Hoffmann-la Roche Inc.

Chembridge Corporation

Sloan-kettering Institute for Cancer Research

Vivasor, Inc.

F. Hoffmann-la Roche Ag

Alexander Chucholowski

Henrietta Dehmlow

Johannes Aebi

Jean Ackermann

Thomas Weller

Ulrike Obst

Sabine Wallbaum

Hans Peter Wessel

Olivier Morand

Leo Alig

Kurt Hilpert

Holger Kuehne

Tong Zhu

Daniel Bur

Lutz Weber

Sergey Zozulya

Eric Argirios Kitas

Narendra Panday

Vlad Edward Gregor

Jason Conrad Pickens

Yahua Liu

Hans-Peter Maerki

Rajendran Vairagoundar

Rene Trussardi

Bernd Kuhn

Uwe Grether

Hans G Richter

Rainer Eugen Martin

Gang Chen

Zhenwei Miao

Konrad H Bleicher

Minmin Yang

Yufeng Hong

Matthew Wright

Yan Zheng

Thomas R Webb

Katrin Groebke

Alexey Vyacheslavovich Anikin

Denise Blum

Charles Chamchoumis Mikel

Luyong Jiang

Mohan Santhanam Thiruvazhi

Zheng Yan

Douglas Eric McGrath

Vidyasagar Gantla

Danny Peter Claude McGee

Elisabeth Von Der Mark

Goverdhan Reddy Vavilala

Aleksander Kadushkin

Eric Joseph Niesor

Gregory Martin Benson

Hakim Djaballah

Alisher B Khasanov

Bernd Michael Loeffler

Sergey Sviridov

Franz Schuler

Harold E Varmus

David Shum

Romel Somwar

Hong D Zhang

Alexander Kadushkin

Xavier Marie Warot

Alexey Anikin

Ranendran Vairagoundar

Charles Mikel

Douglas Eric Mcgrath

Jason C Pickens

Danny Peter Claude Mcgee

Mohan Santhanam Thiruvahi

Vidyasagar Reddy Gantla

Thomas Roy Webb

Danny Peter Mcgee

There is disclosed an improved ADC (antibody drug conjugate) type composition having at least two different drug payloads conjugated to a single targeting protein. More specifically, the present disclosure attaches a first drug conjugate to a dual Cysteine residue on a targeting protein and a second drug conjugate with a different drug to a Lys residue on the targeting protein.

Drug-conjugates with a targeting molecule and two different drugs

The present invention is directed to pyridazinone compounds of formula (I) and furan compounds of formula (II), pharmaceutical compositions of compounds of formula (I) and (II), kits containing these compounds, methods of syntheses, and a method of treatment of a proliferative disease in a subject by administration of a therapeutically effective amount of a compound of formulae (I) or (II). Both classes of compounds were identified through screening of a collection of small molecule libraries. 

Substituted pyridazines as EGFR and/or KRAS inhibitors

Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use. 

Tyrosine kinase inhibitors

The present invention provides compounds capable of modulating tyrosine kinases, compositions comprising the compounds and methods of their use.

Heterocyclic compounds useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders

Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.

Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders

The invention is concerned with novel benzimidazole derivatives of formula (I) wherein Rto Rare as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to Farnesoid-X-receptors (FXR) and can be used to treat diseases which are modulated by FXR agonists such as diabetes and dyslipidemia.

Benzimidazole derivatives

The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

2,3-Oxidosqualene-lanosterol cyclase inhibitors

The present invention relates to pyrrolidine derivatives useful as inhibitors of metalloproteases, e.g. zinc proteases, and which are effective in treating disease states associated with vasoconstriction.

Pyrrolidine derivatives

The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Dihydroindole and tetrahydroquinoline derivatives

The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R, E, Xto Xand Gand Gare as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.

N-(4-carbamimidoyl-phenyl)-glycine derivatives

The present invention relates to piperidine derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

2,3-oxidosqualene-lanosterol cyclase inhibitors

Analine derivatives as OSC inhibitors

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San Diego, CA, United States of America

Alexander Chucholowski