公开(公告)号：EP1571146A4

公开(公告)日：2010-09-01

申请号：EP03778753

申请日：2003-12-09

申请人： ONO PHARMACEUTICAL CO

发明人： HABASHITA HIROMU ,  KOKUBO MASAYA ,  SHIBAYAMA SHIRO ,  TADA HIDEAKI ,  TANIHIRO TATSUYA

IPC分类号： C07D213/74 ,  A61K31/506 ,  A61K31/517 ,  A61P3/00 ,  A61P9/00 ,  A61P25/00 ,  A61P29/00 ,  A61P31/00 ,  A61P31/18 ,  A61P35/00 ,  A61P37/00 ,  A61P37/08 ,  A61P43/00 ,  C07D221/22 ,  C07D239/48 ,  C07D239/95 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D493/10

CPC分类号： C07D221/22 ,  C07D239/48 ,  C07D239/95 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D493/10

公开(公告)号：EP2190826A2

公开(公告)日：2010-06-02

申请号：EP08798753.3

申请日：2008-08-27

申请人： IRM LLC

发明人： MARSILJE, Thomas H. ,  LU, Wenshuo ,  CHEN, Bei ,  HE, Xiaohui ,  BURSULAYA, Badry ,  LEE, Christian Cho-Hua ,  GRAY, Nathanael S.

IPC分类号： C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/506 ,  A61P35/00 ,  A61P37/00 ,  A61P31/00

CPC分类号： C07D403/12 ,  C07D239/48 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

摘要： The invention provides novel pyrimidine derivatives of formula (1) and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF- 1 R) or anaplastic lymphoma kinase (ALK).

公开(公告)号：EP1904457A4

公开(公告)日：2010-06-02

申请号：EP06784727

申请日：2006-06-08

申请人： RIGEL PHARMACEUTICALS INC

发明人： LI HUI ,  THOTA SAMBAIAH ,  CARROLL DAVID ,  ARGADE ANKUSH ,  TSO KIN ,  SRAN ARVINDER ,  CLOUGH JEFFREY ,  KEIM HOLGER ,  BHAMIDIPATI SOMASEKHAR ,  TAYLOR VANESSA ,  COOPER ROBIN ,  SINGH RAJINDER ,  WONG BRIAN

IPC分类号： C07D239/48 ,  A61K31/505 ,  A61P35/00 ,  A61P37/06 ,  A61P37/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D498/04

CPC分类号： C07D413/12 ,  A61K31/343 ,  A61K31/436 ,  A61K31/505 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/695 ,  A61K38/13 ,  A61K39/3955 ,  A61K45/06 ,  C07D239/42 ,  C07D239/48 ,  C07D285/22 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D413/14 ,  C07D417/12 ,  C07D498/04 ,  C07F7/0812 ,  C07F7/10

公开(公告)号：EP2176240A1

公开(公告)日：2010-04-21

申请号：EP08768583.0

申请日：2008-06-18

申请人： Actimis Pharmaceuticals, Inc.,

发明人： LY, Tai, Wei

IPC分类号： C07D239/48 ,  A61K31/33 ,  A61P11/06

CPC分类号： C07D239/48

摘要： Provided are amine salts of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl}-acetic acid, processes for their preparation, pharmaceutical compositions containing them, and their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease.

公开(公告)号：EP2170838A1

公开(公告)日：2010-04-07

申请号：EP08768582.2

申请日：2008-06-18

申请人： Actimis Pharmaceuticals, Inc.,

发明人： LY, Tai, Wei ,  LI, Hui-yin

IPC分类号： C07D239/48 ,  A61K31/33 ,  A61P11/06 ,  A61P29/00

CPC分类号： C07D239/48 ,  Y10T428/2982

摘要： Provided herein are particulates of {4,6-bis(dimethylamino)-2-(4-(4-(trifluoromethyl)benzamido)benzyl)pyrimidin-5-yl}acetic acid in amorphous or crystalline forms, processes for their preparation, pharmaceutical compositions comprising them, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a CRTH2-mediated disorder or disease.

公开(公告)号：EP1786782B1

公开(公告)日：2010-03-31

申请号：EP05790029.2

申请日：2005-08-11

申请人： Amgen Inc.

发明人： BERGERON, Philippe ,  FARTHING, Christopher N. ,  JONES, Stuart D. ,  LIEBESCHUETZ, John W. ,  LIVELY, Sarah E. ,  MCGEE, Lawrence R. ,  MCKENDRY, Sharon ,  SHEPPARD, David ,  YOUNG, Stephen C.

IPC分类号： C07D239/48

CPC分类号： C07D239/47 ,  C07D213/75 ,  C07D237/22 ,  C07D239/42 ,  C07D239/46 ,  C07D239/48 ,  C07D239/52 ,  C07D239/54 ,  C07D239/58

摘要： Compounds, compositions and methods are provided that are useful in. the treatment or preventionTof a condition or disorder mediated by PPARϜ or PPARδ. In particular, the compounds of the invention modulate the function of PPARϜ or PPARδ. The subject methods are particularly useful in the treatment and/or prevention of diabetes, obesity, hypercholesterolemia, rheumatoid arthritis and atherosclerosis. The subject, compounds include bisaryl-sulfonamides that have general formula (I): wherein Ar, R1, X, Y, Z. W, L, B and R2 are described herein.

公开(公告)号：EP2146779A1

公开(公告)日：2010-01-27

申请号：EP08719431.2

申请日：2008-04-07

申请人： Pfizer Products Inc.

发明人： LUZZIO, Michael, Joseph ,  AUTRY, Christopher, Lowell ,  BHATTACHARYA, Samit, Kumar ,  FREEMAN-COOK, Kevin, Daniel ,  HAYWARD, Matthew, Merrill ,  HULFORD, Catherine Angela ,  NELSON, Kendra, Louise ,  XIAO, Jun ,  ZHAO, Xumiao

IPC分类号： A61P35/00 ,  C07D239/48 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  A61K31/506 ,  A61K31/53

CPC分类号： C07D401/12 ,  C07D239/48 ,  C07D241/20 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D475/00

摘要： The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.

公开(公告)号：EP1270560B1

公开(公告)日：2010-01-13

申请号：EP02018455.2

申请日：1999-11-01

申请人： Janssen Pharmaceutica NV

发明人： De Cort, Bart ,  De Jonge, Marc Rene ,  Heeres, Jan ,  Ho, Chih Yung ,  Janssen, Paul Andriaan Jan ,  Kavash, Robert W. ,  Koymans, Lucien Maria Henricus ,  Kukla, Michael Joseph ,  Ludovici, Donald William ,  Van Aken, Koen Jeanne Alfons ,  Andries, Koenraad Jozef Lodewijk Marcel

IPC分类号： C07D239/48 ,  C07D239/46 ,  C07D239/50 ,  C07D401/12 ,  A61K31/505 ,  A61P31/18

CPC分类号： A61K31/505 ,  A61K31/5513

公开(公告)号：EP2121633A2

公开(公告)日：2009-11-25

申请号：EP08709605.3

申请日：2008-02-11

申请人： Merck & Co., Inc. ,  Merck Sharp & Dohme Limited

发明人： BLURTON, PETER ,  FLETCHER, Stephen ,  TEALL, Martin ,  HARRISON, Timothy ,  MUNOZ, Benito ,  RIVKIN, Alexey ,  HAMBLETT, Christopher ,  SILIPHAIVANH, Phieng ,  OTTE, Karin

IPC分类号： C07D239/48 ,  C07D239/50 ,  C07D401/02 ,  C07D401/14 ,  A61K31/506 ,  A61P25/00 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D403/04 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D239/48 ,  C07D239/95 ,  C07D241/20 ,  C07D285/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D495/04

摘要： Compounds of formula (I) selectively inhibitproduction of Aβ(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition ofA(β) in the brain.

公开(公告)号：EP2114901A1

公开(公告)日：2009-11-11

申请号：EP07858201.2

申请日：2007-12-28

申请人： Tibotec Pharmaceuticals

发明人： GUILLEMONT, Jérôme Emile Georges ,  MORDANT, Céline Isabelle

IPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/06 ,  A61K31/505 ,  A61K31/506 ,  A61P31/18

CPC分类号： C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D405/12 ,  C07D409/12 ,  C07D417/06

摘要： HIV replication inhibitors of formula (I). R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; -C(=O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R8 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxy- carbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; -C(=O)R9; cyano; -S(=O)rR9; -NH-S(=O)2R9; -NHC(=O)H; -C(=O)NHNH2; -NHC(=O)R9; Het; -Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, -C(=O)NR5aR5b; -CH(OR5c)R5d; -CH2-NR5eR5f; -CH=NOR5a; -CH2-O-C2-6alkenyl; -CH2-O-P(=O)(OR5g)2; -CH2-O-C(=O)-NH2; -C(=O)-R5d; X is -NR1-, -O-, -CH2-, -S-; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.