MODULATOR

摘要

The present disclosure relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein Z is selected from OH, NHCH2CH2F, NHCH(Me)CH2OH and NHCH2CH2OH; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3 and nitro; Y is a polar functional group selected from OH, NO2, CN, COR3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is phenyl or pyridyl; and B is (CH2)n where n is 0; with the proviso that: (i) when A is phenyl, and Z is OH, X—Y is other than C≡C—(CH2)2CO2H, C≡C—(CH2)2CO2Me, (CH2)4CO2H. Uses of such compounds as medicaments for the treatment of a muscular disorder, a gastrointestinal disorder, or for controlling spasticity or tremors are provided.

主权项

1. A compound of formula I, or a pharmaceutically acceptable salt thereof, wherein Z is OR1 or NR1R2 wherein each of R1 and R2 is independently H, or a hydrocarbyl group; X is an alkylene, alkenylene, or alkynylene group, each of which may be optionally substituted by one or more substituents selected from alkyl, COOH, CO2-alkyl, alkenyl, CN, NH2, hydroxy, halo, alkoxy, CF3, and nitro; Y is a polar functional group selected from OH, NO2, CN, COR.3, COOR3, NR3R4, CONR3R4, SO3H, SO2—R3, SO2NR3R4 and CF3, where each of R3 and R4 is independently H or a hydrocarbyl group; A is phenyl or pyridyl; and B is (CH2)n where n is 0; with the proviso that: (i) when A is phenyl, and Z is OH, X—Y is other than C≡C—(CH2)2OH, C≡C—(CH2)2OH, C≡C—(CH2)2CO2Me, (CH2)4CO2H; and (ii) when A is phenyl, and Z is OMe, X—Y is other than C≡C—(CH2)4OH; —(CH2)4—CHO, cis-CH═CH—(CH2)3OH, trans-CH═CH—(CH2)3OH; and wherein the compound is other than 1-(N-octylcarbamoyl)methyl-3-carboxmidopyridinuim chloride, 3-methylcarbamoyl-1-dodecyloxycarbonylmethyl-pyridinium or 6-aminomethylpyridine-2-carboxylic acid ethyl ester.