Somatostatin analogues

Claim 2

A compound of the formula: ##STR4## its linear precursor intermediates or non-toxic acid addition salts thereof in which X 2 is H, NH 2 , Ala--Gly--, Ala--D--Ala, Gly--Gly--Gly--, lower alkanoyl or benzoyl; X 4 is Arg, His or Lys; X 5 is His, Tyr or Glu; X 8 is Trp or D--Trp; X 10 is Val, α--Abu, Leu, Phe or Tyr; and X 14 is Cys, D--Cys or --NH(CH 2 ) 2 --S--.

Claim 3

The compound of claim 1 in which X 10 is Val, α-Abu or Leu.

Claim 4

The compound of claim 1 which is [des--Ala 1 --Gly 2 , Arg 4 , His 5 , D-Trp 8 , Val 10 ]somatostatin.

Claim 5

The compound of claim 1 which is [des--Ala 1 --Gly 2 , Arg 4 , Glu 5 , D-Trp 8 , α-Abu 10 ]somatostatin.

Claim 6

A compound of Claim 1 of the formula: ##STR5## in which R is hydrogen, an α-amino protecting group, lower alkanoyl or benzoyl; R 1 and R 8 are hydrogen or a thio protecting group; R 2 is hydrogen or a protecting group for N g of Arg, N im of His or the amino group of Lys; R 3 is hydrogen or a protecting group for N im of His or the hydroxyl group of Tyr; R 4 is hydrogen or an amino protecting group; R 5 is hydrogen or a hydroxyl protecting group for Tyr; R 6 and R 7 are hydrogen or a hydroxyl protecting group for Thr and Ser; where Y 2 is Ala--Gly--, Ala--D--Ala--or Gly--Gly--Gly--; n is 0 or 1; X 4 is Arg, His or Lys; X 5 is His, Tyr or Glu; X 8 is Trp or D-Trp; X 10 is Val, α-Abu, Leu, Phe or Tyr; Y 14 is Cys or D-Cys; p is 0 or 1 and Z is --OH or --O--CH 2 --[polystyrene resin support] with the proviso that R--R 7 are hydrogen when Z is --OH and R 1 -R 7 are other than hydrogen when Z is --O--CH 2 --[polystyrene resin support].

Claim 7

The compound of claim 1 which is tert-Butyloxycarbonyl-S-p-methoxybenzyl-L-cysteinyl-N g -toxyl-L-arginyl-N im -tosyl-L-histidyl-L-phenylalanyl-L-phenylalanyl-D-tryptophyl-N.sup..epsilon. -2-chlorobenzyloxycarbonyl-L-lysyl-L-valyl-O-benzyl-L-threonyl-O-benzyl-L-seryl-S-p-methoxybenzyl-L-cysteinyl hydroxymethyl polystyrene ester.

Claim 8

The compound of claim 1 which is tert-Butyloxycarbonyl-S-p-methoxybenzyl-L-cysteinyl-N g -tosyl-L-arginyl-Υ-benzyloxy-L-glutamyl-L-phenylalanyl-L-phenylalanyl-D-tryptophyl-N.sup.ε -2-chlorobenzyloxycarbonyl-L-lysyl-L-ε-aminobutyryl-L-phenylalanyl-O-benzyl-L-threonyl-O-benzyl-L-seryl-S-p-methoxybenzyl-L-cysteinyl hydroxymethyl polystyrene ester.