Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders.
Type:
Grant
Filed:
January 28, 2005
Date of Patent:
April 24, 2007
Assignee:
Warner-Lambert Company
Inventors:
Mark Barvian, Richard John Booth, John Quin, III, Joseph Thomas Repine, Derek J. Sheehan, Peter Laurence Toogood, Scott Norman Vanderwel, Hairong Zhou
Abstract: The present invention provides compounds of Formula I wherein W, Q, E, D, R6, R7, R8, Y, K, R9, R10, R12, G, and the double bond denoted “*” have any of the values defined therefore in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cardiovascular diseases, and cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
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: 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 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: Phenylamino benzhydroxamic acid derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as psoriasis and restenosis.
Type:
Grant
Filed:
October 12, 2005
Date of Patent:
January 30, 2007
Assignee:
Warner-Lambert Company
Inventors:
Stephen Douglas Barrett, Alexander James Bridges, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Haile Tecle
Abstract: Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3–7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases.
Type:
Grant
Filed:
June 21, 2000
Date of Patent:
January 30, 2007
Assignee:
Warner-Lambert Company
Inventors:
William Alexander Denny, Gordon William Rewcastle, Ellen Dobrusin, James Bernard Kramer, Dennis Joseph McNamara, Howard Daniel Hollis Showalter, Peter Laurence Toogood
Abstract: The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in which the omega chain contains a ring structure, in an ophthalmologically compatible carrier. The invention further relates to the preparation of said compositions and their use for treatment of glaucoma or ocular hypertension.
Type:
Grant
Filed:
November 25, 2003
Date of Patent:
January 16, 2007
Assignee:
Pharmacia Aktiebolag
Inventors:
Johan Wilhelm Stjernschantz, Bahram Resul
Abstract: The present invention relates to N-methyl-substituted benzamidazole derivatives of formula (I): as defined in the specification; pharmaceutical compositions and methods of use thereof.
Type:
Grant
Filed:
July 22, 2004
Date of Patent:
January 9, 2007
Assignee:
Warner-Lambert Company, LLC
Inventors:
Stephen Douglas Barrett, Cathlin Marie Flamme, Michael David Kaufman, Jared Bruce John Milbank, Haile Tecle, Joseph Scott Warmus
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 is directed to formulations comprising 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Methods of treating diseases related to abnormal PK activity utilizing the formulations comprising these compounds and methods of making these formulations are also disclosed.
Abstract: The present invention relates to certain sulfonamido-substituted geometrically restricted indolinones of the formula: wherein R1–R12 and X are variables defined herein. The sulfonamido-substituted geometrically restricted indolinones of the preferred embodiments of the present invention 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.
Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
Type:
Grant
Filed:
February 4, 2005
Date of Patent:
July 18, 2006
Assignee:
Warner-Lambert Company
Inventors:
Gordon William Rewcastle, Julie Ann Spicer, Stephen Douglas Barrett, Michael David Kaufman, Jared Bruce John Milbank, Haile Tecle
Abstract: The present invention relates to certain 2-indolinone compounds which modulate the activity of protein kinases (“PKs”) and phosphatases. 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:
December 2, 2003
Date of Patent:
July 4, 2006
Assignee:
Sugen, Inc.
Inventors:
Peng Cho Tang, G. Davis Harris, Xiaoyuan Li
Abstract: This invention provides a novel polymorphic form of N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, as well a pharmaceutical compositions and therapeutic methods utilizing the polymorphic form.
Abstract: The present invention is directed to Mannich base prodrugs of certain 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives that modulate the activity of protein kinases (“PKs”). Pharmaceutical compositions comprising these compounds, methods of treating diseases related to abnormal PK activity utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Type:
Grant
Filed:
December 24, 2003
Date of Patent:
May 30, 2006
Assignees:
Sugen, Inc., Pharmacia & Upjohn Company LLC
Inventors:
Malcolm Wilson Moon, Walter Morozowich, Ping Gao, Peng Cho Tang
Abstract: Disclosed are compounds of the formula wherein R2, R5, R6, R7, and R8 are as defined herein. These compounds and their pharmaceutical compositions are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cdks and growth factor-mediated kinases.
Type:
Grant
Filed:
January 23, 2001
Date of Patent:
May 30, 2006
Assignee:
Warner-Lambert Company
Inventors:
Richard John Booth, Ellen Myra Dobrusin, Vara Prasad Venkata Nagendra Josyula, Dennis Joseph Mc Namara, Peter Laurence Toogood
Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.
Type:
Grant
Filed:
August 27, 2003
Date of Patent:
May 30, 2006
Assignee:
Sugen, Inc.
Inventors:
Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui