C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/14 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) C07D 209/04 (2006.01) C07D 209/08 (2006.01) C07D 209/10 (2006.01) C07D 231/56 (2006.01) C07D 401/04 (2006.01) C07D 403/14 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01)
Patent
CA 2048027
3-Arylindole or 3-arylindazole derivatives having formula (see formula I) wherein Ar is optionally substituted phenyl or a heteroaromatic group; R1-R4 are independently selected from hydrogen, halogen, alkyl, alkoxy, hydroxy, nitro, alkylthio, alkylsulphonyl, alkyl- or dialkylamino, cyano, trifluoromethyl, or trifluoromethylthio; the dotted lines designate optional bonds; X is N or a group CR6 wherein R6 is hydrogen, halogen, trifluoromethyl or alkyl, or X is CH2; Y is N or CH, or Y is C; R5 is hydrogen, cycloalkyl, cycloalkylmethyl, alkyl or alkenyl, optionally substituted with one or two hydroxy groups, or R5 is a group taken from structures 1a and 1b: (see formula 1a, 1b) wherein n is an integer from 2 - 6; W is O or S; U is N or CH ; Z is -(CH2)m-, m being 2 or 3 , -CH=CH-, 1,2-phenylene or -COCH2- or -CSCH2-; V is O, S, CH2, or NR7; U1 is O, S, CH2 or NR8; and V1 is NR9R10, OR11, SR12 or CR13R14R15, and R7- R15 are independently hydrogen, alkyl, alkenyl, cycloalkyl or cycloalkylalkyl; may be prepared by methods known per se. The compounds are selective centrally acting 5-HT2-antagonists in the brain and are useful in treatment of anxiety, agression, depression, sleep disturbances, migraine, negative symptoms of schizophrenia, drug-induces Parkinsonism and Parkinson's disease.
Andersen Kim
Perregaard Jens Kristian
H. Lundbeck A/s
Robic
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