| 主权项 |
1. A compound having a structural formula
Cap-L-M wherein Cap is selected from the group consisting of wherein ring is an aliphatic or aromatic five or six membered ring, W, X, Y, and Z independently are selected from the group consisting of null, C(R1)2, O, S, and NR1, ring is an aliphatic or aromatic six membered ring, wherein D, E, F, and G independently are selected from the group consisting of C(R1)2, O, and S, or ring is an aliphatic or aromatic five membered ring, wherein D, E, F, and G are selected from the group consisting of null, C(R1)2, and NR1, R1, independently, is selected from the group consisting of null, hydrogen, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C1-6perfluoroalkyl, C1-6perfluoroalkoxy, aryl, heteroaryl, C3-10cycloalkyl, C3-10heterocycloalkyl, C1-6alkylenearyl, C1-6alkyleneheteroaryl, C1-6alkyleneheterocycloalkyl, C1-6alkylenecycloalkyl, ORa, halo, N(Ra)2, SRa, SORa, SO2Ra, CN, C(═O)Ra, CF3, OCF3, NO2, OC(═O)Ra, SO2N(Ra)2, OSO2CF3, C(═O)ORa, C(═O)N(Ra)2, C1-6alkyleneN(Ra)2, C1-6alkyleneC(═O)Ra, C1-6alkyleneORa, C1-6alkyleneSRa, C1-6alkyleneNRaSO2Ra, C1-6alkyleneSORa, C1-6alkyleneCN, C1-6heteroalkyleneCN, C1-6alkyleneC(═O)ORa, C1-6alkyleneOC(═O)N(Ra)2, C1-6alkyleneNRaC(═O)ORa, C1-6alkyleneNRaC(═O)Ra, C1-6alkylene C(═O)N(Ra)2, C1-6alkyleneOC1-6alkyleneC(═O)ORa, C(═O)NRaSO2Ra, C(═O)C1-6alkylenearyl, C(═O)NRaC1-6alkyleneORa, OC1-6alkyleneC(═O)ORa, OC1-6alkyleneN(Ra)2, OC1-6alkyleneORa, OC1-6alkyleneNRaC(═O)ORa, NRaC1-6alkyleneN(Ra)2, NRaC(═O)Ra, NRaC(═O)N(Ra)2, N(SO2C1-6alkyl)2, and NRa(SO2C1-6alkyl), and Ra, independently, is selected from the group consisting of hydrogen, C1-6alkyl, C1-6heteroalkyl, C1-6alkyleneNH2, C1-6alkyleneNH(C1-6alkyl), C1-6alkyleneN(C1-6alkyl)2, C1-6alkyleneNH(C1-6alkyl)2, C1-6alkyleneNHC(═O)(C1-6alkyl), C1-6alkyleneC(═O)NH2, C1-6alkyleneOH, C1-6alkyleneCN, C1-6heteroalkyleneCN, C1-6alkyleneOC1-6alkyl, C1-6alkyleneSH, C1-6alkyleneSC1-6alkyl, C1-6alkyleneNH(SO2C1-6alkyl), aryl, heteroaryl, C3-8cycloalkyl, and C3-10heterocycloalkyl, wherein linker L is attached to any atom D, E, F, or G, wherein ring is an aliphatic or aromatic five or six membered ring, E, F, W, X, Y, Z, R1, and Ra are as defined above, and wherein A is C, N, O, S, B, or P, and L is attached to A, R2, R3 and R4 independently are selected from the group consisting of null, hydrogen, C1-6alkyl, C1-6heteroalkyl, C2-6alkenyl, C1-6perfluoroalkyl, C1-6perfluoroalkoxy, aryl, heteroaryl, C3-10cycloalkyl, C3-8heterocycloalkyl, C1-6alkylenearyl, C1-6alkyleneheteroaryl, C1-6alkyleneheterocycloalkyl, C1-6alkylenecycloalkyl, ORa, halo, N(Ra)2, SRa, SORa, SO2Ra, CN, C(═O)Ra, OC(═O)Ra, C(═O)ORa, C1-6alkyleneN(Ra)2, C1-6alkyleneORa, C1-6alkyleneSRa, C1-6alkyleneC(═O)ORa, C(═O)N(Ra)2, C(═O)NRaC1-6alkyleneORa, OC1-6alkyleneC(═O)ORa, OC1-6alkyleneN(Ra)2, OC1-6alkyleneORa, OC1-6alkyleneNRaC(═O)ORa, NRaC1-6alkyleneN(Ra)2, NRaC(═O)Ra, NRaC(═O)N(Ra)2, N(SO2C1-6alkyl)2, NRa(SO2C1-6alkyl), nitro, and SO2N(Ra)2, and Ra is defined above; L is selected from the group consisting of null, C1-8alkylene, Ra substituted C1-8alkylene, NRa, C(═O), aryl, C(═O)aryl, C(═O)C1-6alkylene, C1-8alkyleneNRa, C1-6alkylenearyleneC1-6alkylene, C2-6alkenylene, C4-8alkdienylene, C1-6alkylenearylene, C1-6alkyleneheteroarylene, Ra substituted C1-6alkyleneheteroarylene, and C2-6alkenylenearyleneC1-6alkylene, and Ra is defined above; M is selected from the group consisting of —C(═O)N(Rb)OH, —O(CH2)1-6C(═O)N(Rb)ORb, —N(Rb)(CH2)1-6C(═O)N(Rb)ORb, —N(Rb)(CH2)1-6C(═O)N(Rb)ORb, arylC(═O)NHOH, —N(OH)C(═O)Rb, heteroarylC(═O)NHOH, —C3-6cycloalkylN—C(═O)CH2SH, —B(ORb)2, —SO2NHRb, —NHSO2NHRb, —NHSO2C1-6alkyl, —SO2C1-6alkyl, —SRc, —C(═O)Re, —P(═O)(ORf)2, —NH—P(═O)(ORf)2, —C(═O)(C(Rb)2)1-6SH, —C(═O)C(═O)NHRb, —C(═O)NHN(Rb)2, —C(═O)NH(CH2)1-3N(Rb)2, —S—(C═O)C1-6alkyl, C3-10heterocycloalkyl optionally substituted with oxo (═O), thioxo (═S), or both, aryl optionally substituted with one or more of C1-6alkyl, —C(═O)Rd, —NH2, and —SH, heteroaryl optionally substituted with —NH2, —SH, or both, —N(H)C(═O)SH, —NHC(═O)NHRd, —NHC(═O)CH2Rd, —NHC(═O)(CH2)1-6SH, —NHC(═O)CH2Hal, —NHC(═S)NHRd, —NHC(═S)CH2Rd, —C(═S)NHRd, —C(═S)CH2Rd, —NHC(═S)CH2Rd, —NHC(═S)CH2Hal, and —(C═O)C1-6alkyl; Rb, independently, is selected from the group consisting of hydrogen, (C═O)CH3, C1-6alkyl, CF3, CH2F, and aryl, or two Rb groups are taken together with the carbon to which they attached to form a C3-8cycloalkyl group; Rc is selected from hydrogen or (C═O)CH3; Rd is NH2 or OH; Re is selected from the group consisting of OH, N(Rb)2, NH(OCH3), N(CH3)OH, C1-6alkyl, CF3, aryl, heteroaryl, C3-8cycloalkyl, NHSO2CH3, NHSO2CF3, and C1-6haloalkyl; Rf independently is hydrogen, methyl, or ethyl; and Hal is halo, or a pharmaceutically acceptable salt, hydrate, or prodrug thereof. |
