Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa

Thomas G Steele

Jian Li

Michael A Patane

Shawn J Stachel

John Howard Hutchinson

Mark E Duggan

Craig Alan Coburn

Robert S Meissner

James J Perkins

Hao Wu

Ben C Askew

Paul J Coleman

John S Wai

Sherman Tim Waddell

Thomas H Graham

Michael J Breslin

Mark W Embrey

Tao Yu

Yonglian Zhang

Abbas M Walji

Wensheng Liu

Scott D Kuduk

Joseph P Vacca

Mark G Bock

Harold G Selnick

John M Sanders

Ian M Bell

Kun Liu

Wasyl Halczenko

Craig A Stump

Christopher D Cox

Michael R Wood

Huw M Nash

Lihong Hu

C Blair Zartman

Richard Soll

Thomas S Reger

Alessia Petrocchi

Jiabing Wang

Xuanjia Peng

Donnette D Staas

Vadim Y Dudkin

David Allen Annis

Christina Di Marco

Melody McWherter

Tong Wang

June J Kim

Ronald Dale Ferguson, Ii

Praveen K Tadikonda

Carol A McVean

Xiaoxing Du

Yaxian Cai

Aiwen Li

Justin T Sheen

Christine Ng Di Marco

Gergely M Makara

Xiaoxiang Du

Xuanjin Peng

Christina Ng Di Marco

Ronald Dale Ii Ferguson

The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R, R, Rand Rare as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridinonetriazine Derivative, and methods of using the 4-Pyridinonetriazine Derivatives for treating or preventing HIV infection in a subject. 

4-pyridinonetriazine derivatives as HIV integrase inhibitors

The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R, Rand Rare as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject. 

Spirocyclic hetercycle compounds useful as HIV integrase inhibitors

The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved. 

Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer's disease

The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Triazolyl PDE10 inhibitors

Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer'S disease

The present invention is directed to compounds of the formula: (wherein variables A, A, A, G, G, G, G, J, E, E, E, R, R, and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Monocyclic CGRP receptor antagonists

The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved. 

3,4-substituted pyrrolidine beta-secretase inhibitors for the treatment of alzheimer's disease

The present invention is directed to phenyl carboxamide compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Phenyl carboxamide compounds useful as beta-secretase inhibitors for the treatment of alzheimer's disease

The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &#x3b1;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &#x3b1;v&#x3b2;3 and/or &#x3b1;v&#x3b2;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.

&#x3b1;v integrin receptor antagonists

The present invention relates to novel alkanoic acid 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, inflammatory arthritis, cancer, and metastatic tumor growth.

&agr;v integrin receptor antagonists

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

Dihydro-polyazanaphthalen-2-one compounds (e.g., dihydroquinazolin-2-one and dihydropteridin-2-one derivatives) and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists

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West Point, PA, United States of America

Thomas G Steele