Patent ID: 9278146
Filing Date: 2016-03-08
CPC Classification: A61K,C07K

Claim Text:
1. A peptide derivative represented by formula (I) where ExP represents a polypeptide that is represented by an amino acid sequence of formula (1), where Ex4(x-y) represents the amino acid sequence starting at a first residue at position x of SEQ ID NO: 1 and ending at a last residue at position y of SEQ ID NO: 1, x is an integer of 1 to 9, y is an integer of 30 to 39, K represents lysine, and n is 0 or 1, wherein the amino acid at position 1 of SEQ ID NO: 1 is the first residue of SEQ ID NO: 1 and the amino acid at position 30 of SEQ ID NO: 1 is the thirtieth residue of SEQ ID NO: 1; an α-amino group at an N-terminus of the polypeptide ExP is not modified, modified with a modifying group having no electric charge, or bonded to the -L-Z group of formula (I), a carboxylic group at a C-terminus of the polypeptide ExP is amidated, the -L-Z group of formula (I) represents a group represented by formula (II), where when n in the formula (1) is 1, l is 0, 1 or 2, and m is an integer of 1 to 30, when n in the formula (1) is 0, l is an integer of 0 to 8, and m is an integer of 0 to 30, the -L-Z group of formula (I) is bonded to a side group of any lysine residue or the α-amino group at the N-terminus of the polypeptide ExP, Z represents a labeling group comprising a radionuclide or isotope thereof, and the modifying group having no electric charge is selected from the group consisting of 9-fluorenylmethyloxycarbonyl group (Fmoc), tert-butoxycarbonyl group (Boc), benzyloxycarbonyl group (Cbz), 2,2,2-trichloroethoxycarbonyl group (Troc), allyloxycarbonyl group (Alloc), 4-methoxytrityl group (Mmt), amino group, alkyl groups having a carbon number of 3 to 20, 9-fluoreneacetyl group, 1-fluorenecarboxylic acid group, 9-fluorenecarboxylic acid group, 9-fluorenone-1-carboxylic acid group, benzyloxycarbonyl group, xanthyl group (Xan), trityl group (Trt), 4-methyltrityl group (Mtt), 4-methoxy-2,3,6-trimethyl-benzenesulfonyl group (Mtr), mesitylene-2-sulfonyl group (Mts), 4,4-dimethoxybenzohydryl group (Mbh), tosyl group (Tos), 2,2,5,7,8-pentamethylchroman-6-sulfonyl group (Pmc), 4-methylbenzyl group (MeBzl), 4-methoxybenzyl group (MeOBzl), benzyloxy group (BzlO), benzyl group (Bzl), benzoyl group (Bz), 3-nitro-2-pyridinesulfenyl group (Npys), 1-(4,4-dimethyl-2,6-diaxocyclohexylidene)ethyl group (Dde), 2,6-dichlorobenzyl group (2,6-DiCl-Bzl), 2-chlorobenzyloxycarbonyl group, 2-bromobenzyloxycarbonyl group, benzyloxymethyl group (Born), cyclohexyloxy group (cHxO), t-butoxymethyl group (Burn), t-butoxy group (tBuO), t-butyl group (tBu), acetyl group (Ac), trifluoroacetyl group (TFA), o-bromobenzyloxycarbonyl group, t-butyldimethylsilyl group, 2-chlorobenzyl group, cyclohexyl group, cyclopentyl group, isopropyl group, pivalyl group, tetrahydropyran-2-yl group, and trimethylsilyl group.