EP 1063888 A1 20010103 - NOVEL HIV INTEGRASE INHIBITORS AND HIV THERAPY BASED ON DRUG COMBINATIONS INCLUDING INTEGRASE INHIBITORS
Title (en)
NOVEL HIV INTEGRASE INHIBITORS AND HIV THERAPY BASED ON DRUG COMBINATIONS INCLUDING INTEGRASE INHIBITORS
Title (de)
NEUE HIV INTEGRASE INHIBITOREN UND AUF INTEGRASE INHIBITOREN EINSCHLIESSENDE MEDIKAMENTZUSAMMENSETZUNGEN BASIERTE HIV-THERAPIE
Title (fr)
NOUVEAUX INHIBITEURS DE VIH INTEGRASE ET TRAITEMENT DU VIH FONDE SUR DES COMBINAISONS DE MEDICAMENTS CONTENANT DES INHIBITEURS D'INTEGRASE
Publication
Application
Priority
- US 9906700 W 19990326
- US 7976498 P 19980327
- US 9320898 P 19980717
Abstract (en)
[origin: WO9948371A1] The present invention includes a group of novel compounds that are demonstrated to potently and selectively inhibit HIV integrase (IN) activity in vitro and to potently inhibit HIV replication in live, cultured cells at non-toxic concentrations. The novel compounds disclosed include 2,3 -di(3,4- dihydroxydihydroxydihydrocinnamoyl) -L-tartaric acid, 2,3 -di-(3,4-dihydroxybenzoyl) -L-tartaric acid, 2,3 -di-(3,4 -dihydroxyphenylacetyl) -L-tartaric acid , 2,3 -di-(3,4,5 -trihydroxybenzoyl -L-tartaric acid, 2,3-dicaffeoyldiamidopropionic acid, 1,2,-dicaffeoyl -L-glyceric acid, bis, -3,4 -dicaffeoyldiamidobenzoic acid, di-3,4 -dihydroxybenzylidene succinic acid, di-3,4 -dihydrodihydroxybenzylidine succinic acid, 2,3 -dicaffeoyl-L-serine, bis-dicaffeoyl -L-isoserine and 1,4-dicaffeoyl -L-lysine. Tests of integrase inhibitors with 2',3'-dideoxycytidine, zidovudine and nelfinavir (protease inhibitor) indicated a potent synergy against reverse transcriptase inhibitor resistant virus. The potential benefit from the addition of integrase inhibitors to combination drug therapies is significant.
IPC 1-7
IPC 8 full level
A61K 45/06 (2006.01)
CPC (source: EP)
A61K 45/06 (2013.01)
Citation (search report)
See references of WO 9948371A1
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9948371 A1 19990930; AU 3366899 A 19991018; EP 1063888 A1 20010103
DOCDB simple family (application)
US 9906700 W 19990326; AU 3366899 A 19990326; EP 99915065 A 19990326