Antiinflammatory compsn. contg. tryptophan di:peptide - useful in human or veterinary medicine

摘要

Antiinflammatory compsns. contain >=1 cpd. of formula R1-Trp(X)-YR2 (I) or its acid or base salts. R1 = H, 1-4C alkanoyl, is not >10 C aralkanoyl, aroyl, tert, butoxycarbonyl (BOC), 1,7,7-trimethylbicyclo 2,2,1 heptan-2-yloxycarbonyl (IbOC) or 2-nitrophenylthio (NPS): X is H or formyl attached to the indole N atom of Trp. Y = Gly, aminolaevulinoyl, Leu, Val, Ala, sarcosyl or azaglycryl. R2 = lower alkoxy, (OH, NH, (opt. substd by or 2 lower alkyl) glucosamino, pyridylamino or piperazino). The following (I) are new cpds. N-Boc-Trp(H)-Z(Z= Leu, D, L-alpha-aminolaevulinic acid (or its methyl ester), glycinamide, Leu-methyl ester, sarcosine methyl ester, alanine methyl ester, glycine methyl ester (with Trp in D, L-form), glycine-4-methylpiperazide, glycine-3-pyridylamide glycine-4-benzylpiperazide or glycine-4-diphenylmethylpiperazide); Trp-D,L-alpha-aminolaevulinic acid; N-R1'-Trp-glycine methyl ester (R11=IBOC, NPS of trifluoroacetyl); N-BOC-1-formyl- or N, 1 diforml Trp-glycine-methyl ester (all amino acid and have L-configuration unless stated (otherwise). (I) do not have the side-effects of known antiinflammatories such as indomethacin. They are formulated conventionally for use of human or veterinary medicine pref. for a daily dose of 0.3-6 mg/kg per day, esp. in units of 0.1-1 mg/kg.