Warner-lambert Company

Other

Michigan State University

James Marino Hamby

Annette M Doherty

James Bernard Kramer

Diane H Boschelli

Sylvester R Klutchko

Mel C Schroeder

Howard D Showalter

Clifton J Blankley

Robert Lee Panek

William Alexander Denny

Annette Marian Doherty

Brian Desmond Palmer

Ellen Myra Dobrusin

Howard Daniel Hollis Showalter

Cleo Connolly

Sonya Shah Khatana

John C Hodges

Joseph Thomas Repine

James S Kaltenbronn

Peter Laurence Toogood

Clarke Bentley Taylor

Alan Robert Saltiel

Jetze J Tepe

Chris Limberakis

David W Fry

Andrew Mark Thompson

Mark Robert Barvian

Denton Wade Hoyer

Roy Thomas Winters

Jessica Elizabeth Reed

Zhipei Wu

Stuart James Decker

Cleo J Chivikas Connolly

Hussein Osman Hallak

Christopher James Deur

Susanne A Trumpp-Kallmeyer

Sylvester Klutchko

The invention relates to compositions comprising substituted imidazoline compounds including prodrugs, and salts thereof. In some embodiments, the invention relates to the use of these compositions as therapeutic agents, preferably for the treatment of arthritis or cancer. In further embodiments, The invention relates to the pharmaceutical compositions with effective amounts of substituted imidazoline compounds disclosed herein that function as agonist or antagonists of the genetic expression or interactions with transcription factor NF-&#x3ba;B.

Substituted imidazoline compounds

This invention provides substituted pyrimido-pyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis, as well as angiogenesis and atherosclerosis. The invention compounds have Formula I: where The invention also provides pharmaceutical formulations comprising a compound of Formula I together with a pharmaceutically acceptable carrier, diluent, or excipient therefor, and a method for treating angiogenesis using said compounds.

Bicyclic pyrimidines and bicyclic 3,4-dihydropyprimidines as inhibitors of cellular proliferation

This invention provides phenyl-substituted pyrimidopyrimidines, dihydropyrimido-pyrimidines, pyridopyrimidines, naphthyridines, and pyridopyrazines of the general formula: that inhibit cyclin-dependent kinase and tyrosine kinase enzymes, methods and intermediate compounds for their synthesis, as well as pharmaceutical compositions and methods for their use in treating, inhibiting or preventing maladies associated with cell proliferative disorders, including angiogenesis, atherosclerosis, restenosis, and cancer.

Kinase inhibitors

This invention provides antiangiogenic compounds of the Formula (I), which are useful for treating diseases, resulting from uncontrolled cellular proliferation such as cancer, atherosclerosis, rheumatoid arthritis, and psoriasis.

2-(4-Pyridyl)amino-6-dialkoxyphenyl-pyrido[2,3-d]pyrimidin-7-ones

Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation.

Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular proliferation

Naphthyridinones for inhibiting protein tyrosine kinase and cell cycle

Benzimidazoles of Formula I below are inhibitors of protein tyrosine kinases, and are useful in treating cellular proliferation. ##STR1## The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.

Benzimidazoles for inhibiting protein tyrosine kinase mediated cellular

6-Aryl naphthyridines are inhibitors of protein tyrosine kinase, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating atherosclerosis, restenosis, psoriasis, as well as bacterial infections.

6-aryl naphthyridines for inhibiting protein tyrosine kinase mediated

N-oxides of amino containing 6-aryl pyrido�2,3-d!-pyrimidine 7-imines, 7-ones, and 7-thiones have the formula ##STR1## where A and B are linkers, Ar is aryl, R.sub.2 is aklyl, X is O, S, or NH, or NAcyl, and R.sub.5 and R.sub.6 are alkyl. The compounds are inhibitors of protein tyrosine kinases and cyclin-dependent kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.

N-oxides of amino containing pyrido �2,3-D! pyrimidines

6-Aryl pyrido�2,3-d!pyrimidines and naphthyridines are inhibitors of protein tyrosine kinase, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating atherosclerosis, restenosis, psoriasis, as well as bacterial infections.

6-Aryl pyrido�2,3-d! pyrimidines and naphthyridines for inhibiting

6-Aryl pyrido�2,3-d!pyrimidine 7-imines, 7-ones, and 7-thiones are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.

Pyrido�2, 3-d!pyrimidines for inhibiting protein tyrosine kinase

Methods of treating proliferative diseases or viral, inflammatory, allergic and cardiovascular diseases, and restenosis are disclosed. The present invention demonstrates the use of N,N'-piperazinylbis-�2-amino-1-imidazolin-2-yl)-2-imidazolines!, 2-amino-1-(2-imidazolin-2-yl)-2-imidazolines, and N,N'-alkylene-bis�2-amino-1-(2-imidazolin-2-yl)-2-imidazolines!, their derivatives, and salts thereof, to antagonize the association of a protein tyrosine kinase with a substrate regulatory protein. The present invention also demonstrates the use of pharmaceutical compositions employing N,N'-piperazinylbis�2-amino-1-imidazolin-2-yl)-2-imidazolines!, 2-amino-1-(2-imidazolin-2-yl)-2-imidazolines, and N,N'-alkylenebis-�2-amino-1-(2-imidazolin-2-yl)-2-imidazolines!, their derivatives, and salts thereof, to antagonize the association of a protein tyrosine kinase with substrate regulatory protein. The present invention also relates to novel N,N'-piperazinylbis�2-amino-1-imidazolin-2-yl)-2-imidazolines!.

Substituted imidazolinyl-imidazolines as antagonists of SH-2 binding and

6-Aryl pyrido[2,3-d]pyrimidine 7-imines, 7-ones, and 7-thiones are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.

Pyrido [2,3-D]pyrimidines for inhibiting protein tyrosine kinase

The invention concerns novel renin-inhibitory peptides which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma and diseases caused by retroviruses. Processes for preparing the peptides novel intermediates in the processes, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.

Renin inhibitors containing C-terminal dihydroxy amides

The invention concerns novel renin-inhibitory compounds which are useful for treating renin-associated hypertension, congestive heart failure, hyperaldosteronism, glaucoma, and diseases caused by retroviruses including HTLV-I, -II, and -III. Processes for preparing the compounds, novel intermediates useful in the preparation thereof, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, congestive heart failure, or hyperaldosteronism.

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Ann Arbor, MI, United States of America

James Marino Hamby