Terlipressin-octadecanedioic acid conjugate for vasoconstrictive therapy

A method of treating or managing a condition in a living subject, the method comprising steps of:

• administering to the subject a pharmaceutical composition;
• wherein the pharmaceutical composition comprises:
• a compound characterized by formula (FX1):
• A1-X1—X2-A2 (FX1);
• wherein:
• A1 is a carboxylic acid group, a carboxylate anion, or a carboxylate ester;
• X1 is a substituted or unsubstituted and saturated or unsaturated C1-C50 aliphatic group;
• X2 is a linker group selected from the group consisting of a direct bond, an organic group, —O—, —S—, —S(═O)—, —S(═O)2—, —S—S—, —N═, ═N—, —N(H)—, —N═N—N(H)—, —N(H)—N═N—, —N(OH)—, —N(═O)—, and any combination thereof;
• and
• A2 is a peptide, the peptide being terlipressin or a substituted or unsubstituted derivative, a substituted or unsubstituted natural or synthetic analogue, a substituted or unsubstituted variant, a substituted or unsubstituted isomer, or a substituted or unsubstituted fragment of terlipressin.

A compound characterized by formula (FX10):

• (A1-X1-A2-)nA2 (FX10);
• wherein:
• each A1 is independently a carboxylic acid group, a carboxylate anion, or a carboxylate ester;
• each X1 is independently a substituted or unsubstituted and saturated or unsaturated C1-C50 aliphatic group;
• each X2 is independently a linker group selected from the group consisting of a direct bond, an organic group, —O—, —S—, —S(═O)—, —S(═O)2—, —S—S—, —N═, ═N—, —N(H)—, —N═N—N(H)—, —N(H)—N═N—, —N(OH)—, —N(═O)—, and any combination thereof;
• and
• A2 is a peptide, the peptide being terlipressin or a substituted or unsubstituted derivative, a substituted or unsubstituted natural or synthetic analogue, a substituted or unsubstituted variant, a substituted or unsubstituted isomer, or a substituted or unsubstituted fragment of terlipressin;
• and
• n is an integer selected from the range of 1 to 10,
• or a pharmaceutically acceptable salt thereof.