Vanilloid receptor ligands, pharmaceutical compositions containing them, process for making them, and use thereof for treating pain and other conditions

摘要

Vanilloid receptor ligand compounds corresponding to formula I:;
a process for producing such compounds, pharmaceutical compositions containing them, and the use of such compounds to treat pain and various other vanilloid receptor mediated conditions.

主权项

1. A compound corresponding to formula I: wherein n is 1 or 2; R1 represents H; F; Cl; Br; I; methyl; ethyl; —NO2; —NH2; —OH; —NH —C(═O)—R13; —OR16; —SR17; —S(═O)2—NR22R23; or —S(═O)2 —R27; R2 represents H; F; Cl; Br; I; methyl; ethyl; —NO2; —NH2; —OH; —NH—C(═O)—R13; —OR16; —SR17; —S(═O)2—NR22R23 or —S(═O)2—R27; R3 represents H; F; Cl; Br; I; methyl; ethyl; —NO2; —NH2; —OH; —NH —C(═O)—R13; —OR16; —SR17; —S(═O)2—NR22R23 or —S(═O)2 —R27; R4 represents H; F; Cl; Br; I; methyl; ethyl; —NO2; —NH2; —OH; —NH —C(═O)—R13; —OR16; —SR17; —S(═O)2—NR22R23 or —S(═O)2 —R27; R5 represents H; F; Cl; Br; I; methyl; ethyl; —NO2; —NH2; —OH; —NH —C(═O)—R13; —OR16; —SR17; —S(═O)2—NR22R23 or —S(═O)2 —R27; R6 represents hydrogen or an alkyl group selected from the group consisting of isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl, and n-propyl; R7 represents hydrogen or —OH; R8 represents —SF5; —O—CF3; tert-butyl or —C(CH3)2(CH2OH); T stands for C—R35; U stands for C—R36; V stands for C—R37, and W stands for C—R38; R13, R16, R17, R22, R23, and R27 each independently represent a group selected from the group consisting of methyl, ethyl, and n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, and ethenyl; R35, R36, and R37 each represent H; R38 represents NHR39, wherein R39 represents methyl, ethyl, and n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, or (3,3)- dimethylbutyl; —NR40R41, wherein R40 and R41 together with the nitrogen atom to which they are bound form a group selected from the group consisting of pyrrolidinyl, piperdinyl, and moropholinyl, wherein the heterocycloaliphatic moiety may be unsubstituted or substtitued by 1, 2, 3, 4, or 5 groups R57; —OR42, wherein R42 represents methyl, ethyl, n-propyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-hexyl, (3,3)-dimethylbutyl, cycopentyl, or cyclohexyl; or —SR43, wherein R43 represents cyclohexyl; R57 represents an alkyl group selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, and isobutyl; or a salt thereof.