发明名称 PAIN RELIEF COMPOUNDS
摘要 The present invention relates to the use of compounds for the treatment or prevention of pain in mammals, in particularly in human beings, and also to a process for preparing these compounds.
申请公布号 US2015274633(A2) 申请公布日期 2015.10.01
申请号 US201214369674 申请日期 2012.12.31
申请人 ECOLE NATIONALE SUPERIEURE DE CHIMIE DE CLERMONT FERRAND ;UNIVERSITE D AUVERGNE CLERMONT I 发明人 DUCKI Sylvie;BENNIS Khalil;ESCHALIER Alain;BUSSEROLLES Jerome;LESAGE Florian;RODRIGUES Nuno;VIVIER Delphine
分类号 C07C57/60;C07F9/09;C07D209/42;C07C229/34;C07C255/41;C07D307/54 主分类号 C07C57/60
代理机构 代理人
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.
地址 AUBIERECEDEX FR