摘要 |
PCT No. PCT/GB94/02558 Sec. 371 Date May 14, 1996 Sec. 102(e) Date May 14, 1996 PCT Filed Nov. 21, 1994 PCT Pub. No. WO95/14672 PCT Pub. Date Jun. 1, 1995A class of substituted isoxazole and pyrazole derivatives of formula (I), or a salt thereof of or a prodrug thereof, wherein the broken circle represents two non-adjacent double bonds whereby the five-membered ring containing X and Y is aromatic; one of X and Y represents nitrogen, and the other of X and Y represents oxygen or N-R5; R1 represents hydrogen, C1-6 alkyl or trifluoromethyl; R2 and R3 independently represent hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, -ORa, -SRa, -SORa, -SO2Ra, -SO2NRaRb, -NRaRa, -NRaCO2Rb, -CORa, -CO2Ra or -CONRaRb, R4 represents hydrocarbon or a heterocyclic group; R5 represents hydrogen or C1-6 alkyl; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group, are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia. <IMAGE> (I)
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申请人 |
MERCK, SHARP & DOHME, LTD. |
发明人 |
BOURRAIN, SYLVIE;NEDUVELIL, JOSEPH GEORGE;LEESON, PAUL DAVID;SHOWELL, GRAHAM ANDREW |