Macrocycle inhibitors of proteinA / proteinA de proteinA de providina programenta 1 (PD-1) / programendo de death 1 (PD-L1) and difference 80 (B7-1) CD80 (B7-1) / scheduled death alliance 1 (PD-L1)
MILLER, MICHAEL MATTHEW,MAPELLI, CLAUDIO,ALLEN, MARTIN PATRICK,BOWSHER, MICHAEL S.,BOY, KENNETH M.,GILLIS, ERIC P.,LANGLEY, DAVID R.,MULL, ERIC,LANGLEY, DAVID R.,SANGHVI, NISHITH,SUN, LI-QIANG,TENNEY,
申请号：
PE2015001957
公开号：
PE20151671A1
申请日:
2014.03.13
申请国别(地区):
PE
年份:
2015
代理人:
摘要：
It refers to the macroscopical epoxy foam with the same pharmaceutically acceptable formula (I) or salt. Its characteristics are as follows: a es-ch [C (o) NH2] - (CH2) n-ch2-s-ch2 - * * *,-CH[C（O）NH2]-（CH2）N-CH2-S（O）-CH2-**-CH[C（O）NH2]-（CH2）N-CH2-S（O）2-CH2-**-CH[C（o）NH2]-（CH2）n-ch2-*o-ch[C（o）NH2]-（CH2）n-ch=ch-*，Among them, * is the carbon linkage； n is 0 or 1； R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are an independent non natural amino acid transverse chain； RA, re, RJ and rk are independent h or methyl； RC, RF, Rh, RR, RM and RN are h； Rb is methyl； RD is h or methyl； RG is h or methyl； Or Rb and R2, RD and R4, or RG and R7, and other related atoms, including, inter Alia, Azerbaijan, pyridine, pyridine, morphine, pyridinediol, pyridine or pyridine. The macrocyclic cucumber of formula (I) inhibits the interaction of protein / protein ppd-1 / PD-L1 and PD-L1 / CD80, so it is useful in the treatment of various diseases,Including cancer and infectious diseasesSE REFIERE A PEPTIDOS MACROCICLICOS DE FORMULA (I) O SALES DEL MISMO FARMACEUTICAMENTE ACEPTABLES, QUE SE CARACTERIZAN PORQUE A ES -CH[C(O)NH2]-(CH2)n-CH2-S-CH2-*, -CH[C(O)NH2]-(CH2)n-CH2-S(O)-CH2-*, -CH[C(O)NH2]-(CH2)n-CH2-S(O)2-CH2-*, -CH[C(O)NH2]-(CH2)n-CH2-* O -CH[C(O)NH2]-(CH2)n-CH=CH-*, ENTRE OTROS, DONDE * INDICA EL PUNTO DE UNION A CARBONILO； n ES 0 o 1； R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 Y R13 SON INDEPENDIENTEMENTE UNA CADENA LATERAL DE AMINOACIDO NO NATURAL, ENTRE OTROS； Ra, Re, Rj Y Rk SON INDEPENDIENTEMENTE H O METILO； Rc, Rf, Rh, Ri, Rm Y Rn SON H； Rb ES METILO； Rd ES H O METILO； Rg ES H O METILO； O Rb Y R2, Rd Y R4, O Rg Y R7, ENTRE OTROS, JUNTO CON LOS ATOMOS A LOS CUALES ESTAN UNIDOS FORMAN AZETIDINA, PIRROLIDINA, MORFOLINA, PIPERIDINA O PIPERAZINA, ENTRE OTROS. LOS PEPTIDOS MACROCICLICOS DE FORMULA (I) INHIBEN LA INTERACCION PROTEINA/PROTEINA PPD-1/PD-L1 Y PD-L1/CD80, POR LO CUAL SON UTILES EN LA TERAPIA DE VARIAS ENFERMEDADES, INCLUSIVE CANCER Y ENFERMEDADES INF
