主权项 |
1. A compound of formula (A): wherein:
R represents:
a saturated, partially or totally unsaturated, aromatic or non-aromatic, substituted or non-substituted, 5-, 6- or 7-membered carbocycle;a saturated, partially or totally unsaturated, aromatic or non-aromatic, substituted or non-substituted, 5-, 6- or 7-membered heterocycle;a saturated, partially or totally unsaturated, aromatic or non-aromatic, substituted or non-substituted, 9-, 10-, 11-, 12-, 13- or 14-membered condensed carbocycle;a saturated, partially or totally unsaturated, aromatic or non-aromatic, substituted or non-substituted, 9-, 10-, 11-, 12-, 13- or 14-membered condensed heterocycle;Q represents a hydrogen atom, a halogen, a C1-C6 alkyl group, a C1-C6 alkyl-amine group, a —CN, —NR1R2, —C(O)OR1, a —NR3C(O)OR4 group;Q, R and the carbon atoms to which they are bounded, form a saturated, partially or totally unsaturated, aromatic or non-aromatic, substituted or non-substituted, carbocycle, heterocycle, 5-, 6-, 7-, 8-, 9-, 10-, 11-, 12-, 13- or 14-membered condensed carbocycle or, 5-, 6-, 7-, 8-, 9-, 10-, 11-, 12-, 13- or 14-membered condensed heterocycle;X represents O, —CH2, S, NR1;E, identical or different, represents a group —CHG1;n represents 0, 1, 2 or 3;T represents:
a hydrogen atom;a substituted or non-substituted, branched or non-branched C1-C12 alkyl group;a group of formula -(L)m−P(O)(OT1)2 wherein:
L, identical or different, represents a group —CHG2, O;m represents 0, 1, 2 or 3;T1 represents an hydrogen atom, a C1-C6 alkyl group, a benzyl;a residue of an amino acid linked to its N-terminal position;an aryl group;a C1-C6 alkyl-aryl group;a C1-C6 alkyl-heterocycle group;a C2-C6 alkenyl-aryl group;a C2-C6 alkenyl-heterocycle group;a C2-C6 alkynyl-aryl group;a C2-C6 alkynyl-heterocycle group;a saturated or partially unsaturated, non-aromatic, substituted or non-substituted, 5- or 6-membered carbocycle;a saturated, partially or totally unsaturated, aromatic or non-aromatic, substituted or non-substituted, 5- or 6-membered heterocycle;a saturated, partially or totally unsaturated, aromatic or non-aromatic, substituted or non-substituted, 8-, 9- or 10-membered condensed heterocycle;R1 represents a hydrogen atom, a C1-C6 alkyl group;R2 represents a hydrogen atom, a C1-C6 alkyl group, —OH;R3 represents a hydrogen atom, a C1-C6 alkyl group;R4 represents a hydrogen atom, a C1-C6 alkyl group, a C1-C6 alkyl-aryl group;G1 represents a hydrogen atom, a C1-C6 alkyl group, —OH, a group of formula -(L1)q−P(O)(OR7)2 wherein:
L1, identical or different, represents O, S, CHR8, —NR8; q represents 0, 1, 2, 3, 4, 5 or 6;R7 and R8 independently represent a hydrogen atom or a C1-C6 alkyl group, a benzyl;G2 represents a hydrogen atom, a C1-C6 alkyl group, —OH, a benzyl; as well as an isomer or a pharmaceutically acceptable salt of this compound, for the use for the treatment and/or the prevention of pain excluding i) cinnamyl 3-4-dihydroxy-α-cyanocinnamate (CDC), ii) ethyl 3-4-dihydroxy-α-cyanocinnamate (EDHBCA), iii) 2-ethylthiophenyl 3-4-dihydroxy-α-cyanocinnamate (TEDHBCA), iv) N-(3′-phenylpropyl)-3,4-dihydroxybenzylidenecyanoacetamide (Tyrphostin B46), v) 1-carboxy-1-cyano-2(3,4-dihydroxyphenyl)ethylene, vi) 1-carboxy-1-cyano-2-phenylethylene, vii) 1-carboxy-1-carboxy-2(4-hydroxyphenyl)ethylene, viii) 1-carboxy-1-cyano-2(3,4-dihydroxyphenyl)ethylene, ix) 1-carboxy-1-cyano-2(4,5-dihydroxyphenyl)ethylene, x) 1-carboxy-1-cyano-2(4-methoxyphenyl)ethylene, xi) 1-carboxy-1-cyano-2(4-fluorophenyl)ethylene, xii) 1-carboxy-1-cyano-2(4-chlorophenyl)ethylene, xiii) 1-carboxy-1-cyano-2(4-hydroxy-3,5-methoxyphenyl)ethylene, xiv) 1-carboxy-1-cyano-2(4-hydroxyphenyl)ethylene, xv) 1-carboxy-1-cyano-2(4-formylphenyl)ethylene xvi) 1-carboxy-2(4-hydroxyphenyl)ethylene, xvii) compound of formula xviii) compound of formula xix) compound of formula xx) 2-ethoxybenzene 3-4-dihydroxy-α-cinnamate (CAPE), xxi) 3-(3,4-dihydroxyphenyl)-2-propenoic acid, xxii) methyl 3-(3,4-dihydroxyphenyl)-2-propenoate, xxiii) ethyl 3-(3,4-dihydroxyphenyl)-2-propenoate, xxiv) lauryl 3-(3,4-dihydroxyphenyl)-2-propenoate, xxv) tert-butyl 3-(3,4-dihydroxyphenyl)-2-propenoate, xxvi) iso-pentyl 3-(3,4-dihydroxyphenyl)-2-propenoate, xxvii) butyl 3-(3,4-dihydroxyphenyl)-2-propenoate, xxviii) octanyl3-(3,4-dihydroxyphenyl)-2-propenoate, xxix) iso-propyl 3-(3,4-dihydroxyphenyl)-2-propenoate, xxx) iso-butyl 3-(3,4-dihydroxyphenyl)-2-propenoate, xxxi) benzyl 3-(3,4-dihydroxyphenyl)-2-propenoate, xxxii) phenethyl3-(3,4-dihydroxyphenyl)-2-propenoate. |