Somatostatin antagonists

Details Somatostatin antagonists Somatostatin antagonists

A - Human Necessities

61

K

A61K 38/00 (2006.01) A61K 38/12 (2006.01) A61K 38/31 (2006.01) C07K 5/00 (2006.01) C07K 14/655 (2006.01)

Patent

CA 2439498

The present invention is directed to a somatostatin antagonist according to formula (I), wherein A1 is an optionally substituted aromatic .prop.-amino acid; A2 is an optionally substituted aromatic .prop.-amino acid; A3 is Dab, Dap, Lys or Orn; A4 is .beta.-Hydroxyvaline, Ser, Hser, or Thr; A5 is an optionally substituted D- or L-aromatic .sigmav.-amino acid; and Y1 is OH, NH2 or NHR1, where R1 is (C1-6)alkyl; wherein each said optionally substituted aromatic .sigmav.-amino acid is optionally substituted with one or more substituents each independently selected from the group consisting of halogen, NO2, OH, CN, (C1-6)alkyl, (c2-6)alkenyl, (c2-6)alkynyl, (C1-6)alkoxy, Bzl, O- Bzl, and NR9R10, where R9 ad R10 each is independently H, O, or (C1-6)alkyl; and wherein the amine nitrogen of each of amide peptide bond and the amino group of A1 of formula (I) is optionally substituted with a methyl group, provided that there is at least one said methyl group; or a pharmaceutically acceptable salt thereof, and to uses thereof.

La présente invention concerne un antagoniste de la somatostatine de la formule (I) ou un sel pharmaceutiquement acceptable dudit antagoniste, et leurs utilisations. Dans ladite formule, A?1¿ est un acide .prop.-amino aromatique éventuellement substitué; A?2¿ est un acide .prop.-amino aromatique éventuellement substitué; A?3¿ est Dab, Dap, Lys ou Orn; A?4¿ est .beta.-Hydroxyvaline, Ser, Hser, ou Thr; A?5¿ est un acide .sigmav.-amino aromatique D- ou L- éventuellement substitué; et Y?1¿ est OH, NH¿2? ou NHR?1¿, R?1¿ étant alkyle (C¿1-6?). Chaque acide .sigmav.-amino aromatique éventuellement substitué est éventuellement substitué par un ou plusieurs substituants choisis chacun, indépendamment, dans le groupe constitué par halogène, NO¿2?, OH, CN, alkyle (C¿1-6?), alcényle (c¿2-6?), alkynyle (c¿2-6?), alcoxy (C¿1-6?), Bzl, O-Bzl, et NR?9¿R?10¿, R?9¿ et R?10¿ étant chacun, indépendamment, H, O, ou alkyle (C¿1-6?). L'azote amine de chaque liaison peptidique amide et du groupe amino de A?1¿ de la formule (I) est éventuellement substitué par un groupe méthyle, à condition qu'existe au moins ledit groupe méthyle.

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