Actelion Pharmaceuticals Ltd

Grunenthal Gmbh

Thomas Giller

Kurt Hilpert

Volker Breu

Heinz Fretz

Anja Fecher

Matthias Steger

Oliver Valdenaire

Eva Caroff

Olivier Valdenaire

Markus Isler

Günter Schwalm

Andreas Bernkop-SCHNÜRCH

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

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

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Wintersingen, Switzerland

Thomas Giller