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Modified melanin receiver to blend with clove
专利权人:
IPSEN PHARMA S.A.S.
发明人:
申请号:
ARP160101279
公开号:
AR104529A2
申请日:
2016.05.05
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
The current situation involves the ligation of melanocytes, especially type 4 melanocytes, which is helpful for the treatment of sensitive diseases caused by this receptor, such as obesity, diabetes and sexual dysfunction. 1. Requirement 1: the compound represented by formula (1) has the property that X1 is the remaining part (2) of the formula;X2 is another formula (3);A¹ is Cys; A² is a Glu, D-Ala; A³ is His; A⁴ is D-2-Nal, D-Phe; A⁵ is Arg; A⁶ is Trp; A⁷ is Cys, Pen; R¹ is H, C₁₋₁₀ alkyl or substituted C₁₋₁₀ alkyl; R² and R³ are each, independently, H, C₁₋₁₀ alkyl,C₁₋₁₀ heteroalkyl substituted with NRᵃRᵇ or cyclohexyl where Rᵃ and Rᵇ is hydrogen or R² and R³ can be joined to form a cyclohexyl; R⁴ is OH or NH₂;R83099 and r8310s are respectively c83218c833128320; 8320a is an independent class H.C₁₋₁₀ heteroalkyl substituted with NRᵃRᵇ or cyclohexyl where Rᵃ and Rᵇ is hydrogen or R⁵ and R⁶ can be joined to form cyclohexyl; R⁷ and R⁸ are each, independently, H, C₁₋₁₀ alkyl,C₁₋₁₀ heteroalkyl substituted with NRᵃRᵇ or cyclohexyl where Rᵃ and Rᵇ is hydrogen; or R⁷ and R⁸ can join to form a cyclohexyl; R⁹ is H; and n is 0, characterized in that they are selected from the group consisting of: Hydantoin (C (O) - (Arg-Gly)) - cycle (Cys-Glu-His-D-Phe-Arg-Trp-Cys) -NH₂ ( SEQ ID No. 13);Hidanto na (C (O) - (Nle-Gly)) - ciclo (Cys-Glu-His-D-Phe-Arg-Trp-Cys) -NH (SEQ ID N 14)Hidanto na (C (O) - (Gly-Gly)) - ciclo (Cys-Glu-His-D-Phe-Arg-Trp-Cys) -NH (SEQ ID N 15)Hidanto na (C (O) - (Nle-Gly)) - ciclo (Cys-D-Ala-His-D-Phe-Arg-Trp-Cys) -NH (SEQ ID N 16)Hidanto na (C (O) - (Gly-Gly)) - ciclo (Cys-D-Ala-His-D-Phe-Arg-Trp-Cys) -NH (SEQ ID N 17)Hidanto na (C (O) - (Nle-Gly)) - ciclo (Cys-D-Ala-His-D-Phe-Arg-Trp-Pen) -NH (SEQ ID N 18)Hidanto na (C (O) - (Gly-Gly)) - ciclo (Cys-D-Ala-His-D-Phe-Arg-Trp-Pen) -NH (SEQ ID N 19)Hidanto na (C (O) - (Ala-Gly)) - ciclo (Cys-D-Ala-His-D-Phe-Arg-Trp-Cys) -NH (SEQ ID N 20)Hidanto na (C (O) - (D-Ala-Gly)) - ciclo (Cys-D-Ala-His-D-Phe-Arg-Trp-Cys) -
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