Patent ID: 7109230
Filing Date: 2006-09-19
Classification: A61K,A61P,C07D,C07K,C12N,G16B,G16C,Y02A

Abstract:
1. An HIV protease inhibitor represented by a formula: wherein X is a 5-7 membered non-aromatic monocyclic heterocycle, wherein said heterocycle is fused or bridged with one or more 3-7 membered non-aromatic monocyclic heterocycle to form a polycyclic system, wherein any of said heterocyclic ring systems contains one or more heteroatoms selected from O and S; wherein any sulfur may be optionally be substituted by one or two oxygen atoms; and wherein any of said ring systems optionally contains 1 to 6 substituents selected from the group consisting of R2, R3, R5, and R6; A is OCONH or CONH; B is  wherein D is aralkyl optionally substituted with one or more groups selected from alkyl, halo, nitro, cyano, CF A′ is N(D′)E′, wherein D′ is selected from alkyl, alkenyl, alkynyl, aryl, cycloalkyl, and aralkyl, optionally, substituted by alkyl, halo, nitro, cyano, CF  and E′ is —SO X′ is  wherein R is selected from the group consisting of H, alkyl, aryl, alkenyl,alkynyl, cycloalkyl, and cycloalkenyl, optionally substituted by halo, hydroxy, alkoxy, aryloxy, cycloallcoxy, cyano, nitro, alkylthio, arylthio, cycloalkylthio, amino, or mono- or dialkylamino, mono- or diarylamino, mono- or di-cycloalkylamino, alkanoyl, cycloalkanoyl, aroyl, carboxamido, mono- or dialkylcarboxamido, mono- or diarylcarboxainido, sulfonamido, mono- or dialkylsulfonamido, mono- or diarylsulfonamido, alkylsulfinyl, alkylsulfonyl, arylsulfinyl, arylsulfonyl, cycloalkylsulfinyl, and cycloalkylsulfonyl; R2 is H or C1-C6 alkyl; optionally substituted by C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, or C5-C8 cycloalkenyl; which groups may be optionally substituted with one or more substituents selected from the group consisting of halo, OR, ROH, R-halo, NO2, CN, CO R3 is selected from the grouy consisting of C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, and C5-C8 cycloalkenyl; which groups may be optionally substituted with one or more substituents selected from the group consisting of halo, OR2, R2—OH, R2-halo, NO R4 is selected from the group consisting of halo, OR8, R2—OH, R3—OH, R2-halo, R3-halo, NO R5 is selected from the group consisting of OR8, N(R8) R6 is aryl wherein said aryl may be optionally substituted with one or more groups selected from aryl, R2, R3, halo, OR2, R2OH, R2-halo, NO R7 is selected from the group consisting of C(O) R8 is R2, R3, or R6; each n is independently 1 or 2; its stercoisomeric forms; and its pharmacologically acceptable salts.