Novartis Ag

Christine Fritsch

Sauveur-Michel Maira

Carlos Garcia-Echeverria

Emmanuelle Di Tomaso

Pascal Furet

Robin Alec Fairhurst

Andrea Vaupel

Catherine Leblanc

Leon Murphy

Marc Gerspacher

Darrin Stuart

Edwige Liliane Jeanne Lorthiois

Xizhong Huang

Cristian Massacesi

Jürgen Hans-Hermann Hinrichs

Peter Finan

Rainer Wilcken

Paul Leslie Nicklin

Cristina Montserrat Nieto-Oberhuber

Jean-Baptiste Georges Armand Langlois

Christophe Mura

Marie-Caroline Germa

Markus Boehm

Jan Cosaert

Saskia Maria Brachmann

Christian René Schnell

Susan Wee

Ranjana Tavorath

Tobi Nagel

Tengfei Li

Milen Todorov

Nicolas Warin

The present invention relates to compounds of formula (I) or a pharmaceutically acceptable salt form thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of disease.

Compounds and compositions for inhibiting the activity of HIF2-alpha and their methods of use

The present invention relates to methods of treating or preventing a proliferative disease in a patient in need thereof by orally administering a therapeutically effective amount of an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof for at least two five-consecutive day cycle, wherein said compound is not administered to the patient for a period of about two days to about three days between said five-consecutive day cycles; the use of said compound of formula (I) or a pharmaceutically acceptable salt thereof for the manufacture of a medicament for treating or preventing a proliferative disease administered in accordance with said dosage regimen; therapeutic regimen comprising administration of said compound of formula (I) or a pharmaceutically acceptable salt thereof in accordance with said dosage regimen; and related pharmaceutical compositions and packages thereof.

Dosage regimen for an alpha-isoform selective phosphatidylinositol 3-kinase inhibitor

The present invention relates to selective cancer treatment regimes based on assaying for the presence or absence of a glutamine or a nucleic acid that encodes glutamine at position 859 of the catalytic p110&#x3b1; subunit of PI3K; methods for producing a transmittable form of information for predicting the responsiveness of patient to (S)-Pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide), or a pharmaceutically acceptable salt thereof; and a kit thereof.

Pharmaceutical diagnostic

A pharmaceutical combination comprising (a) the phosphatidylinositol 3-kinase (PI3K) inhibitor compound (S)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]thiazol-2-yl}-amide) or a pharmaceutically acceptable salt thereof, and (b) at least one mitogen activated protein kinase (MEK) inhibitor or a pharmaceutically acceptable salt, and optionally at least one pharmaceutically acceptable carrier, for simultaneous, separate or sequential administration; the uses of such combination in the treatment of proliferative diseases; and methods of treating a subject suffering from a proliferative disease comprising administering a therapeutically effective amount of such combination.

Synergistic combinations of PI3K- and MEK-inhibitors

The invention relates to the use of compounds of formula (I) in the treatment of mammalian target of rapamycin (mTOR) kinase dependent diseases, methods of use of said compounds in the treatment of said diseases in a warm-blooded animal, especially a human, pharmaceutical preparations comprising said compounds for the treatment of said diseases and said compounds for use in the treatment of said diseases.

Imidazoquinolines as dual lipid kinase and mTOR inhibitors

The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.

Combination of (a) a phosphoinositide 3-kinase inhibitor and (b) a modulator of RAS/RAF/MEK pathway

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Steinbach, France

Christine Fritsch