Novartis Ag

Ciba-geigy Corporation

Novartis Corporation

Novartis Finance Corporation

Silvio Ofner

Siem J Veenstra

Walter Schilling

Yves Auberson

Hans Allgeier

Robert Mah

Marc Gerspacher

Siem Jacob Veenstra

Claudia Betschart

Andreas Von Sprecher

Fabrizio Gasparini

Silvio Roggo

Pierre Acklin

Jürgen Wagner

Dirk Behnke

Michel Biollaz

Vinod Shashikant Chaudhari

Manuel Koller

Joachim Nozulak

Henri Mattes

Wolfgang Froestl

Chetan Pandit

Terance William Hart

David Orain

Simona Cotesta

Johanne Renaud

Sangamesh Badiger

Nicolas Soldermann

Robert Moretti

Philipp Floersheim

Jürgen Hans-Hermann Hinrichs

Vittorio Rasetti

Kaspar Zimmerman

The invention provides compounds of formula I wherein n, A, R, R', R&#x2033;, R, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.

Acetylene derivatives having MGluR 5 antagonistic activity

The invention relates to compound of the formula (I), in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it. 

Diaza-spiro[5.5]undecanes

The present invention relates to 1H-Quinazoline-2,4-dione derivatives of formula(I) wherein the substituents are defined as in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them.

Quinazoline derivatives

The invention provides compounds of formula (I) wherein m, n, A, R, R', R&#x2033;, R, X and Y are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals in the treatment of e.g. nervous system disorders 

Acetylene derivatives having mGluR 5 antagonistic activity

Substituted aminoalkane phosphonic acids

2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives

The invention relates to novel N-(3,5-bis-trifluoromethyl-benzoyl)-2-benzyl-4-(azanaphthoyl-amino)-piperi dines of the formula ##STR1## wherein X and Y are each independently of the other N and/or CH and the ring A is unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of lower alkyl, lower alkoxy, halogen, nitro and trifluoromethyl; and the salts thereof, to the use thereof, to processes for the preparation thereof and to pharmaceutical compositions comprising a compound according to the invention or a pharmaceutically acceptable salt thereof.

Aroyl-piperidine derivatives

1-acyl-4-aliphatylaminopiperidine compounds

1-aryl-2-acylamino-ethane compounds and their use as neurokinin

1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalized carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the .alpha. position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.

1-acylpiperidine compounds

Compounds of formula I ##STR1## wherein rings A and B are as defined in the specification, have valuable pharmacological properties and are particularly effective as NK1 antagonists and substance P antagonists. Said compounds are prepared in a manner known per se.

Chromone Derivatives

1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 is carbonyl, oxo-lower-alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the .alpha. position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.

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Munchenstein, Switzerland

Silvio Ofner