Patent ID: 7285566
Filing Date: 2007-10-23
Classification: C07K,C12N,G16B

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, N, S, or P; wherein any nitrogen forming part of the heterocycles may optionally be substituted by R2, R3, R6, R7 or O; wherein any sulfur may be optionally be substituted by one or two oxygen atoms; wherein any P may be optionally be substituted by one or more of O NR2, or S, and any of said ring systems optionally contains 1 to 6 substituents selected from the group consisting of R2, R3, R5, and R6; A is ZCZNH, wherein Z is; B is wherein D is selected from alkyl, alkenyl, alkynyl, aryl, cycloalkyl, or 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, or aralkyl optionally substituted by alkyl, halo, nitro, cyano, CF X′ is selected from the group consisting of (a)  wherein said groups are substituted with one or more of the following groups: wherein G′ and R′ cannot both be H; G′ and R′ are each independently: and X″ is selected from O or NR″; SO S(O) wherein B′ and B″ cannot both be H or methyl; B′ and B″ are independently: wherein U and U′ are each independently U″ and U′″ are each independently U and U′ cannot both be H unless one of U″ and U′″ is not H; U″ and U′″ cannot both be H unless one of U and U′ is not H; M′ is O, NR9, or NH, except where R9 is CO Z′″ is O or NR9 Q′ is O, NR9, or CU″U′″; R9 is CO wherein R is H or alkyl, aryl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclo, heteroaryl; optionally substituted by halo, hydroxy, alkoxy, aryloxy, cycloalkoxy, heteroaryloxy, cyano, nitro, alkylthio, arylthio, cycloalkylthio, amino, or mono- or dialkylamino, mono- or diarylamino, mono- or di-cycloalkylamino, mono- or di- heteroarylamino, alkanoyl, cycloalkanoyl, aroyl, heteroaroyl, carboxamido, mono- or dialkylcarboxamido, mono- or diarylcarboxamido, sulfonamido, mono- or dialkylsulfonamido, mono- or diarylsulfonamido, alkylsulfinyl, alkylsulfonyl, arylsulfinyl, arylsulfonyl, cycloalkylsulfinyl, cycloalkylsulfonyl, heteroarylsulfinyl, heteroarylsulfonyl; R2 is H or C1-C6 alkyl; optionally substituted by C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C5-C8 cycloalkenyl, heterocyclo; which groups may be optionally substituted with one or more substituents selected from the group consisting of halo, OR, ROH, R-halo, NO R3 is C2-C6 alkenyl, C2-C6 alkynyl, C3-C8 cycloalkyl, C5-C8 cycloalkenyl, or heterocyclo; 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 halo, OR8, R2-OH, R3-OH, R2-halo, R3-halo, NO R5 is OR8, N(R8) R6 is aryl or heteroaryl, wherein said aryl or heteroaryl may be optionally substituted with one or more groups selected from aryl, heteroaryl, R2, R3, halo, OR2, R2OH, R2-halo, NO R7 is C(O) R8 is R2, R3, or R6; each n is independently 1 or 2; its stereoisomeric forms; and its pharmacologically acceptable salts.