Analogs of extended n-terminal somatostatin

Details Analogs of extended n-terminal somatostatin Analogs of extended n-terminal somatostatin

C - Chemistry, Metallurgy

07

K

530/7.26

C07K 14/655 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1243300

ANALOGS OF EXTENDED N-TERMINAL SOMATOSTATIN ABSTRACT Somatostatin-28 has the formula: H-Ser-Ala-Asn-Ser -Asn-Pro-Ala-Met-Ala-Pro-Arg-Glu-Arg-Lys-Ala- Gly-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH. Analogs have been synthesized that are more potent than somatostatin-28, and these analogs or pharmaceutically acceptable salts thereof, dispersed in a pharmaceutically acceptable liquid or solid carrier, can be administered to mammals in the same manner as somatostatin. In the analogs, Leu may be substituted in the 8-position in combination with D-Trp in the 22-position and/or Tyr in the 25-position. D-Cys may also be substituted in the 28-position, and D-Ser may be substituted in the 27-position. Certain residues may also be deleted. D-Trp22 somatostation-28 has surprisingly been found to be insulin-selective when administered in vivo and is useful for the treatment of insulinoma.

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