David Smith , Christopher John Tame , Caroline Wilson , James Michael Woolven
IPC分类号： A61K31/506 , C07D417/14 , A61K31/5377 , A61K31/541 , A61P11/00 , A61P37/08 , A61P37/00 , A61P37/06 , A61P29/00 , A61P31/18 , A61P7/06 , A61P25/00 , A61P11/06 , A61P11/08 , A61P17/00 , A61P17/06 , A61P3/10 , A61P5/16 , A61P27/02 , A61P1/00 , C07D417/12
CPC分类号： C07D513/04 , C07D417/12 , C07D417/14
摘要： The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity.
摘要翻译：本发明涉及某些新化合物。具体地，本发明涉及式（I）的化合物及其盐。本发明的化合物是激酶活性的抑制剂，特别是Itk活性。

8. 发明申请

US20080221108A1 Anthranilic Acid Derivatives As Hm74A Receptor Agonists 审中-公开
标题翻译：邻氨基苯甲酸衍生物作为Hm74A受体激动剂
公开(公告)号：US20080221108A1
公开(公告)日：2008-09-11
申请号：US11815350
申请日：2006-02-14
申请人： Richard Hatley , Andrew McMurtrie Mason , Ivan Leo Pinto , Ian Edward David Smith
发明人： Richard Hatley , Andrew McMurtrie Mason , Ivan Leo Pinto , Ian Edward David Smith
IPC分类号： A61K31/196 , C07D271/06 , C07D253/10 , A61K31/4245 , A61P3/00 , A61P9/10 , A61K31/53 , C07C63/06
CPC分类号： C07C235/24 , C07D253/10 , C07D271/06 , C07D401/04
摘要： Therapeutically active anthranilic acid derivatives of Formula (I) wherein R1, R2 and W, are as defined in the specification, processes for the preparation of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, particularly in the treatment of diseases in which under-activation of the HM74A receptor contributes to the disease or in which activation of the receptor will be beneficial, are disclosed.
摘要翻译：其中R 1，R 2和W的式（I）的治疗活性的邻氨基苯甲酸衍生物如说明书中所定义，用于制备所述衍生物，药物制剂含有活性化合物和化合物在治疗中的用途，特别是在治疗其中HM74A受体的活化不足有助于疾病或其中受体的活化将是有益的疾病方面。

9. 发明申请

US20100179128A1 XANTHINE DERIVATIVES AS SELECTIVE HM74A AGONISTS 审中-公开
标题翻译： XANTHINE衍生物作为选择性HM74A激动剂
公开(公告)号：US20100179128A1
公开(公告)日：2010-07-15
申请号：US12063432
申请日：2006-08-08
申请人： Richard Jonathan Daniel Hatley , Jag Paul Heer , John Liddle , Andrew McMurtrie Mason , Ivan Leo Pinto , Shahzad Sharooq Rahman , Ian Edward David Smith
发明人： Richard Jonathan Daniel Hatley , Jag Paul Heer , John Liddle , Andrew McMurtrie Mason , Ivan Leo Pinto , Shahzad Sharooq Rahman , Ian Edward David Smith
IPC分类号： A61K31/55 , C07D473/04 , A61K31/522 , C07D519/00 , A61K31/5377 , A61P3/06 , A61P3/10 , A61P3/04 , A61P9/04 , A61P9/10 , A61P7/02 , A61P13/12
CPC分类号： C07D473/04 , C07D473/06
摘要： The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial
摘要翻译：本发明涉及作为黄嘌呤衍生物的式（I）化合物，制备所述衍生物的方法，含有这些活性化合物的药物制剂，以及该化合物在治疗中的用途，例如， HM74A受体的激活有助于该疾病或受体活化将是有益的

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