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1. 发明申请

WO2013095903A1 NOVEL GH-RH ANALOGS WITH POTENT AGONISTIC EFFECTS 审中-公开
标题翻译：新的GH-RH模拟与POTENT激发效应
公开(公告)号：WO2013095903A1
公开(公告)日：2013-06-27
申请号：PCT/US2012/067690
申请日：2012-12-04
申请人： SCHALLY, Andrew, V. , CAI, Ren-Zhi , ZARANDI, Marta , UNIVERSITY OF MIAMI , UNITED STATES OF AMERICA REPRESENTED BY THE DEPARMENT OF VETERANS AFFAIRS
发明人： SCHALLY, Andrew, V. , CAI, Ren-Zhi , ZARANDI, Marta
IPC分类号： C07K14/60 , A61K38/25
CPC分类号： C07K14/60 , A61K38/00 , C07K14/61
摘要： The synthetic peptides have the sequence: [RrA\ A 2 , A 6 , A 8, A 11 , A 12 , A 15 , A 20 , A 21 , A 22 , Nle 27 , A 28 , A 29 , A30]hGH-RH(1 -30)-R 2 (SEQ ID NO: 1 ) wherein R 1 is Ac, Tfa, or is absent, A 1 is Tyr, Dat, or N-Me-Tyr, A 2 is Ala, D-Ala, Abu, or D-Abu, A 6 is Phe or Fpa5, A 8 is Asn, Ala, Gin, Thr, or N-Me-Ala, A 11 is Arg, His, or Har, A 12 is Orn, or Lys(Me)2, A 15 is Abu or Ala A 20 is Arg, His, or Har, A 21 is Orn, or Lys(Me)2, A 22 is Leu, or Orn, A 28 is Ser, or Asp, A 29 is Arg, Har, Agm, D-Arg, or D-Har, A 30 is Arg, Agm, Ada, Amc, Aha, Apa, Har, D-Arg, D-Har, Gab, Gin, D-GIn, Gin-Gab, D-Gln-Gab, or is absent, R 2 is -NH 2 , -OH, -NHR 2 , -N(R 2 ) 2 , or -OR 2 , in which R 2 is any of C 1-12 alkyl, C 2-12 alkenyl, or C 2-12 alkinyl, provided that if A 29 is Agm then A 30 and R 2 are absent A 1 is N-Me-Tyr only, and pharmaceutically acceptable salts thereof.
摘要翻译：合成肽具有以下序列：[RrA / A2，A6，A8，A11，A12，A15，A20，A21，A22，Nle27，A28，A29，A30] hGH-RH（1-30）-R2（SEQ ID NO ：1）其中R1是Ac，Tfa或不存在，A1是Tyr，Dat或N-Me-Tyr，A2是Ala，D-Ala，Abu或D-Abu，A6是Phe或Fpa5，A8是 Asn，Ala，Gin，Thr或N-Me-Ala，A11是Arg，His或Har，A12是Orn或Lys（Me）2，A15是Abu或Ala A20是Arg，His或Har，A21 是Orn或Lys（Me）2，A22是Leu或Orn，A28是Ser或Asp，A29是Arg，Har，Agm，D-Arg或D-Har，A30是Arg，Agm，Ada，Amc ，Aha，Apa，Har，D-Arg，D-Har，Gab，Gin，D-Gln，Gin-Gab，D-Gln-Gab，或不存在，R 2是-NH 2，-OH，-NHR 2，-N （R2）2或-OR2，其中R2是C1-12烷基，C2-12烯基或C2-12炔基中的任何一个，条件是如果A29是Agm，则A30和R2不存在A1是N-Me-Tyr 仅及其药学上可接受的盐。

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