Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Pfizer Corporation

Khs Gmbh

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Frank Zenke

Christiane Amendt

Dirk Finsinger

Hans-Peter Buchstaller

Alfred Jonczyk

Kai Schiemann

Dieter Dorsch

Christian Sirrenberg

Guenter Hoelzemann

Matthias Wiesner

Matthias Grell

Ulrich Emde

Werner Mederski

Oliver Schadt

Manfred Baumgarth

Timo Heinrich

Thomas Fuchss

David Bruge

Lars Thore Burgdorf

Mireille Krier

Wolfgang Staehle

Manja Friese-Hamim

Johannes Gleitz

Hartmut Greiner

Astrid Zimmermann

Jeyaprakashnarayanan Seenisamy

Roland Kellner

Marat Alimzhanov

Michel Calderini

Maria Kordowicz

Diane Hahn

Tanja Henzler

Joerg Bomke

Felix Rohdich

Helmut Reubold

Heike Dahmen

Djordje Musil

Thomas Herget

Nina Heiss

Andreas Schroeder

Patricia Soulard

Martin Falk

Keyvan Tadjalli Mehr

Thorsten Knoechel

Holger Enderle

Simone Ganz

Sebastian Droste

Burkhard Becher

Verena Wuensche

Janet Schache

The present invention relates to combination therapies useful for the treatment of cancer. In particular, the invention relates to a therapeutic combination which comprises a PD-1 antagonist, an ATR inhibitor and a platinating agent.

Combination of a PD-1 antagonist, an ATR inhibitor and a platinating agent for the treatment of cancer

Described are cyclic amide compounds of the formula (I): in which R, R, R, R, R, R, X and Y have the meanings as described. The compounds are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.

Cyclic amides as MetAP-2 inhibitors

Compounds according to Claim, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.

Pyrrolidinone derivatives as MetAP-2 inhibitors

The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).

Imidazo[4,5-C]quinolines as DNA-PK inhibitors

The compound 4-(2-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-2,7-naphthyridin-1-ylamine and pharmaceutically usable salts and/or tautomers thereof. The use of this compound for the treatment of tumors, tumor growth, tumor metastases and/or AIDS.

7-azaindole-2,7-naphthyridine derivative for the treatment of tumours

The invention relates to a method for screening compounds, which inhibit MetAP2 activity, by providing a cellular system or a sample thereof being capable of expressing MetAP2 and/or EEF1A, incubating at least a portion of the system with compounds to be screened, and detecting MetAP2 inhibition by determining EEF1A with N-terminal methionine residue (MetEEF1A). Another object of the invention concerns a method for monitoring physiological and/or pathological conditions, which are caused, mediated and/or propagated by MetAP2 activity, by administering an effective amount of at least a single compound to a mammal in need of such treatment and determining MetEEF1A in a biological sample withdrawn from the mammal. The invention also relates to the use of EEF1A as biomarker.

Use of EEF1A as biomarker and a method of screening MetAP2 inhibitors

The invention relates to compounds of the formulae (I), (II) and (III) in which R1, R2, R3, R4, Y, W, W, L, A, Alk, Cyc, Ar, Het, Het, Hal and n have the meaning indicated in Claim, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of their salts.

Morpholinylquinazolines

The present invention relates to novel bipyridyl derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.

Bipyridyl derivatives

The present invention relates to novel pyrido[2,3-b]pyrazine compounds of formula (I): and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.

Pyrido [2, 3-B] pyrazine compounds and their therapeutical uses such as for inhibiting ATP consuming proteins and treating diseases associated therewith

The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).

Imidazo[4,5-c]quinolines as DNA-PK inhibitors

Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

Heteroarylaminoquinolines as TGF-beta receptor kinase inhibitors

Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W, W, Wand Whave the meaning according to claim, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

Hetaryl-[1,8]naphthyridine derivatives

Compounds of the formula I in which R, R, Rand Rhave the meanings indicated in Claim, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.

Pyrrolidinones as MetAP-2 inhibitors

Compounds of the formula (I), in which R, X, Y, Z, Rand Rhave the meanings indicated in claim, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours. 

Pyrrolidone derivatives for use as MetAP-2 inhibitors

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Darmstadt, Germany

Frank Zenke