EP 0641306 A1 19950308 - CARBOCYCLIC AND HETEROCYCLIC HIV PROTEASE INHIBITORS.
Title (en)
CARBOCYCLIC AND HETEROCYCLIC HIV PROTEASE INHIBITORS.
Title (de)
CARBOCYCLISCHE UND HETEROCYCLISCHE HIV-PROTEASE-LUHIBITOREN.
Title (fr)
INHIBITEURS CARBOCYCLIQUES ET HETEROCYCLIQUES DE LA PROTEASE DU HIV.
Publication
Application
Priority
- US 9204705 W 19920604
- US 71073491 A 19910604
Abstract (en)
[origin: WO9221647A1] 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(=NR<7>)NHR''; R7 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'', CF3 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.
IPC 1-7
C07C 69/757; C07C 49/497; C07C 35/06; C07D 333/48; C07D 335/02; A61K 31/215; A61K 31/045; A61K 31/12; A61K 31/38
IPC 8 full level
A61K 31/045 (2006.01); A61K 31/12 (2006.01); A61K 31/215 (2006.01); A61K 31/38 (2006.01); A61K 31/381 (2006.01); A61K 31/382 (2006.01); A61P 31/12 (2006.01); C07C 35/21 (2006.01); C07C 45/59 (2006.01); C07C 49/497 (2006.01); C07C 49/747 (2006.01); C07C 67/313 (2006.01); C07C 69/757 (2006.01); C07D 333/48 (2006.01); C07D 335/02 (2006.01)
CPC (source: EP)
A61P 31/12 (2017.12); C07C 35/21 (2013.01); C07C 45/59 (2013.01); C07C 49/747 (2013.01); C07C 69/757 (2013.01); C07D 333/48 (2013.01); C07D 335/02 (2013.01)
Citation (search report)
See references of WO 9221647A1
Designated contracting state (EPC)
AT BE CH DE DK ES FR GB GR IT LI LU MC NL SE
DOCDB simple family (publication)
WO 9221647 A1 19921210; EP 0641306 A1 19950308; JP H06508146 A 19940914
DOCDB simple family (application)
US 9204705 W 19920604; EP 92914474 A 19920604; JP 50065393 A 19920604