2 - amino - benzoxazole sulfonamide inhibitors of wide spectrum of HIV Protease, Pharmaceutical Composition and Method for inhibiting in vitro retroviral Replication, and use of these compounds in the manufacture of medicinal products

摘要

2-amine-benzo-p-sulfosamide (1),Nitrous oxide, salt, stereoisomer form, racemic mixture, by-product, ester or its metabolite, wherein R1 and R8 are independent,Hydrogen, C1-6 tar, c12-6 alquenilo C1-6, arilalquilo C1-6, cycloquilo c3-7, cycloquil c3-7, cycloquil C1-6, arilo, het1-tar C1-6, het2 or het2-tar C1-6; R1 may also be a (r11a) (r11b) N-C (r10a) (r10b) - ch9 - wherein R9, r10a and 10r10b are independent of each other,hydrogen, C1-4 alkyloxycarbonyl, carboxyl, aminocarbonyl, mono- or di (C1-4 alkyl) aminocarbonyl, C3-7 cycloalkyl, C2-6 alkenyl, C2-6 alkynyl, or C1-4 alkyl optionally substituted with aryl, Het1, Het2, C3-7 cycloalkyl, C1-4 alkyloxycarbonyl, carboxyl, aminocarbonyl, mono- or di (C1-4 alkyl) aminocarbonyl, aminosulfonyl, C1-4S (O) t alkyl, hydroxy, cyano, halogen or optionally mono- or amino disubstituted, where the substituents are selected, independently of each other,from the group consisting of C1-4 alkyl, aryl, C1-4 arylalkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-4 alkyl, Het1, Het2, Het1-C1-4 alkyl and Het2-C1-4 alkyl; whereby R9, R10a and the carbon atoms to which they are attached can also form a C3-7 cycloalkyl radical; when L is -O-C1-6-C-alkanediyl (= O) - or -NR8-C1-6-C-alkanediyl (= O) -,then R9 can also be oxo; R11a is hydrogen, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, aryl, optionally mono- or disubstituted aminocarbonyl, optionally mono- or disubstituted C1-4 -alkylcarbonyloxy, C1-4 alkyloxycarbonyl, aryloxycarbonyl, Het1-oxycarbonyl, Het2 -oxycarbonyl, C 1-4 aryloxycarbonylalkyl, C 1-4 aryl alkoxycarbonyl, C 1-7 alkylcarbonyl, C 3-7 cycloalkylcarbonyl, C 3-7 cycloalkylcarbonyloxy, C 1-4 cycloalkylcarbonyloxy, C 1-4 alkylcarbonyloxy, C1-4, arylcarbonyloxy, aryloxycarbonyloxy, Het1-carbonyl, Het1-carbonyloxy, Het1-C1-4 alkyloxycarbonyl, Het2-carbonyloxy,Het2-c1-4 C1-4, het2-c1-4, C1-4, C1-4 or C1-4 tar is optionally replaced with ariloxi, ariloxi, het2, halogen or hydroxy; in these substances, the alternatives in the amino group are independently selected,del grupo formado por alquilo C1-4 arilo arilalquilo C1-4 cicloalquilo C3-7 cicloalquil C3-7 alquilo C1-4 Het1 Het2 Het1-alquilo C1-4 y Het2-alquilo C1-4 R11b es hidr geno cicloalquilo C3-7 alquenilo C2 1. From the tar groups of C1-4, arilo, arilalquilo C1-4, cycloquilo c3-7, cycloquil c3-7, cycloquil c3-7, C1-4, het1, het2, het1-c1-4 and het2-c1-4, r11b can be combined with other molecules through a sulfur group; t is independent, 0, 1 or 2; R2 is hydrogen or C1-6; L is - C (= O)-O-C (3DO) --NR8-C (O) -,-O-alkane c1-6-c (= O) -,-Nr8 alkane c1-6-c (= O) -,-S (3DO) 2--O-S (3DO) 2--Nr8-s (= O) 2, wherein group C (= O) or group s (= O) 2 is associated with NR2 fraction; therefore, C1-6 alkane fraction can be replaced by hydroxyl, arilo, het1 and het2; R3 is C1-6, arilo, cyclo-7, cyclo-7, cycloquil c3-7 C1-4 or arilalquilo C1-4; R4 is C14, carbon chloride, hydrocarbon, C14. 1. Tar of carbamate, thyroid carbamate, thyroid c3-7, acrylonitrile c2-6 or C1-6, which is selectively replaced by one or more alternative substitutes;Substitutes consisting of arilo, het1, het2, cycloquilo c3-7, C1-4, C1-4, carboxyl, aminobonilo, mono-o di (C1-4 tar) aminobenzene, aminosulfonilo, C1-4 tar s (= O) t, hydroxi, Ciano, halogen and any single monkey - or discustuido are selected independently,A group consisting of C1-4, arilo, arilalquilo C1-4, cichoil quilo c3-7, cichoil quil c3-7, C1-4 tar, het1, het2, het1-c1-4 and het2-tar C1-4; R5 is hydrogen or C1-6 tar; R6 is hydrogen or C1-6 tar; pharmaceutical composition, "In vitro" inhibition of antiretroviral replication and use of these compounds in drug manufacture. Formula compound (1) is used as an inhibitor of asarctic proteome, especially HIV proteome, so it has an inhibitory effect on HIV.