Indoletetralins having dopaminergic activity

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/60 (2006.01) A61K 31/335 (2006.01) A61K 31/40 (2006.01) C07D 209/58 (2006.01) C07D 307/92 (2006.01) C07D 307/93 (2006.01) C07D 409/12 (2006.01) C07D 491/04 (2006.01) C07D 491/052 (2006.01) C07D 493/04 (2006.01)

Patent

CA 2157586

A compound of formula (I) and pharmaceutically acceptable salts thereof, where Z is R3 and X and Y form (a), or X is R3 and Y and Z form (a), (b) or (c); R1 and R2 are independently hydrogen, C1-6 alkyl, C3-7 cycloalkyl, -CH2-C3-7 cycloalkyl, phenyl (option-ally substituted with halogen or C1-6 alkyl), -thiophenyl (option-ally substituted with halogen or C1-6 alkyl), or C1-6 alkyl phenyl; R3 are independently hydrogen, halogen, -O-C1-6 alkyl or C1-6 alkyl; R4 is a valence bond, CH2 or oxygen; R5 and R6 are independently hydrogen, sulfur, -S--C1-6 alkyl, halogen, CON(R3)2, -COCF3, -COC1-6 alkyl, -CO phenyl, oxygen, -CHO, CN except that when Y and Z form (b), R1 and R2 are hydrogen or a C1-6 alkyl and R3 is hydrogen, then at least one of R5 and R6 must be other than hydrogen. These compounds and derivatives thereof exhibit dopamine-receptor stimulating activ-ity in mammals which are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders which respond to dopamine-receptor stimulation.

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