Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gmbh

Merck Patent Gesellschaft MIT Beschraenkter Haftung

E. Merck, Patentabteilung

Tioga Pharmaceuticals, Inc.

Rudolf Gottschlich

Christoph Seyfried

Gerd Bartoszyk

Klaus-Otto Minck

Helmut Prucher

Henning Bottcher

Helmut Wahlig

Rolf Bergmann

Hans-Heinrich Hausberg

Karl-August Ackermann

Hartmut Greiner

Andrew Barber

Werner Rogalski

Joachim Leibrock

Anton Haase

Rosmarie Steinigeweg

Simon Lawrence Goodman

Jurgen Seubert

Richard Kirchlechner

Dieter Dorsch

Hans-Peter Buchstaller

Rolf Gericke

Joachim Gante

Andreas Bathe

Elvira Dingeldein

Henning Böttcher

Horst Juraszyk

Christoph Van Amsterdam

Matthias Wiesner

Bernd Helfert

Frank Mauler

Henning Boettcher

Henning B&ouml;ttcher

Harry Schwartz

Juergen Harting

Michael Arlt

Wighard Strehlow

Ingeborg Stein

Helmut Pr&uuml;cher

Walter Hameister

Christian Noe

J&uuml;rgen Harting

Wolfgang St&auml;hle

Andrew Barbar

Manfred Stohrer

Michael Berger

Juergen Seubert

Henning Bottch

Jens Budak

Jürgen Harting

The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I:where

Heterocyclic aminoalkylpyridine derivatives as psychopharmaceuticals

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

Indol-3-yl derivatives

Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.

Dibenzoazulene derivatives for treating thrombosis, osteoporosis, arteriosclerosis

Piperidinylmethyloxazolidinone derivative

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

Disclosed herein are pharmaceutical preparations which are suitable for the treatment of postoperative ileus and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,

Kappa-opiate agonists effective in the treatment of postoperative ileus

Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,

Kappa-opiate agonists for inflammatory bowel disorders

A benzylpiperidine compound of formula I ##STR1## in which R.sup.1 is H, Hal or nitro,

Benzylpiperidine derivatives

Thienopyridone derivatives of the formula I ##STR1## in which B is CH or N, ##STR2## is ##STR3## R is H, ##STR4## R.sup.1, R.sup.2 and R.sup.5 are in each case H, A or Hal, R.sup.3 and R.sup.4 are in each case H, A, OH, OA, Hal, CF.sub.3 , NO.sub.2, NH.sub.2, NHA, N(A).sub.2 or NHAc,

Thienopyridones

Novel 4-aryloxy- or 4-arylthiopiperidine derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 are each, independently of one another, phenyl radicals which are unsubstituted or mono or disubstituted by A, OH, OA, aryloxy with 6-10 C atoms, aralkyloxy with 7-11 C atoms, --0--(CH.sub.2).sub.n --0--, Hal, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NA.sub.2, NHAc, NAAc, NHSO.sub.2 A and/or NASO.sub.2 A,

4-aryloxy- and 4-arylthiopiperidine derivatives

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

Novel oxazolidinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, Z and n have the meanings defined herein, and their salts have effects on the central nervous system, in particular calming effects.

Oxazolidinones

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Reinheim, Germany

Rudolf Gottschlich