公开(公告)号：EP0641306A1

公开(公告)日：1995-03-08

申请号：EP92914474.0

申请日：1992-06-04

申请人： SMITHKLINE BEECHAM CORPORATION

发明人： CHENERA, Balan ,  DES JARLAIS, Renee, Louise ,  DREYER, Geoffrey, Bainbridge

IPC分类号： A61K31 ,  A61P31 ,  C07C35 ,  C07C45 ,  C07C49 ,  C07C67 ,  C07C69 ,  C07D333 ,  C07D335

CPC分类号： C07D333/48 ,  C07C35/21 ,  C07C45/59 ,  C07C49/747 ,  C07C69/757 ,  C07D335/02

摘要： Compounds of formula (I) wherein R1 and R4 are OH, (CHR5)mCOR6, (CHR5)mCH(OH)R5 or R5; R2 and R3 are H, C1-8alkyl, Het, C3-10cycloalkyl, Het-C1-8alkyl, C2-8alkenyl, Het-C2-8alkenyl, C3-10cycloalkyl-C1-8alkyl or C3-10cycloalkyl-C2-8alkenyl; R5 is R2 or R2 mono- or di-substituted by G; R6 is H, OH, OR', R2, N(R')2, AA or NHC(=NR7)NHR''; R¿7? is H, CN, COR' or SO2R'; R' is H, C1-6alkyl, C3-10cycloalkyl or C1-8alkyl-C3-10cycloalkyl; R'' is R', COR', C(O)OR' or CON(R')2; G is OR', OC(O)R', OC(O)N(R')2, halogen, COR6, NR'-AA, NHCOR', SO2N(R')2, NHSO2N(R')2, NHC(=NR?7¿)NHR'', CF¿3? or N(R')2; AA is one or two amino acids; Z is CH2, CHOH, CHN(R')2, CHNHCOOR, S, SO, SO2, SONH, O, CHCH2OH, CHCO2H, C=O, NR'', N(O)R' or C=NHOR'; Q is CHOH, S, SO or SO2; m is 0, 1 or 2; n is 0 or 1; and pharmaceutically acceptable salts thereof, inhibit the HIV-1 protease and are useful in the treatment of AIDS.