Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2002-05-10
2009-11-24
Stockton, Laura L. (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C548S222000
Reexamination Certificate
active
07622490
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)—, —C1-6alkanediyl-C(═O)—, —NR8—C1-6alkanediyl-C(═O)—, —S(═O)2—, —O—S(═O)2—, —NR9-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: 0445926 (1991-09-01), None
patent: 0499299 (1992-08-01), None
patent: 0721331 (1996-07-01), None
patent: WO 9405263 (1994-03-01), None
patent: WO-95/06030 (1995-03-01), None
patent: WO 9506030 (1995-03-01), None
patent: WO 9622287 (1996-07-01), None
patent: WO-96/28463 (1996-09-01), None
patent: WO 9628418 (1996-09-01), None
patent: WO 9628463 (1996-09-01), None
patent: WO 9628464 (1996-09-01), None
patent: WO 9628465 (1996-09-01), None
patent: WO 9718205 (1997-05-01), None
patent: WO 9744014 (1997-11-01), None
patent: WO 9842318 (1998-10-01), None
patent: WO 9910326 (1999-03-01), None
patent: WO 9933792 (1999-07-01), None
patent: WO 9933793 (1999-07-01), None
patent: WO 9933795 (1999-07-01), None
patent: WO 9933815 (1999-07-01), None
patent: WO 9967254 (1999-12-01), None
patent: WO 9967417 (1999-12-01), None
Dunn et al., Genome Biology, Mar. 2002, 3(4), pp. 1-7.
Souillac, et al., Characterization of Delivery Systems, Differential Scanning Calorimetry in Encyclopedia of Controlled Drug Delivery, 1999, John Wiley & Sons, pp. 212-227.
Vippagunta et al., Advanced Drug Delivery Reviews, 48 (2001), pp. 3-26.
Benet, L. et al., “Pharmacokinetics: The Dynamics of Drug Absorption, Distribution, and Elimination.”,Goodman and Gilman's The Pharmacological Basis of Therapeutics, Eighth Edition, 1992, pp. 13-18, McGraw-Hill Inc.
Cross, et al., “Rules For The Nomenclature of Organic Chemistry, Section E: Stereochemistry.”Pure&Applied Chemistry, 1976, pp. 13-30, vol. 45., Pergamon Press, Great Britain.
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 Isolates from Patients Treated with Antiretroviral Drugs.”,Antimicrobial Agents and Chemotherapy, Feb. 1998, pp. 269-276, vol. 42, No. 2.
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 166, (1998), pp. 45-53.
Pauwels, R. at al., “Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds”, Journal of Virological Methods, 20, (1988), pp. 309-321.
PCT Intl. Search Recport, PCT/EP2002/05212, Sep. 2, 2002.
De Bethune Marie-Pierre T. M. M. G
De Kock Herman Augustinus
Surleraux Dominique Louis Nestor Ghislain
Tahri Abdellah
Vendeville Sandrine Marie Helene
Stockton Laura L.
Tibotec Pharmaceuticals Ltd.
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