Actelion Pharmaceuticals Ltd

Matthias Steger

Kurt Hilpert

Volker Breu

Heinz Fretz

Thomas Giller

Oliver Valdenaire

Markus Gude

Eva Caroff

Julien Pothier

Anja Fecher

Markus Riederer

Markus Isler

Günter Schwalm

The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent 'chemoattractant receptor-homologous molecule expressed on Th2 cells' antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.

2-sulfanyl-benzoimidazol-1-yi-acetic acid derivatives as CRTH2 antagonists

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

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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Zurich, Switzerland

Matthias Steger