Chiron Corporation

Novartis Vaccines & Diagnostics, Gmbh

Novartis Ag

Timothy D Machajewski

Paul A Renhowe

Cynthia Shafer

Sabina Pecchi

Christopher McBride

William R McCrea

Elisa Jazan

Daniel J Poon

Clarke Bentley Taylor

Carla C Heise

Maureen McKenna

Martin Sendzik

Aaron Matthew Smith

Qiong Zhang

Paul Andrew Barsanti

Marion Wiesmann

Jeff Xianming Jin

Eric Harwood

Savithri Ramurthy

Keith Bruce Pfister

Augustus O Okhamafe

Shuguang Zhu

Xiao Shang

Allan S Wagman

Yasheen Zhou

Xiaodong Lin

Simon C Ng

Stephen David Harrison

Yi Xia

Zhi-Jie Ni

Barry Haskell Levine

David M Ryckman

Abran Q Costales

Alice C Rico

Kris Mendenhall

Peter E Haroldsen

Teresa E Pick

Nathan Brammeier

Zilin Huang

Baoqing Gong

William R Antonios-McCrea

Mary Ellen Wernette Hammond

Yongjin Xu

Zheng Chen

Shaopei Cai

Kelly Wayman

Alison Hannah

Johanna M Jansen

Dirksen Bussiere

Joyce Chou

Eliza Jazan

Barry H Levine

Teresa Thomas

Joel Benjamin Silver

Clarke Taylor

Joel B Silver

Kristin Brinner

Zhenhai Gao

Zilin Hunag

John Dolan

Emil Samara

Jayesh Vora

Brandon M Doughan

X Michael Wang

Nathan c/o Novartis Vaccines And Diagnostics Inc Brammeier

Alice c/o Novartis Vaccines And Diagnostics Inc Rico

Paul A c/o Novartis Vaccines And Diagnostics Inc Renhowe

Teresa c/o Novartis Vaccines And Diagnostics Inc Pick

Paul A c/o Novartis Vaccines And Diagnostics Inc Barsanti

Abran c/o Novartis Vaccines And Diagnostics Inc Costales

Xiaodong c/o Novartis Vaccines And Diagnostics Inc Lin

Daniel c/o Novartis Vaccines And Diagnostics Inc Poon

Yi c/o Novartis Vaccines And Diagnostics Inc Xia

Marc S Tesconi

Cynthia M Shafer

David Ryckman

William R Mccrea

William Antonios-McCrea

Dan Gu

John Tulinsky

New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Heterocyclic compounds and uses thereof

Novel imidazole compounds of the general formula 

Heteroaryl-substituted imidazole compounds and uses thereof

Methods of treating cancer using 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one are provided. In particular, the methods are effective for the treatment of solid tumors or leukemias, including prostate, colorectal, breast, multiple myeloma, pancreatic, small cell carcinoma, acute myelogenous leukemia, chronic myelogenous leukemia, or myelo-proliferative disease. Further provided are methods of measuring the amount of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one and determining a metabolic profile therefore.

Methods of treating cancer and related methods

Methods of inhibiting fibroblast growth factor receptor 3 and treating various conditions mediated by fibroblast growth factor receptor 3 are provided that include administering to a subject a compound of Structure I, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I have the following structure where and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting fibroblast growth factor receptor 3 and for use in treating conditions mediated by fibroblast growth factor receptor 3 such as multiple myeloma. 

Inhibition of FGFR3 and treatment of multiple myeloma

Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nervous system diseases.

2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-ones

Organic compounds having the formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the organic compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compounds or pharmaceutically acceptable salts of the organic compounds with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation according to the invention to a patient in need thereof.

Quinolinone derivatives

Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes. 

Benzimidazole quinolinones and uses thereof

Organic compounds having the structural formula I are provided where the variables have the values described herein and Rand Rjoin together to form a 6 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group. Pharmaceutical formulations include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Heterocyclic compounds

A method for synthesizing a 4-amino substituted quinolinone includes reacting a substituted or unsubstituted 2-benzimidazolyl-2-acetate with a substituted or unsubstituted 2-aminobenzonitrile in the presence of a base or an acid. A 4-amino substituted quinolinone compound is formed by the reaction, and the 4-amino substituted quinolinone compound comprises a benzimidazole group.

Organic compounds having the structural formula I are provided where the variables have the values described herein and Rand Rjoin together to form a 6 membered substituted or unsubstituted ring including at least one O, N, or S atom, and Z is an O, S, NH or NR group.  Pharmaceutical formulations include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.

Organic compounds having the structure I are provided where the variables have the values described herein. Pharmaceutical formulations and medicaments include the organic compound or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier and may be prepared by mixing the organic compound or a pharmaceutically acceptable salt of the organic compound with a carrier and water. A method of treating a patient includes administering a pharmaceutical formulation or medicament according to the invention to a patient in need thereof.

Indazole benzimidazole compounds

Heterocyclic derivatives of quinolinone benimidazoles

Growing community of inventors

Emeryville, CA, United States of America

Timothy D Machajewski