Merck + Co., Inc.

Wasyl Halczenko

George D Hartman

Mark E Duggan

John Howard Hutchinson

Melissa S Egbertson

Ben C Askew

William L Laswell

John J Baldwin

Michael A Patane

Gerald E Stokker

Robert S Meissner

Jiabing Wang

Paul J Coleman

Steven D Young

Kenneth L Shepard

John D Prugh

Nathan C Ihle

Steven M Pitzenberger

Theresa M Williams

Robert L Smith

Craig A Stump

Otto D Hensens

John S Wai

James J Perkins

Ta J Lee

Edward S Inamine

Brian T Phillips

Laura M Vassallo

Garry R Smith

David R Houck

Cecilia A Hunt

Amy E Krause

Edward J Cragoe, Jr

David A Claremon

Gerald S Ponticello

Neville J Anthony

William F Hoffman

Samuel L Graham

William C Lumma, Jr

Byron H Arison

Soumya P Sahoo

Gideon A Rodan

Robert P Gomez

Michael J Breslin

Terrence M Ciccarone

Thomas G Steele

Azriel Schmidt

Shun-ichi Harada

David B Whitman

Kelly Michelle Solinsky

Laura M Turchi

Harvey Schwam

Donghui Cui

Thomayant Prueksaritanont

Dwight A Towler

Aiwen Li

Laura A Libby

Raju Subramanian

Xiaojun Fang

Charles M Habecker

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.

Integrin receptor antagonists

Compounds of structural formula (I) as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of agonizing the androgen receptor in a patient, and in particular the method wherein the androgen receptor is antagonized in the prostate of a male patient or in the uterus of a female patient and agonized in bone and/or muscle tissue. These compounds are useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including: osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, post-menopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, aplastic anemia and other hematopoietic disorders, pancreatic cancer, renal cancer, arthritis and joint repair, alone or in combination with other active agents. In addition, these compounds are useful as pharmaceutical composition ingredients alone and in combination with other active agents.

Androgen receptor modulators and methods for use thereof

The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.

&agr;V integrin receptor antagonists

The present invention relates to novel compounds formed by metabolic conversion of compounds of structural formula (1), pharmaceutical compositions containing such compounds, and their use as &agr;v&bgr;3 integrin receptor antagonists. The compounds of the present invention are useful for inhibiting bone resorption, restenosis, angiogenesis, diabetic retinopathy, macular degeneration, inflammatory arthritis, cancer, and metastatic tumor growth. They are particularly useful for inhibiting bone resorption and for the treatment and prevention of osteoporosis.

&agr; v integrin receptor antagonists

Biaryl substituted imidazole compounds useful as farnesyl-protein

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha.v.beta.3, .alpha.v.beta.5, and/or .alpha.v.beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.

A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.

Sulfonamide fibrinogen receptor antagonists

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha.v.beta.3, .alpha.v.beta.5 and/or .alpha.v.beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, and tumor growth and metastasis.

The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.

Inhibitors of farnesyl-protein transferase

A fibrinogen receptor antagonist which is 3(R)-�2-(Piperidin-4-yl)ethyl!-2-piperidon-1-ylacetyl-3(S)-(3-pyridyl)-.be ta.-alanine.

Fibrinogen receptor antagonist

Fibrinogen receptor antagonists having the structure, for example, of ##STR1## for example ##STR2##

Fibrinogen receptor antagonists

A fibrinogen receptor antagonist which is 5-�(4-Piperidinyl)methoxy!-2-indolecarbonyl-2(S)-phenylsulfonyl-amino-.bet a.-alanine.

Growing community of inventors

Lansdale, PA, United States of America

Wasyl Halczenko