Janssen Pharmaceutica Nv

Ortho-mcneil Pharmaceutical Corp.

Beta Pharma, Inc.

Ortho Pharmaceutical Corporation

Beta Pharma (shanghai) Co., Ltd.

Michael Nicholas Greco

Michael Hawkins

Eugene Powell

Harold R Almond

Don Zhang

Jirong Peng

Michael John Costanzo

Bruce E Maryanoff

Michael Alan Green

Victoria Lynn Wilde

Mark J Macielag

Yue-Mei Zhang

Bart L DeCorte

Lawrence De Garavilla

Robert E Boyd

Rui Zhang

Kirk L Sorgi

Sergio Cesco-Cancian

Marcel A Janssen

Michael J Humora

Michael H Parker

Donald Gilmore Walker

Christopher Norman Nilsen

Mitul N Patel

Yun Qian

Alfons H Raeymaekers

Donald William Ludovici

Eddy J Freyne

Christopher A Teleha

Hong Ye

Margery Connelly

William Joel Hoekstra

Bin Benjamin Zhu

William V Murray

Guozhang Xu

Dennis J Hlasta

Brian Christopher Shook

Jay M Matthews

Edward Charles Lawson

Daniel J Parks

Barry A Springer

Shyamali Ghosh

Eric D Strobel

Leonard Robert Hecker

Michele Ann Weidner-Wells

Devraj Chakravarty

Michael J Hawkins

Methods of treating EGFR mutant-related cancers with a combination of an EGFR inhibitor of Formula (I) and the CDK4/6 inhibitor of Formula (II) and use of combinations of these compounds in the manufacture of medicaments for the treatment of EGFR mutant-related cancers are disclosed:

Treatment of EGFR mutant-related cancers using a combination of EGFR and CDK4/6 inhibitors

The present disclosure provides [1,2,4]triazolo[4,3-b][1,2,4]triazine, [1,2,4] triazolo[4,3-b]pyridazine, and [1,2,3]triazolo[4,5-b]pyrazine derivatives, and pharmaceutically acceptable salts, solvates or prodrugs thereof, as tyrosine kinase c-MET inhibitors, which are useful as novel anticancer and/or anti-inflammatory agents.

Organophosphorus-substituted compounds as c-MET inhibitors and therapeutic uses thereof

A pharmaceutical formulation of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (compound 1), in particular methanesulfonic acid salt thereof, and methods of using the pharmaceutical formulation for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGER), such as various cancers, are disclosed.

Pharmaceutical formulations of-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylaminde and salts thereof

This application discloses novel substituted 2-anilinopyrimidine derivatives, and pharmaceutically acceptable salts, solvates, prodrugs, and compositions thereof, which are useful for the treatment or prevention of diseases or medical conditions mediated by epidermal growth factor receptors (EGFRs), including but not limited to a variety of cancers.

Substituted 2-anilinopyrimidine derivatives as EGFR modulators

2-Aminopyrimidine-substituted 2H-indazole compounds of formula (I), where Ris hydrogen, and their prodrugs, where Ris a metabolizable group under physiological conditions, as cyclin-dependent kinase (CDK) and cell-proliferation inhibitors, and therapeutic uses and methods of preparation thereof, are disclosed. These compounds, and pharmaceutically acceptable salts, solvates, prodrugs, and pharmaceutical compositions thereof, are useful for treating diseases and disorders associated with activity of cyclin-dependent kinases, in particular CDK4/6, including but not limited to various cancers and inflammation-related diseases or conditions. 

2H-indazole derivatives as CDK4 and CDK6 inhibitors and therapeutic uses thereof

A pharmaceutical formulation of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (compound 1), in particular methanesulfonic acid salt thereof, and methods of using the pharmaceutical formulation for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed.

Pharmaceutical formulations of N-(2-(2-(dimethylamino) ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and salts thereof

Methods of using substituted 2-anilinopyrimidine derivatives, and pharmaceutically acceptable salts, solvates, or compositions, for the treatment of brain cancers, in particular EGFR-mediated metastatic brain cancer, are disclosed.

2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers

Crystalline forms of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (1) and its pharmaceutically acceptable salts and compositions thereof useful for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed.

Pharmaceutical salts N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof

Indazole compounds of formula (I) as cyclin-dependent kinase (CDK) and cell-proliferation inhibitors, and therapeutic uses and methods of preparation thereof, are disclosed. These compounds, and pharmaceutically acceptable salts, solvates, prodrugs, and pharmaceutical compositions thereof, are useful for treating diseases and disorders associated with activity of cyclin-dependent kinases, in particular CDK4/6, including but not limited to various cancers and inflammation-related diseases or conditions. 

2-H-indazole derivatives as cyclin-dependent kinase (CDK) inhibitors and therapeutic uses thereof

The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders.

Benzimidazole derivatives useful as CB-1 inverse agonists

Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the CB1 receptor. Such compounds are represented by Formula (I)  

Chemically modified quinoline and quinolone derivatives useful as CB-1 inverse agonists

The present invention is directed to cinnoline derivatives pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders.

Cinnoline derivatives useful as CB-1 receptor inverse agonists

The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders.

Indazole derivatives useful as CB-1 inverse agonists

Growing community of inventors

Lansdale, PA, United States of America

Michael Nicholas Greco