- Synthesis and biological evaluation of novel hexahydro-pyrido[3′, 2′:4,5]pyrrolo[1,2-a]pyrazines as potent and selective 5-HT2C receptor agonists
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Further lead optimization efforts on previously described 1,2,3,4,10,10a-hexahydro-1H-pyrazino[1,2-a]indoles led to the new class of 5,5a,6,7,8,9-hexahydro-pyrido[3′,2′:4,5]pyrrolo[1,2-a]pyrazines culminating in the discovery of (5aR,9R)-2-[(cyclopropylmethoxy)methyl]-5,5a,6, 7,8,9-hexahydro-9-methyl-pyrido[3′, 2′:4,5]pyrrolo[1,2-a]pyrazine 18 as a potent, full 5-HT2C receptor agonist with an outstanding selectivity profile and excellent hERG and phospholipidosis properties.
- Richter, Hans G. F.,Adams,Benardeau,Bickerdike,Bentley,Blench,Cliffe,Dourish,Hebeisen,Kennett,Knight,Malcolm,Mattei,Misra,Mizrahi,Monck,Plancher,Roever,Roffey,Taylor,Vickers
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p. 1207 - 1211
(2007/10/03)
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- 5HT2C RECEPTOR AGONISTS FOR THE TREATMENT OF DIABETES AND OBESITY
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The present invention refers to chemical compounds of formula (I), as well as pharmaceutically acceptable salts, esters and produgs thereof, wherein R1 to R5 have the significance given in claim 1. They can be used for the preparation of medicaments.
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Page/Page column 62
(2010/02/10)
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- Piperazine derivatives
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The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.
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