Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Merk Patent Gmbh

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Ulrich Emde

Hans-Peter Buchstaller

Kai Schiemann

Werner Mederski

Frank Zenke

Thomas Fuchss

Dirk Finsinger

Johannes Gleitz

Christiane Amendt

Norbert Beier

Markus Klein

Christine G Charon

Lars Thore Burgdorf

Christina Esdar

Christoph Saal

David Bruge

Hans Peter Buchstaller

Joerg Bomke

Denis Carniato

Wolfgang Staehle

Oliver Poeschke

Helmut Reubold

Oliver Block

Tobias Schlueter

Michael Maiwald

Stefan Bender

Nina Heiss

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 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

A variety of specific compounds within the scope of formula I which are useful as PI3K inhibitors and can be employed for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumours, and pharmaceutical compositions and kits containing said specific compounds.

Quinoxalines derivatives and pharmaceutical compositions and kits

Compounds of the formula (I), in which X, X, L, Y, R, R, R, R, R, R, R, R, Rhave the meanings indicated in claim, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.

Pyridinylimidazolone derivatives for the inhibition of PI3 kinases

Compounds of the formula (I), in which X, Rand Rhave the meanings indicated in claim, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.

Pyrazolopyrimidine derivatives

Novel heterocyclic compounds of the formula I in which R, R, R, R, R, R, R, R, Rand Rhave the meanings indicated in Claimare activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.

Beta-amino acid derivatives for treatment of diabetes

The present invention relates to novel compounds of general formula (I) and uses thereof.

5-oxo-2,3,4,5-tetrahydro-benzo[b]oxepine-4-carboxylic acid amides and 2,3-dihydro-benzo[b]oxepine-4-carboxylic acid amides for treatment and prevention of diabetes typ 1 and 2

The invention relates to a novel process for preparing enantiomerically enriched or pure tetrahydroquinoline derivatives by reacting a chiral dihydropyran-methylamine C with a aldehyde B and an aniline A in a multicomponent one pot synthesis in the presence of a protonic acid or lewis acid with a suitable solvent. A, B, C have the meaning as described in the specification.

Process for preparing tetrahydroquinoline derivatives

Novel heterocyclic compounds of the formula I in which R, R, R, R, R, R, R, Alk and D have the meanings indicated in claimare activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.

N-(pyrazole-3-yl)-benzamide derivatives as glucokinase activators

Compounds of the formula (I), in which W, R, R, R, R, R, R, Rand Rhave the meanings indicated in Claim, can be employed, inter alia, for the treatment of tumors. 

Tetrahydroquinolines for use as modulators of the mitotic motor protein Eg5

The invention relates to a process for the manufacture of enantiomerically enriched or pure compounds of formula I wherein R, R, R, R, Rand Q are defined as in claim 1 as well as their crystalline forms for the treatment of proliferative diseases such as cancer.

Polymorphic forms and process

Disclosed are compounds of formula (I), wherein W, R, R, R, R, R, R, R, and Rhave the meanings indicated in claim. Said compounds can be used for the treatment of tumors, among other things. 

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Darmstadt, Germany

Ulrich Emde