Global Patent Index - EP 1039886 A4

EP 1039886 A4 2001-05-16 - HIV/FIV PROTEASE INHIBITORS HAVING A SMALL P3 RESIDUE

Title (en)

HIV/FIV PROTEASE INHIBITORS HAVING A SMALL P3 RESIDUE

Title (de)

EIN KLEINER P3 REST AUFWEISENDE HIV/FIV PROTEASE HEMMER

Title (fr)

INHIBITEURS DE PROTEASES DE VIH/VIF PRESENTANT UN PETIT RESTE P3

Publication

EP 1039886 A4 (EN)

Application

EP 98963800 A

Priority

  • US 9825964 W
  • US 6795997 P

Abstract (en)

[origin: WO9929311A1] With the help of X-ray structural analyses of drug-resistant HIV proteases and molecular modeling, a new type of inhibitor with a small P3 residue has been developed. These inhibitors are effective against HIV and its drug-resistant mutants, as well as FIV. Modification of existing HIV protease inhibitors by reducing the size of the P3 residue has the same effect. This finding provides a new strategy for the development of HIV protease inhibitors effective against the wild type and drug-resistant mutants and further supports that FIV protease is a useful model for drug-resistant HIV proteases, which often are developed through reduction in size of the binding region for the P3 group or the combined P3 and P1 groups.

IPC 1-7 (main, further and additional classification)

A61K 31/045; A61K 31/13; A61K 31/135; A61K 31/165; A61K 31/38; A61K 31/405; A61K 31/47; A61K 38/05; C07C 205/02; C07C 211/09; C07C 215/18; C07D 207/16; C07D 217/16; C07D 217/26; C07D 277/24; C07D 277/28; C07K 5/062; C07K 5/065

IPC 8 full level (invention and additional information)

C07D 207/16 (2006.01); C07D 213/40 (2006.01); C07D 217/26 (2006.01); C07D 277/24 (2006.01); C07D 277/28 (2006.01); C07D 401/12 (2006.01); C07K 5/06 (2006.01); C07K 5/062 (2006.01); C07K 5/065 (2006.01); A61K 38/00 (2006.01)

CPC (invention and additional information)

C07D 213/40 (2013.01); C07D 207/16 (2013.01); C07D 217/26 (2013.01); C07D 277/28 (2013.01); C07D 401/12 (2013.01); C07K 5/06026 (2013.01); C07K 5/06043 (2013.01); C07K 5/06052 (2013.01); C07K 5/0606 (2013.01); C07K 5/06069 (2013.01); C07K 5/06078 (2013.01); A61K 38/00 (2013.01)

Citation (search report)

  • [X] WO 9721100 A1 19970612 - SCRIPPS RESEARCH INST [US], et al
  • [X] WO 9206996 A1 19920430 - UPJOHN CO [US]
  • [X] WO 9200948 A1 19920123 - SMITHKLINE BEECHAM CORP [US]
  • [X] SLEE D H ET AL: "SELECTIVITY IN THE INHIBITION OF HIV AND FIV PROTEASE:INHIBITORY AND MECHANISTIC STUDIES OF PYRROLIDINE-CONTAINING ALPHA-KETO AMIDE AND HYDROXYETHYLAMINE CORE STRUCTURES", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY,US,AMERICAN CHEMICAL SOCIETY, WASHINGTON, DC, vol. 117, no. 48, 6 December 1995 (1995-12-06), pages 11867 - 11878, XP000647306, ISSN: 0002-7863
  • [X] ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, vol. 35, no. 11, 1991, pages 2209 - 2214, XP000983237
  • [X] BUDT, K-H, ET AL.: "HIV protease inhibitor HOE/BAY 793, structure-activity relationships in a series of C2-symmetric diols", BIORG. MED. CHEM., vol. 3, no. 5, 1995, pages 5559 - 571, XP000983261
  • See also references of WO 9929311A1

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 9929311 A1 19990617; AU 1904599 A 19990628; EP 1039886 A1 20001004; EP 1039886 A4 20010516

INPADOC legal status


2009-07-17 [REG HK WD] APPLICATIONS WITHDRAWN, DEEMED TO BE WITHDRAWN, OR REFUSED AFTER PUBLICATION IN HONG KONG

- Document: HK 1032907

2008-11-26 [18D] APPLICATION DEEMED TO BE WITHDRAWN

- Effective date: 20080429

2007-05-30 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20050224

2005-04-13 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20050224

2001-05-16 [A4] DESPATCH OF SUPPLEMENTARY SEARCH REPORT

- Effective date: 20010402

2001-05-16 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A4

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

2000-11-08 [RAP1] TRANSFER OF RIGHTS OF AN APPLICATION

- Owner name: THE SCRIPPS RESEARCH INSTITUTE

2000-10-04 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 20000710

2000-10-04 [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

2000-10-04 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO:

- Free text: AL PAYMENT 20000710;LT PAYMENT 20000710;LV PAYMENT 20000710;MK PAYMENT 20000710;RO PAYMENT 20000710;SI PAYMENT 20000710