COMPOUNDS PROMOTING GROWTH HORMONE RELEASE Russian patent published in 2001 - IPC

Abstract RU 2167881 C2

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes novel compound of the general formula (I): A-B-C-D-E-(-F)p where p = 0 or 1; A means imidazolyl-C1-6-alkanoic acid, imidazolyl-C1-6-alkenoic acid, amino-C1-6-alkanoic acid, L- or D-α-amino acid taken among the group consisting of H-His, H-D-Ala, H-Aib; B means D-Trp, D-2-Nal or D-Phe; C means Ala or Gly; D means Trp or N-aralkylglycine; E means D-Phe if p = 1 or E means -NH-CH-(CH2R)3-CO-R4 or -NH-CH-(CH2R)3-CH-R4 if p = 0 where R3 means phenyl and R4 means -N(R5)6 where each R5 and R6 means independently hydrogen atom or lower alkyl; F means -NH-CH(R10)-CH2)v-R7- if p = 1 where v is a whole number from 1 to 8 and R7 means -N(R8)-R9) where each R8 and R9 means independently hydrogen atom; R10 means -H, -COOH, CO-R11 or CH2- where R11 means -N(R12)-(R13) where each R12 and R13 is hydrogen atom independently under condition that at least one amide bond between A and B, B and C, C and D, D and E or between K and F is substituted with aminomethylene if p = 1; or E means -NH-CH-(CH2-R3)CH2-R4 if p = 0; or R10 means CH2-R11 if p = 1; or pharmaceutically acceptable salt of this compound. Compounds show the enhanced resistance to proteolytic cleavage by enzymes due to substitution of amide bond (-CO-NH-) with aminomethylene one (-CH2NH-) or by addition of N-aralkylglycine. Invention describes also pharmaceutical composition used for stimulation of growth hormone release from hypophysis. EFFECT: new compound indicated above, valuable properties. 15 cl, 19 ex

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RU 2 167 881 C2

Authors

Nil'S Langelann Jokhansen

Esper Lau

Kell' Madsen

Bekhrenn Fridrikh Lunt

Genning Tegersen

Birgit Sekhested Khansen

Dates

2001-05-27Published

1994-12-22Filed