Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Dirk Wienke

Wolfgang Staehle

Kai Schiemann

Frank Stieber

Christos Tsaklakidis

Birgitta Leuthner

Timo Heinrich

Melanie Schultz

Mireille Krier

Christa Burger

Ansgar Wegener

Manja Friese-Hamim

Oliver Poeschke

Michael Busch

Ingo Kober

Brigitta Leuthner

Frank Czauderna

Compounds of the formula I in which R, X, X, X, X, R, Rand q 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.

Piperazine derivatives as FASN inhibitors

The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.

Benzyl piperidine compounds as lysophosphatidic acid (LPA) receptor antagonist

Compounds of the formula I in which R, R, R, X, X, X, X, n1, n2, n3 and n4 have the meanings indicated in claim are inhibitors of Tankyrase, 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. 

Hydropyrrolopyrrole derivatives for use as fatty acid synthase inhibitors

The present invention relates to novel pyrazolopyridinone derivatives according to formula (I) and a process of manufacturing thereof. These pyrazolopyridinone derivatives can be used as LPA receptor antagonists for the treatment of various herein disclosed diseases.

Pyrazolopyridinone derivatives as LPA receptor antagonists

The present invention relates to compounds of the formula (I), in which R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, M, M, M, M, Y, Y, V, W, n, m and o have the meanings given in Claim, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.

Inhibitors of sphingosine kinase

The present invention relates to compounds of the formula (I), in which R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, R, M, M, M, Y, Y, V, W, n, m and o have the meanings given herein, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.

The present invention relates to pyridopyrimidine derivatives according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.

2, 5-diamino-substituted pyrido [4, 3-D] pyrimidines as autotaxin inhibitors against cancer

Compounds of the formula (I), in which R, R, R, R, R, R, R, R, R, Q and W have the meanings indicated in Claim, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumors.

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Darmstadt, Germany

Dirk Wienke