公开(公告)号：EP1910378B1

公开(公告)日：2012-06-20

申请号：EP06761122.8

申请日：2006-07-17

申请人： Boehringer Ingelheim International GmbH

发明人： BAILEY, Murray, D. ,  FORGIONE, Pasquale ,  LLINAS-BRUNET, Montse ,  POUPART, Marc-André

IPC分类号： C07D495/04 ,  A61K31/4709 ,  A61K31/4365 ,  A61P31/12 ,  C07D215/22 ,  C07D401/12 ,  C07D413/04

CPC分类号： C07K5/06034 ,  C07K5/06026 ,  C07K5/06191

摘要： The compounds of formula I wherein R1, R2, R3, R4 and R5 are defined herein, are useful as inhibitors of the hepatitis C virus NS3 protease The invention further relates to azalactone compounds of the formula (II) which can be reacted with an amide anion to produce the HCV NS3 protease inhibitors of formula (I)

公开(公告)号：EP1415992B1

公开(公告)日：2012-05-02

申请号：EP02762760.3

申请日：2002-08-08

申请人： Daiichi Sankyo Company, Limited

发明人： OHTA, Toshiharu, DAIICHI PHARMACEUT. CO. LTD ,  KOMORIYA, Satoshi, DAIICHI PHARMACEUT. CO. LTD ,  YOSHINO, Toshiharu, DAIICHI PHARMACEUT. CO. LTD ,  UOTO, Kouichi, DAIICHI PHARMACEUT. CO. LTD ,  NAKAMOTO, Yumi, DAIICHI PHARMACEUT. CO. LTD ,  NAITO, Hiroyuki, DAIICHI PHARMACEUT. CO. LTD ,  MOCHIZUKI, Akiyoshi, DAIICHI PHARMACEUT. CO.LTD ,  NAGATA, Tsutomu, DAIICHI PHARMACEUT. CO. LTD ,  KANNO, Hideyuki, DAIICHI PHARMACEUT. CO. LTD ,  HAGINOYA, Noriyasu, DAIICHI PHARMACEUT. CO. LTD ,  YOSHIKAWA, Kenji, DAIICHI PHARMACEUT. CO. LTD ,  NAGAMOCHI, Masatoshi, DAIICHI PHARMACEUT. CO. LTD ,  KOBAYASHI, Syozo, DAIICHI PHARMACEUT. CO. LTD ,  ONO, Makoto, DAIICHI PHARMACEUT. CO. LTD

IPC分类号： C07D401/12 ,  C07D417/12 ,  C07D417/14 ,  C07D401/14 ,  C07D209/42 ,  C07D487/04 ,  C07D513/04 ,  C07D498/04 ,  C07D513/14 ,  C07K5/06 ,  C07K5/08 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/4439 ,  A61P7/02

CPC分类号： C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04 ,  C07K5/06191 ,  C07K5/0827

摘要： Compounds represented by the following general formula (1), salts thereof, solvates of the same or N-oxides of the same: Q1-Q2-T0-N(R1)-Q3-N(R2)-T1-Q4 (1) wherein R1 and R2 represent each hydrogen, etc.; Q1 represents optionally substituted, saturated or unsaturated 5- or 6-membered hydrocarbyl, etc.; Q2 represents a single bond, etc.; Q3 represents the following group; (wherein Q5 represents C1-8 alkylene, etc.); and T0 and T1 represent each carbonyl, etc. These compounds are useful as preventives and/or remedies for brain infarction, cerebral embolism, myocardial infarction, angina, pulmonary infarction, pulmonary embolism, Buerger’s disease, bottom venous thrombosis, disseminated intravascular coagulation, thrombosis following artificial valve/joint replacement, thrombosis and reocclusion following circulation reconstruction, systemic inflammatory responsive syndrome (SIRS), multiple organ dysfunction (MODS), thrombosis in extracorporeal circulation or blood coagulation in collecting blood.

摘要翻译： （1）表示的化合物，其盐，相同的溶剂化物或相同的N-氧化物：Q1-Q2-T0-N（R1）-Q3-N（R2）-T1-Q4（1） 其中R1和R2代表每个氢等; Q1表示任选取代的饱和或不饱和的5或6元烃基等; Q2代表单键等; Q3代表以下组别; （其中Q5表示C1-8亚烷基等）; 这些化合物可用作脑梗塞，脑栓塞，心肌梗塞，心绞痛，肺梗塞，肺栓塞，伯格氏病，下肢静脉血栓形成，弥散性血管内凝血，血栓形成等的预防剂和/或治疗剂 继循环重建，全身炎症反应综合征（SIRS），多器官功能障碍（MODS），体外循环中的血栓形成或血液凝固后的人工瓣膜/关节置换，血栓形成和再闭塞。

公开(公告)号：EP2433938A1

公开(公告)日：2012-03-28

申请号：EP10769780.7

申请日：2010-04-28

申请人： Kyowa Hakko Kirin Co., Ltd.

发明人： UESAKA Noriaki ,  SAWADA, Takashi ,  KANDA, Tomoyuki

IPC分类号： C07D417/14 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/4365 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/5377 ,  A61P25/14 ,  A61P25/16 ,  A61P43/00 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04

CPC分类号： C07D495/04 ,  A61K31/198 ,  A61K31/427 ,  A61K31/435 ,  A61K31/4355 ,  A61K31/436 ,  A61K31/4365 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/506 ,  A61K31/5377 ,  C07D417/14 ,  C07D491/048 ,  C07D491/052

摘要： Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R 1 represents aryl and the like, and R 2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.

公开(公告)号：EP2093228B1

公开(公告)日：2012-02-22

申请号：EP07816580.0

申请日：2007-10-16

申请人： Tianjin Hemay Bio-Tech Co., Ltd.

发明人： ZHANG, Hesheng

IPC分类号： C07D495/04 ,  C07D487/04 ,  A61K31/4365 ,  A61K31/437 ,  A61P35/00 ,  A61P31/00 ,  A61P37/00 ,  A61P9/00 ,  A61P9/10 ,  A61P5/00

CPC分类号： C07D487/04 ,  C07D495/04

摘要： Compounds represented by formula (I) or (II) against cell releasing TNF α, their pharmaceutically acceptable salts or hydrates and preparation methods and uses thereof, in which A, B and E represent CH2, CO respectively; D represents S, NH, NC1-6 alkyl; R represents H, R3 ; R1 represents 1-4 same or different radical(s) selected from the group consisting of F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2; R2 represents F, CF3, H or C1-4 alkyl.

公开(公告)号：EP2415774A1

公开(公告)日：2012-02-08

申请号：EP10758053.2

申请日：2010-03-31

申请人： Shanghai Institute of Pharmaceutical Industry ,  Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd.

发明人： YUAN, Zhedong ,  CHENG, Xingdong ,  YANG, Yulei ,  TONG, Ling ,  YU, Xiong ,  ZHANG, Laifang ,  ZHOU, Wenliang

IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P7/02

CPC分类号： A61K31/4365 ,  C07D495/04

摘要： The present application discloses crystals of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]p yridine hydrobromate, crystal compositions and pharmaceutical compositions comprising them and their use. The crystals of prasugrel hydrobromate of the present application possess excellent stability and solubility.

摘要翻译： 本申请公开了2-乙酰氧基-5-（± - 环丙基羰基-2-氟苄基）-4,5,6,7-四氢噻吩并[3,2-c]吡啶氢溴酸盐的晶体，晶体组合物和包含它们的药物组合物， 他们的使用。 本申请的普拉格罗氢溴酸盐晶体具有优异的稳定性和溶解性。

公开(公告)号：EP2414346A1

公开(公告)日：2012-02-08

申请号：EP10707839.6

申请日：2010-03-09

申请人： Merck Patent GmbH

发明人： SCHULTZ, Melanie ,  SCHIEMANN, Kai ,  STAEHLE, Wolfgang

IPC分类号： C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04 ,  A61K31/423 ,  A61K31/428 ,  A61K31/4365 ,  A61K31/437 ,  A61P35/00

CPC分类号： C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D495/04

摘要： The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.

公开(公告)号：EP2409701A1

公开(公告)日：2012-01-25

申请号：EP11174384.5

申请日：2011-07-18

申请人： Sanovel Ilac Sanayi ve Ticaret A.S.

发明人： Cifter, Ümit ,  Türkyilmaz, Ali ,  Öner, Levent

IPC分类号： A61K31/4365 ,  A61K9/50 ,  A61K9/20 ,  A61P7/02 ,  A61P9/00

CPC分类号： A61K9/5073 ,  A61K9/5026 ,  A61K9/5036 ,  A61K31/4365

摘要： The present invention relates to pharmaceutical granules comprising prasugrel hydrochloride, said granules comprising at least one coating layer containing pullulan.

摘要翻译： 本发明涉及包含普拉格雷盐酸盐的药物颗粒，所述颗粒包含至少一个含有支链淀粉的包衣层。

公开(公告)号：EP2409689A1

公开(公告)日：2012-01-25

申请号：EP11174408.2

申请日：2011-07-18

申请人： Sanovel Ilac Sanayi ve Ticaret A.S.

发明人： Cifter, Ümit ,  Türkyilmaz, Ali ,  Öner, Levent

IPC分类号： A61K9/20 ,  A61K31/4365 ,  A61P7/02 ,  A61P9/00 ,  A61K9/50

CPC分类号： A61K9/205 ,  A61K9/0056 ,  A61K9/2018 ,  A61K9/2081 ,  A61K9/5036 ,  A61K31/4365

摘要： A solid pharmaceutical tablet formulation, comprising prasugrel, or a pharmaceutically acceptable salt thereof and pullulan as a filling agent.

摘要翻译： 一种固体药物片剂，其包含普拉格雷或其药学上可接受的盐和支链淀粉作为填充剂。

公开(公告)号：EP2257169A4

公开(公告)日：2012-01-11

申请号：EP09714399

申请日：2009-02-11

申请人： MERCK SHARP & DOHME

发明人： DEBENHAM JOHN S ,  HALE JEFFREY J ,  MADSEN-DUGGAN CHRISTINA B ,  WALSH THOMAS F

IPC分类号： C07D495/04 ,  A61K31/4365 ,  A61P7/00

CPC分类号： C07D495/04

公开(公告)号：EP2398810A1

公开(公告)日：2011-12-28

申请号：EP10706423.0

申请日：2010-02-16

申请人： Vertex Pharmaceuticals Incorporated

发明人： ARONOV, Alex ,  BANDARAGE, Upul, Keerthi ,  COTTRELL, Kevin ,  DAVIES, Robert ,  KRUEGER, Elaine ,  LEDEBOER, Mark ,  LEDFORD, Brian ,  LE TIRAN, Arnaud ,  LIAO, Yusheng ,  MESSERSMITH, David ,  WANG, Tiansheng ,  XU, Jinwang

IPC分类号： C07D513/04 ,  A61K31/4365 ,  A61P25/00

CPC分类号： C07D513/04

摘要： The present invention relates to compounds (I) useful as inhibitors of PBK, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.