Abstract: The present invention relates to diagnosing abnormal cell proliferation in biological samples and screening for drugs which inhibit, reduce or abolish cell growth, especially tumorigenic cell growth, by detecting a phosphovariant isoform of a guanine nucleotide exchange factor biomarker, such as the novel GEF-H1S.
Type:
Application
Filed:
November 30, 2010
Publication date:
June 30, 2011
Applicant:
SUGEN, INC.
Inventors:
Tod R. Smeal, Marinella G. Callow, Bahija Jallal, Sergey Zozulya, Mikhail L. Gishizky
Abstract: The present invention relates to diagnosing abnormal cell proliferation in biological samples and screening for drugs which inhibit, reduce or abolish cell growth, especially tumorigenic cell growth, by detecting a phosphovariant isoform of a guanine nucleotide exchange factor biomarker, such as the novel GEF-H1S.
Type:
Grant
Filed:
September 11, 2008
Date of Patent:
January 18, 2011
Assignee:
Sugen, Inc.
Inventors:
Tod R. Smeal, Marinella G. Callow, Bahija Jallal, Sergey Zozulya, Mikhail L. Gishizky
Abstract: The present invention relates to pyrrole substituted-2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Type:
Grant
Filed:
September 6, 2006
Date of Patent:
August 11, 2009
Assignees:
Sugen, Inc., Pharmacia & Upjohn Co.
Inventors:
Peng Cho Tang, Todd Anthony Miller, Xiaoyuan Li, Connie Li Sun, Chung Chen Wei, Shahrzad Shirazian, Congxin Liang, Tomas Vojkovsky, Asaad S. Nematalla, Michael Hawley
Abstract: The present invention relates to diagnosing abnormal cell proliferation in biological samples and screening for drugs which inhibit, reduce or abolish cell growth, especially tumorigenic cell growth, by detecting a phosphovariant isoform of a guanine nucleotide exchange factor biomarker, such as the novel GEF-H1S.
Type:
Grant
Filed:
July 2, 2003
Date of Patent:
October 21, 2008
Assignee:
Sugen, Inc.
Inventors:
Tod R. Smeal, Marinella G. Callow, Bahija Jallal, Sergey Zozulya, Mikhail L. Gishizky
Abstract: The present invention relates to methods for treatment or prevention of neoplasia disorders using protein tyrosine kinase inhibitors of the formula I: wherein R1, R2, R3, R4, R5, R6, and R7 are defined herein, in combination with cyclooxygenase inhibitors, in particular cyclooxygenase-2 selective inhibitors.
Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Type:
Grant
Filed:
August 28, 2006
Date of Patent:
August 14, 2007
Assignees:
Sugen, Inc., Pharmacia & Upjohn Company
Inventors:
Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu (Alan) Jin, Paul M. Herrinton, Michael A. Mauragis
Abstract: The present invention relates to compounds of the Formulae (I)-(IV), wherein R1-R6, R11-R13, X and Y are defined herein, and their pharmaceutically acceptable salts.
Abstract: Aminopyridine and aminopyrazine compounds of formula (1), compositions including these compounds, and methods of their use are provided.
Type:
Grant
Filed:
February 26, 2004
Date of Patent:
June 12, 2007
Assignee:
Sugen, Inc.
Inventors:
Jingrong Jean Cui, Dilip Bhumralkar, Iriny Botrous, Ji Yu Chu, Lee A. Funk, Cathleen Elizabeth Hanau, G. Davis Harris, Lei Jia, Joanne Johnson, Stephen A. Kolodziej, Pei-Pei Kung, Xiaoyuan (Sharon) Li, Jason (Qishen) Lin, Jerry Jialun Meng, Mitchell David Nambu, Christopher G. Nelson, Mason Alan Pairish, Hong Shen, Michelle Tran-Dube, Allison Walter, Fang-Jie Zhang, Jennifer Zhang
Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.
Type:
Grant
Filed:
June 25, 2003
Date of Patent:
May 15, 2007
Assignees:
Yissum Research and Development Company of the Hebrew University of Jerusalem, Sugen, Inc.
Inventors:
Hui Chen, Aviv Gazit, Alexander Levitzki, Klaus Peter Hirth, Elaina Mann, Peng Cho Tang, Laura K. Shawver, Jianming Tsai
Abstract: The present invention relates to (2-oxindol-3-ylidenyl)acetic acid derivatives which modulate the activity of protein kinases and are therefore useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity c-kit kinase.
Abstract: The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1? position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety.
Type:
Grant
Filed:
February 24, 2004
Date of Patent:
April 10, 2007
Assignee:
Sugen, Inc.
Inventors:
Peng Cho Tang, Connie Li Sun, Gerald McMahon, Klaus Peter Hirth, Laura Kay Shawver
Abstract: The present invention relates to novel 3-hetero-arylidene-2-indolinone compounds and physiologically acceptable salts thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Abstract: The present invention relates to substituted imidazopyrazines of the general Formula I which modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Type:
Grant
Filed:
May 14, 2004
Date of Patent:
March 6, 2007
Assignee:
Sugen Inc.
Inventors:
Connie Li Sun, Congxin Liang, Ping Huang, G. Davis Harris, Jr., Huiping Guan
Abstract: Compounds of Formula I are useful as mediators of protein kinases and have activity as cell proliferation inhibitors: where X, R1–R7 and R9 are as defined herein.
Abstract: The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Type:
Grant
Filed:
March 8, 2004
Date of Patent:
January 2, 2007
Assignee:
Sugen Inc.
Inventors:
Peng Cho Tang, Congxin Liang, Todd Miller, Kenneth E. Lipson
Abstract: The present invention relates to 8-amino-aryl-substituted imidazopyrazines which modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Type:
Grant
Filed:
February 20, 2004
Date of Patent:
January 2, 2007
Assignee:
Sugen Inc.
Inventors:
Connie Li Sun, Congxin Liang, Ping Huang, G. Davis Harris, Jr., Huiping Guan
Abstract: The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.