Title:
BROADSPECTRUM 2-(SUBSTITUTED-AMINO)-BENZOTHIAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS
Document Type and Number:
WIPO Patent Application WO2002083657
Kind Code:
A3
Abstract:
The present invention concerns the compounds having the formula (I), N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R>1< and R>8< each are H, optionally substituted C>1-62<-6alkenyl, C>3-7, Het<2>; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C(=O)-, -O-C(=O)-, -NR8-C(=O)-, -O-C1-6alkanediyl-C(=O)-, -NR8-C1-62-<, -NR8-S(=O)>2<; R3 is C>1-63-73-71-41-44< is H, C>1-41-43-72-62-61-61-62-<, C>1-61-61-62-<; R>5< is H, OH, C>1-6C1-6alkyl, Het<2>C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het<1>, Het<1O>, Het<2>, Het<2>O, aryl, arylO, C1-6alkyloxycarbonylamino or amino; and in case -A- is other than C1-6alkanediyl then R<6> may also be C1-6alkyl, Het<1>C1-4alkyl, Het<1>OC1-4alkyl, Het<2>C1-4alkyl, Het<2>OC1-4alkyl, arylC1-4alkyl, arylOC1-4alkyl or aminoC1-4alkyl; whereby each of the amino groups in the definition of R<6> may optionally be substituted; R<5> and -A-R<6> taken together with the nitrogen atom to which they are attached may also form Het<1> or Het<2>. 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.
Inventors:
SURLERAUX DOMINIQUE LOUIS NEST (BE)
WIGERINCK PIET TOM BERT PAUL (BE)
GETMAN DANIEL (US)
VERSCHUEREN WIM GASTON (BE)
VENDEVILLE SANDRINE (BE)
DE BETHUNE MARIE-PIERRE (BE)
DE KERPEL JAN OCTAAF ANTOON (BE)
MOORS SAMUEL LEO CHRISTIAAN (BE)
DE KOCK HERMAN AUGUSTINUS (BE)
VOETS MARIEKE CHRISTIANE JOHAN (BE)
WIGERINCK PIET TOM BERT PAUL (BE)
GETMAN DANIEL (US)
VERSCHUEREN WIM GASTON (BE)
VENDEVILLE SANDRINE (BE)
DE BETHUNE MARIE-PIERRE (BE)
DE KERPEL JAN OCTAAF ANTOON (BE)
MOORS SAMUEL LEO CHRISTIAAN (BE)
DE KOCK HERMAN AUGUSTINUS (BE)
VOETS MARIEKE CHRISTIANE JOHAN (BE)
Application Number:
PCT/EP2002/001788
Publication Date:
February 13, 2003
Filing Date:
February 14, 2002
Export Citation:
Assignee:
TIBOTEC PHARM LTD (IE)
SURLERAUX DOMINIQUE LOUIS NEST (BE)
WIGERINCK PIET TOM BERT PAUL (BE)
GETMAN DANIEL (US)
VERSCHUEREN WIM GASTON (BE)
VENDEVILLE SANDRINE (BE)
DE BETHUNE MARIE-PIERRE (BE)
DE KERPEL JAN OCTAAF ANTOON (BE)
MOORS SAMUEL LEO CHRISTIAAN (BE)
DE KOCK HERMAN AUGUSTINUS (BE)
VOETS MARIEKE CHRISTIANE JOHAN (BE)
SURLERAUX DOMINIQUE LOUIS NEST (BE)
WIGERINCK PIET TOM BERT PAUL (BE)
GETMAN DANIEL (US)
VERSCHUEREN WIM GASTON (BE)
VENDEVILLE SANDRINE (BE)
DE BETHUNE MARIE-PIERRE (BE)
DE KERPEL JAN OCTAAF ANTOON (BE)
MOORS SAMUEL LEO CHRISTIAAN (BE)
DE KOCK HERMAN AUGUSTINUS (BE)
VOETS MARIEKE CHRISTIANE JOHAN (BE)
International Classes:
A61K31/428; A61K31/4439; A61K31/496; A61K31/5377; A61P31/14; A61P31/18; A61P43/00; C07D277/82; C07D417/12; C07D493/04; (IPC1-7): C07D277/82; A61K31/428; C07D493/04; C07D401/12; C07D417/12; A61P31/18
Domestic Patent References:
| WO1999065870A2 | 1999-12-23 | |||
| WO1996028463A1 | 1996-09-19 | |||
| WO1995006030A1 | 1995-03-02 |
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