Synaptic Pharmaceutical Corporation

Merck + Co., Inc.

Donghui Cui

Dhanapalan Nagarathnam

Ben E Evans

Bharat Lagu

Kanyin E Zhang

Kamlesh P Vyas

Hanumath P Kari

Michael Dunn

Margaret R Davis

John Howard Hutchinson

Mark E Duggan

Wasyl Halczenko

Byron H Arison

Thomayant Prueksaritanont

Raju Subramanian

Xiaojun Fang

This invention is directed to dihydropyrimidines which are selective antagonists for human &agr; receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr; receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Dihydropyrimidines and uses thereof

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

This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;,receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;,receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

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Newtown, PA, United States of America

Donghui Cui