AGONISTS AND ANTAGONISTS OF 5-HT2C RECEPTORS

摘要

The invention relates to compounds of general formula (Ib) wherein: X1 is -O-, -S- or -N(R27)-; Y1 is -O-, -S- or -N(R27)- or -CH2 ; Ra C3-8 cycloalkyl, monocyclic or bicyclic aryl having from 6 to 10 carbon atoms in ring(s), wherein only one ring is aromatic, and one or several atoms in ring(s) are other than carbon and selected from nitrogen, sulfur, oxygen, and selenium, wherein each of said cycloalkyl, aryl and heteroaryl may be optionally substituted in one or several positions; R20 and R21 independently of each other are hydrogen, halogen or C1-4-alkyl; or wherein R20 and R21 together with the carbon atoms to which they are bound form benzene to form a quinoxaline ring or thiophene to form a thieno[3,4-b]pyrazine ring, optionally mono- or disubstituted by halogen; R22 is hydrogen, hydroxy, C1-4-alkyl or C1-4-alkoxycarbonyl; R23 and R24 independently of each other are hydrogen, C1-4-alkyl; R25 is hydrogen or C1-4-alkyl; R26 is hydrogen, C1-4-alkyl or is linked to a carbon atom in Ra adjacent to the atom binding to Y1 to form a 5- or 6-membered ring which may contain 0, 1 or 2 heteroatoms, wherein said ring is optionally substituted with methyl; R27 is hydrogen or C1-4-alkyl, preferably methyl or ethyl; and y and z independently of each other are 1 or 2, and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods. The proposed new compounds are bound with 5-HT2C receptors as agonists and antagonists and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders.