Derivatives of benzoylecgonine, ecgonine and ecgonidine as...

C - Chemistry – Metallurgy – 07 – D

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C07D 451/06 (2006.01) A61K 31/395 (2006.01) C07D 451/02 (2006.01) C07D 451/12 (2006.01)

Patent

CA 2151618

A compound of formula (I), formula (II) or formula (III), wherein R1 is selected from the group consisting of H; branched or unbranched alkyl, alkenyl and alkynyl, said alkyl, alkenyl and alkynyl being optionally substituted with OH, SH, NH2 or halogen; COCH3; COPh; and COBn; R2 is selected from the group consisting of branched or unbranched alkyl, alkeayl and alkynyl, said alkyl, alkenyl and alkynyl being optionally substituted with OH, SH, NH2 or halogen; aryl; Het; and benzyl; R3 is selected from the group consisting of branched or unbranched alkyl, alkenyl and alkynyl, said alkyl, alkenyl and alkynyl being optionally substituted with OH, SH, NH2 or halogen; R4 is selected from the group consisting of H; and branched or unbranched alkyl, alkenyl and alkynyl, said alkyl, alkenyl and alkynyl being optionally substituted with OH, SH, NH2 or halogen; and X is selected from the group consisting of OH; SH; NH2; and halogen: which are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain.

Composé de formule (I), (II) ou (III), R1 étant choisi dans le groupe comprenant H, alkyle, alcényle et alcynyle, ramifiés ou droits, lesdits alkyle, alcényle et alcynyle étant éventuellement à substitution OH, SH, NH2 ou halogène; COCH3; COPh et COBn; R2 étant choisi dans le groupe comprenant alkyle, alcényle et alcynyle ramifiés ou droits, lesdits alkyle, alcényle et alcynyle étant éventuellement à substitution OH, SH, NH2 ou halogène; aryle; Het et benzyle; R3 étant choisi dans le groupe comprenant alkyle, alcényle et alcynyle ramifiés ou droits, lesdits alkyle, alcényle et alcynyle étant éventuellement à substitution OH, SH, N2 ou halogène; R4 étant choisi dans le groupe comprenant H; alkyle, alcényle et alcynyle ramifiés ou droits, lesdits alkyle, alcényle et alcynyle étant éventuellement à substituion OH, SH, NH2 ou halogène; et X étant choisi dans le groupe comprenant OH, SH, NH2, halogène. Lesdits composés sont utiles pour atténuer les symptômes des troubles des immunorégulateurs, des troubles neuromusculaires, des troubles articulaires, des troubles des tissus conjonctifs, des troubles circulatoires et de la douleur.

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