| 主权项 |
1. A compound of Formula (I): or a pharmaceutically acceptable salt, racemic or scalemic mixture, diastereomer or enantiomer thereof, wherein, D is selected from the group consisting of M is Z is selected from the group consisting of covalent bond and —O—; Ar is phenyl substituted with 0 to 4 halogen, C1-C6 alkyl or C1-C4 alkoxy; and
G is each R38 is independently selected from the group consisting of halo, —C(O)O—(CH2)nNR36R39, —(CH2)jNR39(CH2)iS(O)j(C1-C6 alkyl), —(CH2)jNR39(CH2)nR36, —C(O)NR36R39, —C(O)(CH2)jNR39(CH2)nR36, —(CH2)nP(═O)(C1-C6alkyl)2, —(CH2)jNR39CH2(CH2)nP(═O)(C1-C6alkyl)2, —NR13C(X1)NR13-arylP(═O)(C1-C6alkyl)2 and —NR13C(X1)NR13-heteroarylP(═O)(C1-C6alkyl)2, —(CH2)jNR39(CH2)i[O(CH2)j]x(CH2)jR99, —(CH2)jNR39(CH2)iSO(0-2)(CH2)i[O(CH2)i]j(CH2)jR99, —(CH2)j—NR39(CH2)jR100 wherein each j is an integer independently ranging from 0 to 4, n is an integer ranging from 0 to 6, x is an integer ranging from 1-6, each i is an integer independently ranging from 1 to 3, and the —(CH2)i— and —(CH2)n— moieties of the foregoing R38 groups are optionally substituted, and optionally include a carbon-carbon double or triple bond where n is an integer between 2 and 6; R36 is selected from the group consisting of H, —OH, C1-C6 alkyl, —O—C1-C6 alkyl, C3-C10 cycloalkyl, —(CH2)n(C6-C10 aryl), —(CH2)n(5-10 membered heterocyclyl) and —(CH2)nA4R37, wherein each n is an integer independently ranging from 0 to 6, A4 is selected from the group consisting of a covalent bond, O, S, SO, SO2, and the alkyl, cycloalkyl, aryl and heterocyclyl moieties of the foregoing R36 groups are optionally substituted, with the proviso that when R36 and R39 are both attached to the same nitrogen, then R36 and R39 are not both bonded to the nitrogen directly through an oxygen; each R37 and R41 is independently selected from H, —C1-C6 alkyl, —O—C1-C6 alkyl, —O—C3-C10 cycloalkyl, —O—(CH2)n(C6-C10 aryl), —O—(CH2)n(5-10 membered heterocyclyl), optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C10 cycloalkyl, optionally substituted —O—(CH2)nA4-C1-C6 alkyl, optionally substituted —O—(CH2)nA4-C2-C6 alkenyl, optionally substituted —O—(CH2)nA4-C2-C6 alkynyl and optionally substituted —O—(CH2)nA4-C3-C10cyclaoalkyl; R39 is selected from the group consisting of H, —OH, C1-C6 alkyl, —C(O)—C1-C6alkyl, —SO2—C(O)—O—C1-C6alkyl-aryl and a protecting group used to protect secondary amino groups, with the proviso that when R36 and R39 are both attached to the same nitrogen, then R36 and R39 are not both bonded to the nitrogen directly through an oxygen; each R40 is independently selected from H, alkyl, —(CH2)n(C6-C10 aryl), C3-C10 cycloalkyl, and —(CH2)n(5-10 membered heterocyclyl), wherein n is an integer ranging from 0 to 6; R99 at each occurrence is independently selected from the group consisting of —H, halogen, trihalomethyl, —CN, —NO2, —NH2, —OR3, —NR3R4, —S(O)0-2R3, —S(O)2NR3R3, —C(O)OR3, —C(O)NR3R3, —N(R3)SO2R3, —N(R3)C(O)R3, —N(R3)CO2R3, P(═O)(OH)2, —P(═O)(C1-C6alkyl)2, —SO3H —C(O)R3, C1-C4 alkoxy, C1-C4 alkylthio, —O(CH2)0-6aryl, —O(CH2)0-6heteroaryl, —(CH2)0-5(aryl), —(CH2)0-5(heteroaryl), -, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, —CH2(CH2)0-4-T2, wherein the aryl, heteroaryl, C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl are optionally substituted; R100 is a 12 to 24-membered optionally substituted heteroalicyclic macrocycle containing 4 to 8 oxygen atoms; each R3 is independently selected from the group consisting of —H and R4; R4 is selected from the group consisting of a (C1-C6)alkyl, an aryl, a lower arylalkyl, a heterocyclyl and a lower heterocyclylalkyl, each of which is optionally substituted, or R3 and R4, taken together with a common nitrogen to which they are attached, form an optionally substituted five- to seven-membered heterocyclyl, the optionally substituted five- to seven-membered heterocyclyl optionally containing at least one additional annular heteroatom selected from the group consisting of N, O, S and P; each R13 is independently selected from the group consisting of —H, halogen, trihalomethyl, —CN, —NO2, —NH2, —OR3, —NR3R4, —S(O)0-2R3, —S(O)2NR3R3, —C(O)OR3, —C(O)NR3R3, —N(R3)SO2R3, —N(R3)C(O)R3, —N(R3)CO2R3, —C(O)R3, —C(O)SR3, C1-C4 alkoxy, C1-C4 alkylthio, —O(CH2)0-6aryl, —O(CH2)0-6heteroaryl, —(CH2)0-5(aryl), —(CH2)0-5(heteroaryl), —(CH2)0-5(cycloalkyl), C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, —CH2(CH2)0-4-T2, an optionally substituted C1-4 alkylcarbonyl, and a saturated or unsaturated three- to seven-membered carboxyclic or heterocyclic group, wherein the aryl, heteroaryl, C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl are optionally substituted; two R13, together with the atom or atoms to which they are attached, can combine to form a heteroalicyclic optionally substituted with between one and four of R60, wherein the heteroalicyclic can have up to four annular heteroatoms, and the heteroalicyclic can have an aryl or heteroaryl fused thereto, in which case the aryl or heteroaryl is optionally substituted with an additional one to four of R60; R60 is selected from the group consisting of —H, halogen, trihalomethyl, —CN, —NO2, —NH2, —OR3, —NR3R4, —S(O)0-2R3, —SO2NR3R3, —CO2R3, —C(O)NR3R3, —N(R3)SO2R3, —N(R3)C(O)R3, —N(R3)CO2R3, —C(O)R3, an optionally substituted (C1-C6)alkyl, an optionally substituted aryl, an optionally substituted heteroarylalkyl and an optionally substituted arylalkyl; or two R60, when attached to a non-aromatic carbon, can be oxo; Q is C1-C6alkyl or a three- to ten-membered ring system, optionally substituted with between zero and four of R20; each R20 is independently selected from the group consisting of —H, halogen, trihalomethyl, —O-trihalomethyl, oxo, —CN, —NO2, —NH2, —OR3, —OCF3, —NR3R4, —S(O)0-2R3, —S(O)2NR3R3, —C(O)OR3, —C(O)NR3R3, —N(R3)SO2R3, —N(R3)C(O)R3, —N(R3)C(O)OR3, —C(O)R3, —C(O)SR3, C1-C4 alkoxy, C1-C4 alkylthio, —O(CH2)0-6aryl, —O(CH2)0-6heteroaryl, —(CH2)0-5(aryl), —(CH2)0-5(heteroaryl), C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, —CH2(CH2)0-4-T2, an optionally substituted C1-4 alkylcarbonyl, C1-4 alkoxy, an amino optionally substituted by C1-4 alkyl optionally substituted by C1-4 alkoxy and a saturated or unsaturated three- to seven-membered carboxyclic or heterocyclic group and wherein the aryl, heteroaryl, C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl are optionally substituted; T2 is selected from the group consisting of —OH, —OMe, —OEt, —NH2, —NHMe, —NMe2, —NHEt and —NEt2; and X1 is selected from the group consisting of O, S, CH2, N—CN, N—O-alkyl, NH and N(C1-C6alkyl); X3 and X4 are each independently selected from the group consisting of —H, halogen, cyano, nitro, C1-C6 alkyl, or X3 and X4 together with the atom to which they are attached form a C3-C4 cycloalkyl. |
