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New glucagon-like peptide analogs, composition, and methods of use
专利权人:
BETTA PHARMACEUTICALS CO.; LTD.
发明人:
HU, SHAOJING,TAN, FENLAI,WANG, YANPING,MA, CUNBO,HU, YUNYAN,CAO, HONG,ZHAO, XIANGDONG,LONG, WEI,WANG, YINXIANG,DING, LIEMING
申请号:
ES10851547
公开号:
ES2528496T3
申请日:
2010.05.17
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A GLP-1 analogue of formula I or a pharmaceutically acceptable salt or composition thereof: Xaa7 is L-His, D-histidine, deamino-histidine, 2-aminohistidine, β-hydroxy-histidine, homohistidine, α-fluoromethyl-histidine , or α-methyl-histidine; wherein: Q is linker II, III or IV: ** Formula ** wherein: R1 is hydrogen, (C1-C6) alkyl, or (C1-C6) alkoxy, R2 is hydrogen, (C1) alkyl -C6), or (C1-C6) alkoxy, R3 is hydrogen, (C1-C6) alkyl or forms a 5-8 membered ring with R1 or R2, X is hydrogen, fluorine, hydroxy, trifluoromethyl, or oxygen , Y is hydrogen, hydroxyl, fluorine, or (C1-C6) alkyl, Z is nitrogen, carbon, oxygen, or sulfur, W does not exist when Z is nitrogen, oxygen, or sulfur; W is hydrogen or fluorine when Z is carbon; Xaa14 is serine, or histidine; and one or more carbon atoms of Xaa14 are optionally substituted with one or more alkyl groups; Xaa16 is valine, lysine or leucine; and one or more carbon atoms of Xaa16 are optionally substituted with one or more alkyl groups; or Xaa16 is lysine bound with TU, where, T is γ-glutamic acid, β-alanine, γ-aminobutyric acid, HOOC (CH2) nCOOH, or ** Formula ** where n is 1, 2, 3, 4 , 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, or 27; k is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, and m is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; U exists and is a fatty acid with a length of 8 to 20 carbons only when T is γ-glutamic acid, β-alanine, γ-aminobutyric acid or ** Formula ** where k is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10, and m is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; Xaa18 is serine, arginine, or lysine; and one or more of the Xaa18 carbon atoms are optionally substituted with one or more alkyl groups.Un análogo de GLP-1 de fórmula I o una sal o composición farmacéuticamente aceptable del mismo: Xaa7 es L-His, D-histidina, desamino-histidina, 2-aminohistidina, β-hidroxi-histidina, homohistidina, α- fluorometil-histidina, o α-metil-histidina; en donde: Q es el enlazador II, III o IV:**Fórmula** e
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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