首页> 外国专利> 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)

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)

机译:蛋白质A /蛋白质A de providina程序1(PD-1)/程序性死亡1(PD-L1)和差异80(B7-1)CD80(B7-1)/预定死亡联盟1(PD-L1)的大环抑制剂)

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 3DCH-AMONG OTHERS, WHERE * INDICATES THE POINT OF UNION TO CARBONYL; n IS 0 or 1; R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 AND R13 ARE INDEPENDENTLY A SIDE CHAIN OF NON-NATURAL AMINO ACID, AMONG OTHERS; Ra, Re, Rj and Rk ARE INDEPENDENTLY H OR METHYL; Rc, Rf, Rh, Ri, Rm, and Rn ARE H; Rb IS METHYL; Rd IS H O METHYL; Rg IS H O METHYL; OR Rb AND R2, Rd AND R4, OR Rg AND R7, AMONG OTHERS, TOGETHER WITH THE ATOMS TO WHICH THEY ARE UNITED ARE AZETIDINE, PIRROLIDINE, MORPHOLINE, PIPERIDINE OR PIPERAZINE, AMONG OTHERS. THE MACROCYCLIC PEPTIDES OF FORMULA (I) INHIBIT THE PROTEIN / PROTEIN INTERACTION PPD-1 / PD-L1 AND PD-L1 / CD80, SO THEY ARE USEFUL IN THE THERAPY OF SEVERAL DISEASES,Including cancer and infectious diseases
机译:它是指具有相同的可药用式(I)或盐的宏观环氧泡沫塑料。其特征如下:es-ch [C(o)N​​H2]-(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 3DCH-以及其他化合物,其中*表示联盟点为羰基; n为0或1; R1,R2,R3,R4,R5,R6,R7,R8,R9,R10,R11,R12和R13独立地是非天然氨基酸的侧链; Ra,Re,Rj和Rk独立地为H或甲基; Rc,Rf,Rh,Ri,Rm和Rn是H; Rb是甲基; Rd是甲基Rg是甲基。或Rb和R2,Rd和R4或Rg和R7,以及其他原子,一起被结合在一起的是氮杂环丁烷,吡咯烷定,吗啉,哌啶或哌哌嗪等。式的大环肽(I)抑制蛋白质/蛋白质相互作用PPD-1 / PD-L1和PD-L1 / CD80,因此它们可用于治疗多种疾病,包括癌症和传染病

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