| 摘要 |
<p>1. A compound of the general formula: wherein: E is O or S; G and G' are independently selected from R<1> or H; Ph is phenylene; D is selected from C(O), C(S) and S(O)2; B' is a saturated, unsaturated or partially saturated monocyclic or bicyclic ring system optionally comprising up to 4 heteroatoms selected from N, O, or S and selected from the formulae: wherein each of Ph and B' optionally comprises up to 3 substituents, wherein: the first of said substituents, if present, is selected from R<1>, R<2>, R<4> or R<5>, the second of said substituents, if present, is selected from R<1> or R<4>, and the third of said substituents, if present, is R<1>; wherein each R<1> is independently selected from 1,2-methylenedioxy, 1,2-ethylenedioxy, R<6> or (CH2)n-Y; wherein n is 0, 1 or 2; and Y is selected from halogen, CN, NO2, CF3, OCF3, OH, SR<6>, S(O)R<6>, SO2R<6>, NH2, NHR<6>, N(R<6>)2, NR<6>R<8>, COOH, COOR<6> or OR<6>; each R<2> is independently selected from (C1-C4)-straight or branched alkyl, or (C2-C4) straight or branched alkenyl or alkynyl; and each R<2> optionally comprises up to 2 substituents, wherein: the first of said substituents, if present, is selected from R<1>, R<4> and R<5> and the second of said substituents, if present, is R<1>; R<3> is selected from monocyclic or bicyclic ring system optionally comprising up to 4 heteroatoms selected from N, O, or S, and wherein CH2 adjacent to said N, O or S maybe substituted with C(O); and each R<3> optionally comprises up to 2 substituents, wherein the first of said substituents, if present, is selected from R<1>, R<2>, R<4> or R<5>, the second of said substituents, if present, is selected from R<1> or R<4>, and the third of said substituents, if present, is R<1>; each R<4> is independently selected from OR<5>, OC(O)R<6>, OC(O)R<5>, OC(O)OR<6>, OC(O)OR<5>, OC(O)N(R<6>)2, OP(O)(OR<6>)2, SR<6>, SR<5>, S(O)R<6>, S(O)R<5>, SO2R<6>, SO2R<5>, SO2N(R<6>)2, SO2NR<5>R6, SO33R<6>, C(O)R<5>, C(O)OR<5>, C(O)R<6>, C(O)OR<6>, NC(O)C(O)R<6>, NC(O)C(O)R<5>, NC(O)C(O)OR<6>, NC(O)C(O)N(R<6>)2, C(O)N(R<6>)2, C(O)N(OR<6>)R<6>, C(O)N(OR<6>)R<5>, C(NOR<6>)R<6>, C(NOR<6>)R<5>, N(R<6>)2, NR<6>C(O)R<1>, NR<6>C(O)R<6>, NR<6>C(O)R<5>, NR<6>C(O)OR<6>, NR<6>C(O)OR<5>, NR<6>C(O)N(R<6>)2, NR<6>C(O)NR<5>R<6>, NR<6>SO2R<6>, NR<6>SO2R<5>, NR<6>SO2N(R<6>)2, NR<6>SO2NR<5>R<6>, N(OR<6>)R<6>, N(OR<6>)R<5>, P(O)(OR<6>)N(R<6>)2, and P(O)(OR<6>)2; each R<5> is a monocyclic or a bicyclic ring system consisting of 5 to 6 members per ring, wherein said ring system optionally comprises up to 4 heteroatoms selected from N, O, or S, and wherein a CH2 adjacent to said N, O or S maybe substituted with C(O); and each R<5> optionally comprises up to 3 substituents, each of which, if present, is R<1>; each R<6> is independently selected from H, (C1-C4)-straight or branched alkyl, or (C2-C4)-straight or branched alkenyl; and each R<6> optionally substituted with R<7>; R<7> is a monocyclic or a bicyclic ring system consisting of 5 to 6 members per ring, wherein said ring system optionally comprises up to 4 heteroatoms selected from N, O, or S, and wherein a CH.sub.2 adjacent to said N, O or S maybe substituted with C(O); and each R<7> optionally comprises up to 2 substituents independently chosen from H, (C1-C4)-straight or branched alkyl, or (C2-C4)-straight or branched alkenyl; 1,2-methylenedioxy, 1,2-ethylenedioxy, or (CH2)n-Z; wherein n is 0, 1 or 2 and Z is selected from halogen, CN, NO2, CF3, OH, S(C1-C4)alkyl, SO(C1-C4)alkyl, SO2(C1-C4)alkyl, NH2, NH(C1-C4)alkyl, N((C1-C4)alkyl)2, N((C1-C4)alkyl)R<8>, COOH, C(O)O(C1-C4)alkyl or O(C1-C4)alkyl; and R<8> is an amino protecting group; and wherein any carbon atom in any R<2> or R<6> may be substituted with O, S, SO, SO2, NH or N(C1-C4)alkyl; wherein if Ph has no additional substituents, and all of said substituents present are on B' are R<1>, then at least one of said R<1> substituents is not chloro, bromo or iodo; and wherein B and B' are not simultaneously unsubstituted phenyl. 2. The compound according to claim 1 having the formula: wherein: K is selected from R<1> and R<4>; and J is selected fromR1, R2, and R4. 3. The compound according to claim 2, wherein D is -C(O)-. 4. The compound according to claim 2, wherein E is oxygen. 5. The compound according to claim 2, wherein J is NR<6>C(O)R<5> or NR<6>C(O)R<6>. 6. The compound according to claim 5, wherein J is NR<6>C(O)R<6>. 7. The compound according to claim 6, wherein J is N(CH3)C(O)R<6>. 8. The compound according to claim 2, wherein K is (CH2)n-Y. 9. The compound according to claim 8, wherein K is OCH3. 10. The compound according to claim 2, wherein G is hydrogen. 11. The compound according to claim 2, wherein: D is -C(O)-; E is oxygen; K is OCH3; and G is hydrogen. 12. The compound according to claim 2, wherein J is R<2>. 13. The compound according to claim 12, wherein E is oxygen. 14. The compound according to claim 12, wherein J is R<2> substituted with R<4>. 15. The compound according to claim 14, wherein R<4> is NR<6>C(O)OR<5> or NR<6>C(O)OR<6>. 16. The compound according to claim 12, wherein K is (CH2)n-Y. 17. The compound according to claim 16, wherein K is OCH3. 18. The compound according to claim 12, wherein: D is -C(O)-; E is oxygen; K is OCH3; and G is hydrogen. 19. The compound according to claim 1, wherein is selected from the group comprising compounds 2-27, 29-31, 39-51, 53-69, 71-86, 88-89, 91-102 and 104-162 as given below in tables IB and IC: Table IB G K B' 2 H H 3-methoxyphenyl 3 H H 3-thienyl 4 H H 3,4-difluorophenyl 5 H H 2,5-dimethoxyphenyl 6 H H 3-methylthiophenyl 7 H H 3-bromophenyl 8 H H 3-cyanophenyl 9 H H 3-trifluoromethyl-4-chlorophenyl 10 H H 2-methyl-3-chlorophenyl 11 H H 2-methoxy-5-methylphenyl 12 H H 2-methoxyphenyl 13 H H 3-methoxyphenyl 14 H H 2,5-dimethoxyphenyl 15 H H 3-nitrophenyl 16 H H 4-nitrophenyl 17 H H 3-methylphenyl 18 H H 3-trifluoromethylphenyl 19 H H 2-trifluoromethylphenyl 20 H H 3-fluorophenyl 21 H H 4-phenoxyphenyl 22 H H 3-chlorophenyl 23 H H 3-chloro-4-fluorophenyl 24 H H 3-aminophenyl 25 H H 3-(hydroxymethyl)phenyl 26 H H 3-acethylenylphenyl 27 H H 3-hydroxyphenyl 29 H H 3-pyridinyl 30 H H 4-pyridinyl 31 H H 2-(5-methyl)thiazolyl 39 H H 3,4-ethylenedioxyphenyl 40 H H 3-methyl-4-nitrophenyl 41 H H 3-trifluoromethyl-4-nitrophenyl 42 H 3-chloro phenyl 43 H 3-chloro 3-methylphenyl 44 - - - 45 H 3-chloro phenyl 46 H 3-fluoro 3-methylphenyl 47 H H 3-carbomethoxymethylphenyl 48 H H 3-carbomethoxyethylphenyl 49 H H 3-dimethlaminophenyl 50 H H 3-[2-(2-methyl)dioxolanyl)phenyle 51 H H 3-aminocarbonylphenyl 53 H H 3-furanyl 54 H H 3-carboxymethylphenyl 55 H 3-methoxy 3-methylphenyl 56 H 3-methoxy 3-nitrophenyl 57 H 3-chloro 3-carbomethoxymethylphenyl 58 H H 3-amino-5-methylphenyl 59 H 3-methoxy 3-aminophenyl 60 H 3-bromo 3-methylphenyl 61 H 3-chloro 3-chloro-4-(5-oxsazolyl)phenyl 62 H 3-chloro 4-(2-methypyridyl)l 63 H 3-chloro 3-carboxymethylphenyl 64 H 3-bromo 3-nitrophenyl 65 H 3-bromo 3-aminophenyl 66 H H 3-[5-(2-methylpyrimidinyl)]phenyl 67 H H 3-(5-oxazolyl)phenyl 68 H 3-chloro 2-thienyl 69 H 3-chloro 3-thienyl 71 H 3-chloro 3-methoxycarbamoylphenyl 72 H 3-chloro 3-acetamidophenyl 73 H 3-chloro 3-iodophenyl 74 H 3-methyl phenyl 75 H 3-methyl 3-methylphenyl 76 3-chloro 3-methylphenyl 77 H 3-methylphenyl 78 H 3-chloro 3-nitrophenyl 79 H 3-chloro 3-aminophenyl 80 H H 3-(cyclohexylsulfamoyl)phenylo 81 H H 3-(methylsulfamoyl)phenyl 82 H H 3-(phenylsulfamoyl)phenyl 83 H 3-methoxy 3-benzyloxycarbamoylphenyl 84 H 3-methoxy 3-acetamodophenyl 85 H 3-chloro 4-(2-methyl)furanyl 86 H 3-chloro 5-(2-methyl)thienyl 88 H 3-carbomethoxy 3-methylphenyl 89 H 3-carbomethoxy 3-nitrophenyl 91 H 3-chloro 4-(2-nitro)thienyl 92 H 3-chloro 4-(2-hydrpxyamino)thienyl 93 H 3-chloro 3-(N-methyl)trifluoroacetamidophenyl 94 H 3-chloro 3-(methylamino)phenyl 95 H 3-chloro 4-(2-amino)thienyl 96 H 3-methoxy 3-trifluoroacetamidophenyl 97 H 3-methoxy 3-(N-methyl)trifluoroacetamidophenyl 98 H 3-methoxy 3-(3`-picolyloxycarbamoyl)phenyl 99 H 3-methoxy 3-phenoxycarbamoyl)phenyl 100 H 3-methoxy 3-difluoroacetamidophenyl 101 H 3-acetoxymethyl 3-methylphenyl 102 H 3-hydroxymethyl 3-methylphenyl 104 H H 3-nitro-4-fluorophenyl 105 H 3-methoxy 3-(aminomethyl)phenyl[(TFA] 106 H 3-methoxy 5-(N-acetoxy)indolinyl 107 H 3-methoxy 3-(N-methyl)acetamidophenyl 108 H 3-methoxy 3-[(2-oxo-2-3,4,5-trimethoxyphenyl)acetyl)amino]phenyl 109 H 3-amino 3-methylphenyl 110 H 3-methoxy 3-benzamidophenyl 111 H 3-methoxy 3-phenylacetamodophenyl 112 H 3-methoxy 3-phenylureidophenyl 113 H 3-methoxy 3-(t-butoxycarbamoylmethyl)phenyl 114 H 3-methoxy 3-(cyclopentylacetamido)phenyl Table IC L 116 NHC(O)O-t-butyl 117 NHC3C(O)O-T-butyl 118 NHC(O)O-methyl 119 NHC(O)O-phenyl 120 NHC(O)O-(S)-3-tetrahydrofuranyl 121 NHC(O)O-2-picolinyl 122 NHC(O)O-(S)-5-oxazolidinonylmethyl 123 NHC)O)O-4-carbomethoxyphenyl 124 NHC(O)O-isobutyl 125 NHC(O)O-allyl 126 NHC(O)O-5-(1,3-dioxanyl) 127 NHC(O)O-4-acetamidobenzyl 128 NHC(O)O-furfuryl 129 NHC(O)O-thiofurfuryl 130 NHC(O)O-methoxyethyl 131 NHC(O)O-4-tetrahydropyranyl 132 NHC(O)O-cyclohexyl 133 NHC(O)O-cyclopentyl 134 NHC(O)O-2-hydroxyethyl 135 NHC(O)O-cyclohesylmethyl 136 NHC(O)O-(R,S)-3-tetrahydrofuranyl 137 NHC(O)O-3-pyridyl 138 NHC(O)O-benzyl 139 NHC(O)O-3-(t-boc-amino)propyl 140 NHC(O)O-4-hydroxybutyl 141 NHC(O)O-5-hydroxypentyl 142 NHC(O)O-(R,S)-3-pyranyl 143 NHC(O)O-3-(N-t-BOC)piperidinyl 144 NHC(O)O-(R)-3-(2-oxo-4,4-dimethyl)furanyl 145 NHC(O)O-3-methylthiopropyl 146 NHC(O)O-4-[(2,2-dimethyl)-1,3-dioxanyl]methyl 147 NHC(O)O-2-di(hydroxymethyl)ethyl 148 NHC(O)O-4-(N-t-BOC)piperidinylmethyl 149 NHC(O)O-3-(N-t-BOC)piperidinylmethyl 150 NHC(O)O-(dibenzyloxymethyl)methyl 151 NHC(O)O-di(hydroxymethyl)methyl 152 NHC(O)O-2-(N-t-BOC)piperidinylmethyl 153 NHC(O)O-3-piperidinyl-TFA 154 NHC(O)O-(R,S)-(2-tetrahydropyranyl)methyl 155 NHC(O)O-4-piperidinylmethyl-TFA 156 NHC(O)O-(R,S)-3-tetrahydrofuranylmethyl 157 NHC(O)O-3-methylsulfonylpropyl 158 NHC(O)O-piperidinylmethyl-TFA 159 NHC(O)O-2-piperidinyl-TFA 1</p> |
