Broadspectrum substituted oxindole sulfonamide HIV protease...

Details Broadspectrum substituted oxindole sulfonamide HIV protease... Broadspectrum substituted oxindole sulfonamide HIV protease...

2007-04-03

2007-04-03

McKane, Joseph K. (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C514S444000, C514S461000, C514S465000, C548S487000, C548S469000, C548S518000, C548S516000, C549S060000, C549S465000

Reexamination Certificate

active

10524451

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;R5aand R5bis C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or C1-6alkyl, optionally substituted on one or more atoms; R5aand R5bmay also be hydrogen, aryl, Het1, Het2; R6is hydrogen or C1-6alkyl optionally substituted on one ore more carbon atoms. 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: 0499299 (1992-08-01), None
patent: 0499299 (1992-08-01), None
patent: 0721331 (1996-07-01), None
patent: WO 94/05263 (1994-03-01), None
patent: WO 95/06030 (1995-03-01), None
patent: WO 95/09615 (1996-04-01), 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 99/33792 (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 99/65870 (1999-12-01), None
patent: WO 99/67254 (1999-12-01), None
patent: WO 99/67417 (1999-12-01), None
patent: WO 01/72708 (2001-10-01), None
Goodman, et al., “Biotransformation of Drugs”, The Pharmacological Basis of Therapeutics, p. 13-18, 8thEdition, 1990.
Hertogs, 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, vol. 42, (1998) pp. 269-276.
Augustijns, 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. 44-54.
International Search Report mailed Nov. 26, 2003 for PCT/EP03/50379.

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