MACROC\u00cdCLICOS peptides that inhibit Protein \/ Protein interactions, Protein of programmed Death 1 (pd-1) \/ PD ligand 1 (pd-l1) and PD - L1 \/ CD80
SUN, LI,QIANG - ZHAO, QIAN,MULL, ERIC,GILLIS, ERIC P.,BOWSHER, MICHAEL S.,LI, LING,ALLEN, MARTIN PATRICK,MILLER, MICHAEL MATTHEW,SCOLA, PAUL MICHAEL,LANGLEY, DAVID R.
申请号:
ARP170100881
公开号:
AR108186A1
申请日:
2017.04.05
申请国别(地区):
AR
年份:
2018
代理人:
摘要:
Macrocyclic peptides that inhibit Protein \/ Protein interactions pd-1 \/ pd-l1 and pd-l1 \/ CD80, and therefore, are useful for the Improvement of various diseases.Including Cancer and Infectious Diseases.Claim 1: a compound characterized by the formula (1) or a Salt of the pharmaceutical acceptable from the point of view, where: to select a linkOr a compound of the formula (2) Group: \"Where the Wavy line *\" indicates the point of Union of the carbonyl Group and the \"Wavy line\" indicates the point of Union of the atom of nitrogen 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 and P is 0, 1 or 2 r\u02e3 is selected from Hydrogen, amino,Hydroxy and methyl r\u00b9\u2074 and r\u00b9\u2075 are selected irrespective of hydrogen and methyl and r\u1dbb is selected from Hydrogen and - C (o) nhr\u00b9\u2076 where r\u00b9\u2076 is selected from Hydrogen, chr\u00b9\u2077c (- OR) nh\u2082,- chr\u00b9\u2077c (OR) nhchr\u00b9\u2078c (o) and (OR) nh\u2082 - chr\u00b9\u2077c nhchr\u00b9\u2078c (OR) nhch\u2082c (OR) nh\u2082 where r\u00b9\u2077 is selected from Hydrogen and - ch\u2082oh,And where r\u00b9\u2078 is selected from Hydrogen and Hydrogen or Methyl r\u1d5b is a natural amino acid side chain \"The Wavy line *\" indicates the point of Union of the carbonyl Group and the Wavy line \Da \"indicates the point of Union with the nitrogen Atom r\u1d9c, r\u1da0, r\u02b0, r\u2071, r\u1d50 are Hydrogen and r\u207f r\u1d43, r\u1d49, r\u02b2 r\u1d4f are selected and each independently Hydrogen and methyl r\u00b9\u2070 is indolilc\u2081\u208b\u2083alquilo,Where the party is indolilo optionally replaced with a selected Group of c\u2081\u208b\u2086alcoxi, c\u2081\u208b\u2086alcoxicarbonilo, c\u2081\u208b\u2086alcoxicarbonilc\u2081\u208b\u2083alquilo (c\u2081\u208b\u2086alquil) s (o) (OR) c\u2081\u208b\u2083alquilo, \u2082nhcArils (OR) \u2082nhc c\u2081\u208b\u2083alquilo arilc\u2081\u208b\u2083alquils (OR), (OR) \u2082nhc c\u2081\u208b\u2083alquilo c\u2083\u208b\u2086cic