主权项 |
1. A compound of Formula (I): or pharmaceutically acceptable salts, hydrates or solvates thereof wherein: R1 is (C1-C4) alkyl or (C1-C4) perfluoroalkyl; R2 is alkyl, substituted alkyl, acyl, substituted acyl, halo, heteroalkyl, substituted heteroalkyl, —NO2, —N3, —OH, —S(O)kR100, —OR101, —NR102R103, —CONR104R105, —CO2R106 or —OC(O)R107; R3 and R4 are independently hydrogen, deuterium, fluoro, hydroxy or methoxy; R5 is hydrogen, (C1-C3) alkyl, substituted (C1-C4) alkyl or (C1-C3) perfluoroalkyl; R6 is R7 is isopropyl, sec-butyl, isobutyl, or t-butyl; R8 is hydrogen, (C1-C4) alkyl substituted (C1-C4) alkyl, benzyl or substituted benzyl; R9 is methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, t-butyl, (C2-C4) alkenyl or (C2-C4) alkynyl; R10 is hydrogen, OH, ═O, (C1-C4) alkyl, (C1-C4) substituted alkyl, —CO2R108 or —CONR109R110, R11 is hydrogen, OH, ═O, (C1-C4) alkyl, (C1-C4) substituted alkyl, —CO2R111 or —CONR112R113, R12 is hydrogen, OH, ═O, (C1-C4) alkyl, (C1-C4) substituted alkyl, —CO2R114 or —CONR115R116; R13 is hydrogen or halogen; R101, R102, R103, R104, R105, R106, R107, R108, R109, R110, R111, R112, R113, R114, R115 and R116 are independently hydrogen, alkyl, substituted alkyl, acyl, substituted acyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroalkyl, substituted heteroalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl or substituted heteroarylalkyl; and k is 0, 1 or 2; n is 0, 1, 2 or 3; wherein substituted with reference to a saturated carbon atom is limited to —Ra, halo, —O−, ═O, —ORb, —SRb, —S−, ═S, —NRcRc, ═NRb, ═N—ORb, trihalomethyl, —CF3, —CN, —OCN, —SCN, —NO, —NO2, ═N2, —N3, —S(O)2Rb, —S(O)2NRb, —S(O)2O−, —S(O)2ORb, —OS(O)2Rb, —OS(O)2O−, —OS(O)2ORb, —P(O)(O−)2, —P(O)(ORb)(O−), —P(O)(ORb)(ORb), —C(O)Rb, —C(S)Rb, —C(NRb)Rb, —C(O)O−, —C(O)ORb, —C(S)ORb, —C(O)NRcRc, —C(NRb)NRcRc, —OC(O)Rb, —OC(S)Rb, —OC(O)O−, —OC(O)ORb, —OC(S)ORb, —NRbC(O)Rb, —NRbC(S)Rb, —NRbC(O)O−, —NRbC(O)ORb, —NRbC(S)ORb, —NRbC(O)NRcRc, —NRbC(NRb)Rb and —NRbC(NRb)NRcRc, where Ra is selected from the group consisting of alkyl, cycloalkyl, heteroalkyl, cycloheteroalkyl, aryl, arylalkyl, heteroaryl and heteroarylalkyl; each Rb is independently hydrogen or Ra; and each Rc is independently Rb or alternatively, the two Rcs are taken together with the nitrogen atom to which they are bonded form a 4-, 5-, 6- or 7-membered cycloheteroalkyl which may optionally include from 1 to 4 of the same or different additional heteroatoms selected from the group consisting of O, N and S; and substituted with reference to an unsaturated carbon atom or an nitrogen atom in a heteroalkyl group is limited to —Ra, halo, —O−, —ORb, —SRb, —S−, —NRcRc, trihalomethyl, —CF3, —CN, —OCN, —SCN, —NO, —NO2, —N3, —S(O)2Rb, —S(O)2O−, —S(O)2ORb, —OS(O)2Rb, —OS(O)2O−, —OS(O)2ORb, —P(O)(O−)2, —P(O)(ORb)(O−), —P(O)(ORb)(ORb), —C(O)Rb, —C(S)Rb, —C(NRb)Rb, —C(O)O−, —C(O)ORb, —C(S)ORb, —C(O)NRcRc, —C(NRb)NRcRc, —OC(O)Rb, —OC(S)Rb, —OC(O)O−, —OC(O)ORb, —OC(S)ORb, —NRbC(O)Rb, —NRbC(S)Rb, —NRbC(O)O−, —NRbC(O)ORb, —NRbC(S)ORb, —NRbC(O)NRcRc, —NRbC(NRb)Rb and —NRbC(NRb)NRcRc where Ra, Rb and Rc are as defined above; provided that when R1 and R5 are methyl, R2, R3, R4, R10, R11, R12 and R13 are hydrogen and R6 is that: R7 is not isopropyl, R8 is not hydrogen and R9 is not n-propyl; R7 is not isopropyl, R8 is not hydrogen and R9 is not isobutyl; R7 is not isopropyl, R8 is not hydrogen and R9 is not isopropyl; provided that when R1 and R5 are methyl, R3 is —OCH3, R2, R4, R10, R11, R12 and R13 are hydrogen and R6 is that: R7 is not isopropyl, R8 is not hydrogen and R9 is not isopropyl; provided that when R1 and R5 are methyl, R2, R3, R4, R10, R11 and R12 are hydrogen, R13 is bromine and R6 is that: R7 is not isopropyl, R8 is not hydrogen and R9 is not isopropyl; R7 is not isopropyl, R8 is not hydrogen and R9 is not isobutyl; provided that when R1 is n-propyl, R5 is methyl, R2, R3, R4, R10, R11 and R12 are hydrogen, R13 is bromine and R6 is that: R7 is not isopropyl, R8 is not hydrogen and R9 is not isopropyl; provided that when R2, R3, R4, R10, R11, R12 and R13 are hydrogen and R6 is that: R1 is not allyl; provided that when R1 is ethyl, R5 is methyl, R2, R3, R4, R10, R11, R12 and R13 are hydrogen and R6 is that: R7 is not isopropyl, R8 is not hydrogen and R9 is not isopropyl; provided that when R1 is n-propyl, R5 is methyl, R2, R3, R4, R10, R11, R12 and R13 is hydrogen and R6 is that: R7 is not isopropyl, R8 is not hydrogen and R9 is not isopropyl; provided that when R1 is CH2OCOCH3, R5 is methyl, R2, R3, R4, R10, R11, R12 and R13 are hydrogen and R6 is that: R7 is not isopropyl, R8 is not hydrogen and R9 is not isobutyl; R7 is not isopropyl, R8 is not hydrogen and R9 is not isopropyl; provided that when R1 is CH2OH, R5 is methyl, R2, R3, R4, R10, R11, R12 and R13 are hydrogen and R6 is that: R7 is not isopropyl, R8 is not hydrogen and R9 is not isobutyl; R7 is not isopropyl, R8 is not hydrogen and R9 is not isopropyl; provided that when R1 and R5 are methyl and R2, R3 and R4 are hydrogen that: R6 is not provided that when R1 and R5 are methyl and R2, R3 and R4 are hydrogen that: R6 is not provided that when R1 and R5 are methyl and R2, R3 and R4 are hydrogen that: R6 is not |