Bayer Pharma Aktiengesellschaft

Bayer Intellectual Property Gmbh

Bayer Aktiengesellschaft

Dana-farber-cancer Institute Inc.

The Broad Institute, Inc.

Antje Margret Wengner

Philip Lienau

Gerhard Siemeister

Knut Eis

Marcus Koppitz

Hans Briem

Benjamin Bader

Volker Schulze

Dirk Kosemund

Ulf Bömer

Ulrich Lücking

Lars Wortmann

Hans Schick

Wilhelm Bone

Simon Holton

Detlef Stöckigt

Ulrich Klar

Matthew Meyerson

Anne Mengel

Hartmut Schirok

Timothy A Lewis

Martin Lange

Heidi Greulich

Mark Jean Gnoth

Roland Neuhaus

Detlev Sülzle

Ningshu Liu

Amaury Ernesto Fernandez-Montalvan

Rolf Bohlmann

Hans-Georg Lerchen

Lars Bärfacker

Ludwig Zorn

Rolf Jautelat

Jens Ackerstaff

Ulrich Bothe

Ursula Mönning

Judith Günther

Tobias Marquardt

Marion Hitchcock

Florian Puehler

Andrea Hägebarth

Georg Kettschau

Clara Christ

Ursula Krenz

Donald Bierer

Kirstin Petersen

Holger Siebeneicher

Olaf Prien

Franz Von Nussbaum

Stefan Prechtl

Julien Lefranc

Joanna Grudzinska-Goebel

Dieter Moosmayer

Uwe Eberspächer

Xiaoyun Wu

Michael Brüning

Ulrike Sack

Tobias Heinrich

Alex Burgin

Jörg Fanghänel

Vera Pütter

Luc De Waal

Monica Schenone

Cornelia Preusse

Katja Haike

Juliane Paul

Li Liu

Keith Graham

Christian Stegmann

Manuel Ellermann

Charlotte Christine Kopitz

Reinhard Nubbemeyer

Holger Steuber

Jens Schröder

Sven Golfier

Horst Irlbacher

Katrin Nowak-Reppel

Nicole Schmidt

Roman Hillig

Andreas Sutter

Ildikó Terebesi

Bernard Händler

Florian Prinz

Andreas Schlicker

Joszef Bálint

Katrin Nowak-reppel

Florian Pühler

Ulrich Lucking

Judith Gunther

Hans (deseased) Schick

Ulf BÖMER

Philipp Lienau

Hassan Y Harb

Ashley Eheim

Lars BÄRFACKER

Michael Bruening

The present invention features improved compounds, especially methods of identifying patients having cancer using biomarkers (e.g., PDE3A, SLFN12 and/or CREB3L1) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., Compounds 1-6 disclosed herein).

Compounds, compositions and methods for cancer patient stratification and cancer treatment

The present invention covers 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine (in the following called 'Compound A'), an inhibitor of ATR kinase, for use in a method of treating a hyper-proliferative disease in a subject. Preferably the hyper-proliferative disease or the subject is characterized by one or more biomarker(s) selected from The present invention also covers a kit comprising Compound A together with means to detect one or more of the aforementioned biomarker(s) and a method for identifying a subject having a hyper-proliferative disease disposed to respond favorably to Compound A, wherein the method comprises the detection of one or more of the aforementioned biomarker(s). Further, the invention covers a method of determining whether a subject having a hyper-proliferative disease will respond to the treatment with Compound A, wherein the method comprises the detection of one or more of the aforementioned biomarker(s) in a sample of the subject.

Inhibitor of ATR kinase for use in a method of treating a hyper-proliferative disease

The present invention covers an ATR kinase inhibitor, particularly 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(H-pyrazol-5-yl)-1,7-naphthyridine ('Compound A'), for use in the treatment of a hyper-proliferative disease in a subject, wherein the hyper-proliferative disease or the subject is or has been characterized by one or more biomarker(s), wherein the biomarker(s) comprise(s) a) one or more functional mutations in one or more gene(s)/protein(s) selected from RBBP8, APOBEC3A, APOBEC3B, CLSPN, ERCC, HUS1, MAD2L2, PGBD5, POLD1, RAD1, TIMELESS and/or TIPIN; and/or b) the expression of a fusion gene encoding a fusion protein selected from EWSR-ERG, EWSR1-FLI1, SS18-SSX and/or SS18-SSX2 gene/protein.

Predictive markers for ATR kinase inhibitors

The present invention covers combinations of at least two components, component A and component B, comprising component A being an inhibitor of ATR kinase, particularly an inhibitor of ATR kinase selected from VX-803, VX-970, AZD-6738, a compound of general formula (I) described herein, a compound of general formula (Ib) described herein and Compound A described infra, and component B being a PD-1/PD-L1 inhibitor described herein. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.

Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors

The present invention covers combinations of at least two components, component A and component B, comprising component A being an ATR kinase inhibitor, particularly Compound A, and component B being a PARP inhibitor, such as olaparib. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particurlarly for the treatment of a hyper-proliferative disease.

Combination of ATR kinase inhibitors with PARP inhibitors

The present invention relates to substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients.

2-(morpholin-4-yl)-1,7-naphthyridines

The present invention features improved compounds, especially the compound having the structure (1). Compositions and methods of identifying patients having cancer using biomarkers (e.g., PDE3A, PDE3B, SLFN12 and/or CREB3L1) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention. 

Compounds, compositions and methods for cancer treatment

The present invention features improved Compounds, especially (I) methods of identifying patients having Cancer using biomarkers (e.g., PDE3A, SLFN12 and/or CREB3L1) that correlate with drug sensitivity and consequently treating a stratified patient population with an agent of the invention (e.g., Compounds 1-6 disclosed herein). 

The present invention covers heteroarylbenzimidazole compounds of general formula (I) in which R, R, R, Rand Rare as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative and/or inflammatory disorders, as a sole agent or in combination with other active ingredients. 

Heteroarylbenzimidazole compounds

The present invention relates to 5-substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative disease as a sole agent or in combination with other active ingredients. 

5-substituted 2-(morpholin-4-yl)-1,7-naphthyridines

Compounds of formula (I) which are inhibitors of Bub 1 kinase, processes for their production and their use as pharmaceuticals.

Substituted benzylindazoles for use as BUB1 kinase inhibitors in the treatment of hyperproliferative diseases

Substituted benzylindazoles for use as Bub1 kinase inhibitors in the treatment of hyperproliferative diseases

Described herein are pharmaceutical combinations and compositions comprising a) a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or a salt thereof, and b) one more additional active agents. The pharmaceutical combinations described herein may be useful for treating non-Hodgkin's lymphoma (NHL), particularly 1st line, 2nd line, relapsed, refractory, indolent or aggressive non-Hodgkin's lymphoma (NHL); follicular lymphoma (FL); chronic lymphocytic leukemia (CLL); marginal zone lymphoma (MZL); diffuse large B-cell lymphoma (DLBCL); mantle cell lymphoma (MCL); transformed lymphoma (TL); or peripheral T-cell lymphoma (PTCL).

Use of substituted 2,3-dihydroimidazo[1,2-C]quinazolines for treating lymphomas

The present invention relates to amido-substituted imidazopyridazine compounds of general formula (I): in which A, E, R2, R3, R4 and n are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. 

Amido-substituted imidazopyridazines useful in the treatment of hyper-proliferative and/or angiogenesis disorders

Growing community of inventors

Berlin, Germany

Antje Margret Wengner