Bristol-myers Squibb Compnay

Angex Pharmaceutical, Inc.

University of South Florida

The United States Government As Represented by the Department of Veterans Affairs

Oregon Health & Science University

Bristol-myers Squibb

Oxigene, Inc.

Francis Lee

Ashvinikumar V Gavai

George V Delucca

Claude A Quesnelle

Wen-Lian Wu

John S Tokarski

Derek J Norris

Daniel O'Malley

Patrice Gill

Zhiqiang Yang

John Qiang Tan

Brian E Fink

Yufen Zhao

Lukas C Amler

Peter Shaw

Craig R Fairchild

Fei Huang

Xia Han

Karen A Reeves

Christopher Paul Leamon

Soong-Hoon Kim

Wayne D Vaccaro

Iontcho Radoslavov Vlahov

Maria N Jure-Kunkel

John E Starrett, Jr

Gregory D Vite

Wen-Ching Han

Andrew P Degnan

Haiquan Fang

David K Bol

Joan Carboni

Matthew D Hill

William D Schmitz

Michael C Heinrich

Sunil Kumar Mandal

Kapil N Bhalla

Hong Huang

Mikkel V DeBenedetto

Tai W Wong

Charles F Albright

Ronald B Rowley

Donna Marie Barten

Claude Quesnelle

The present disclosure describes carbamate and urea compounds as novel multikinase inhibitors and methods for preparing them. The pharmaceutical compositions comprising such multikinase inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders associated with kinases are also described.

Carbamate and urea compounds as multikinase inhibitors

The present disclosure describes novel IDO inhibitors and methods for preparing them. The pharmaceutical compositions comprising such IDO inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders are also described.

Cyclic compounds as immunomodulating agents

The present disclosure describes novel TRK kinase inhibitors and methods for preparing them. The pharmaceutical compositions comprising such TRK kinase inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders are also described.

Macrocyclic compounds as TRK kinase inhibitors and uses thereof

The present invention is directed to tricyclic compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.

Tricyclic compounds as anticancer agents

A method of treating a proliferative disease, such as cancer, is disclosed. The method comprises administering to a mammal in need thereof synergistically therapeutically effective amounts of: (i) (2R,3S)&#x2014;N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-di-hydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide; (ii) 2-deoxy-2,2-difluorocytidine monohydrochloride (beta-isomer); and (iii) optionally, one or more additional anticancer agents.

Combination therapy for the treatment of proliferative diseases

Disclosed are compounds of Formula (I) and/or salts thereof: wherein Ris &#x2014;CHCHCF; Ris &#x2014;CHCHCFor &#x2014;CHCHCHCF; Ris H, &#x2014;CH, or R; Ris H or R; Ring A is phenyl or pyridinyl; and R, R, R, R, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds.

Bis(fluoroalkyl)-1,4-benzodiazepinone compounds and prodrugs thereof

Methods of treating Tau-associated diseases, preferably tauopathies, are described using epothilone D that exhibit good brain penetration, long half-life, and high selective retention in brain, and provides effective therapies in treating tauopathies including Alzheimer's disease.

Use of epothilone D in treating Tau-associated diseases including Alzheimer's disease

Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: Ris &#x2014;CHCFor &#x2014;CHCHCF; Ris &#x2014;CHCF, &#x2014;CHCHCF, or &#x2014;CHCHCHCF; Ris H or &#x2014;CH; each Ris independently F, Cl, &#x2014;CN, &#x2014;OCH, and/or &#x2014;NHCHCHOCH; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.

Bisfluoroalkyl-1,4-benzodiazepinone compounds

The invention described herein relates to methods of identifying and treating individuals with protein tyrosine kinase associated disorders that have, or may, become resistant to treatment with a kinase inhibitor such as imatinib due to a gain-of-function mutation in KIT tyrosine kinase.

Methods of identifying and treating individuals exhibiting mutant kit protein

Compositions and methods are disclosed which are useful of the treatment and prevention of proliferative disorders.

Combination of anti-CTLA4 antibody with dasatinib for the treatment of proliferative diseases

The present invention is directed to aziridinyl epothilone compounds as further described herein, and/or pharmaceutically-acceptable salts and/or solvates thereof having the following Formula: 

Aziridinyl-epothilone compounds

Here, the inventors disclose the treatment of imatinib mesylate resistant chronic myelogenous leukemia cells with a cotreatment of vorinostat (SAHA, suberoylanilide hydroxamic acid) and dasatinib, a dual Abl/Src kinase (TK) inhibitor. Combined treatment of cultured human CML and BaF3 cells with vorinostat and dasatinib induced more apoptosis than either agent alone, as well as synergistically induced loss of clonogenic survival, which was associated with greater depletion of Bcr-Abl, p-CrkL and p-STAT5 levels. Co-treatment with dasatinib and vorinostat also attenuated the levels of Bcr-AblE255K and Bcr-AblT315I and induced apoptosis of BaF3 cells with ectopic expression of the mutant forms of Bcr-Abl. Finally, co-treatment of the primary CML cells with vorinostat and dasatinib induced more loss of cell viability and depleted Bcr-Abl or Bcr-AblT315I, p-STAT5 and p-CrkL levels than either agent alone.

Method of treating chronic myelogenous leukemia cells

Growing community of inventors

Yardley, PA, United States of America

Francis Lee