CYCLIC PEPTIDES OR THEIR PHARMACEUTICALLY ACCEPTABLE SALTS, A METHOD OF THEIR SYNTHESIS Russian patent published in 1997 - IPC

Abstract RU 2095368 C1

FIELD: chemistry of peptides. SUBSTANCE: products: cyclic peptides of theformula(I):X-R1-R2-Asp-Val-R6-Thr-R8-Asn-R10-Thr-R12-Leu-Arg-Lys-R16-Ala- -R19-Lys- where: R1 - His, N-CH3-Ala; R2 - Ala, Ser; R6 - group: -NH-C(Q)-C(O)- where: Q - (lower) alkylaryl being aryl can be free or substituted in ring with one or some substituents taken from: OH, OCH3, F, Cl, J, ; R8 - Asp, Ala, Glu; R10 - Tyr that is free or substituted with lower alkoxy-group; or R6 where Q - (lower)-alkylphenyl; R12 - Arg, Lys or Orn; R16 - Ala or Gln; R17 - Nle or Ala; R19 - Ala or Val; R22 - Tyr or R6 where Q - (lower) alkylphenyl; R24 - Ala or Asn; R26 - Ile, Val, Leu; R27 - Lys or Leu; R28 - Asn, Thr, Lys; X - hydrogen or acyl; Y - NH2, OH or R29-R30-R31 - Z where Z - NH2; R29 - Gly or Ala; R30 - Gly or Ala; R31 - Met, Cys (Asm), Ala, Thr, or their pharmaceutically acceptable salts. Method of synthesis of peptides (I) involves making peptide chain by solid-phase method on polymeric carrier, splitting off protective groups to obtain amino-group with free by-side chain at the corresponding positions that is necessary for formation of cyclic covalent linkage between these protective groups, splitting off protective groups and polymer-carrier by treatment with the corresponding reagent and if necessary in the presence of so additions as cation acceptors. The synthesized compounds show broncholytic effect and used in medicine. EFFECT: improved method of synthesis. 57 cl, 6 tbl

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RU 2 095 368 C1

Authors

Devid Robert Bolin[Us]

Margaret O"Donnell[Us]

Dates

1997-11-10Published

1992-10-08Filed