Global Patent Index - EP 1063888 A1

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

EP 1063888 A1 20010103 (EN)

Application

EP 99915065 A 19990326

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

A01N 43/42; A01N 37/10; A01N 43/04

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