| 主权项 |
1. A compound of Formula I:or a pharmaceutically acceptable derivative thereof, wherein
Ar1 is Y is Ar2 is Ar3 is -(3- to 7-membered)heterocycle which is unsubstituted or substituted with 1 or 2 independently selected R6 groups; Z is
(a) —(C1-C6)alkyl which is unsubstituted or substituted with 1 or 2 —OR12 groups,(b) —(C2-C6)alkenyl which is unsubstituted or substituted with 1 or 2 —OR12 groups,(c) —OR12, or(d) —C(O)OR7; L1 and L2 are each independently a bond, —(C1-C6)alkylene, —(C2-C6)alkenylene, or —(C2-C6)alkynylene, each of which —(C1-C6)alkylene, —(C2-C6)alkenylene, or —(C2-C6)alkynylene is unsubstituted or substituted with 1 or 2 —OR7 groups; R1 is —H, -halo, —NO2, —CN, —OR7, —N(R7)2, —(C1-C4)alkyl, —C(halo)3, —CH(halo)2, —CH2(halo), —OC(halo)3, —OCH(halo)2, or —OCH2(halo); each R2 is independently -halo, —OR7, —CN, —NO2, —N(R7)2, —(C1-C10)alkyl, —(C2-C10)alkenyl, —(C2-C10)alkynyl, or -phenyl; X is O, S, N—CN, or N—OR7; each R3 is independently:
(a) —(C1-C6)alkyl, —(C1-C6)alkyl-OR13, —C(O)R13, —C(O)OR13, —N(R13)C(O)R13, or —C(O)N(R13)2;(b) two R3 groups together form ═O;(c) two R3 groups together form a (C2-C6)bridge, which is unsubstituted or substituted with 1, 2 or 3 independently selected R13 groups, and which bridge optionally contains —HC═CH— within the (C2-C6)bridge; or(d) two R3 groups together form R4 is —H, -halo, —(C1-C6)alkyl, —CH2OR7, —CH2(halo), —CH(halo)2, —C(halo)3, —OC(halo)3, —OR7, —SR7, —C(O)OR7, —C(O)RD, —OC(O)R7, —OC(O)N(R8)2.—NR7C(O)R13.—C(O)N(R8)2. —S(O)2R7, or —NO2; R5 is —H, —(C1-C6)alkyl, —(C3-C8)cycloalkyl, —(C1-C6)alkyl-OC(O)R7, —C(O)R7, or —C(O)N(R8)2; Ak is —(C1-C6)alkylene, —(C2-C6)alkenylene, or —(C2-C6)alkynylene; Rd and Re are each independently —H or —(C1-C6)alkyl; each R6 is independently —(C1-C6)alkyl or two R6 groups together form ═O; each R7 is independently —H or —(C1-C6)alkyl; each R8 is independently —H, —(C1-C6)alkyl, —(C2-C6)alkenyl, —(C2-C6)alkynyl, —(C3-C8)cycloalkyl, or phenyl; each R9 is independently —(C1-C6)alkyl, —(C2-C6)alkenyl, —(C2-C6)alkynyl, —(C3-C8)cycloalkyl, —(C5-C8)cycloalkenyl, -phenyl, -(3- to 7-membered)heterocycle, —(C1-C6)haloalkyl, —(C2-C6)haloalkenyl, —(C2-C6)haloalkynyl, —(C1-C6)hydroxyalkyl, —(C2-C6)hydroxyalkenyl, —(C2-C6)hydroxyalkynyl, —(C1-C6)alkoxy(C1-C6)alkyl, —(C1-C6)alkoxy(C2-C6)alkenyl, —(C1-C6)alkoxy(C2-C6)alkynyl, —CN, -halo, —N3, —NO2, —CH═NR13, —N(R13)2, —NR13OR13, OR13, —SR13, —O(CH2)bOR13, —O(CH2)bSR13, —O(CH2)bN(R13)2, —N(R13)(CH2)bOR13, —N(R13)(CH2)bSR13, —N(R13)(CH2)bN(R13)2, —N(R13)C(O)R13, —C(O)R13, —C(O)OR13, —OC(O)R13, —OC(O)OR13, —S(O)R13, —S(O)2R13, —S(O)2N(R13)2, —S(O)2, -(3- to 7-membered)heterocycle, —C(O)N(R13)2, —(C1-C6)alkyl-C═N—OR13, —(C1-C6)alkyl-C(O)N(R13)2, —(C1-C6)alkyl-NHS(O)2N(R13)2, or —(C1-C6)alkyl-C(═NH)—N(R13)2, each of which -phenyl, -(3- to 7-membered)heterocycle, or —(C3-C8)cycloalkyl is unsubstituted or substituted with 1, 2 or 3 independently selected R13 groups; each R10 is independently:
(a) —(C1-C6)alkyl, —(C2-C6)alkenyl, —(C2-C6)alkynyl, —(C3-C8)cycloalkyl, —(C5-C8)cycloalkenyl, or -phenyl, each of which is unsubstituted or substituted with 1 or 2 —OH groups;(b) —CH2CH2(halo), —CH2CH(halo)2, —CH2C(halo)3, —C(halo)3, —CH(halo)2, —CH2(halo), —CN, -halo, —N3, —NO2, —CH═NR13, —N(R13)2, —NR13OR13, —OR13, —C(O)R13, —C(O)OR13, —OC(O)R13, —OC(O)OR13, —SR13, —S(O)R13, or —S(O)2R13; or(c) two R10 groups on adjacent carbon atoms together form a (C1-C2)alkylenedioxy bridge, which is unsubstituted or substituted 1, 2 or 3 independently selected R13 groups; each R12 is independently —H, —(C1-C6)alkyl, —(C3-C8)cycloalkyl, —C(O)R13, —C(O)OR13, or —C(O)N(R13)2; each R13 is independently —H, —(C1-C6)alkyl, —(C2-C6)alkenyl, —(C2-C6)alkynyl, —(C3-C8)cycloalkyl, —(C5-C8)cycloalkenyl, -phenyl, -benzyl, —(C1-C6)haloalkyl, —(C1-C6)hydroxyalkyl, —(C1-C6)alkoxy(C1-C6)alkyl, —(C1-C6)alkyl-N(R8)2, or —C(O)N(R8)2; Y1, Y2, Y3 are each independently C, N, or O; wherein no more than one of Y1, Y2, or Y3 can be 0, no more than two of Y1, Y2, or Y3 can be N, and for each Y1, Y2, and Y3 that is N, the N is bonded to one R14 group. and for each Y1, Y2, and Y3 that is C, the C is bonded to two R5 groups, provided that there are no more than a total of two (C1-C6)alkyl groups substituted on all of Y1, and Y3; Ya and Yb are each independently —H, -halo, or —(C1-C6)alkyl, or Ya and Yb, together with the carbon to which they are attached, form a 3-8 member carbocyclic ring; is ═O, ═S, ═C(R7)2, ═CH(C2-C6)alkenyl, —N(R7)2, or ═N—OR5; Ra is —H, —(C1-C6)alkyl, —(C3-C8)cycloalkyl, —CH2—C(O)Rc, —(CH2)—C(O)ORc, —(CH2)—C(O)N(Rc)2, —(CH2)2—ORc, —(CH2)2—S(O)2N(Rc)2, or —(CH2)2—N(Rc)S(O)2Rc; Rb is:
(a) —H, —(C1-C6)alkyl, —(C3-C8)cycloalkyl, -(3- to 7-membered)heterocycle, —N(Rc)2, —N(Rc)—(C3-C8)cycloalkyl, or —N(Rc)-(3- to 7-membered)heterocycle, each of which -(3- to 7-membered)heterocycle or —(C3-C8)cycloalkyl is unsubstituted or substituted with 1, 2 or 3 independently selected R13 groups; or(b)-phenyl, -(5- or 6-membered)heteroaryl, —N(Rc)-phenyl, or —N(Rc)-(5- to 10-membered)heteroaryl, each of which is unsubstituted or substituted with 1, 2 or 3 independently selected R13 groups; each Rc is independently —H or —(C1-C4)alkyl; each R14 is independently —H, —(C1-C6)alkyl, —C(O)R13, —S(O)R13, —S(O)2R13, each halo is independently —F, —Cl, —Br, or —I; h is the integer 0 or 1; k is the integer 0 or 1; n is the integer 0, 1, or 2; m is the integer 0, 1, or 2; p is the integer 0 or 1; q is the integer 0, 1, 2, 3, or 4; s is the integer 0, 1, 2, 3, 4, or 5; t is the integer 0, 1,2, or 3; u is the integer 0, 1, 2 or 3; v is the integer 0, 1, 2 or 3; b is the integer 1 or 2; and c is the integer 0, 1, or 2;
provided that when Ar1 is then Ar2 is not |
