Anti-obesity 1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles
AssigneesHoffmann-La Roche Inc., Vernalis Research Limited
InventorsJonathan Mark Bentley, Paul Hebeisen, Patrizio Mattei, Marc Muller, Hans Richter, Stephan Roever, Sven Taylor
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Abstract
The present invention is directed to 1,2,3,4,10,10a,-hexahydropyrazino[1,2-a]indole derivatives as well as pharmaceutically acceptable salts, solvates and esters thereof, wherein R1 to R8 have the significance given in claim 1 be used in the form of pharmaceutical preparations for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes insipidus, obesity and sleep apnea.
Claims8
A compound of formula I-C:
- wherein
- R12, R13 and R14 are independently hydrogen, halogen, trifluoromethyl, lower alkyl, lower alkoxy lower alkyl, lower alkoxy lower alkoxy lower alkyl, halo lower alkoxy, lower alkyl aminocarbonyl or di-lower alkyl aminocarbonyl, cyano;
- R26 is (CH2)n—Y, hydroxy lower alkyl, lower alkoxycarbonyl lower alkyl or carbamoyl lower alkyl;
- R27 is hydrogen or lower alkyl;
- Y is oxazolidinone, cyclobutanonyl, [1,2,4]triazol-3-yl, [1,2,4]oxadiazol-3-yl, [1,2,4]triazol-3-one-5-yl, tetrazolyl, [1,3,4]oxadiazol-2-yl, [1,3,4]thiadiazol-2-yl, 1H-imidazol-2-yl or 1H-imidazol-4-yl;
- and
- n is 0, 1, 2 or 3.
Dependencies are inferred from the claim text.