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1. 发明公开

EP2920178A1 NOVEL HETEROCYCLIC DERIVATIVES AS MODULATORS OF KINASE ACTIVITY 有权
标题翻译：新型杂环衍生物作为激酶活性调节剂（化p70S6和AKT）
公开(公告)号：EP2920178A1
公开(公告)日：2015-09-23
申请号：EP13802772.7
申请日：2013-11-15
申请人： Merck Patent GmbH
发明人： LAN, Ruoxi , HUCK, Bayard R. , CHEN, Xiaoling , XIAO, Yufang
IPC分类号： C07D487/04 , A61K31/505 , A61P35/00
CPC分类号： C07D498/04 , A61K31/496 , A61K31/517 , A61K31/519 , A61K31/5383 , A61K45/06 , A61N5/10 , A61N2005/1098 , C07D239/70 , C07D471/04 , C07D475/06 , C07D487/04
摘要： The invention provides novel imidazol-piperidinyl derivatives of the formula (I) in which R1, R2, W, X1, X2, X3, X4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

2. 发明公开

EP1971611A1 ANTI-VIRAL COMPOUNDS 有权
标题翻译：抗病毒化合物
公开(公告)号：EP1971611A1
公开(公告)日：2008-09-24
申请号：EP06849251.1
申请日：2006-12-20
申请人： ABBOTT LABORATORIES
发明人： Betebenner, David.A. , Degoey, David.A. , Maring, Clarence.J. , Krueger, Allan.C. , Iwasaki, Nobuhiko. , Rockway, Todd.W. , Cooper,Curt.S. , Anderson, David.D. , Donner, Pamela.L. , Green, Brian.E. , Kempf, Dale.J. , Liu, Dachun. , Mcdaniel, Keith.F. , Madigan, Darold.L. , Motter, Christopher. E. , Pratt, John.K. , Shanley, Jason.P. , Tufano, Michael.D. , Wagner, Rolf. , Zhang, Rong. , Molla, Akhteruzzaman. , Mo, Hongmei. , Pilot-Matias, Tami.J. , Masse, Sherie, VL. , Carrick, Robert.J. , He, Weping. , Lu, Liangjun. , Grampovnik, David. J.
IPC分类号： C07D495/04 , C07D471/04 , C07D513/04
CPC分类号： C07D487/04 , C07D471/04 , C07D475/06 , C07D495/04 , C07D513/04
摘要： Compounds effective in inhibiting replication of Hepatitis C virus ('HCV') or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, co-formulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
摘要翻译：公开了有效抑制丙型肝炎病毒（“HCV”）或其他病毒复制的化合物。本发明还涉及包含此类化合物的组合物，此类化合物与其他抗病毒剂或治疗剂的共同配制或共同施用，用于合成此类化合物的方法和中间体，以及使用此类化合物治疗 HCV或其他病毒感染。

3. 发明公开

EP1954699A1 PYRIDO-,PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS 有权
标题翻译：吡啶，吡唑啉酮和PYRIMIDOPYRIMIDINDERIVATE AS mTOR抑制剂
公开(公告)号：EP1954699A1
公开(公告)日：2008-08-13
申请号：EP06808609.9
申请日：2006-11-20
申请人： Kudos Pharmaceuticals Ltd
发明人： HUMMERSONE, Marc, Geoffrey , GOMEZ, Sylvie , MENEAR, Keith, Allan , SMITH, Graeme, Cameron, Murray , MALAGU, Karine , DUGGAN, Heather, Mary, Ellen , COCKCROFT, Xiao-Ling Fan , HERMANN, Gesine, Johanna
IPC分类号： C07D475/06 , C07D475/08 , C07D487/04 , A61K31/495 , A61P35/00
CPC分类号： C07D475/08 , C07D475/06 , C07D487/04
摘要： There is provided compounds of formula (I), which are suitable for the treatment of cancer.

4. 发明公开

EP1419158A1 PTERIDINONE DERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 有权
标题翻译：蝶啶酮衍生物作为趋化因子受体活性调节剂
公开(公告)号：EP1419158A1
公开(公告)日：2004-05-19
申请号：EP02749129.9
申请日：2002-08-09
申请人： Astrazeneca AB
发明人： BONNERT, Roger, Victor , CAGE, Peter, Alan , HUNT, Simon, Frazer , WALTERS, Iain, Alastair, Stewart , AUSTIN, Rupert, Philip
IPC分类号： C07D475/06 , A61K31/505 , A61P19/02
CPC分类号： C07D475/06
摘要： The invention provides certain pteridinone compounds of formula (I), processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

5. 发明授权

EP0901374B1 TETRAHYDROPTERIDINES AND PYRIDYLPIPERAZINES FOR TREATMENT OF NEUROLOGICAL DISORDERS 失效
标题翻译：四氢蝶啶和吡啶基哌嗪治疗神经系统疾病
公开(公告)号：EP0901374B1
公开(公告)日：2003-12-10
申请号：EP97926590.7
申请日：1997-05-19
申请人： Bristol-Myers Squibb Pharma Company
发明人： WILDE, Richard, Gerald
IPC分类号： A61K31/495 , A61K31/505 , C07D487/06 , C07D487/16
CPC分类号： C07D471/04 , C07D475/06
摘要： Corticotropin releasing factor (CRF) antagonists of formula (I) and their use in treating anxiety, depression, and other psychiatric and neurological disorders.
摘要翻译：式（I）的促肾上腺皮质素释放因子（CRF）拮抗剂及其在治疗焦虑症，抑郁症和其他精神病和神经疾病中的用途。

6. 发明授权

EP1259508B1 NOVEL BIARYLCARBOXAMIDES 有权
标题翻译：新型双氨基甲酰胺
公开(公告)号：EP1259508B1
公开(公告)日：2003-10-15
申请号：EP01904770.3
申请日：2001-02-15
申请人： AstraZeneca AB
发明人： PHILLIPS, Eifion, AstraZeneca Wilmington , SCHMIESING, Richard, AstraZeneca Wilmington
IPC分类号： C07D453/02 , C07D453/06 , C07D487/08 , A61K31/439 , A61P25/00
CPC分类号： C07D513/04 , C07D453/02 , C07D475/06

7. 发明公开

EP1328319A1 7-AMINO-2-ALKYLTHIOPTERIDIN-4-YL-AMINES FOR THE TREATMENT OF CHEMOKINE-RELATED DISEASES 有权
标题翻译：用于治疗与趋化因子有关的疾病的7-氨基-2-烷基哌啶-4-基 - 胺
公开(公告)号：EP1328319A1
公开(公告)日：2003-07-23
申请号：EP01977001.5
申请日：2001-10-16
申请人： AstraZeneca AB
发明人： BONNERT, Roger , WALTERS, Iain
IPC分类号： A61P17/06 , A61P29/00
CPC分类号： C07D475/06
摘要： Pteridine compounds of formula (I) in which R?1, R2, R3 and R4¿ are as specified in the claims, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in the treatment of inflammatory diseases such as psoriasis, rheumatoid arthritis, diseases in which angiogenesis is assocated with raised CXCR2 chemokine levels (diabetic retinopathy) and COPD. The compounds are ligands for chemokine receptors and medical indications mentioned in the description include: diseases of the respiratory tract (COPDD, asthma, bronchitis, rhinitis, fibroid lung, pneumonia, etc.), diseases of the bones and joints (arthritis, etc.), skin-diseases (psoriasis, etc), diseases of the gastrointestinal tract, diseases in other tissues and systemic disease (multipe sclerosis, atherosclerosis, AIDS, type 1 diabetes, leprosy, sepsis, etc.), allograft rejection, cancers, cystic fibrosis, stroke, burn wounds, skin ulcers, reproductive disease and more.
摘要翻译：其中R 1，R 2，R 3和R 4如权利要求中所述的式（I）的蝶啶化合物，其制备中使用的方法和中间体，含有它们的药物组合物以及它们在治疗炎性疾病例如牛皮癣，类风湿性关节炎，其中血管发生与升高的CXCR2趋化因子水平（糖尿病视网膜病变）和COPD相关的疾病。该化合物是趋化因子受体的配体，说明书中提及的医学适应症包括：呼吸道疾病（COPDD，哮喘，支气管炎，鼻炎，纤维性肺，肺炎等），骨骼和关节疾病（关节炎等）），皮肤疾病（牛皮癣等），胃肠道疾病，其他组织中的疾病和全身性疾病（多发性硬化，动脉粥样硬化，艾滋病，1型糖尿病，麻风病，败血症等），同种异体移植排斥，癌症，纤维化，中风，烧伤，皮肤溃疡，生殖系统疾病等等。

8. 发明公开

EP0574906A3 Piperazine and homopiperazine derivatives, pharmaceutical compositions containing them and process for preparing the same 失效
标题翻译：哌嗪和高哌嗪衍生物，含有它们的药物组合物及其制备方法
公开(公告)号：EP0574906A3
公开(公告)日：1994-04-13
申请号：EP93109664.8
申请日：1993-06-17
申请人： NISSHIN FLOUR MILLING CO., LTD.
发明人： Zubovics, Zoltán Dr. , Goldschmidt née Horváth, Katalin Dr. , Szilágyi née Farago, Katalin Dr. , Ferenc, Andrási Dr. , Hodula née Szentkuti, Eszter Dr. , Toldy, Lajos Dr. , Sutka, Klára Dr. , Fittler, Zsuzsanna , Sebestyén, Lászlo , Görgényi née Kiss, Katalin Dr. , Sziráki, István Dr. , Gyimesi, Jozsef Dr. , Vitkoczi née Kardos, Valéria
IPC分类号： C07D239/50 , C07D403/04 , C07D475/08 , A61K31/525 , A61K31/50 , A61K31/505 , C07D239/95 , C07D237/22
CPC分类号： C07D239/95 , C07D237/20 , C07D239/50 , C07D475/06 , C07D475/08 , Y02P20/55
摘要： The lipid peroxidation inhibiting piperazine and homopiperazine derivatives of the general formula (I) and the pharmaceutically acceptable acid addition salts thereof,
Lip stands for hydrogen ; C 15-20 alkyl ; C 10-20 alkanoyl or C 10-20 alkenoyl ; trityl optionally substituted by halogen ; adamantyl ; 1- or 2-naphthyloxy or oxo-substituted tetrahydronaphthyloxy; or an amine protective group commonly used e.g. in the peptide chemistry;
摘要翻译：通式（I）的脂质过氧化抑制哌嗪和高哌嗪衍生物及其药学上可接受的酸加成盐，Lip代表氢; C15-20烷基; C10-20链烷酰基或C10-20链烯酰基; 三苯甲基，其任选被卤素取代; 金刚烷基; 1-或2-萘氧基或氧代 - 取代的四氢萘氧基; 或通常使用的胺保护基例如在肽化学中;

9. 发明公开

EP3183251A1 NOVEL N2, N4, N7, 6-TETRASUBSTITUTED PTERIDINE-2,4,7-TRIAMINE AND 2, 4, 6, 7-TETRASUBSTITUTED PTERIDINE COMPOUNDS AND METHODS OF SYNTHESIS AND USE THEREOF 审中-公开
标题翻译：新型N2，N4，N7,6-四取代的哒啶-2,4,7-三胺和2,4,6,7-四取代的卟啉化合物及其合成方法和用途
公开(公告)号：EP3183251A1
公开(公告)日：2017-06-28
申请号：EP15833999.4
申请日：2015-08-21
申请人： Janus Biotherapeutics, Inc.
发明人： LIPFORD, Grayson B. , ZEPP, Charles M.
IPC分类号： C07D475/08 , C07D475/00 , C07D475/10
CPC分类号： C07D475/08 , A61K31/165 , A61K31/496 , A61K31/519 , A61K31/5375 , C07D475/00 , C07D475/02 , C07D475/06
摘要： Compounds as immune system modulators bearing a pteridine core are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing autoimmunity disease using the same are described.
摘要翻译：描述了带有蝶啶核心的免疫系统调节剂的化合物。描述了包含其的药物组合物，其制备方法，以及使用该组合物治疗或预防自身免疫疾病的方法。

10. 发明授权

EP2818469B1 Intermediates for the preparation of modulators of toll-like receptors 有权
标题翻译：中间体Toll样受体调节剂的制备
公开(公告)号：EP2818469B1
公开(公告)日：2017-02-15
申请号：EP14158708.9
申请日：2009-12-07
申请人： GILEAD SCIENCES, INC.
发明人： Desai, Manoj, C. , Halcomb, Randall, L. , Hrvatin, Paul , Hui, Hon Chung , McFadden, Ryan , Roethle, Paul, A. , Yang, Hong
IPC分类号： C07D403/12
CPC分类号： A61K31/519 , A61K31/527 , A61K31/5377 , A61K31/551 , A61K31/573 , A61K31/683 , A61K31/7056 , A61K31/7072 , A61K31/708 , A61K38/16 , A61K38/21 , A61K38/212 , A61K45/06 , C07D403/12 , C07D475/06 , C07D475/08 , C07D475/10 , C07D475/12 , C07D487/04 , Y02A50/385 , Y02A50/387 , Y02A50/389 , Y02A50/391 , Y02A50/393 , Y02A50/395
摘要： Provided are intermediates for the production of modulators of toll-like receptors with the following structures:
摘要翻译：提供的是用于生产具有以下结构toll样受体调节剂的中间体：

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