Hoffmann-la Roche Inc.

Actelion Pharmaceuticals Ltd

F. Hoffmann-la Roche Ag

Volker Breu

Werner Neidhart

Georges Hirth

Marcel Muller

Henri Ramuz

Martine Clozel

Jean-Marie Cassal

Kaspar Burri

Bernd-Michael Loffler

Eric Vieira

Wolfgang Wostl

Philippe Pflieger

Kurt Hilpert

Daniel Bur

Hans-Peter M&auml;rki

Frank Dautzenberg

Philippe Coassolo

S&eacute;bastien Roux

Thomas Giller

Matthias Heinrich Nettekoven

Heinz Stadler

Alfred Binggeli

Walter Fischli

Heinz Fretz

Anja Fecher

Maurice Wilhelm

Matthias Steger

Oliver Valdenaire

Rolf Guller

Patrizio Mattei

Hans Peter Wessel

Hans-Peter Maerki

Philippe Guerry

Peter Weiss

Christian Oefner

Hans-Peter Marki

Eva Caroff

Marcel M Uller

Bernd-Michael L Offler

Rolf Huber

Günter Schwalm

Markus Isler

Olivier Valdenaire

The invention relates to guanidine derivatives of formula (I) where: A represents a chain of 3-6 carbon atoms, one of which can be replaced by &#x2014;N(R')&#x2014; or &#x2014;O&#x2014; and R&#x2032; is H or a substituent; the ring skeleton only contains both double bonds of the thiazole component; the pharmaceutically-acceptable acid addition salts of basic compounds of formula (I), the pharmaceutically-acceptable salts of compounds of formula (I), comprising acid groups, with bases, the pharmaceutically-acceptable esters of hydroxy or carboxyl group containing compounds of formula (I) and the solvates or hydrates thereof, which exhibit a neuropeptide FF receptor antagonist effect. The above are suitable for the treatment of pain and hyperalgesia, withdrawal symptoms in alcohol, psychotropic and nicotine dependencies, for improvement or cure of said dependencies, for regulation of insulin excretion, food intake, memory functions, blood pressure, electrolyte and energy management and for treatment of urinary incontinence. The above can be produced using generally used methods and processed to give medicaments. 

Guanidine derivatives and their use as neuropeptide FF receptor antagonists

The invention relates to the guanine derivatives of general formula (I), and to hydrates or solvents thereof, for use as neuropeptide FF receptor antagonists in the treatment of pains and hyperalgesia, of withdrawal symptoms of addiction to alcohol, psychotropic drugs or nicotine and in the prevention of or recovery from these addictions, for the regulation of insulin release, food intake, memory functions, blood pressure, electrolyte and energy metabolism, and in the treatment of urinary incontinence 

Guanidine derivatives

Quinoline and quinazoline derivatives can be used in the form of pharmaceutical preparations as Neuropeptide Y antagonists for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.

Neuropeptide Y antagonists

Pyrrolidone carboxamides of formula (I) where R=a group of formula (a) or (b), R=phenyl, heteroalkyl, aryloxy, alkoxy, alkanoyl or &#x2014;NRRand R, X, R, R, Rand Rhave the meanings given in the description and the claims, pharmaceutically applicable acid addition salts with basic compounds of formula (I), pharmaceutically applicable salts of acid compounds of formula (I) with bases, pharmaceutically applicable esters of hydroxy- or carboxy-group containing compounds of formula (I) and hydrates and solvates thereof, inhibit the interaction of neuropeptide Y (NPY) with one of the neuropeptide receptor subtypes (NPY-Y5) and are particularly suitable for the prevention and treatment of arthritis, diabetes and especially eating disorders and obesity. The above can be produced by known methods and converted into a galenic dosage form.

Pyrrolidone carboxamides

Piperidine derivatives, their manufacture and use as medicaments is described. The compounds are useful for treating diseases associated with restenosis, glaucoma, cardiac infarct, high blood pressure and end organ damage, e.g. cardiac insufficiency and kidney insufficiency.

Naphthalenyl piperidines as renin inhibitors

Pyrimidine derivatives have been found to be useful as neuropeptide Y receptor ligands and particularly as antagonists. These pyrimidine derivatives may be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, diabetes, eating disorders, and obesity.

Pyrimidine derivatives

Heterocyclic sulfonamides

Naphthalenylmethoxypiperidines as renin inhibitors

Heterocyclic sulfamides

Piperidine derivatives

Piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the piperidine derivatives of general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Z, m and n are as described herein.

Piperidine derivative having renin inhibiting activity

Compounds of formula I ##STR1## wherein R.sup.1 signifies phenyl, substituted phenyl or heterocyclyl;

Aryl-  and hetaryl-sulfonamide derivatives, their preparation and their

Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Z, m and n are as described herein.

Piperidine derivatives having renin inhibiting activity

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Schliengen, Germany

Volker Breu