ANALOGS OF CYCLIC SOMATOSTATIN Russian patent published in 2004 - IPC

FIELD: organic chemistry, hormones, pharmacy.

SUBSTANCE: invention relates to compounds of the formula (I) or (II)

or to their pharmaceutically acceptable salts wherein each Y and Z in each case represents independently D- or L-natural or non-natural α-amino acid; n in each case means independently 0 or 4, (I) under condition that both n can't mean simultaneously 0; and 0 or 4 (II) wherein indicated amino acids (in I) represent the chain: X¹-X²-X³-X⁴ wherein X¹ represents Tyr or Trp residues that can be protected with the Boc-group; X² represents D-Trp; X represents Lys that can be protected with the Boc-group; X⁴ represents Nal, Tyr or Thr; m = 0; a means hydrogen atom (H) or R¹; b means -OH or -OR¹; for (II) X¹ represents natural or non-natural D- or L-isomer of Phe, Trp or Tyr wherein when X¹ means Tyr then the aromatic ring in its by-side chain is substituted with R⁶ optionally; X² represents D- or L-isomer of Trp; X³ represents Lys; X⁴ represents natural or non-natural D- or L-amino acid Nal, Thr, Tyr or Ser wherein when X⁴ represents Tyr then the aromatic ring disposed in its by-side chain can be substituted with R⁶ optionally; or when X⁴ represents Ser or Thr then oxygen atom disposed in its by-side chain can be substituted with one or some R¹ wherein R¹ represents hydrogen atom (H), or (C₁-C₄)-alkyl (I); for (II) R¹ means hydrogen atom (H), (C₁-C₄)-alkyl or aryl-(C₁-C₄)-alkyl; R² represents hydrogen atom (H) or substituted phenyl-(C₁-C₄)-alkyl for (I); for (II): R² means substituted phenyl-(C₁-C₄)-alkyl; R³ and R each represents independently hydrogen atom (H), or substituted aryl that can be substituted with one or some substitutes taken among the group consisting of hydroxy-group (OH), (C₁-C₄)-alkyl and (C₁-C₄)-alkoxy-group; in each case R⁵ represents hydrogen atom (H); R³ and R each represents independently hydrogen atom (H) or optionally substituted fragment taken among the group consisting of (C₁-C₄)-alkyl and aryl being optionally substituted fragment is substituted with one or some substituted taken among the group consisting of -OH and (C₁-C₄)-alkoxy-group; in each case R⁵ represents independently hydrogen atom (H); R⁶ represents in each case aryl-(C₁-C₄)-alkyl. Invention relates to two pharmaceutical compositions used for the selective binding with at least one of subtype of the human somatostatin receptor comprising in the effective dose compound of the formula (I) of compound of the formula (II).

EFFECT: valuable medicinal properties of compounds.

17 cl, 2 tbl, 22 ex