Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft MIT Beschr&auml;nkter Haftung

Tioga Pharmaceuticals, Inc.

Karl-August Ackermann

Rudolf Gottschlich

Christoph Seyfried

Gerd Bartoszyk

Hartmut Greiner

Wilfried Rautenberg

Alfred Jonczyk

Guenter Hoelzemann

Helmut Prucher

Andrew Barber

Helene Crassier

Jaume Adan

Elisabet Rosell-Vives

Michael Wolf

Wolfgang Staehle

Joachim Leibrock

Andreas Bathe

Christoph Van Amsterdam

Bernd Helfert

Frank Mauler

Gunter Holzemann

Michael Gassen

Henning B&ouml;ttcher

Francesc Mitjans

Thomas Welge

Ingeborg Stein

Anton Haase

Helmut Pr&uuml;cher

J&uuml;rgen Harting

Gema Tarrason

Rudlof Gottschlich

Andrew Barbar

Claudia Cases

Manfred Stohrer

Marta Soler Riera

Rochust Jonas

Hanse-Michael Eggenweiler

Jens Budak

Compounds of the formula (I), in which R, R, R, R, Het, X and X' have the meanings indicated in claim, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours. 

4-Amino-5-oxo-8-phenyl-5H-pyrido(2,3-D) pyrimidine derivatives as tyrosine kinase and raf kinase inhibitors for the treatment of tumours

The invention relates to compounds of formula (I) wherein R, R, R, R, R, R, R, R, R, X and X' have the designations cited in patent claim. Said compounds are inhibitors of tyrosine kinases, especially TIE-2, and Raf kinases, and can, inter alia, be used for the treatment of tumors. 

Pyridopyrimidinones

The invention relates to compounds of formula (I), wherein R , R and A have the meanings given in claim 1, are potent 5-HT antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).

Piperidine alcohols

Imidazopyridine derivatives as phosphodiesterase VII inhibitors

The invention relates to a novel process for the alternative preparation of N-methyl-N-&lsqb;(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl&rsqb;-2,2-diphenylacetamide or N-methyl-N-&lsqb;(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidin-1-yl)ethyl&rsqb;-2,2-diphenylacetamide, and the novel compounds N-methyl-N-&lsqb;(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethane&rsqb; and N-methyl-N&lsqb;(1R)-1-phenyl-2-((3R)-3-hydroxypyrrolidin-1-yl) ethane&rsqb;, which are prepared as intermediates.

Method for producing enantiomer-free N-methyl-N-&lsqb;(1S)-1-phenyl-2-((3S)-3-hydroxypyrolidine-1-yl)ethyl&rsqb;-2,2-diphenylacetamide

Quinolin-2-(1H)-ones

Novel arylacetamides of the formula I ##STR1## in which Q is R.sup.4 --CH(CH.sub.2 Z)--NA--, ##STR2## R.sup.1 is Ar, cycloalkyl with 3-7 C atoms or C.sub.4 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.7 -alkyl,

Acrylacetamides

Novel acetamides of the formula I ##STR1## in which Q, R, X and Y have the meanings defined herein, have analgesic and neuroprotective properties and bind with high affinity to kappa receptors.

Acetamides

Novel 1-(2-arylethyl)-pyrrolidines of the formula ##STR1## in which, Ar is a phenyl group which is unsubstituted or monosubstituted by OH, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA or NH--SO.sub.2 --A,

1-(2-arylethyl)-pyrrolidines

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Ober-Ramstadt, Germany

Karl-August Ackermann