Patent ID: 8293870
Filing Date: 2012-10-23
Classification: A61K,A61P,C07K

Abstract:
1. A method of inhibiting mucin hypersecretion in a mammal, the method comprising administering to the mammal a mucin hypersecretion-inhibiting amount of a N-terminal- and/or C-terminal-chemically modified peptide or a pharmaceutical composition comprising said chemically modified peptide, which peptide consists of an amino acid sequence selected from the group consisting of: (a) an amino acid sequence of from 7 to 23 contiguous amino acids of a reference sequence, GAQFSKTAAKGEAAAERPGEAAVA (SEQ ID NO:1); and (b) an amino acid sequence substantially identical to the sequence defined in (a); wherein, in (a) and (b), (i) the C-terminal amino acid of said chemically modified peptide is amidated at the C-terminal carboxyl group with ammonia, a C1 to C24 aliphatic alkyl amine, a hydroxyl-substituted C2 to C24 aliphatic alkyl amine, a linear 2-(C1 to C24 aliphatic alkyl)oxyethylamine group, or an omega-methoxy-poly(ethyleneoxy)n-ethylamine group, where n is from 0 to 10 or esterified at the C-terminal carboxyl group with a C1 to C24 aliphatic alkyl alcohol or a 2-(omega-methoxy-poly(ethyleneoxy)n)-ethanol group, where n is from of 0 to 10; and the N-terminal amino acid of the peptide is not chemically modified; or (ii) the C-terminal amino acid of said chemically modified peptide is optionally amidated at the C-terminal carboxyl group with ammonia, a C1 to C24 aliphatic alkyl amine, a hydroxyl-substituted C2 to C24 aliphatic alkyl amine, a linear 2-(C1 to C24 aliphatic alkyl)oxyethylamine group, or an omega-methoxy-poly(ethyleneoxy)n-ethylamine group, where n is from 0 to 10 or esterified at the C-terminal carboxyl group with a C1 to C24 aliphatic alkyl alcohol or a 2-(omega-methoxy-poly(ethyleneoxy)n)-ethanol group, where n is from of 0 to 10; and the N-terminal amino acid of the peptide is alkylated at the N-terminal amine with a C1 to C24 aliphatic alkyl group, a linear 2-(C1 to C24 aliphatic alkyl)oxyethyl group, or an omega-methoxy-poly(ethyleneoxy)n-ethyl group, where n is from 0 to 10, or acylated at the N-terminal amine with a trifluoroacetic acid, benzoic acid, a C with the proviso that said chemically modified peptide contains no more than 23 amino acids; and wherein said chemically modified peptide has a mucin hypersecretion-inhibiting effect when administered to a mammal in a mucin hypersecretion-inhibiting amount.