Merck Patent Gmbh

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Merck Patent Gesellschaft

3-dimensional Pharmaceuticals, Inc.

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Ortho-mcneil Pharmaceutical Corp.

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Merk Patent Gmbh

Werner Mederski

Dieter Dorsch

Christos Tsaklakidis

Bertram Cezanne

Norbert Beier

Johannes Gleitz

Mathias Osswald

Klaus-Otto Minck

Pierre Schelling

Ingeborg Lues

Rolf Gericke

Thomas Fuchss

Markus Klein

Hans-Peter Buchstaller

Maria Christadler

Claus J Schmitges

Claudia Wilm

Sabine Bernotat-Danielowski

Florian Lang

Christopher Barnes

Ulrich Emde

Richard M Soll

Mark R Player

Hanns Wurziger

Frank Zenke

Guido Melzer

James M Rinker

Horst Juraszyk

Gerhard Barnickel

Lars Thore Burgdorf

Daljit Singh Dhanoa

Christoph Van Amsterdam

Bao-Ping Zhao

Joachim Gante

Johannes Sombroek

Ralf M Devant

Soheila Anzali

James Vickers

Andreas Bathe

Clemens Kuehn

David Maillard

Heinz-Hermann Bokel

Michael Lange

Edoardo Burini

Maria Devant, Legal Representative

Thorsten Hartig

Edward Jaegar

Christopher Bames

Maria Devant

Bertram Cezane

Dalijit Dhanoa

Bao-Ping Zhoa

Johannes Gleiltz

Matthias Osswald

Tobias Schlueter

Edward Jaeger

A solid form of 1-(4-{[6-Amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methy}-4-fluoro-piperidin-1-yl)-propenone, or pharmaceutically acceptable salts thereof, is useful as a BTK inhibitor.

Crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone, salt forms thereof, and processes to obtain

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

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.

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.

Morpholinylbenzotriazines for use in cancer therapy

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 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 heterocyclic compounds of the formula (I), in which R, D, W, T and T' have the meanings indicated in Claim, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.

Heterocyclic carbonyl compounds

The invention relates to compounds of the formulae (I), (II) and (III), 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) by reaction of compounds of the formula (II) or (III) and optionally conversion of a base or acid of the compounds of the formula (I) into one of its salts

Pyrazoloquinolines

Novel compounds of the formula (I), in which W, T, R, R, R, R, R, Rand Xhave the meanings indicated in Patent Claim, are suitable as antidiabetics.

[object Object]

Novel compounds of the formula I, in which X, Y, R, R', R, R, R, R, R, R, R, R, R, Rand n have the meanings indicated in Patent Claim, are suitable as antidiabetics 

3-aminoimidazo [1,2-A] pyridine derivatives as SGLT inhibitors

Novel compounds of the formula (I), in which W, T, R, R, R, R, Rand Rhave the meanings indicated in Patent Claim (), are suitable as antidiabetics. 

3-aminoimidazo 1,2-A pyridine derivatives having an SGLT1- and SGLT2-inhibiting action for the treatment of type 1 and type 2 diabetes

Novel compounds of the formula (I), in which D, E, G, W, X, Y, T, Rand Rare as defined in Patent Claim, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors. 

Carbonyl compounds

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Zwingenberg, Germany

Werner Mederski