Broadspecturm 2-amino-benzoxazole sulfonamide hiv protease inhibitors

A compound having the formula

• 82
• an N-oxide, salt, stereoisomeric form, racemic mixture, prodrug, ester or metabolite thereof, wherein
• R1 and R8 are, each independently, hydrogen, C1-6alkyl, C2-6alkenyl, arylC1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl, aryl, Het1, Het1C1-6alkyl, Het2, Het2C1-6alkyl;
• R1 may also be a radical of formula
• 83
• wherein
• R9, R10a and R10b are, each independently, hydrogen, C1-4alkyloxycarbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or C1-4alkyl optionally substituted with aryl, Het1, Het2, C3-7cycloalkyl, C1-4alkyloxycarbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, aminosulfonyl, C1-4alkylS(O)t, hydroxy, cyano, halogen or amino optionally mono- or disubstituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-4alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, Het1, Het2, Het1C1-4alkyl and Het1C1-4alkyl;
• whereby R9, R10a and the carbon atoms to which they are attached may also form a C3-7cycloalkyl radical;
• when L is —O—C1-6alkanediyl-C(═O)— or —NR8—C1-6alkanediyl-C(═O)—, then R9 may also be oxo;
• R11a is hydrogen, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, aryl, aminocarbonyl optionally mono- or disubstituted, aminoC1-4alkylcarbonyloxy optionally mono- or disubstituted, C1-4alkyloxycarbonyl, aryloxycarbonyl, Het1oxycarbonyl, Het2oxycarbonyl, aryloxycarbonylC1-4alkyl, arylC1-4alkyloxycarbonyl, C1-4alkylcarbonyl, C3-7cycloalkylcarbonyl, C3-7cycloalkyl-C1-4alkyloxycarbonyl, C3-7cycloalkylcarbonyloxy, carboxylC C4alkyl-carbonyloxy, C1-4alkylcarbonyloxy, arylC1-4alkylcarbonyloxy, arylcarbonyloxy, aryloxycarbonyloxy, Het1 carbonyl, Het1carbonyloxy, Het1C1-4alkyloxycarbonyl, Het2carbonyloxy, Het2C1-4alkylcarbonyloxy, Het2C1-4alkyloxycarbonyloxy or C1-4alkyl optionally substituted with aryl, aryloxy, Het2 or hydroxy;
• wherein the substituents on the amino groups are each independently selected from C1-4alkyl, aryl, arylC1-4alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, Het1, Het2, Het1C1-4alkyl and Het2C1-4alkyl;
• R11b is hydrogen, C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl, aryl, Het1, Het2 or C1-4alkyl optionally substituted with halogen, hydroxy, C1-4alkylS(═O)t, aryl, C3-7cycloalkyl, Het1, Het2, amino optionally mono- or disubstituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, Het1, Het2, Het1C1-4alkyl and Het2C1-4alkyl;
• whereby R11b may be linked to the remainder of the molecule via a sulfonyl group;
• t is, each independently, zero, 1 or 2;
• R2 is hydrogen 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 whereby either the C(═O) group or the S(═O)2 group is attached to the NR2 moiety;
• whereby the C1-6alkanediyl moiety is optionally substituted with a substituent selected from hydroxy, aryl, Het1 and Het2 R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl R4 is hydrogen, C1-4alkyloxycarbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl, or C1-6alkyl optionally substituted with one or more substituents each independently selected from aryl, Het1, Het2, C3-7cycloalkyl, C1-4alkyloxycarbonyl, carboxyl, aminocarbonyl, mono- or di(C1-4alkyl)aminocarbonyl, aminosulfonyl, C1-4alkyl S(═O)t, hydroxy, cyano, halogen and amino optionally mono- or disubstituted where the substituents are each independently selected from C1-4alkyl, aryl, arylC1-4alkyl, C3-7cycloalkyl, C3-7cycloalkyl-C1-4alkyl, Het1, Het2, Het1C1-4alkyl and Het2C1-4alkyl;
• R5 is hydrogen or C1-6alkyl;
• R6 is hydrogen or C1-6alkyl.