| 主权项 |
1. A compound having the formula (I): or a pharmaceutically acceptable salt thereof, wherein:
A is —NH2;X is O, N, S or CH2;Y is N or —C(R6)—;R1 is H, R2 is H, —C(O)—(C1-C6 alkyl) or or R1 and R2 join to form a group having the formula: R3 is C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C7 cycloalkyl;R4 and R5 are each independently selected from H, —OR12, —NHC(O)OR12, —NHC(O)N(R12)2, —N(R12)2 and —NHC(O)R12;R6 is H, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, halo, —OR12, —SR12, —N(R12)2, C3-C7 cycloalkyl, C6-C10 aryl, 5- or 6-membered monocyclic heteroaryl or 9- or 10-membered bicyclic heteroaryl;R7 is H, C6-C10 aryl, 5- or 6-membered monocyclic heteroaryl, 9- or 10-membered bicyclic heteroaryl, or —(C1-C3 alkylene)-C(O)O—(C1-C6 alkyl), wherein said C6-C10 aryl group, said 5- or 6-membered monocyclic heteroaryl group and said 9- or 10-membered bicyclic heteroaryl group can be optionally substituted with R13,R8 is H, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl or benzyl, wherein said C1-C6 alkyl can be optionally substituted with a group selected from halo, —OR12, —SR12, guanidino, —N(R12)2, —C(O)OR12, —C(O)N(R12)2, —NHC(O)R12, 5- or 6-membered monocyclic heteroaryl and 9- or 10-membered bicyclic heteroaryl, and wherein said phenyl group and said benzyl group can be optionally substituted with up to 2 groups, each independently selected from C1-C6 alkyl, halo and —OR12;R9 is H, C1-C6 alkyl, C3-C7 cycloalkyl, phenyl or benzyl, wherein said C1-C6 alkyl can be optionally substituted with a group selected from halo, —OR12, —SR12, guanidino, —N(R12)2, —C(O)OR12, —C(O)N(R12)2, —NHC(O)R12, 5- or 6-membered monocyclic heteroaryl and 9- or 10-membered bicyclic heteroaryl, and wherein said phenyl group and said benzyl group can be optionally substituted with up to 2 groups, each independently selected from C1-C6 alkyl, halo and —OR12;R10 is H, C1-C20 alkyl, C2-C20 alkenyl, —(C1-C3 alkylene)m-(C3-C7 cycloalkyl), —(C1-C3 alkylene)m-(C6-C10 aryl) or —(C1-C3 alkylene)m-adamantyl, wherein said C1-C20 alkyl group, said C2-C20 alkenyl group, said C6-C10 aryl group and said adamantyl group can be optionally substituted with up to three groups, each independently selected from halo, —OR12, —C(O)OR12, CN, NO2, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C3-C7 cycloalkyl, C6-C10 aryl, 5- or 6-membered monocyclic heteroaryl, 9- or 10-membered bicyclic heteroaryl, —N(R12)2, —C(O)N(R12)2—SR12, —S(O)R12, —S(O)2R12, —S(O)2N(R12)2, —NHC(O)R12, —NHC(O)OR12 and —NHC(O)N(R12)2;R11 is H, C1-C20 alkyl, C2-C20 alkenyl, —(C1-C3 alkylene)m-(C3-C7 cycloalkyl), C3-C7 cycloalkyl, —(C1-C3 alkylene)m-C6-C10 aryl or —(C1-C3 alkylene)m-adamantyl, 5- or 6-membered monocyclic heteroaryl, 9- or 10-membered bicyclic heteroaryl, wherein said C1-C20 alkyl group, said C2-C20 alkenyl group, said C6-C10 aryl group, said adamantyl group, said 5- or 6-membered monocyclic heteroaryl group and said 9- or 10-membered bicyclic heteroaryl group can be optionally substituted with up to five groups, each independently selected from C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C7 cycloalkyl, C6-C10 aryl, 5- or 6-membered monocyclic heteroaryl, 9- or 10-membered bicyclic heteroaryl, halo, —OR12, —SR12, —S(O)R12, —S(O)2R12, —S(O)2N(R12)2, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, —O—(C1-C6 haloalkyl), —CN, —NO2, —N(R12)2, —C(O)OR12, —C(O)N(R12)2 and —NHC(O)R12, —NHC(O)OR12 and —NHC(O)N(R12)2;each occurrence of R12 is independently H, C1-C10 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, —(C1-C3 alkylene)m-(C3-C7 cycloalkyl)m-(C1-C3 alkylene)m-(C6-C10 aryl), —(C1-C3 alkylene)m-(4 to 7-membered heterocycloalkyl), —(C1-C3 alkylene)m-(5- or 6-membered monocyclic heteroaryl) or —(C1-C3 alkylene)m-(9- or 10-membered bicyclic heteroaryl), wherein said C3-C7 cycloalkyl group, said C6-C10 aryl group, said 4 to 7-membered heterocycloalkyl group, said -5- or 6-membered monocyclic heteroaryl group or said 9- or 10-membered bicyclic heteroaryl group can be optionally substituted with R16;R13 represents from one to five substituent groups, each independently selected from C1-C6 alkyl, halo, —OR12, —SR12, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, —O—(C1-C6 haloalkyl), —CN, —NO2, —N(R12)2, —C(O)OR12, —C(O)N(R12)2 and —NHC(O)R12, or any two R13 groups on adjacent ring carbon atoms can combine to form —O—R14—O—;R14 is [C(R15)2]n—;each occurrence of e is independently H or C1-C6 alkyl;R16 represents from one to five substituent groups, each independently selected from C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, halo, —OR17, —SR17, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, —O—(C1-C6 haloalkyl), —CN, —NO2, —N(R17)2, —C(O)OR17, —C(O)N(R17)2 and —NHC(O)R17;each occurrence of R17 is independently H, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, —(C1-C3 alkylene)m-(C3-C7 cycloalkyl)m-(C1-C3 alkylene)m-(C6-C10 aryl), —(C1-C3 alkylene)m-(4 to 7-membered heterocycloalkyl), —(C1-C3 alkylene)m-(5- or 6-membered monocyclic heteroaryl) or —(C1-C3 alkylene)m-(9- or 10-membered bicyclic heteroaryl);R18 is H, C1-C6 alkyl, —O(C1-C6 alkyl), C1-C6 alkynyl, C1-C6 alkenyl, or CN; andeach occurrence of m is independently 0 or 1, andeach occurrence of n is independently 1, 2, or 3. |
