PAUL MICHAEL SCOLA,ERIC MULL,MARTIN PATRICK ALLEN,QIAN ZHAO,LI SUN,ERIC P. QIANG - GILLIS,CLAUDIO MAPELLI
申请号：
ARP150104168
公开号：
AR103093A1
申请日:
2015.12.17
申请国别(地区):
AR
年份:
2017
代理人:
摘要：
Macrocyclic peptides that inhibit the interaction of protein / protein ppd-1 / PD-L1 and PD-L1 / CD80, thus contributing to the improvement of various diseases including cancer and infectious diseases. Claim 1: a compound characterized by a formula (1) or a salt acceptable from the agent, in which (2) is selected from the link of the formula group,Corrugated line * indicates the connection point with carbide group, corrugated line indicates the connection point with nitrogen atom； Z is 0, 1 or 2； W is 1 or 2； n is 0 or 1； m is 1 or 2； m is 0 or 1； P is 0, 1 or 2； r739 selects hydrogen, amine, hydrogen Xi and methyl； R183088 and r183099 are independent of hydrogen and methyl； r761111 is selected from hydrogen y-c (o) nhr18310；Where r8310 is selected from the hydrogen gas, - chr18311； (o) nh8322；-CHR¹⁷C (O) NHCHR¹⁸C (O) NH₂ and -CHR¹⁷C (O) NHCHR¹⁸C (O) NHCH₂C (O) NH₂；e. R-831111y-ch-8322oh was selected, and hydrogen and methyl were selected in r-831222； r7515a was the transverse chain of hydrogen or a natural amino acid； r758080；R75848,R688a,Rⁱ and Rᵐ are hydrogen； Rⁿ is hydrogen or methyl, or Rᵛ and Rⁿ form a pyrrolidine ring； Rᵃ is hydrogen or methyl； Rʲ is selected from hydrogen, C₁₋₆ alkoxy-C₁₋₆ alkyl, C₁₋₆ alkyl, carboxy-C₁₋₆ alkyl, halo-C₁₋₆ alkyl, hydroxy-C₁₋₆ alkyl, (NRᵃRᵇ) C₁₋₆ alkyl, wherein Rᵃ and Rᵇ are independently selected from hydrogen and C₁₋₆ alkyl； and phenyl-C₁₋₆ alkyl, where phenyl is optionally substituted with 1, 2, 3, 4 or 5 groups independently selected from C₁₋₆ alkoxy, C₁₋₆ alkyl, cyano, halo and nitro； R¹,R2,R3,R830808,R83099,R8310,R8311th,R8322,R8313,R830404,R1,The selection of R1: and R1: 3 is independent of the transverse chain of a natural amino acid and the transverse chain of an unnatural amino acid； or R1,R2,R3,R830808,R83099,R8310,R8311th,R8322,R8313,R830404,R1,R¹² and R¹³ can each independently form a ring with the corresponding proximal R group as described below； Rᵇ is selected from C₁₋₆ alkoxy-C₁₋₆ alkyl, C₁₋₆ alkyl, carboxy-C₁₋
