![用于治疗性干预的Y2/Y4选择性受体激动剂](/CN/2008/1/43/images/200810215724.jpg)
基本信息:
- 专利标题: 用于治疗性干预的Y2/Y4选择性受体激动剂
- 专利标题(英):Y2/Y4 selective receptor agonists for therapeutic interventions
- 申请号:CN200810215724.2 申请日:2005-03-17
- 公开(公告)号:CN101361967A 公开(公告)日:2009-02-11
- 发明人: T·施瓦茨
- 申请人: 7TM制药联合股份有限公司
- 申请人地址: 丹麦霍尔肖姆
- 专利权人: 7TM制药联合股份有限公司
- 当前专利权人: 7TM制药联合股份有限公司
- 当前专利权人地址: 丹麦霍尔肖姆
- 代理机构: 上海专利商标事务所有限公司
- 代理人: 范征
- 优先权: PA200400436 2004.03.17 DK; 0503111.7 2005.02.14 GB; 60/558,932 2004.04.01 US; 60/585,964 2004.07.06 US
- 分案原申请号: 2005800086660
- 主分类号: A61K38/17
- IPC分类号: A61K38/17 ; A61P1/16 ; A61P3/04 ; A61P3/06 ; A61P3/10 ; A61P7/02 ; A61P9/00 ; A61P9/10 ; A61P9/12 ; A61P15/00 ; A61P19/02 ; A61P25/00 ; A61P35/00
Y receptor agonists which are selective for Y2 and Y4 receptors over the Y1 receptor are useful for treatment of, for example obesity, are (a) PP-fold peptides or PP-fold peptides mimics which have (i) a C-terminal Y receptor-recognition amino acid sequence represented by -X-Thr-Arg-X3-Arg-Tyr-C(=0)NR1R2 wherein R1 and R1 are independently hydrogen or C1-C6 alkyl, X is Val, lle, Leu or Ala, and X3 is Gln or Asn, or a conservatively substituted variant thereof in which Thr is replaced by His or Asn and/or Tyr is replaced by Trp or Phe; and/or Arg is replaced by Lys, and (ii) an N-terminal Y receptor-recognition amino acid sequence represented by H2N-X1-Pro-X2- (Glu or Asp)- wherein X1 is not present or is amino acid residue, and X2 is Leu or Ser or conservative substitutions of Leu or Ser, or (b) the said agonists comprise a C-terminal Y receptor-recognition amino acid sequence as defined in (i) above, said Y receptor-recognition sequence being fused to an amphiphilic amino acid sequence domain comprising at least one alpha helical turn adjacent the N-terminus of the said hexapeptide sequence, said turn being constrained in a helical configuration by a covalent intramolecular link, and optionally an N-terminal sequence which commences with a Y receptor-recognition amino acid sequence as defined in (ii) above.
IPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K38/00 | 含肽的医药配制品 |
--------A61K38/04 | .在完全确定的序列中最多有20个氨基酸的肽;其衍生物 |
----------A61K38/17 | ..来源于动物;来源于人类 |