Serotonin 5ht1a agonists

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/04 (2006.01) A61K 31/335 (2006.01) A61K 31/40 (2006.01) C07D 209/14 (2006.01) C07D 209/46 (2006.01) C07D 319/20 (2006.01)

Patent

CA 2049803

ABSTRACT The present invention is directed to a new class of compounds of the formula: Image in which B is represented a C1-4 alkylene bridging group, Alk is represented by a linear alkylene bridging group con- taining from 2-8 carbon atoms which may optionally be mono- substituted at one carbon atom with a C1-4 alkyl, phenyl, substituted phenyl, or alkylphenyl substituent in which the phenyl ring may be optionally substituted; D is represented by a bond or an ethenylene bridging group; X, Y and Z are each independently represented by hydrogen, C1-4 alkyl, phenyl, substituted phenyl or alkylphenyl in which the phenyl ring may be optionally substituted; R1 is represented by a substituent selected from the group consisting of hyd- rogen, halogen, C1-4 alkyl, C1-5 alkoxy, CF3, OCF3, OH, NO2, CN, -NR2R3, -CONR2R3, -COOR4, -CH2SO2NR2R3, -SO2NR2R3, and -OCH2COOR4; R2 and R3 are each independently represented by H or a C1-4 alkyl; R4 is represented by H, C1-4 alkyl, phenyl, substituted phenyl or an alkylphenyl substituent in which the phenyl ring may be optionally substituted; Het is represented by one of the following substituents: Image or Image which are serotonin 5HT1A and 5HTlD agonists and may be used in the treatment of anxiety, depression, migraine, stroke and hypertension as well as pharmaceutical and diagnostic compositions containing them.

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