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Humán növekedési hormont felszabadító hormon-analógok
专利权人:
INSTYTUT FARMACEUTYCZNY;ZAKLADY FARMACEUTYCZNE POLPHARMA S.A.
发明人:
IZDEBSKI JAN,KUNCE DANUTA,ORLOWSKA ALICJA,WITKOWSKA EWA,SZELEJEWSKI WIESLAW,KUTNER ANDRZEJ,BANKOWSKI KRZYSZTOF,FRACKIEWICZ ELZBIETA
申请号:
HU0401589
公开号:
HU229220B1
申请日:
2002.10.30
申请国别(地区):
HU
年份:
2013
代理人:
摘要:
Growth hormone-releasing hormone analogs having the amino acid sequence of the formula: Dat-Ala-Asp-Ala-Ile-Phe-Thr-Asn-Ser-Tyr10-R11-R12-VAL-Leu-Ala-Gln-Leu-Ser-Ala-R20-R21-Leu-Leu-Gln-Asp-Ile-Nle-Asp-R29-NH2 (I), wherein R11 is hArg, Gab or Gap; R12 is hArg, Orn, Gab or Gap; R20 is hArg, hArg, Gab or Gap; R21 is hArg, Orn, Gab or Gap; R29 is D-Arg, hArg, Gab or Gap; and their pharmaceutically acceptable salts. Said peptides are potent and selective stimulators of GH release and they are highly resistant to enzymatic degradation. Said peptides are prepared using the solid phase synthesis method, by introducing suitable derivatives of lysine, 2,4-diaminobutyric acid or 2,3-diaminopropionic acid at appropriate positions in the peptide chain attached to a polymeric support, deprotecting side-chain amino groups and reacting free amino groups with a guanidinating agent, removing all remaining t-butyloxycarbonyl protective groups, and cleaving the synthesized peptide from the support, followed by purification and optionally, converting the peptide into a pharmaceutically acceptable salt.
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