Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C548S222000

Reexamination Certificate

active

07863306

ABSTRACT:
The present invention concerns the compounds having the formulaN-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1and R8each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2is H or C1-6alkyl; L is —C(═O)—, —O—C(═O)—, —NR8—C(═O)—, —O—C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR8—S(═O)2; R3is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4is H, C1-4alkylOC(═O), carboxyl, aminoC(═O), mono- or di(C1-4alkyl)aminoC(═O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5and R6are H or C1-6alkyl. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.

REFERENCES:
patent: 0103553 (1989-02-01), None
patent: 0445926 (1996-08-01), None
patent: 0499299 (2000-08-01), None
patent: 0721331 (2001-12-01), None
patent: WO 94/05263 (1994-03-01), None
patent: WO 95/06030 (1995-03-01), None
patent: WO 96/22287 (1996-07-01), None
patent: WO 96/28418 (1996-09-01), None
patent: WO 96/28463 (1996-09-01), None
patent: WO 96/28464 (1996-09-01), None
patent: WO 96/28465 (1996-09-01), None
patent: WO 97/18205 (1997-05-01), None
patent: WO 97/44014 (1997-11-01), None
patent: WO 98/42318 (1998-10-01), None
patent: WO 99/10326 (1999-03-01), None
patent: WO 99/33792 (1999-07-01), None
patent: WO 99/33793 (1999-07-01), None
patent: WO 99/33795 (1999-07-01), None
patent: WO 99/33815 (1999-07-01), None
patent: WO 99/67254 (1999-12-01), None
patent: WO 99/67417 (1999-12-01), None
Augustijns, P., et al. “Drug Absorption Studies of Prodrug Esters Using the Caco-2 Model: Evaluation of Ester Hydrolysis and Transepithelial Transport”, International Journal of Pharmaceutics, vol. 166 pp. 45-53 (1998).
Benet, L., et al. “Pharmacokinetics: The Dynamics of Drug Absorption, Distribution, and Elimination”, Goodman and Gilman's The Pharmacological Basis of Therapeutics, Eighth Edition pp. 13-18 (1992).
Cross, L., et al. “Rules For The Nomenclature of Organic Chemistry, Section E: Sterochemistry”, Pure & Applied Chemistry pp. 13-30 vol. 45 (1976).
Dunn, B, et al. “Retroviral Proteases”, Genome Biology Review 3(4) pp. 1-7 (2002).
Hertogs, K., et al. “A Rapid Method for Simultaneous Detection of Phenotypic Resistance to Inhibitors of Protease and Reverse Transcriptase in Recombinant Human Immunodeficiency Virus Type 1 Isolate sfrom Patients Treated With Antiretroviral Drug”, Antimocribial Agents and Chemotherapy, pp. 269-276 (1998).
Pauwels, R., et al. “Rapid and Automated Tetrazolium-Based Colorimetric Assay for the Detection of Anti-HIV Compound”, Journal of Virological Methods, pp. 309-321 (1988).
Souillac, P., et al. “Characterizatoin of Delivery Systems, Differential Scanning Calorimetry in Engyclopedia of Controlled Drug Delivery”, John Wiley & Sons, pp. 212-227 (1999).
Vippagunta, S., et al. “Crystalline Solids”, Advanced Drug Delivery Reviews, 48 pp. 3-26 (2001).
International Search Report for International Application No. PCT/EP2002/005212, mailed Sep. 2, 2002.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Broadspectrum 2-amino-benzoxazole sulfonamide HIV protease... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-2663850

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.