The Dupont Merck Pharmaceutical Company

E.i. Dupont De Nemours and Company

Dupont Pharmaceuticals Company

Bristol-myers Squibb Pharma Company

Other

Prabhakar Kondaji Jadhav

Carl Nicholas Hodge

Patrick Y Lam

James David Rodgers

Douglas G Batt

William John Pitts

John Wityak

Bruce E Smart

Robert K Kobos

George Vincent De Lucca

Charles Joseph Eyermann

Rene Arentzen

Lawrence R McGee

Joanne M Smallheer

Michael Ernest Pierce

Shuaige Wang

George C Emmett

Joanne Marie Smallheer

Ashok Shenvi

Christina Howard Fernandez

Soo Sung Ko

Subramaniam Sabesan

Matthew Ernst Voss

Arnold J Repta

Joseph J Petraitis

Munir A Hussain

Robert Newton

Francis J Woerner

Patrick Yuk-Sun Lam

Mary E Neville

Wayne F Daneker

Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors

This invention relates to novel heterocycles which are useful as antagonists of the &agr; &bgr; integrin, the &agr; &bgr; integrin, and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Integrin antagonists

Isoxazoline fibrinogen receptor antagonists

This invention relates to novel isoxazolines of formula (I):

This invention relates to novel isoxazolines and isoxazoles of formula (I):

This invention relates to novel heterocycles which are useful as antagonists of the &agr;,&bgr;,integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, to iontophoretic delivery of such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Integrin inhibitor prodrugs

This invention relates to methods for preparing alkylating agents and use of the agents prepared. In particular, this invention relates to preparation methods for hydroxy halide and organooxy halide alkylating agents and their use for alkylating cyclic urea compounds.

Method for preparing alkylating agents for their use for alkylating

This invention relates to novel substituted caprolactams, including 4-azacaprolactams, and derivatives thereof which inhibit HIV protease and are useful for treatment of HIV disease. Also included in this invention are pharmaceutical compositions containing such caprolactams, and to methods of using such caprolactams for the treatment of HIV disease.

Substitute caprolactams and derivatives thereof useful for treatment of

This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: ##STR1## wherein R.sup.22 and R.sup.23 are allyl.

Substituted cyclic carbonyls and derivatives thereof useful as

This invention relates to novel heterocycles including 3-�1-�3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Integrin receptor antagonists

This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3-���8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspi ro-�4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Spirocycle integrin inhibitors

This invention relates to novel heterocycle compounds including but not limited to 3-�3-�3-(imidazolin-2-yl amino)propyloxy!isoxazol-5-ylcarbonylamino!-2-(benzyloxycarbonylamino)-pro pionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion and the treatment of angiogenic disorders, inflammation, bone degradation, tumors, metastases, thrombosis, and other cell aggregation-related conditions.

This invention relates to substituted cyclic ureas and derivatives thereof, including compounds of formula (II): ##STR1## said compounds being useful as inhibitors of HIV protease. The present invention also relates to pharmaceutical compositions comprising such compounds and to method of using these compounds for the treatment HIV infection. The present invention also relates to the use of such compounds in processes for the identification of HIV protease inhibitors and for the inhibition or detection of HIV in a bodily fluid sample.

Cyclic urea HIV protease inhibitors

Substituted 1,4-diazapine caprolactams useful for treatment of HIV

Growing community of inventors

Wilmington, DE, United States of America

Prabhakar Kondaji Jadhav