Merck Sharp + Dohme Corp.

Schering Corporation

Schering-plough Corporation

Pharmacopeia Inc.

Pharmacopeia Drug Discovery, Inc.

Scheeing Corporation

Christopher W Boyce

Kevin D McCormick

Robert G Aslanian

Xianhai Huang

Younong Yu

Michael Berlin

Pietro Mangiaracina

Phieng Siliphaivanh

Neng-Yang Shih

Pauline C Ting

David James Witter

Jianhua Chao

Joseph A Kozlowski

Anandan Palani

Stuart B Rosenblum

Jongwon Lim

Kevin J Wilson

Joey Lee Methot

Wing C Tom

Daniel M Solomon

Milana M Maletic

Rongze Kuang

Ashwin Umesh Rao

Dong Xiao

David L Sloman

Purakkattle J Biju

Raman Kumar Bakshi

Umar Faruk Mansoor

Hua Zhou

Andrew William Stamford

John J Piwinski

Amjad Ali

Hongjun Zhang

Robert D Mazzola, Jr

Wei Liu

Brian Alexander McKittrick

Yu Wang

Lei Chen

Junying Zheng

Salem Fevrier

Manuel De Lera Ruiz

Wei Zhou

Mwangi W Mutahi

Walter Won

Li Dong

Chia-Yu Huang

Bo Liang

Ning Shao

Kathryn Ann Lipford

Jie Wu

Ronald D Ferguson

Matthew H Daniels

Henry A Vaccaro

Xiaohong Zhu

Elizabeth Helen Kelley

Danielle Falcone

Brendan O'Boyle

Rong-qiang Liu

Michael Man-Chu Lo

David Joseph Guerin

Yeon-Hee Lim

Qiaolin Deng

Paul Tempest

Qingbei Zeng

Qin Jiang

Heping Wu

Nicolas Zorn

Jun Qin

Henry M Vaccaro

Jianhua Cao

Jae-Hun Kim

Ravi Kurukulasuriya

Ruiyan Liu

Pawan Dhondi

Gioconda V Gallo

William Colby Brown

Joseph Michael Kelly

Ling Tong

Jianmin Fu

Alessia Petrocchi

Rajan Anand

Timothy J Henderson

Xiao Chen

Catherine M White

Christian Fischer

Tao Yu

John P Caldwell

Jayaram R Tagat

Haiqun Tang

Ron Ferguson

Corey E Bienstock

Gang Zhou

Edward Metzger

Zhiqiang Guo

Rachel Nicola MacCoss

Huagang Lu

Shuyi Tang

Judson E Richard

Sylvia Joanna Degrado

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

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).

Compounds that are ERK inhibitors

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). 

Disclosed are compounds of Formula G1: where 'R'. 'R' to &#x201c;R&#x201d;, &#x201c;n&#x201d;, &#x201c;m&#x201d;, &#x201c;p&#x201d;, &#x201c;W&#x201d;, &#x201c;X&#x201d;, &#x201c;Y&#x201d;, and &#x201c;Z&#x201d; are defined herein, which compounds are antagonists of Areceptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2A receptor in the potential treatment or prevention of neurological disorders and diseases in which Areceptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions.

Heterobicyclo-substituted [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with A2A anatagonist properties

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. 

ERK inhibitors

Disclosed are the ERK inhibitors of formula (I) and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I). This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier. This invention also provides a method of inhibiting ERK (i.e., inhibiting the activity of ERK2) in a patient in need of such treatment comprising administering to said patient an effective amount of at least one compound of formula (I). 

Disclosed are compounds of Formula A: (structurally represented) where 'RG1', 'RG2a', &#x201c;RG4&#x201d;, &#x201c;RG5&#x201d;, &#x201c;MG1&#x201d;, &#x201c;n&#x201d; and &#x201c;m&#x201d; are defined herein which compounds are antagonists of A2A receptor. Disclosed herein also are uses of the compounds described herein as antagonists of the A2a receptor in the potential treatment or prevention of neurological disorders and diseases in which A2A receptors are involved. Disclosed herein also are pharmaceutical compositions comprising these compounds and uses of these pharmaceutical compositions. 

[object Object]

The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J, J, R, R, R, R, R, R, R, R, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTHfunction. 

The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J, J, J, R, R, R, R, R, R, R, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTHfunction. 

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1). 

Disclosed are the ERK inhibitors of formula (1.0), having a pyrazolopyridine base structure, and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (1.0). 

This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTHreceptor. 

In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of &#x3b1;2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the &#x3b1;2C adrenergic receptors using such compounds or pharmaceutical compositions.

Biaryl-spiroaminooxzaoline analogues as alpha 2C adrenergic receptor modulators

In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of &#xff;2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the &#xff;2C adrenergic receptors using such compounds or pharmaceutical compositions.

Functionally selective alpha2C adrenoreceptor agonists

Growing community of inventors

Flemington, NJ, United States of America

Christopher W Boyce