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Apoptosis-inducing agents for the treatment of malignant tumors and immune and autoimmune diseases

机译:凋亡诱导剂,用于治疗恶性肿瘤以及免疫和自身免疫性疾病

摘要

1. The compound of formula (I) or a therapeutically acceptable salt thereof, wherein A is N or C (A); A is H, R, OR, SR, S (O) R, SOR, C (O) R, C (O) OR, OC (O) R, NHR, N (R), C (O) NHR, C (O) N (R), NHC (O) R, NRC (O) R, NHC (O) OR, NRC ( O) OR, NHC (O) NH, NHC (O) NHR, NHC (O) N (R), NRC (O) NHR, NRC (O) N (R), SONH, SONHR, SON (R), NHSOR , NRSOR, NHSONHR, NHSON (R), NRSONHR, NRSON (R), C (O) NHNOH, C (O) NHNOR, C (O) NHSOR, C (NH) NH, C (NH) NHR, C (NH ) N (R), NHSONHR, NHSON (CH) R, N (CH) SON (CH) R, F, Cl, Br, I, CN, NO, N, OH, C (O) H, CHNOH, CH ( NOCH), CF, C (O) OH, C (O) NH or C (O) OR; B is H, R, OR, SR, S (O) R, SOR, C (O) R, C (O) OR, OC (O) R, NHR, N (R), C (O) NHR, C (O) N (R), NHC (O) R, NRC (O) R, NHC (O) OR, NRC ( O) OR, NHC (O) NH, NHC (O) NHR, NHC (O) N (R), NRC (O) NHR, NRC (O) N (R), SONH, SONHR, SON (R), NHSOR , NRSOR, NHSONHR, NHSON (R), NRSONHR, NRSON (R), C (O) NHNOH, C (O) NHNOR, C (O) NHSOR, C (NH) NH, C (NH) NHR, C (NH ) N (R), NHSONHR, NHSON (CH) R, N (CH) SON (CH) R, F, Cl, Br, I, CN, NO, N, OH, C (O) H, CHNOH, CH (NOCH), CF, C (O) OH, C (O) NH or C (O) OR; D is H, R, OR, SR, S (O) R, SOR, C (O) R, C (O) OR, OC (O) R, NHR , N (R), C (O) NHR, C (O) N (R), NHC (O) R, NRC (O) R, NHC (O) OR, NRC (O) OR, NHC (O) NH , NHC (O) NHR, NHC (O) N (R), NRC (O) NHR, NRC (O) N (R), SONH, SONHR, SON (R), NHSOR, NRSOR, NHSONHR, NHSON (R) , NRSONHR, NRSON (R), C (O) NHNOH, C (O) NHNOR, C (O) NHSOR, C (NH) NH, C (NH) NHR, C (NH) N (R), NHSONHR, NHSON (CH) R, N (CH) SON (CH) R, F, Cl, Br, I, CN, NO, N, OH, C (O) H, CHNOH, CH (NOCH), CF, C (O) OH, C (O) NH or C (O) OR; E is H, R, OR, SR, S (O) R, SOR, C (O) R, C (O) OR, OC (O) R, NHR , N (R), C (O) NHR, C (O) N (R), NHC (O) R, NRC (O) R, NHC (O) OR, NRC (O) OR, NHC (O) NH , NHC (O) NHR, NHC (O) N (R), NRC (O) NHR, NRC (O) N (R), SONH, SONHR, SON (R), NHSOR, NRSOR, NHSONHR, NHSON (R) , NRSONHR, NRSON (R), C (O) NHNOH, C (O) NHNOR, C (O) NHSOR, C (NH) NH, C (NH) NHR, C (NH) N (R), NHSONHR, NHSON (CH) R, N (CH) SON (CH) R, F, Cl, Br, I, CN, NO, N, OH, C (O) H, CHNOH, C H (NOCH), CF, C (O) OH, C (O) NH or C (O) OR; and Y is H, CN, NO, C (O) OH, F, Cl, Br, I, CF, OCF, CFCF, OCFCF, R, OR, C (O) R, C (O) OR, SR, SOR, NH, NHR, N (R), NHC (O) R, C (O) NH, C (O) NHR, C (O) N (R), NHS (O) R or NHSOR; or E and Y, together with the atoms to which they are attached, are benzene, naphthylene, heteroarene, cycloalkane, cycloalkene, heterocycloalkane or heterocycloalkene; and A, B, and D are independently selected from H, R, OR, SR, S (O) R, SOR, C (O) R, C (O) OR, OC (O) R, NHR, N (R), C (O ) NHR, C (O) N (R), NHC (O) R, NRC (O) R, NHC (O) OR, NRC (O) OR, NHC (O) NH, NHC (O) NHR, NHC ( O) N (R), NRC (O) NHR, NRC (O) N (R), SONH, SONHR, SON (R), NHSOR, NRSOR, NHSONHR, NHSON (R), NRSONHR, NRSON (R), C (O) NHNOH, C (O) NHNOR, C (O) NHSOR, C (NH) NH, C (NH) NHR, C (NH) N (R), NHSONHR, NHSON (CH) R, N (CH) SON (CH) R, F, Cl, Br, I, CN, NO, N, OH, C (O) H, CHNOH, CH (NOCH), CF, C (O)
机译:1.式(I)的化合物或其治疗上可接受的盐,其中A为N或C(A); A是H,R,OR,SR,S(O)R,SOR,C(O)R,C(O)OR,OC(O)R,NHR,N(R),C(O)NHR,C (O)N(R),NHC(O)R,NRC(O)R,NHC(O)OR,NRC(O)OR,NHC(O)NH,NHC(O)NHR,NHC(O)N( R),NRC(O)NHR,NRC(O)N(R),SONH,SONHR,SON(R),NHSOR,NRSOR,NHSONHR,NHSON(R),NRSONHR,NRSON(R),C(O)NHNOH ,C(O)NHNOR,C(O)NHSOR,C(NH)NH,C(NH)NHR,C(NH)N(R),NHSONHR,NHSON(CH)R,N(CH)SON(CH) R,F,Cl,Br,I,CN,NO,N,OH,C(O)H,CHNOH,CH(NOCH),CF,C(O)OH,C(O)NH或C(O)或; B是H,R,OR,SR,S(O)R,SOR,C(O)R,C(O)OR,OC(O)R,NHR,N(R),C(O)NHR,C (O)N(R),NHC(O)R,NRC(O)R,NHC(O)OR,NRC(O)OR,NHC(O)NH,NHC(O)NHR,NHC(O)N( R),NRC(O)NHR,NRC(O)N(R),SONH,SONHR,SON(R),NHSOR,NRSOR,NHSONHR,NHSON(R),NRSONHR,NRSON(R),C(O)NHNOH ,C(O)NHNOR,C(O)NHSOR,C(NH)NH,C(NH)NHR,C(NH)N(R),NHSONHR,NHSON(CH)R,N(CH)SON(CH) R,F,Cl,Br,I,CN,NO,N,OH,C(O)H,CHNOH,CH(NOCH),CF,C(O)OH,C(O)NH或C(O)或; D是H,R,OR,SR,S(O)R,SOR,C(O)R,C(O)OR,OC(O)R,NHR,N(R),C(O)NHR,C (O)N(R),NHC(O)R,NRC(O)R,NHC(O)OR,NRC(O)OR,NHC(O)NH,NHC(O)NHR,NHC(O)N( R),NRC(O)NHR,NRC(O)N(R),SONH,SONHR,SON(R),NHSOR,NRSOR,NHSONHR,NHSON(R),NRSONHR,NRSON(R),C(O)NHNOH ,C(O)NHNOR,C(O)NHSOR,C(NH)NH,C(NH)NHR,C(NH)N(R),NHSONHR,NHSON(CH)R,N(CH)SON(CH) R,F,Cl,Br,I,CN,NO,N,OH,C(O)H,CHNOH,CH(NOCH),CF,C(O)OH,C(O)NH或C(O)或; E是H,R,OR,SR,S(O)R,SOR,C(O)R,C(O)OR,OC(O)R,NHR,N(R),C(O)NHR,C (O)N(R),NHC(O)R,NRC(O)R,NHC(O)OR,NRC(O)OR,NHC(O)NH,NHC(O)NHR,NHC(O)N( R),NRC(O)NHR,NRC(O)N(R),SONH,SONHR,SON(R),NHSOR,NRSOR,NHSONHR,NHSON(R),NRSONHR,NRSON(R),C(O)NHNOH ,C(O)NHNOR,C(O)NHSOR,C(NH)NH,C(NH)NHR,C(NH)N(R),NHSONHR,NHSON(CH)R,N(CH)SON(CH) R,F,Cl,Br,I,CN,NO,N,OH,C(O)H,CHNOH,CH(NOCH),CF,C(O)OH,C(O)NH或C(O)或; Y是H,CN,NO,C(O)OH,F,Cl,Br,I,CF,OCF,CFCF,OCFCF,R,OR,C(O)R,C(O)OR,SR,SOR ,NH,NHR,N(R),NHC(O)R,C(O)NH,C(O)NHR,C(O)N(R),NHS(O)R或NHSOR; E和Y连同它们所连接的原子一起是苯,萘,杂芳烃,环烷烃,环烯烃,杂环烷烃或杂环烯烃;和A,B和D独立地选自H,R,OR,SR,S(O)R,SOR,C(O)R,C(O)OR,OC(O)R,NHR,N(R ),C(O)NHR,C(O)N(R),NHC(O)R,NRC(O)R,NHC(O)OR,NRC(O)OR,NHC(O)NH,NHC(O) )NHR,NHC(O)N(R),NRC(O)NHR,NRC(O)N(R),SONH,SONHR,SON(R),NHSOR,NRSOR,NHSONHR,NHSON(R),NRSONHR,NRSON (R),C(O)NHNOH,C(O)NHNOR,C(O)NHSOR,C(NH)NH,C(NH)NHR,C(NH)N(R),NHSONHR,NHSON(CH)R ,N(CH)SON(CH)R,F,Cl,Br,I,CN,NO,N,OH,C(O)H,CHNOH,CH(NOCH),CF,C(O)

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