Ecteinascidin compounds as anti -inflammatory agents

Details Ecteinascidin compounds as anti -inflammatory agents Ecteinascidin compounds as anti -inflammatory agents

A - Human Necessities

61

K

A61K 31/4995 (2006.01) A61P 29/00 (2006.01)

Patent

CA 2583464

We have found anti-inflammatory activity in the ecteinascidin compounds. Such compounds have been widely described, and may have the following general formula (I), wherein: R5 is OH, alkoxy or alkanoyloxy; R6 is hydrogen, alkyl, alkenyl, alkynyl or aryl; R12 is hydrogen, alkyl, alkenyl, alkynyl or aryl; R16 is hydrogen, alkyl, alkenyl, alkynyl or aryl; R17 is OH, alkoxy or alkanoyloxy; R18 is OH, alkoxy or alkanoyloxy; R21 is H, OH, CN or another nucleophilic group; and Ra is hydrogen and Rb is optionally substituted amino, or Ra with Rb form a carbonyl function =O, or Ra, Rb and the carbon to which they are attached form a tetrahydroisoquinoline group.

L'invention concerne la découverte d'une activité anti-inflammatoire dans les composés d'ecteinascidine. De tels composés ont été largement décrits et peuvent être de formule générale suivante (I), dans laquelle: R5 représente OH, alcoxy ou alkanoyloxy; R6 désigne hydrogène, alkyle, alcényle, alkynyl ou aryle; R12 représente hydrogène, alkyle, alcényle, alkynyl ou aryle; R16 désigne hydrogène, alkyle, alcényle, alkynyl ou aryle; R17 représente OH, alcoxy ou alkanoyloxy; R18 désigne OH, alcoxy ou alkanoyloxy; R21 représente H, OH, CN ou un autre groupe nucléophile; et Ra représente hydrogène et Rb désigne un élément amino éventuellement substitué ou Ra avec Rb forment une fonction carbonyle =O ou Ra, Rb et le carbone sur lequel ils sont fixés forment un groupe tétrahydroisoquinoline.

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