Patent ID: 6716854
Filing Date: 2004-04-06
Classification: A61K,A61P

Abstract:
A method for treating restless legs syndrome in a patient suffering therefrom, comprising administration of an effective amount of a compound of formula II or a pharmaceutically acceptable salt thereof, wherein:n is 0-3; R1 and R2 are independently H (provided only one is H at the same time), â€”OH (provided R4 is other than hydrogen), CN, CH2CN, 2- or 4-CF3, CH2CF3, CH2CHF2, CH&boxH;CF2, (CH2)2CF3, ethenyl, 2-propenyl, OSO2CH3, OSO2CF3, SSO2CF3, COR4, COOR4, CON(R4)2, SOxCH3 (where, x is 0-2), SOxCF3, O(CH2)xCF3, SO2N(R4)2, CH&boxH;NOR4, COCOOR4, COCOON(R4)2, C1-8 alkyls, C3-8 cycloalkyls, CH2OR4, CH2(R4)2, NR4SO2CF3, NO2, halogen, a phenyl at positions 2, 3 or 4, thienyl, furyl, pyrrole, oxazole, thiazole, N-pyrroline, triazole, tetrazole or pyridine; R3 is hydrogen, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, â€”(CH2)mâ€”R5 (where m is 1-8), CH2SCH3 or a C4-C8 alkyl bonded to said nitrogen and one of its adjacent carbon atoms inclusive to form a cyclic structure; R4 is independently hydrogen, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl, 3,3,3-trifluoropropyl, 4,4,4-trifluorobutyl, â€”(CH2)mâ€”R5 where m is 1-8; R5 is phenyl, phenyl (substituted with a CN, CF3, CH2CF3, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkyl-methyl, C2-C8 alkenyl, C2-C8 alkynyl), 2-thiophenyl, 3-thiophenyl, â€”NR6CONR6R7, or â€”CONR6R7; R6 and R7 are independently hydrogen, C1-C8 alkyl, C3-C8 cycloalkyl, C4-C9 cycloalkylmethyl, C2-C8 alkenyl or C2-C8 alkynyl; and with the proviso that when R1 is 2-CN or 4-CN, R2 is H, R3 is n-Pr and n is 1 or 3 then such compound is a pure enantiomer.