Merck Sharp + Dohme Corp.

Zhiqiang Guo

Scott D Edmondson

Andrew William Stamford

Amjad Ali

Shrenik K Shah

Michael W Miller

Michael Man-Chu Lo

Ping Liu

Gregori J Morriello

Harold B Wood

Cheng Zhu

Bowei Wang

Alexander Pasternak

John D Schreier

Feroze Ujjainwalla

Lin Yan

Izzat Tiedje Raheem

Timothy J Henderson

Haifeng Tang

Christopher W Boyce

Robert K Baker

Songnian Lin

Duane E DeMong

Zhi-Cai Shi

John S Debenham

Helen Y Chen

Liping Wang

Petr Vachal

William Bert Geiss

Milana M Maletic

Wanying Sun

Rajan Anand

Richard Berger

Timothy A Blizzard

Brian T Campbell

Jiayi Xu

Yuping Zhu

Brent Whitehead

Zhiyong Hu

Jason W Szewczyk

Timothy John Hartingh

Lehua Chang

Joel M Harris

Jessica Frie

Vincent Colandrea

Kallol Basu

Edward Metzger

Qinghong Fu

Libo Xu

Bart Harper

Nam Fung Kar

Rui Zhang

Kake Zhao

Ming Wang

Brian Cato

Jun Wang

Candido Gude

Yong Huang

Sunita V Dewnani

Byron Dubois

Wenlang Fu

James Dellureficio

Dennis H Leung

Megan Macala

Ning Qi

Ronald Dale Ferguson

Vincent J Colandrea

Duane E Demong

William B Geiss

The present invention relates to methods for producing a stable amorphous dispersion of a pharmaceutically active substance having poor water solubility by applying low frequency acoustic energy to a mixture comprising the active substance and at least one polymer and heating the mixture until a stable amorphous dispersion is formed. The methods of the invention are an effective means of converting a crystalline API to a substantially amorphous and stable form, i.e., wherein the crystallinity is less than about 5%. The methods of the invention result in more complete amorphization, increased solubility, drug loading and stability as compared typical amorphization or literature methods.

Methods for preparing stabilized amorphous drug formulations using acoustic fusion

Compounds of Formula I: I and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines. 

Antiviral oxime phosphoramide compounds

The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.

Inhibitors of the renal outer medullary potassium channel

Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.

Antiviral beta-amino acid ester phosphodiamide compounds

Substituted cyclopropyl compounds of the formula I and the pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. Another aspect of the invention that is of interest relates to compounds of formula 1a. 

Substituted cyclopropyl compounds, compositions containing such compounds and methods of treatment

A compound having the structure: useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy. 

Diazeniumdiolate heterocyclic derivatives

Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. 

Substituted cyclopropyl compounds useful as GPR119 agonists

Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. 

A compound having the structure useful for treating hypertension, Pulmonary Arterial Hypertension (PAH), congestive heart failure, conditions resulting from excessive water retention, cardiovascular disease, diabetes, oxidative stress, endothelial dysfunction, cirrhosis, pre-eclampsia, osteoporosis or nephropathy.

Primary amine diazeniumdiolate heterocyclic derivatives

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Morganville, NJ, United States of America

Zhiqiang Guo