Bayer Intellectual Property Gmbh

Bayer Pharma Aktiengesellschaft

Bayer Healthcare Pharmaceuticals Inc.

Ningshu Liu

Ulf Bömer

Ursula Mönning

William Johnston Scott

Manfred Möwes

Kai Thede

Arne Scholz

Andrea Hägebarth

Reiner Fischer

Philip Lienau

Christoph-Stephan Hilger

Knut Eis

Antje Margret Wengner

Stefan Golz

Eckhard Bender

Franziska Siegel

Juliane Paul

Daniel Basting

Katja Haike

Dieter Lang

Volkhart Min-Jian Li

Hartmut Rehwinkel

Wahed Ahmed Moradi

Thomas Maier

Thomas Beckers

Ludwig Zorn

Detlev Sülzle

Jens Ackerstaff

Orlin Petrov

Philipp Buchgraber

Marcus Bauser

Simon Holton

Stuart Ince

Dirk Schneider

Florian Puehler

Thomas Bär

Matthias Vennemann

Michael Gerisch

Oliver Politz

Anja Richter

József Bálint

Ulf Boemer

Armin Zülch

Swen Hölder

Gerrit Beneke

Andrea Haegebarth

Michaela Bairlein

Florian Dehmel

Sarah Wagner

Claudia Schneider

Maher Najjar

Isabelle Genvresse

Michael Jeffers

Andreas Strub

Carol Pena

Thomas Schwarz

Ursula Moenning

Manfred Moewes

Ulf BÖMER

Uif BÖMER

Barbara Beckers

The present invention relates to: * combinations of: component A: one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2) as defined herein, or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: anti-Programmed Cell Death Protein 1 (also referred to as 'PD-1' or “CD279” (cluster of differentiation 279)) antibody (anti-PD-1 mAb) as defined herein; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially; independently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; * use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and * a kit comprising such a combination.

Combinations of copanlisib with anti-PD-1 antibody

This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

2-amino-N-[7-methoxy-2, 3-dihydroimidazo-[1,2-c] quinazolin-5-yl] pyrimidine-5-carboxamides

The present invention relates to * combinations of: &#x22c5; component A: one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2), or a physiologically acceptable salt, solvate, hydrate or &#x22c5; stereoisomer thereof; &#x22c5; component B: one or more substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]-triazin-4-amine compounds of general formula (B), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; &#x22c5; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially, &#x22c5; dependently of one another by the oral, intravenous, topical, local installations, &#x22c5; intraperitoneal or nasal route; * use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; * a kit comprising such a combination; * use of biomarkers which is the loss of tumor suppressor PTEN or FBXW7, for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based dosage to increase sensitivity and/or to overcome resistance; * a method of determining the loss of tumor suppressor PTEN or FBXW7; and a method for determining perturbations in PIK3CA, PIK3CB, PIK3CD, PIK3CG, PIK3R1, PIK3R2, PIK3R3, PIK3R4, PIK3R5, FGFR1, FGFR2, FGFR3 and/or FGFR4.

Substituted 2,3-dihydroimidazo[1,2-C]quinazoline-containing combinations

The present invention relates to the use of 2,3-dihydroimidazo[1,2-c]quinazoline compounds, and of pharmaceutical compositions containing such compounds, for the treatment or prophylaxis of multiple myeloma, as a sole agent or in combination with other one or more other active ingredients.

Use of substituted 2, 3-dihydroimidazo[1,2-c]quinazolines for the treatment of myeloma

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: &#x2014;use of a 2,3-dihydroimidazo[1,2-c]quinazoline compound, or of a pharmaceutical composition containing same, as a sole active agent, or of a combination of a) said compound or a pharmaceutical composition containing said compound and b) one or more further active agents, for the preparation of a medicament for the treatment or prophylaxis of cancer; &#x2014;combinations of a) said compound and b) one or more further active agents; &#x2014;a pharmaceutical composition comprising said compound as a sole active agent for the treatment of breast cancer; &#x2014;a pharmaceutical composition comprising a combination of a) said compound and b) one or more further active agents; &#x2014;use of biomarkers involved in the modification of Bel expression, HER family expression and/or activation, PIK3CA signaling and/or loss of PTEN for predicting the sensitivity and/or resistance of a cancer patient to said compound and providing a rationale-based synergistic combination as defined herein to increase sensitivity and/or to overcome resistance; and &#x2014;a method of determining the level of a component of one or more of Bcl expression, HER family expression and/or activation, PIK3CA signaling and/or loss of PTEN.

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

The present invention relates to substituted N-(phenyl-heteroaryl)-3-acetylamino-benzamides and N-[3-(acetylamino)phenyl]-phenyl-heteroaryl-carboxamides of general formula (I) as described and defined herein, 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 such as cancer, wherein i.a.: Lrepresents an optionally substituted methylene or ethylene group; Lrepresents &#x2014;N(H)&#x2014;C(&#x2550;O)&#x2014; or &#x2014;C(&#x2550;O)&#x2014;N(H)&#x2014;; Rrepresents an optionally substituted 5- to 8-membered heterocycloalkyl, 4- to 10-membered heterocycloalkenyl, aryl, heteroaryl or &#x2014;N(R7)(Ci-C6-alkyl) group; Rrepresents an optionally substituted 5- or 6-membered heteroaryl group; Rrepresents an optionally substituted phenyl group. 

Compounds

The present invention relates to combinations of at least two components, component A and component B, component A being an inhibitor of PI3K kinase, and component B being a pharmaceutically acceptable salt of radium 223. Another aspect of the present invention relates to the use of such combinations as described supra for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of cancer with bone metastases.

Combination of PI3K-inhibitors

The present invention relates to combinations of at least two components, component A and component B, component A being an inhibitor of PI3K kinase, and component B being radium 223, particularly a pharmaceutically acceptable salt of radium-223. Another aspect of the present invention relates to 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 breast and prostate cancer as well as their bone metatases.

Described herein arc methods of treating non-Hodgkin's lymphoma (NHL), wherein the non-Hodgkin's lymphoma (NHL) is selected from the group consisting of 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); and peripheral T-cell lymphoma (PTCL). comprising administering to a patient in need thereof a 2,3-dihydroimidazo[1,2-c] quinazolinc compound, or a salt thereof.

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

Aminoalcohol substituted 2,3-dihydroimidazo[1,2-C]quinazoline derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis

The present invention relates to amido-substituted azole compounds of general formula (I), in which X, X, R, R, R, R, Rand Rare as defined in the claims which are inhibitors of TNKS1 and/or TNKS2, 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 neoplasms, as a sole agent or in combination with other active ingredients. 

Amido-substituted azole compounds

The present invention relates to alkoxy-substituted 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (I) in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of 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. 

Alkoxy-substituted 2,3-dihydroimidazo[1,2-C]quinazolines

The present invention relates to substituted phenoxypyridine compounds of general formula (I); in which R1, R2 and R3 are as defined in the claims, to methods of preparing said compounds, to intermediates for the preparation of 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. 

Arylaminoalcohol-substituted 2,3-dihydroimidazo[1,2-C]quinolines

The invention relates to substituted 3-(biphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-ones, in particular for therapeutic purposes, to pharmaceutical compositions and to their use in therapy, in particular for the prophylaxis and therapy of neoplastic disorders.

Substituted 3-(biphenyl-3-yl)-4-hydroxy-8-methoxy-1-azaspiro[4.5]dec-3-en-2-one

Growing community of inventors

Berlin, Germany

Ningshu Liu