Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Merk Patent Gmbh

Ryvu Therapeutics S.a.

Thomas Fuchss

Werner Mederski

Hans-Peter Buchstaller

Ulrich Emde

Kai Schiemann

Frank Zenke

Norbert Beier

Christos Tsaklakidis

Rolf Gericke

Wolfgang Staehle

Birgitta Leuthner

Florian Lang

Marco Poma

Clemens Kuehn

David Maillard

Ulrich Graedler

Michael Lange

Edoardo Burini

Karl Lang

Axel Becker

Paul Czodrowski

Philipp Lang

Marcel Breuning

Phillipp Lang

Holger Kubas

Marcel Breuníng

Daniel Kuhn

Lisa Koetzner

Christina Schindler

Atropisomers, solid forms, salt forms, and deuterated derivatives of the ATM inhibitor 8-(1,3-Dimethyl-1H-pyrazol-4-yl)-1-(3-fluoro-5-methoxypyridin-4-yl)-7-methoxy-3-methyl-1,3-dihydroimidazo[4,5-c]quinolin-2-one as well as compositions thereof are provided. The stable atropisomers do not interconvert and are represented by the following formulae.

Imidazolonylquinoline compounds and therapeutic uses thereof

Compounds of the formula (I), in which R1, R3, Hetand HET have the meanings given in claim, are ATM kinase inhibitors and can be employed, inter alia, for the treatment of cancer.

Imidazolonylquinolines and the use thereof as ATM kinase inhibitors

A crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be prepared as a pharmaceutical composition.

Crystalline form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol

The invention relates to novel compounds of the formula (I) which 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.

Arylquinazolines

An anhydrous disordered crystalline (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)-phenyl]-(6-methoxy-pyridazin-3-yl)-methanol can be used in pharmaceutical compositions.

Solid form of (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-yl-quinazolin-4-yl)phenyl]-(6-methoxy-pyridazin-3-yl)-methanol

The compounds are imidazolonylquinoline compounds of the following formula and are useful in the inhibition, regulation and/or modulation of signal transduction by kinases, in particular ATM kinase, furthermore for the treatment of diseases which relate to ATM kinase, in particular cancer, and which compounds can be supplied in pharmaceutical compositions and kits.

A compound of formula (IV) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer thereof  These imidazolonylquinoline compounds are useful in the inhibition, regulation and/or modulation of signal transduction by kinases, in particular ATM kinase, furthermore in pharmaceutical compositions, and in their use for the treatment of diseases which relate to ATM kinase, in particular cancer.

Compounds of the formula (I), which are ATM kinase inhibitors and can be employed, inter alia, for the treatment of cancer.

The invention relates to novel compounds of the formula (I) which 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.

Compounds of the formula I in which R, Y, R, X, X, Xand q have the meanings indicated in claim, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

1,3-Disubstituted cyclopentane derivatives

Compounds of the formula I in which R, R, R, R, X, X, X, X, q and W have the meanings indicated in claimare inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.

1,3-diaminocyclopentane carboxamide derivatives

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 invention relates to compounds of the formula (I) in which R1, L 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) 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 a salt thereof.

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Bensheim-Auerbach, Germany

Thomas Fuchss