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DERIVADOS DE PÉPTIDOS INSULINOTRÓPICOS CUYA CARGA N-TERMINAL ESTÁ MODIFICADA
专利权人:
HANMI PHARM. CO.; LTD.
发明人:
申请号:
ARP140100024
公开号:
AR094358A1
申请日:
2014.01.03
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
Claim 2: The Derivative of insulinotropic Peptide according to claim 1, in which the positively charged amino Group of the n-terminal amino acid residue or a natural insulinotropic Peptide, an Analogue or a fragment thereof is modified Chemically to a load Neu Tra or clearly negative.Claim 3: The Derivative of insulinotropic Peptide according to claim 2, wherein the natural insulinotropic Peptide, its Analog or Fragment of the same as the n-terminal residue is histidine.And it is chemically modified to have a neutral charge or burden clearly negative for deletion or substitution of the amino Group to the histidine residue or by deletion of the a - carbon.Claim 5: The Derivative of insulinotropic Peptide according to claim 4, wherein The residue n-terminal insulinotropic Peptide natural Fragment of the same or the similar is replaced with a substance selected from the group consisting of amino histidil des, dimeti L - histidil, B - 4 - hydroxy acetyl imidazopropionilo imidazo -, B - and imidazopropionilo carboxy.Claim 8: The Derivative of insulinotropic Peptide according to claim 1, in which the natural insulinotropic peptide glp-1 is represented by the sequence no. 1, exendin-4 represented by Sequence 2, 3 exendina - represented by the sequence no. 3, oxintomodulin Represented by the sequence no. 5, no. 6 Group represented by the sequence, or their analogues or Fragments.Claim 12: The Derivative of insulinotropic Peptide according to claim 5, in which the Derivative of insulinotropic Peptide is represented by the following Chemical formula (1): r\u00b9 R\u00b2 - X - (1) in the Chemical formula r\u00b9 is selected from the group consisting of amino - His - Tidil, Dimethyl histidil, imidazopropionil - B - hydroxy4 - imidazo - acetyl - Carboxy - and imidazopropionilo B R\u00b2 is nh\u2082 - Oh - or Glu ala Gly THR X is be PHE THR Val Tyr Leu Glu ASP Gly GLN be ala ala Lys Glu PHE ala Val Leu Lys ile TRP Gly ARG Gly ASP giy ASP Leu PHE THR Lys THR be be Glu Glu Glu ala
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