Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Dirk Finsinger

Frank Zenke

Christiane Amendt

Kai Schiemann

Hans-Peter Buchstaller

Ulrich Emde

Christian Sirrenberg

Matthias Wiesner

Matthias Grell

David Bruge

Oliver Schadt

Lars Thore Burgdorf

Wolfgang Staehle

Christina Esdar

Margarita Wucherer-Plietker

Dieter Dorsch

Christoph Seyfried

Gerd Bartoszyk

Andree Blaukat

Manfred Baumgarth

Hartmut Greiner

Johannes Gleitz

Melanie Schultz

Christoph Van Amsterdam

Armin De Meijere

Ulrich Graedler

Michael Arlt

Helmut Reubold

Nina Heiss

Beatrix Blume

Margarita Wucherer-plietker

Suryakanta Dalai

The present invention relates to tetrahydro-tetrazolo[1,5-a]pyrazine compounds of formula (I), wherein Rdenotes &#x2014;R, &#x2014;CH&#x2014;Ror &#x2014;CO&#x2014;R; Rdenotes Ar, Hetaror C-cycloalkyl; and Rdenotes Ar, Hetaror C-cycloalkyl. These compounds are useful for inhibiting the retinoid-related orphan receptor &#x3b3; (ROR &#x3b3;, ROR-gamma) and for the prevention and/or treatment of medical conditions affected by ROR &#x3b3; activity such as rheumatoid arthritis, multiple sclerosis, psoriasis, ulcerative colitis, asthma, autoimmune hepatitis or type 1 and type 2 diabetes. 

Substituted tetrazolo[1,5-a]pyrazines as ROR-gamma inhibitors

Compounds of the formula (I), in which R, R, R, R, R, X, Y, W, Q, Q, Z, s and m have the meanings indicated in Claim, can be employed, inter alia, for the treatment of tumors.

Substituted tetrahydroquinolines

Compounds of the formula I in which X, R, R, R, Rand Rhave the meanings indicated in Claim, are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.

Pyrrolopyridinylpyrimidin-2-ylamine derivatives

The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.

Methylene urea derivatives

The present invention relates to the use of tetrahydro- and dihydroquinazolinones of formula I as protein kinase activators or inhibitors, a method for their manufacture, their use for the preparation of a medicament for the treatment of diseases, their use for the manufacture of a pharmaceutical composition and new tetrahydro- and dihydroquinazolinones. 

Tetrahydro- and dihydroquinazolinones

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

Compounds of the formula I, in which s, k, I, W, R, R, R, and U have the meanings indicated in claim, can be employed, inter alia, for the treatment of tumours. 

Tetrahydroquinoline derivatives

The invention relates to compounds of the formula (I), to the preparation and use thereof for the preparation of a medicament for the treatment of diseases, in particular tumours and/or diseases in the development or course of which kinases are involved. 

Diazepinoes

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. 

Tetrahydroquinolines

Compounds of the formula I, in which R, R, R, R, R, R, R, R, R, Z, Z, Zand Yhave the meanings indicated in claim, can be employed, inter alia, for the treatment of tumours 

Phthalazinones

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 tumours 

2-(hetero)-aryl substituted tetrahydroquinoline derivatives

Compounds of formula (I) and salts thereof, in which the following definitions apply: X is N or CH; Ris H, A, Hal, (CH)Het, (CH)Ar, C-cycloalkyl, CF, NO, CN, C(NH)(OH), or OCF; Ris (CH)Het, (CH)Ar, or C-cycloalkyl, or CF; Rand Rdenote H or an organic radical. Compounds of formula (I) are useful as ligands of 5-HT receptors and useful in the treatment of disorders such as anxiety, depression, obsessive-compulsive disorder and pain. 

Substituted pyrazole compounds

The present invention relates to benzimidazole derivatives of formula I, the use of the compounds of formula I as inhibitors of one or more kinases, the use of the compounds of formula I for the manufacture of a pharmaceutical compositions and methods of treatment, comprising administering said pharmaceutical compositions to patients.

Benzimidazole derivatives as raf kinase inhibitors

Compounds of the formula (I), in which X, Y, Z and Ar have the meanings indicated in claim, are inhibitors of Raf kinase and can be employed, inter alia, for the treatment of tumours 

Growing community of inventors

Darmstadt, Germany

Dirk Finsinger