| 主权项 |
1. A compound of the formula: or a pharmaceutically acceptable salt thereof,wherein:
X is —O—, —N(R), —C(R8)(R9) or —C(O)—; Y is —O—, —N(R), —C(R8)(R9) or —C(O)—; R is H, alkyl or —S(O)2—R9 R1 is H, alkyl or haloalkyl; R2 is H, alkyl or haloalkyl; R3 is H, —N3, —CN; halogen, —OR12, —N(R25)(R26), —C(O)OR12, —C(O)N(R25)(R26), —SO2(R12), R17-alkyl, R17-cycloalkyl, R17-aryl, R17-heterocycloalkyl or R17-heteroaryl; R4 is H, alkyl or haloalkyl; R5 is H, alkyl or haloalkyl; R6 is H or alkyl; R7 is H or alkyl; R8 independently is H or alkyl; R9 independently is H or alkyl; R10 is halogen or —CN; R11 is H, halogen or alkyl; R12 independently is H, R16-alkyl, R16-alkenyl, R17-cycloalkyl, R17-arylalkyl, R17-arylalkenyl, R17-aryl, R17-heteroaryl, R17-heteroarylalkyl or R17-heteroarylalkenyl; R13 is independently is H, R16-alkyl, R16-alkenyl, R17-cycloalkyl, R17-arylalkyl, R17-arylalkenyl, R17-aryl, R17-heteroaryl, R17-heteroarylalkyl or R17-heteroarylalkenyl; R14 is independently is H, R16-alkyl, R16-alkenyl, R17-cycloalkyl, R17-arylalkyl, R17-arylalkenyl, R17-aryl, —C(O)R12, —S(O)2—R12, R17-heteroaryl, R17-heteroarylalkyl or R17-heteroarylalkenyl;
or R13 and R14 taken together with the nitrogen atom to which they are attached are —(CH2)4—, —(CH2)5— or —(CH2)2—N(R8)—(CH2)2—; Het is a 5- or 6-membered heterocycloalkyl, heterocyclenyl or a heteroaryl ring containing 3 to 5 carbon atoms and 1 or 2 heteroatoms selected from the group consisting of N, O or S, with the proviso that there are no adjacent oxygen or sulfur atoms present in said groups, and when Het is a N-containing heteroaromatic group with one heteroatom present, then the ring nitrogen can form an N-oxide or a quaternary group with an alkyl group; wherein: 1) Het is attached to the double bond by a carbon atom ring member of Het; and 2) Het is substituted by 1 to 4 moieties, W,
where each W is independently hydrogen, alkyl, haloalkyl, R17-cycloalkyl, R17-heterocycloalkyl, R16-alkenyl, R17-aryl, R17-heteroaryl, R17-arylalkyl, R17-arylalkenyl, R17-heteroarylalkyl, R17-heteroarylalkenyl, hydroxyalkyl, dihydroxyalkyl, aminoalkyl, alkylaminoalkyl, di-(alkyl)-aminoalkyl, alkoxy, -alkyl-SH, —S-alkyl, alkenyloxy, halogen, —NR13R14, —CN, —OH, —C(O)OR12, —COR12, —OS(O2)CF3, —CH2OCH2CF3, —C(O)NR13NR14, —OCHR15-phenyl, phenoxyalkyl, —NR8COR12, —NR8SO2R12, —C(O)NR13R14, —OC(R15)2COOR12, —OC(R15)2C(O)NR13R14, alkoxy optionally substituted by alkyl, amino or —NR8C(O)OR12, or alkyl optionally substituted with —NR13R14, —NR13COR12, —NR8CONR13R14, NR8C(O)OR12, —NR8S(O)2R12, —NR8S(O)2NR13R14, —C(O)OR12, —CONR13R14 or —OH; R15 independently is H, alkyl, cycloalkyl, alkoxyalkyl, hydroxyalkyl, aminoalkyl or phenyl; R16 is 1 to 3 moieties and each R16 is independently hydrogen, halogen, —OH, alkoxy, -alkyl-SH, —S-alkyl, R24-aryl, R24-heteroaryl, R24-heterocycloalkyl, R24-cycloalkyl, R24-cycloalkenyl, R24-heterocyclenyl, —OC(O)R20, —C(O)OR20, —C(O)R20, —C(O)NR21R22, —NR21R22, —NR8C(O)R20, —NR8C(O)NR21R22, —NR8SO2R20, —OC(O)NR21R22, R23-alkenyloxy, R23-alkynyloxy, R23-heterocycloalkyloxy, R24-cycloalkyloxy, R24-cycloalkenyloxy, R24-aryloxy, R24-heteroaryloxy, R24-cycloalkyl-NH—, —NR8SO2NHR21 or —C(═NOR18)R19; R17 is 1 to 3 moieties and each R17 independently hydrogen, R23-alkyl, halogen, —CN, —NO2, —OH, R23-alkoxy, —OC(O)R20, —C(O)OR20, —C(O)R20, —C(O)NR21R22, —NR21R22, —NR8C(O)R20, —NR8C(O)NR21R22, NR8SO2R20, —OC(O)NR21R22, —S(O)R20, —S(O)2R20, —SR20; —SO2NR21R22, —NHCOR20, —C(NH)—NH2, —C(O)NR21R22, R23-alkenyloxy, R23-alkynyloxy, R24-cycloalkyl, R24-cycloalkenyl, R24-heterocycloalkyl, R24-aryl, R24-heteroaryl, R24-heterocycloalkyloxy, R24-cycloalkyloxy, R24-cycloalkenyloxy, R24-aryloxy, R24-heteroaryloxy, R24-cycloalkyl-NH—, —NR8SO2NHR21 or —C(═NOR18)R19; R18 is H, alkyl, phenyl or benzyl; R19 is H, alkyl, phenyl or benzyl; R20, R21 and R22 are independently hydrogen, alkyl, haloalkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, halocycloalkyl or alkoxyalkyl; R23 is 1 to 3 moieties and each R23 is independently hydrogen, halogen, —OH, alkyl, haloalkyl, alkoxy, —CN, amino, alkylamino, dialkylamino, di(alkyl)amino, haloalkoxy, hydroxyalkyl, —CHO, —C(O)alkylamino, —C(O)alkylamino, —NHC(O)alkyl or —N(alkyl)C(O)alkyl; R24 is 1 to 3 moieties and each R24 is independently hydrogen, halogen, —OH, alkyl, haloalkyl, alkoxy, —CN, amino, alkylamino, dialkylamino, di(alkyl)amino, haloalkoxy, hydroxyalkyl, —CHO, —C(O)alkylamino, —C(O)alkylamino, —NHC(O)alkyl or —N(alkyl)C(O)alkyl; R25 is H, R17-alkyl, R17-cycloalkyl, R17-aryl, R17-heterocycloalkyl, R17-aryl, or R17-heteroaryl; and R26 is H, OH, —C(O)N(R21)(R22), —C(S)N(R21)(R22), —C(O)R12, —S(O)2R12, R17-alkyl, R17-cycloalkyl, R17-aryl, R17-heterocycloalkyl, or R17-heteroaryl. |
