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Exedina-4 derivatives as GLP1 / glucag double effect drugs
专利权人:
SANOFI
发明人:
申请号:
ARP160102248
公开号:
AR105457A2
申请日:
2016.07.22
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
Claim 1: A peptide compound having the formula (1): R¹-Z-R² (1) wherein Z is a peptide moiety having the formula (2): His-X²-X³-Gly-Thr-Phe -Thr-Ser-Asp-Leu-Ser-Lys-Gln-X¹⁴-X¹⁵-X¹⁶-X¹⁷-X¹⁸-Ala-X²⁰-X²¹-Phe-lle-Glu-Trp-Leu-Lys-X²⁸-X²⁹-Gly-Pro -Ser-Ser-Gly-X³⁵-Pro-Pro-Pro-X³⁹-X⁴⁰ (2) X² represents an amino acid residue selected from Ser, D-Ser and Aib, X³ represents an amino acid residue selected from Gln, His and Gln functionalized with a-amino, in which Gln can be functionalized so that an H of the a-NH₂ group is substituted with C₁₋₄ alkyl,X¹⁴ represents an amino acid residue that has a side chain with a group -NH₂,a. The transverse chain group is - nh8322 with the function of - C (o) - r83099;-C (O) O-R-C (O) NH-R-S (o) 8322090 or r83099;Preferably con-c (o) - r83099;en las que R puede ser un resto que comprende hasta 50 o hasta 100 tomos de carbono y opcionalmente hetero tomos seleccionados de hal geno NOS y 2Fo PX representa un residuo de amino cido seleccionado de Glu y Asp X representa un residuo de amino cido seleccionado de X2 831222 represents amino acid residues selected from ASN, Arg, Lys, AIB, Ser, Glu, ALA and ASP, X2 8313 represents amino acid residues x383l099 selected from Gly, ala, D-Ala and thr, and represents amino acid residues selected from ala, Glu, Arg and Lys, X: 8313 indicates yes or no, x8308; 83044 indicates a residual amino acid with a transverse chain of group-nh8322;a. The transverse chain group - nh832222 can selectively have the function of - C (o) - r83099;-C (O) O-R-C (O) NH-R-S (o) 8322090 or r83099;Preferably con-c (o) - r83099;e. R83099 can be the rest, composed of no more than 50 or no more than 100 carbon atoms, optionally composed of heterogenous halogen, N, O, s and / or P, R1 represents the N-terminal group of pepper compound, and selected from nh832283;e. Nh-8322mono-o bifunction, R2 represents the C-terminal group of pepper compound, which is selected from (I) Oh o OH functionality y (II) nh-832222 or nhc232mono-o bisanizat
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