Novartis Vaccines & Diagnostics, Gmbh

Novartis Ag

Carla C Heise

Timothy D Machajewski

Marion Wiesmann

Eric Harwood

Shuguang Zhu

Xiao Shang

Paul A Renhowe

Savithri Ramurthy

Keith Bruce Pfister

Cynthia Shafer

Sabina Pecchi

Christopher McBride

Allan S Wagman

Paul Andrew Barsanti

Stephen David Harrison

Simon C Ng

Zhi-Jie Ni

David M Ryckman

Vivien W Chan

Elisa Jazan

Peter E Haroldsen

William R McCrea

Shaopei Cai

Sang Hoon Lee

Kelly Wayman

Johanna M Jansen

Michel Faure

Alison Hannah

Keith Stewart

Michael Rowe

Dirksen Bussiere

Joyce Chou

Edward Moler

Suzanne Trudel

Emil Samara

Jayesh Vora

Clarke Taylor

Joel B Silver

Glenn C Michelson

Timothy D Dawes

Nguyen Tan

Eleni Venetsanakos

Xiaohua Xin

Esther Masih-Khan

Daniel Lopes De Menezes

Christopher Mcbride

Cynthia M Shafer

William R Mccrea

A method for treating drug-resistant cancer, includes: administering to a patient in need thereof, a compound of formula I, a tautomer of the compound, a salt of the compound, a salt of the tautomer, a mixture thereof, or a pharmaceutical composition comprising the compound, the tautomer, the salt of the compound, the salt of the tautomer, or the mixture, wherein the patient is a cancer patient with drug-resistant cancer, wherein the compound of Formula I is as defined in the application.

Methods for treating drug resistant cancer

The present invention provides a method for determining a response of a mammalian subject having melanoma tumor cells to treatment with a melanoma inhibitory agent. In one aspect, the method comprises (a) determining a first concentration of melanoma inhibitory activity protein (MIA) in a first biological sample taken from the mammalian subject before treatment with the melanoma inhibitory agent; (b) determining a second concentration of MIA in a second biological sample from the mammalian subject taken after treatment with the melanoma inhibitory agent; and (c) comparing the first and second concentrations of MIA, wherein a decrease in the second concentration of MIA measured in the second biological sample as compared to the first concentration of MIA measured in the first biological sample indicates a positive response to the treatment with the melanoma inhibitory agent.

Use of melanoma inhibitory activity (MIA) protein as an early indicator for therapeutic response in melanoma

Methods of utilizing biomarkers to identify patients for treatment or to monitor response to treatment are taught herein. Alterations in levels of gene expression of the biomarkers, particularly in response to FGFR3 inhibition, are measured and identifications or adjustments may be made accordingly.

Effects of inhibitors of FGFR3 on gene transcription

Methods of using compounds having Structure I or the salts or tautomers of the compounds in the treatment of disorders relating to cell adhesion and metastatic processes are presented herein. 

Modulating and measuring cellular adhesion

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

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

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Emeryville, CA, United States of America

Carla C Heise