Use of a compound of depsipeptide derivative dolastina - 15 (Dov nmeval Val Pro Pro Hiva - dpy) for the preparation of a Pharmaceutical composition for the treatment of rheumatoid arthritis in a MamiferOr

摘要

Use of a compound derived depsipeptide Dolastatin 15 (Dov nmeval Val Pro Pro Hiva - dpy) of formula (i) r1r2n CHX - CO - A - B - D - S - (e) (f) (g) - T - u K where: R1 is alkyl cycloalkyl, c1-3;As ciclopropilo; alquilsulfonilo c1-3; fluoroalquilo, as fluoroetilo, difluoretilo, fluoroisopropilo, aminosulfonilo which can be replaced by alkyl,As Methyl alkyl; R2 is Hydrogen, C1 - 3; fluoroalquilo, as fluoroetilo, difluoroetilo, cycloalkyl, fluorisopropilo;Such comociclopropilo; R1 - R2 together can be a Waste pirrolidino or piperidino; is a valilo, isoleucilo, leucilo, isoleucilo - 2.2 - dimetilglicilo, 2 - ciclopropilglicilo,Ciclopentilglicilo 2 -, 3 - butilalanilo ter ter butilglicilo -, 2 -, 3 - cicloexilalanilo2 etilglicilo ciclohexilglicilo -, 2 -, or norvalilo norleucilo residue; b is an n - alkyl - norvalilo - leucilo valilo,,,- isoleucilo - ter - butilglicilo, - 2, - 3 - ter - etilglicilo butilalanilo, - 2, - 2 - ciclopropilglicilo,Norleucilo or residue - 2 - N - alkyl is preferably ciclohexilglicilodonde N - or N - Methyl ethyl propyl; D and E, homoprolilo, hidroxiprolilo, 3,4 - deshidroprolilo fluoroprolilo 3 -, 4 -, metilprolilo,Metilprolilo 4 -, 5 - metilprolilo azetidin - 2 -, carbonyl - dimetilprolilo, 3.3, 4.4 - difluoroprolilo,Oxalidin carbonyl or tiazolidin residue - 4 - 4 - carbonyl; F and G are selected from the group consisting of prolilo Regardless, homoprolilo, hidroxiprolilo,Tiazolidinil - 4 - 1 - - - carbonilo1 aminopentil carbonyl, valilo butilglicilo ter -, 2 -, 3 - isoleucilo, leucilo, ciclohexilalanilo, fenilalanilo, N - metilfenilalanilo, tetrahidroisoquinolil - 2 - histidilo,1 - aminoindil carbonyl - 1 - 2 -, 3 - piridilalanilo, ciclohexilglicilo, norleucilo, norvalilo, neopentilglicilo, tritofanilo, glicilo, 2.2 - dimetilglicilalanilo,3 - beta - alanilo and waste naftilalanilo; X is (such as Hydrogen, alkyl, cycloalkyl c1-5) (such as C3 - 7), - CH2 - cyclohexyl or arylalkyl (such