Global Patent Index - EP 1063888 A1

EP 1063888 A1 2001-01-03 - 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 (EN)

Application

EP 99915065 A

Priority

  • US 9906700 W
  • US 7976498 P
  • US 9320898 P

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 (main, further and additional classification)

A01N 43/42; A01N 37/10; A01N 43/04

IPC 8 full level (invention and additional information)

A61K 45/06 (2006.01)

CPC (invention and additional information)

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

EPO simple patent family

WO 9948371 A1 19990930; AU 3366899 A 19991018; EP 1063888 A1 20010103

INPADOC legal status


2006-05-03 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20051001

2001-01-03 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20001027

2001-01-03 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE