Schering Corporation

Merck Sharp + Dohme Corp.

Pharmacopeia Drug Discovery, Inc.

Pharmacopeia Inc.

Blueprint Medicines Corporation

Schering Coporation

David a. Parry

Kamil Paruch

Timothy J. Guzi

Michael P. Dwyer

Timothy J Guzi

Michael P Dwyer

Ronald J Doll

Viyyoor Moopil Girijavallabhan

Ray Anthony James

Lawrence Wayne Dillard

Kartik M Keertikar

Vinh D Tran

Haengsoon Park

Alan K Mallams

Zhen Min He

Carmen S Alvarez

M Arshad Siddiqui

Thierry Olivier Fischmann

Dinanath F Rane

Marc A Labroli

Jocelyn Rivera

Anil K Saksena

Vincent Stewart Madison

Yi-Tsung Liu

Lianyun Zhao

Jonathan A Pachter

Alan B Cooper

Gerald Wayne Shipps, Jr

Panduranga Adulla P Reddy

Arthur G Taveras

Joseph Michael Kelly

Tin-Yau Chan

Douglas Walsh Hobbs

Jianping Chao

Chad E Knutson

Praveen K Tadikonda

Tzu Tshin Wong

Vidyadhar Madhav Paradkar

Jagdish A Desai

David Benjamin Belanger

James J-s Wang

Patrick J Curran

Shuyi Tang

Panduranga Adulla Reddy

Blake Hamann

Brian Alexander McKittrick

Stephane L Bogen

Corey Strickland

Manami Shizuka

Matthew Ernst Voss

Craig R Gibeau

Yaolin Wang

Latha G Nair

Binyuan Sun

Weidong Pan

Jose S Duca

Tarik Lalwani

Yuan Tian

Yuan Liu

Luis E Torres

Hongbo Zeng

Xiaohua Huang

Cynthia J Aki

Cliff C Cheng

Johan A Ferreira

Tin Yau Chan

David Parry

Yao Ma

Matthew Richards

Brian Robert Lahue

Margarita Kirova-Snover

Zhenmin He

Hua Zhou

John J Baldwin

Neng-Yang Shih

F George Njoroge

Malcolm MacCoss

Ge Li

Neville J Anthony

Michael D Altman

Jason D Brubaker

Janeta Popovici-Muller

Adriano Afonso

Kevin J Wilson

Paul E Fleming

Joey Lee Methot

Douglas Wilson

Yulian Zhang

Solomon D Kattar

Patrick A Pinto

Jason David Katz

Lucian V DiPietro

Rong Zhang

Abdelghani Achab

Yongqi Deng

Jay Weinstein

Bheemashankar A Kulkarni

Matthew Christopher

Meredeth Ann McGowan

Kin Chiu Fong

Kristin E Rosner

Chia-Yu Huang

Bancha Vibulbhan

Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.

Compounds useful for treating disorders related to RET

The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer. 

Purine inhibitors of human phosphatidylinositol 3-kinase delta

The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase. 

Anilinopiperazine derivatives and methods of use thereof

The present invention provides a compound of Formula I (The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. 

Substituted piperidines as HDM2 inhibitors

The compounds are of the class of pyrimidine analogs useful for treating cancer, for example: 

Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors

The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.

Substituted piperidines that increase p53 activity and the uses thereof

In its many embodiments, the present invention provides a method of inhibiting one or more cyclin dependent kinases in a patient comprising administering to said patient a therapeutically effective amount of at least one pyrazolo[1,5-a]pyrimidine compound or a pharmaceutical composition comprising such compound, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. An example pyrazolo[1,5-a]pyrimidine compound useful in the present invention is shown below: 

Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors

In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits. 

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, 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 diseases associated with the CDKs using such compounds or pharmaceutical compositions.

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, 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 diseases associated with the CDKs using such compounds or compositions.

The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase. 

Thiazole Derivatives as protein kinase inhibitors

The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase. 

2-aminothiazole-4-carboxylic amides as protein kinase inhibitors

The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease. 

Heterocyclic amide compounds as protein kinase inhibitors

The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.

Methods for inhibiting protein kinases

N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors

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Chatham, NJ, United States of America

Timothy J Guzi