公开(公告)号：EP2392576A4

公开(公告)日：2012-04-11

申请号：EP09793788

申请日：2009-07-07

申请人： BETA PHARMA INC

发明人： WANG YINXIANG ,  DING LIEMING ,  TAN FENLAI ,  HU YUNYAN ,  HE WEI ,  HAN BIN ,  LONG WEI ,  LIU YONG ,  AL HAIMA ,  ZHANG DON ,  DAVIS CHARLES ,  XIE GUOJIAN

IPC分类号： C07D491/056 ,  A61K31/519 ,  A61P35/00

CPC分类号： C07D491/056 ,  A61K31/519 ,  C07B2200/13

公开(公告)号：EP2402314A1

公开(公告)日：2012-01-04

申请号：EP11182888.5

申请日：2008-04-10

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： Shimatzu, Kazuo ,  Takigawa, Yasushi ,  Fujikura, Hideki ,  Iizuka, Masato ,  Hiratochi, Masahiro ,  Kikuchi, Norihiko

IPC分类号： C07D209/42 ,  A61K31/404 ,  A61K31/407 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/00 ,  A61P13/04 ,  A61P13/12 ,  A61P19/02 ,  A61P19/06 ,  A61P43/00 ,  C07D401/04 ,  C07D405/04 ,  C07D409/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/056

CPC分类号： C07D209/30 ,  A61K31/165 ,  A61K31/404 ,  A61K31/407 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/42 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/056 ,  A61K2300/00

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH 2 , halogen, nitro, alkyl, alkoxy and the like; X 1 , X 2 and X 3 independently represent CR 2 or N; R 1 and R 2 independently represent halogen, cyano, haloalkyl, A-D-E-G; -N(-D-E-G) 2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO 2 and the like.

摘要翻译： 本发明提供了可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常相关疾病，其前药或盐类的药物 它们。 在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X 1，X 2和X 3独立地表示CR 2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G; -N（-D-E-G）2等，式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

公开(公告)号：EP2376498A1

公开(公告)日：2011-10-19

申请号：EP09832768.7

申请日：2009-12-17

申请人： Brock University

发明人： HUDLICKY, Tomas ,  COLLINS, Jonathan

IPC分类号： C07D491/056 ,  A61K31/4355 ,  A61P35/00

CPC分类号： C07D491/056

摘要： The present application relates to novel C-1 substituted analogues of pancratistatin and 7-dexoypancratistatin of Formula (I), pharmaceutical compositions thereof and the use of said compounds of Formula (I) in the treatment of cancer The application also relates to processes for the preparation of said compound of Formula (I) and intermediates thereof.

摘要翻译： 本申请涉及式（I）的新型C-1取代的pancratistatin和7-去氢皮考他汀的类似物，其药物组合物以及所述式（I）化合物在治疗癌症中的用途。本申请还涉及 所述式（I）化合物及其中间体的制备。

公开(公告)号：EP2268643A1

公开(公告)日：2011-01-05

申请号：EP09725130.0

申请日：2009-03-26

申请人： Bristol-Myers Squibb Company

发明人： BENDER, John, A. ,  YANG, Zhong ,  KADOW, John, F.

IPC分类号： C07D491/056 ,  A61K31/407 ,  A61P31/18

CPC分类号： C07D491/056

摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. I

公开(公告)号：EP2268618A1

公开(公告)日：2011-01-05

申请号：EP09718298.4

申请日：2009-02-27

申请人： IRM LLC ,  Novartis AG

发明人： WU, Tom Yao-Hsiang ,  LI, Yongkai ,  CORTEZ, Alex ,  ZOU, Yefen ,  MISHRA, Pranab ,  ZHANG, Xiaoyue ,  SKIBINSKI, David ,  SINGH, Manmohan ,  VALIANTE, Nicholas

IPC分类号： C07D221/12 ,  C07D471/04 ,  C07D471/12 ,  C07D491/056 ,  C07D491/12 ,  C07D495/04 ,  A61K31/4375 ,  A61P37/04

CPC分类号： C07D471/04 ,  C07D221/12 ,  C07D471/14 ,  C07D491/056 ,  C07D495/04

摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors, including TLR7 and TLR8. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine (formula I) wherein: X
3 is N; X
4 is N Or CR
3 ; X
5 is -CR
4 =CR
5 .

公开(公告)号：EP2155722A1

公开(公告)日：2010-02-24

申请号：EP08768067.4

申请日：2008-06-04

申请人： Schering Corporation

发明人： COOPER, Alan ,  DENG, Yongqi ,  SHIPPS, Gerald, W., Jr. ,  SHIH, Neng-Yang ,  ZHU, Hugh ,  KELLY, Joseph ,  DOLL, Ronald ,  NAN, Yang ,  DESAI, Jagdish ,  WANG, James ,  PALIWAL, Sunil ,  TSUI, Hon-Chung ,  BOGA, Sobhana, Babu ,  ALHASSAN, Abdul-Basit ,  GAO, Xiaolei ,  ZHU, Liang ,  PATEL, Mehul

IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/056 ,  A61K31/4245 ,  A61K31/444 ,  A61K31/506 ,  A61P35/00

CPC分类号： C07D401/14 ,  C07D403/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/056

摘要： Disclosed are the ERK inhibitors of formula 1.0: (Chemical formula should be inserted here as it appears on abstract in paper form) and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

公开(公告)号：EP1866292A4

公开(公告)日：2010-01-20

申请号：EP06733153

申请日：2006-03-31

申请人： AUCKLAND UNISERVICES LTD

发明人： HAY MICHAEL PATRICK ,  BLASER ADRIAN ,  DENNY WILLIAM ALEXANDER ,  HICKS KEVIN OWEN ,  LEE HO HUAT ,  PCHALEK KARIN ,  PRUIJN FREDERIK BASTIAAN ,  SIIM BRONWYN GAE ,  WILSON WILLIAM ROBERT ,  YANG SHANGJIN

IPC分类号： C07D253/10 ,  A61K31/53 ,  A61P35/00 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056

CPC分类号： C07D253/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056

公开(公告)号：EP2133332A1

公开(公告)日：2009-12-16

申请号：EP08740190.7

申请日：2008-04-10

申请人： Kissei Pharmaceutical Co., Ltd.

发明人： SHIMIZU, Kazuo ,  TAKIGAWA, Yasushi ,  FUJIKURA, Hideki ,  IIZUKA,Masato ,  HIRATOCHI, Masahiro ,  KIKUCHI, Norihiko

IPC分类号： C07D209/42 ,  A61K31/404 ,  A61K31/407 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/00 ,  A61P13/04 ,  A61P13/12 ,  A61P19/02 ,  A61P19/06 ,  A61P43/00 ,  C07D401/04 ,  C07D405/04 ,  C07D409/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/056

CPC分类号： C07D209/30 ,  A61K31/165 ,  A61K31/404 ,  A61K31/407 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/42 ,  C07D401/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/12 ,  C07D417/04 ,  C07D471/04 ,  C07D491/056 ,  A61K2300/00

摘要： The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof. In the formula (I), T represents nitro or cyano and the like; ring J represents aryl or heteroaryl and the like; Q represents carboxy or 5-tetazolyl and the like; Y represents H, OH, NH 2 , halogen, nitro, alkyl, alkoxy and the like; X 1 , X 2 and X 3 independently represent CR 2 or N; R 1 and R 2 independently represent halogen, cyano, haloalkyl, A-D-E-G, -N(-D-E-G) 2 and the like, in the formula, A represents a single bond, O, S and the like; D and G independently represent optionally substituted alkylene, cycloalkylene, heterocycloalkylene, arylene, heteroarylene and the like; E represents a single bond, O, S, COO, SO 2 and the like.

摘要翻译： 本发明提供了可用作预防或治疗与具有尿酸活性等的异常血清尿酸水平相关的疾病的药剂的化合物。 本发明涉及具有黄嘌呤氧化酶抑制活性的由以下通式（I）表示的（aza）吲哚衍生物，可用作预防或治疗与血清尿酸水平异常相关疾病，其前药或盐类的药物 它们。 在式（I）中，T表示硝基或氰基等; 环J表示芳基或杂芳基等; Q表示羧基或5-四唑基等; Y表示H，OH，NH 2，卤素，硝基，烷基，烷氧基等; X 1，X 2和X 3独立地表示CR 2或N; R 1和R 2独立地表示卤素，氰基，卤代烷基，A-D-E-G，-N（-D-E-G）2等，在式中，A表示单键O，S等; D和G独立地表示任选取代的亚烷基，亚环烷基，亚杂环亚烷基，亚芳基，杂亚芳基等; E表示单键O，S，COO，SO 2等。

公开(公告)号：EP2062050A2

公开(公告)日：2009-05-27

申请号：EP08770047.2

申请日：2008-06-03

申请人： Senomyx, Inc.

发明人： TACHDJIAN, Catherine ,  KARANEWSKY, Donald S. ,  TANG, Xiao-qing ,  LI, Xiaodong ,  ZHANG, Feng ,  SERVANT, Guy ,  CHEN, Qing ,  DARMOHUSODO, Vincent ,  FINE, Richard ,  FOTSING, Joseph R. ,  HAMMAKER, Jeffrey Robert ,  KANG, Xinshan ,  KIMMICH, Rachel, D.A. ,  KLEBANSKY, Boris ,  LIU, Haitian ,  PETROVIC, Goran ,  RINNOVA, Marketa ,  ADAMSKI-WERNER, Sara ,  YAMAMOTO, Jeffrey ,  ZHANG, Hong ,  ZLOTNIK, Albert ,  ZOLLER, Mark

IPC分类号： G01N33/53

CPC分类号： C07D513/04 ,  A23L2/39 ,  A23L2/60 ,  A23L27/30 ,  A23L27/31 ,  A23L27/33 ,  A23L27/34 ,  A23L27/88 ,  C07D215/42 ,  C07D215/54 ,  C07D215/56 ,  C07D239/70 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D285/16 ,  C07D417/04 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/056 ,  C07D493/04 ,  C07D495/04 ,  C07D495/14 ,  C07D513/20 ,  G01N33/566

摘要： The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.

公开(公告)号：EP1954274A2

公开(公告)日：2008-08-13

申请号：EP06844355.5

申请日：2006-11-13

申请人： ChemoCentryx, Inc.

发明人： MELIKIAN, Anita ,  WRIGHT, John Jessen ,  KRASINSKI, Antoni ,  HU, Cheng ,  NOVACK, Aaron

IPC分类号： A61K31/455

CPC分类号： C07D401/06 ,  C07D215/233 ,  C07D401/10 ,  C07D401/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D491/04 ,  C07D491/056 ,  C07D519/00

摘要： Substituted quinolone compounds and compositions are provided along with methods for the use of those compounds in the treatment of diseases and disorders such as cancer.