公开(公告)号：EP1659120A1

公开(公告)日：2006-05-24

申请号：EP06075240.9

申请日：2002-04-11

申请人： GlaxoSmithKline S.p.A.

发明人： Farina, Carlo c/o Nikem Research S.r.l. ,  Gagliardi, Stefania c/o Nikem Research S.r.l. ,  Giardina, Guiseppe Arnaldo, Maria ,  Martinelli, Marisa c/o Nikem Research S.r.l.

IPC分类号： C07D401/06 ,  C07D409/14 ,  C07D215/16 ,  C07D215/52 ,  A61K31/47 ,  A61K31/4709 ,  A61P11/00 ,  A61P25/00 ,  C07D241/00 ,  C07D215/00 ,  C07D333/00

CPC分类号： C07D215/50 ,  C07D215/16 ,  C07D215/52 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/06 ,  C07D487/04

摘要： The present invention relates to certain compounds of formula (I) below or a pharmaceutically acceptable salt or solvate thereof:

wherein, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined in the specification; to a process for preparing such compounds; to a pharmaceutical composition comprising such compounds and to the use of such compounds in medicine.

摘要翻译： 本发明涉及某些下面的式（I）化合物或其药学上可接受的盐或溶剂合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如上所定义 在规范中; 涉及制备这些化合物的方法; 涉及包含这些化合物的药物组合物和在药物中使用这些化合物。

公开(公告)号：EP1656365A1

公开(公告)日：2006-05-17

申请号：EP04741958.5

申请日：2004-07-05

申请人： Akzo Nobel N.V.

发明人： WIERINGA, Johannes, Hubertus ,  VAN DE VEN, Adrianus, Antonius, Martinus ,  KEMPERMAN, Gerardus, Johannes

IPC分类号： C07D401/04 ,  C07D471/14 ,  C07D241/00 ,  C07D213/00 ,  C07D223/00

CPC分类号： C07D401/04 ,  C07D471/14

摘要： The invention provides a method for the preparation of enantiomerically pure mirtazapine, said method comprising a step of ring closure of a compound of formula (II) wherein X is a leaving group, said step comprising treatment with an acid, whereby mirlazapine with enantiomeric excess is formed by the ring closure of the compound of formula (II) with enantiomeric excess by treatment with a suitable acid in the absence of a solvent or a suitable combination of an acid and an organic solvent.

公开(公告)号：EP1656355A2

公开(公告)日：2006-05-17

申请号：EP04820712.0

申请日：2004-06-21

申请人： AMGEN INC.

发明人： CHEN, Jian, J. ,  ASKEW, Ben, C. ,  BISWAS, Kaustav ,  CHAU, Jennifer, N. ,  D'AMICIO, Derin, C. ,  HARRIED, Scott ,  NGUYEN, Thomas ,  QIAN, Wenyuan ,  ZHU, Jiawang ,  FOTSCH, Christopher, H. ,  HAN, Nianhe ,  LI, Aiwen ,  LIU, Qingyian ,  NISHIMURA, Nobuko ,  NOMAK, Rana ,  PETERKIN, Tanya ,  RIAHI, Babak ,  YANG, Kevin ,  YUAN, Chester, Chenguang

IPC分类号： C07D241/00

CPC分类号： C07D241/08 ,  C07D243/08 ,  C07D245/02 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14

摘要： Compounds (I) are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

公开(公告)号：EP1644342A1

公开(公告)日：2006-04-12

申请号：EP04756667.4

申请日：2004-07-06

申请人： NEUROCRINE BIOSCIENCES, INC.

发明人： HUANG, Charles, Q. ,  CHEN, Chen ,  CHEN, Yongsheng ,  GUO, Zhiqiang ,  WADE, Warren ,  ROWBOTTOM, Martin ,  RUETER, Jaimie, K.

IPC分类号： C07D239/54 ,  C07D403/12 ,  A61K31/513 ,  A61P5/06 ,  C07D241/00 ,  C07D239/00 ,  C07D207/00

CPC分类号： C07D239/54 ,  C07D403/12

摘要： GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

公开(公告)号：EP1641777A1

公开(公告)日：2006-04-05

申请号：EP04734662.2

申请日：2004-05-25

申请人： Zentaris GmbH

发明人： GERLACH, Matthias ,  SCHUSTER, Tilmann ,  EMIG, Peter ,  SCHMIDT, Peter ,  BASSNER, Silke ,  GÜNTHER, Eckhard

IPC分类号： C07D401/12 ,  C07D403/12 ,  C07D471/04 ,  A61K31/404 ,  A61P35/00 ,  C07D241/00 ,  C07D221/00

CPC分类号： C07D401/12 ,  C07D403/12 ,  C07D471/04

摘要： The invention relates to indole derivatives used as medicaments for the treatment of tumoral diseases, particularly in case of resistance of medicaments against other active ingredients and metastasing carcinoma.

公开(公告)号：EP0994862B1

公开(公告)日：2005-06-01

申请号：EP98945162.0

申请日：1998-07-09

申请人： SmithKline Beecham plc

发明人： BROMIDGE, Steven, Mark, SmithKline Beecham Phar. ,  MOSS, Stephen, Frederik, SmithKline Beecham Phar

IPC分类号： C07D241/00

CPC分类号： C07D207/325 ,  C07D209/02 ,  C07D209/44 ,  C07D213/40 ,  C07D215/38 ,  C07D215/58 ,  C07D217/08 ,  C07D263/32 ,  C07D277/46 ,  C07D295/096 ,  C07D307/79 ,  C07D307/91 ,  C07D317/66 ,  C07D401/04 ,  C07D487/04

摘要： The invention relates to novel compounds of formula (I) or a salt thereof having pharmacological activity (5-HT6 receptor antagonists), process for their preparation, to compositions containing them and to their use in the treatment of CNS disorders.

公开(公告)号：EP1049474A4

公开(公告)日：2004-12-29

申请号：EP99961838

申请日：1999-11-24

申请人： UNIV CONNECTICUT

发明人： MAKRIYANNIS ALEXANDROS STEARNS ,  KHANOLKAR ATMARAM ,  GOUTOPOULOS ANDREAS

IPC分类号： A61K31/16 ,  C07C233/05 ,  C07C233/09 ,  C07C233/13 ,  C07C233/20 ,  C07C235/06 ,  C07C247/04 ,  A61K31/555 ,  A61K31/40 ,  A61K31/44 ,  A61K31/495 ,  A61K31/535 ,  C07C231/00 ,  C07C233/00 ,  C07D207/00 ,  C07D211/00 ,  C07D241/00 ,  C07D265/30

CPC分类号： A61K31/16 ,  C07C233/05 ,  C07C233/09 ,  C07C233/13 ,  C07C233/20 ,  C07C235/06 ,  C07C247/04

摘要： Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications for relief of pain caused by cancer and nausea caused by chemotherapy, as well as for peripheral pain. The compounds may also be useful as oral and topical contraceptives, in suppression of the immune system, enhancement of appetite and in treatment of psychomotor disorders, multiple sclerosis and hypertension.

摘要翻译： 提出了对大麻素CB1和/或CB2受体位点具有较高亲和力的花生四烯乙醇酰胺的新型类似物。 此外，大多数类似物表现出比花生四烯乙醇酰胺更大的代谢稳定性。 改善的受体亲和力和选择性和/或更高的代谢稳定性使得这些类似物在治疗上作为用于缓解由化疗引起的癌症和恶心以及周围性疼痛引起的疼痛的药物治疗有用。 该化合物还可用作口服和局部避孕药，抑制免疫系统，增强食欲和治疗精神运动障碍，多发性硬化和高血压。

公开(公告)号：EP0988292B1

公开(公告)日：2003-02-12

申请号：EP98937467.3

申请日：1998-06-11

申请人： SCHERING AKTIENGESELLSCHAFT

发明人： BAUMAN, John, G. ,  BUCKMAN, Brad, O. ,  GHANNAM, Ameen, F. ,  HESSELGESSER, Joseph, E. ,  HORUK, Richard ,  ISLAM, Imadul ,  LIANG, Meina ,  MAY, Karen, B. ,  MONAHAN, Sean, D. ,  MORISSEY, Michael, M. ,  NG, Howard, P. ,  WEI, Guo, Ping ,  XU, Wei ,  ZHENG, Wei ,  SHAW, Kenneth J. ,  ZUCHUN, Zhao

IPC分类号： C07D241/00

CPC分类号： C07D295/185 ,  C07D215/18 ,  C07D241/04 ,  C07D241/38 ,  C07D261/14 ,  C07D295/192 ,  C07D307/52 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

摘要： This invention is directed to acyl piperazine derivatives which are useful as anti-inflammatory agents. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat inflammatory disorders in humans.

公开(公告)号：EP1147094A1

公开(公告)日：2001-10-24

申请号：EP00900499.5

申请日：2000-01-14

申请人： NOVO NORDISK A/S ,  AGOURON PHARMACEUTICALS, INC.

发明人： TENG, Min ,  TRUESDALE, Larry, Kenneth ,  BHUMRALKAR, Dilip ,  KIEL, Dan ,  JOHNSON, Michael, D. ,  THOMAS, Christine ,  JORGENSEN, Anker, Steen ,  MADSEN, Peter ,  OLESEN, Preben, Houlberg ,  KNUDSEN, Liselotte, Bjerre ,  PETTERSON, Ingrid, Vivika ,  CORNELIS DE JONG, Johannes ,  BEHRENS, Carsten ,  KODRA, Janos, Tibor ,  LAU, Jesper

IPC分类号： C07D241/00 ,  A61K31/498 ,  A61P3/04 ,  A61P3/10

CPC分类号： C07D401/04 ,  C07D241/42 ,  C07D241/44 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D487/04 ,  C07D491/10

摘要： Novel non-peptide GLP-1 agonists, pharmaceutical compositions comprising them, use of the non-peptide GLP-1 agonists for the preparation of pharmaceutical compositions and methods for the treatment and/or prevention of disorders and diseases wherein an activation of the human GLP-1 receptor is beneficial, especially metabolic disorders such as IGT, Type 1 diabetes, Type 2 diabetes and obesity.

公开(公告)号：EP1049474A1

公开(公告)日：2000-11-08

申请号：EP99961838.2

申请日：1999-11-24

申请人： Makriyannis, Alexandros ,  Khanolkar, Atmaram ,  Goutopoulos, Andreas

发明人： Makriyannis, Alexandros ,  Khanolkar, Atmaram ,  Goutopoulos, Andreas

IPC分类号： A61K31/555 ,  A61K31/535 ,  A61K31/495 ,  A61K31/44 ,  A61K31/40 ,  A61K31/16 ,  C07D265/30 ,  C07D241/00 ,  C07D211/00 ,  C07D207/00 ,  C07C231/00 ,  C07C233/00

CPC分类号： A61K31/16 ,  C07C233/05 ,  C07C233/09 ,  C07C233/13 ,  C07C233/20 ,  C07C235/06 ,  C07C247/04

摘要： Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications for relief of pain caused by cancer and nausea caused by chemotherapy, as well as for peripheral pain. The compounds may also be useful as oral and topical contraceptives, in suppression of the immune system, enhancement of appetite and in treatment of psychomotor disorders, multiple sclerosis and hypertension.