Tibotec Pharmaceuticals Ltd.

Daniel Getman

Herman Augustinus De Kock

Wim Gaston Verschueren

Dominique Louis Nestor Ghislain Surleraux

Piet Tom Bert Paul Wigerinck

Sandrine Vendeville

Jan Octaaf Antoon De Kerpel

Samuel Leo Christiaan Moors

Marieke Christiane Johanna Voets

Marie-Pierre De Bethune

The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein Rand Reach are H, optionally substituted Calkyl, Calkenyl, Ccycloalkyl, aryl, Het, Het; Rmay also be a radical of formula (RR)NC(RR)CR&#x2014;; t is 0, 1 or 2; Ris H or Calkyl; L is &#x2014;C(&#x2550;O)&#x2014;, &#x2014;O&#x2014;C(&#x2550;O)&#x2014;, &#x2014;NR&#x2014;C(&#x2550;O)&#x2014;, &#x2014;O&#x2014;Calkanediyl-C(&#x2550;O)&#x2014;, &#x2014;NR&#x2014;Calkanediyl-C(&#x2550;O)&#x2014;, &#x2014;S(&#x2550;O)&#x2014;, &#x2014;O&#x2014;S(&#x2550;O)&#x2014;, &#x2014;NR&#x2014;S(&#x2550;O); Ris Calkyl, aryl, Ccycloalkyl, CcycloalkylCalkyl, or arylCalkyl; Ris H, CalkylOC(&#x2550;O), carboxyl, aminoC(&#x2550;O), mono- or di(Calkyl)aminoC(&#x2550;O), Ccycloalkyl, Calkenyl, Calkynyl or optionally substituted Calkyl; A is Calkanediyl, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;C(&#x2550;S)&#x2014;, &#x2014;S(&#x2550;O)&#x2014;, Calkanediyl-C(&#x2550;O)&#x2014;, Calkanediyl-C(&#x2550;S)&#x2014; or Calkanediyl-S(&#x2550;O)&#x2014;; Ris H, OH, Calkyl, HetCalkyl, HetCalkyl, optionally substituted aminoCalkyl; Ris CalkylO, Het, HetO, Het, HetO, aryl, arylO, Calkyloxycarbonylamino or amino; and in case &#x2014;A&#x2014; is other than Calkanediyl then Rmay also be Calkyl, HetCalkyl, HetOCalkyl, HetCalkyl, HetOCalkyl, arylCalkyl, arylOCalkyl or aminoCalkyl; whereby each of the amino groups in the definition of Rmay optionally be substituted; Rand &#x2014;A&#x2014;Rtaken together with the nitrogen atom to which they are attached may also form Hetor Het. 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.

Broad spectrum 2-(substituted-amino)-benzothiazole sulfonamide HIV protease inhibitors

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Chesterfield, MI, United States of America

Daniel Getman