Somatostatin analogue octa:peptide(s) with enhanced activity - are useful in the redn. of growth hormone, insulin glucagon, or pancreatic exocrine secretion, and have anticancer activity

摘要

Octapeptide analogues of somatostatin of formula (I) and their pharmaceutically acceptable salts, are new. A1 and A2 = H, 1-12C alkyl, 7-10C phenylalkyl, R1CO or R2OCO, provided that when one of A1 or A2 is R1CO or R2OCO, the other must be H; R1 = 1-20C alkyl, 3-20C alkenyl, 3-20C alkynyl, phenyl, naphthyl or 7-10C phenylalkyl; R2 = 1-10C alkyl or 7-10C phenylalkyl; A3 = CH2-A6; A6 = pentafluorophenyl, naphthyl, pyridyl, or phenyl; A4 = o- m- or p-substd. X-Phe, pentafluoro-Phe, or beta-Nal; X = halogen, H, NO2, OH, NH2 or 1-3C alkyl; As = Thr, Ser, Phe, Val, alpha-aminoisobutyric acid, or Ile, provided that when A3 is phenyl, A1 is H and A2 is H, As cannot be Val; and A7 = Thr, Trp or beta-Nal.