公开(公告)号：EP1962830A2

公开(公告)日：2008-09-03

申请号：EP06846678.8

申请日：2006-12-19

申请人： SmithKline Beecham Corporation

发明人： ADAMS, Jerry, Leroy ,  ADAMS, Nicholas, D. ,  AXTEN, Jeffrey, Michael ,  CHAUDHARI, Amita, M. ,  DHANAK, Dashyant ,  HAMAJIMA, Toshihiro ,  NEWLANDER, Kenneth, Allen ,  PARRISH, Cynthia, A. ,  SARPONG, Martha, A. ,  SILVA, Domingos, J. ,  TANG, Jun

IPC分类号： A61K31/335

CPC分类号： C07D471/04

摘要： The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a number of diseases, including solid tumor cancers and hematological cancers.

公开(公告)号：EP1778214A2

公开(公告)日：2007-05-02

申请号：EP05807320.6

申请日：2005-07-27

申请人： SMITHKLINE BEECHAM CORPORATION ,  Cytokinetics, Inc.

发明人： CHAUDHARI, Amita, M. ,  DHANAK, Dashyant ,  KNIGHT, Steven, David ,  MORGANS, David, J., Jr. ,  PARRISH, Cynthia, A.

IPC分类号： A61K31/335 ,  A61K31/17 ,  A61K31/167 ,  C07C335/16 ,  C07C335/20 ,  C07C275/40 ,  C07C275/32 ,  C07C275/28 ,  C07C233/15 ,  C07D319/06

CPC分类号： C07C275/28 ,  C07C233/15 ,  C07C233/43 ,  C07C259/06 ,  C07C275/30 ,  C07C275/40 ,  C07C275/42 ,  C07C275/64 ,  C07C317/24 ,  C07C317/42 ,  C07C323/44 ,  C07C335/16 ,  C07D209/02 ,  C07D307/79 ,  C07D317/66 ,  C07D319/18

摘要： The invention is directed to certain biphenyl compounds. Specifically, the invention is directed to compounds according to Formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and Y are as defined below, and to pharmaceutically-acceptable salts thereof. The compounds of the invention are KSP inhibitors, particularly human KSP inhibitors, and can be useful for the treatment for a variety of diseases and conditions, such as cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders, fungal disorders, and inflammation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting KSP and treatment of conditions associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention. In an additional aspect, the invention provides methods of screening for compounds that will bind to a KSP kinesin, for example compounds that will displace or compete with the binding of the compounds of the invention. The methods comprise combining a labeled compound of the invention, a KSP kinesin, and at least one candidate agent and determining the binding of the candidate bioactive agent to the KSP kinesin. In a further aspect, the invention provides methods of screening for modulators of KSP kinesin activity. The methods comprise combining a compound of the invention, a KSP kinesin, and at least one candidate agent and determining the effect of the candidate bioactive agent on the KSP kinesin activity.