Bristol-myers Squibb Compnay

Other

E. R. Squibb Sons, Inc.

John T Hunt

Rajeev S Bhide

Katerina Leftheris

Charles Z Ding

Robert Michael Borzilleri

Michael A Poss

Soong-Hoon Kim

Natesan Murugesan

Kyoung S Kim

Raj N Misra

Philip D Stein

Wen-Ching Han

David Brent Rawlins

S David Kimball

Ligang Qian

Kevin R Webster

Zhen-wei Cai

Toomas Mitt

Zhong Chen

George Spector

Jagabandhu Das

John Krapcho

Wayne D Vaccaro

Joel C Barrish

George C Rovnyak

Mark E Salvati

Spencer David Kimball

David M Floyd

Xiao-Tao Chen

Tram N Huynh

Gretchen M Schroeder

Stephanie Barbosa

Tai W Wong

Stephanie A Barbosa

The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

Pyrrolotriazine inhibitors of kinases

In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.

Pyrrolotriazine kinase inhibitors

The present invention provides compounds of formula Iand pharmaceutically acceptable salts thereof. The formula I compounds inhibit the tyrosine kinase activity of growth factor receptors such as VEGFR-2, FGFR-1, PDGFR, HER-1, HER-2, thereby making them useful as anti-cancer agents. The formula I compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.

Disclosed are pyrrolopyridazine compounds of the formula,

Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders

Phenyl sulfonamide endothelin antagonists

Disclosed are quinoline and benzazepine derivatives that inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogenic protein Ras. Thus, the compounds are useful as anti-cancer agents. The compounds are also useful in the treatment of diseases other than cancer.

Inhibitors of farnesyl protein transferase

Aminothiazole inhibitors of cyclin dependent kinases

Non-imidazole benzodiazepine inhibitors of farnesyl protein transferase

Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof. The compounds of formula I are useful in the treatment of a variety of cancers. In addition, the formula I compounds may also be useful in the treatment of diseases other than cancer.

1,2,5-benzothiadiazepine-1,1-dioxides with n-2 imidazolylalkyl

Compounds of the formula ##STR1## inhibit the activity of endothelin. The symbols are defined as follows: R.sup.1, R.sup.2 and R.sup.3 are each independently

Compounds of the formula ##STR1## and pharmaceuticaly acceptable salts thereof. As used in formula I, and throughout the specification, the symbols have the following meanings:

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Princeton, NJ, United States of America

John T Hunt