发明名称 Oxazolidinone compounds and derivatives thereof
摘要 Compounds of Formula (I) and Formula (II) are useful inhibitors of tankyrase. Compounds of Formula (I) and Formula (II) have the following structure: where the definitions of the variables are provided herein.;
申请公布号 US9340549(B2) 申请公布日期 2016.05.17
申请号 US201314383432 申请日期 2013.03.01
申请人 AMGEN INC. 发明人 Bregman Howard;Buchanan John L.;Chakka Nagasree;Dimauro Erin F.;Gunaydin Hakan;Guzman-Perez Angel;Hua Zihao;Huang Hongbing;Huang Xin;Martin Matthew W.;Patel Vinod F.
分类号 C07D413/14;C07D487/04;C07D413/08;C07D413/12;C07D417/12;C07D417/14;C07D471/04;C07D473/00;C07D263/34;C07D519/00;C07D413/10 主分类号 C07D413/14
代理机构 代理人 Friedrichsen Bernard P.
主权项 1. A compound of Formula I:or a pharmaceutically acceptable salt thereof, a tautomer thereof, a pharmaceutically acceptable salt of the tautomer, a stereoisomer of any of the foregoing, or a mixture thereof, wherein: R1 and R2 are (C1-C6)alkyl; R3 is —H; W is selected from pyridyl, phenyl, or phenyl substituted with 1, 2, or 3 substituents independently selected from —F, —Cl, —Br, —I, —C≡N, —NO2, —OH, —O—(C1-C6)alkyl, —OCF3, —CF3, —(C1-C6)alkyl, —NH2, —NH((C1-C4)alkyl), —N((C1-C4)alkyl), —NHSO2, —(C1-C6)alkyl, —NHC(═O)—(C1-C6)alkyl, —C(═O)NH2, —C(═O)NH((C1-C6)alkyl), —C(═O)N((C1-C6)alkyl)2, —C(═O)—(C1-C6)alkyl, —CO2H, —C(═O)—O—(C1-C6)alkyl, —SO2NH2, —SO2N((C1-C6)alkyl), —SO2N((C1-C6)alkyl)2, —SO2—(C1-C6)alkyl, or —SO—(C1-C6)alkyl; X is O; Y is selected from unsubstituted (C4-C7)cycloalkyl, substituted (C4-C7)cycloalkyl, unsubstituted (C4-C7)cycloalkenyl, substituted (C4-C7)cycloalkenyl, unsubstituted (C6-C10)aryl, substituted (C6-C10)aryl, unsubstituted 5 to 10 membered heteroaryl comprising 1, 2, 3, or 4 heteroatoms independently selected from O, S, or N, substituted 5 to 10 membered heteroaryl comprising 1, 2, 3, or 4 heteroatoms independently selected from O, S, or N, unsubstituted 4 to 10 membered heterocyclyl comprising 1, 2, or 3 heteroatoms independently selected from O, S, or N, or substituted 4 to 10 membered heterocyclyl comprising 1, 2, or 3 heteroatoms independently selected from O, S, or N, wherein the substituted (C4-C7)cycloalkyl and substituted (C4-C7)cycloalkenyl are substituted with 1 or 2 substituents independently selected from —F, —Cl, —Br, —I, —C≡N, —NO2, —OH, —O—(C1-C6)alkyl, —OCF3, —OCHF2, —CF3, —(C1-C6)alkyl, —NH2, —NH((C1-C4)alkyl), —N((C1-C4)alkyl)2, —C(═O)NH2, —C(═O)NH((C1-C6)alkyl), —C(═O)N((C1-C6)alkyl)2, —C(═O)—(C1-C6)alkyl, —CO2H, or —C(═O)—O—(C1-C6)alkyl, and wherein the substituted (C6-C10)aryl, substituted 5 to 10 membered heteroaryl, and substituted 4 to 10 membered heterocyclyl are substituted with 1, 2, or 3 substituents independently selected from —F, —Cl, —Br, —I, —C≡N, —NO2, —OH, —O—(C1-C6)alkyl, —OCF3, —OCHF2, —CF3, —(C1-C6)alkyl, —NH2, —NH((C1-C4)alkyl), —N((C1-C4)alkyl)2, —C(═O)NH2, —C(═O)NH((C1-C6)alkyl), —C(═O)N((C1-C6)alkyl)2, —C(═O)—(C1-C6)alkyl, —CO2H, or —C(═O)—O—(C1-C6)alkyl, and further wherein the substituted 4 to 10 membered heterocyclyl may also be substituted with a ═O; Z is selected from unsubstituted (C6-C10)aryl, substituted (C6-C10)aryl, unsubstituted 5 to 10 membered heteroaryl comprising 1, 2, 3, or 4 heteroatoms independently selected from O, S, or N, substituted 5 to 10 membered heteroaryl comprising 1, 2, 3, or 4 heteroatoms independently selected from O, S, or N, unsubstituted 5 to 10 membered heterocyclyl comprising 1, 2, 3 or 4 heteroatoms independently selected from O, S, or N, or substituted 5 to 10 membered heterocyclyl comprising 1, 2, 3, or 4 heteroatoms independently selected from O, S, or N, or Z is selected from —NRb—Z′, —NRc—C(═O)—Z′, or —C(═O)—NRd—Z′, wherein the substituted (C6-C10)aryl, substituted 5 to 10 membered heteroaryl, and the substituted 5 to 10 membered heterocyclyl are substituted with 1, 2, or 3 Q substituents and may additionally be substituted with 0 or 1 of Z′ or —NRe—Z′, and further wherein the substituted 5 to 10 membered heterocyclyl may also be substituted with a ═O; each Q is independently selected from —F, —Cl, —Br, —I, —C≡N, —NO2, —OH, —O—(C1-C6)alkyl, —SH, —S—(C1-C6)alkyl, —OCF3, —OCHF2, —CH2CHF2, —CF3, —(C1-C6)alkyl, —NH2, —NH((C1-C4)alkyl), —N((C1-C4)alkyl)2, —NHSO2—(C1-C6)alkyl, —NHC(═O)—(C1-C6)alkyl, —C(═O)NH2, —C(═O)NH((C1-C6)alkyl), —C(═O)N((C1-C6)alkyl)2, —C(═O)NH—OH, —C(═O)NH—O—(C1-C6)alkyl, —C(═O)—(C1-C6)alkyl, —CO2H, —C(═O)—O—(C1-C6)alkyl, —SO2NH2, —SO2NH((C1-C6)alkyl), —SO2N((C1-C6)alkyl)2, —SO2—(C1-C6)alkyl, —SO—(C1-C6)alkyl, —(C1-C4)alkylene-OH, —(C1-C4)alkylene-O—(C1-C6)alkyl, unsubstituted (C3-C7)cycloalkyl, unsubstituted 5 to 10 membered heterocyclyl comprising 1, 2, 3, or 4 heteroatoms independently selected from O, S, or N, or unsubstituted 3 or 4 membered heterocyclyl comprising 1 heteroatom selected from O, S, or N; Rb is selected from —H or (C1-C6)alkyl; Rc is selected from —H or (C1-C6)alkyl; Rd is selected from —H or (C1-C6)alkyl; Re is selected from —H or (C1-C6)alkyl; Z′ is selected from unsubstituted (C6-C10) aryl, substituted (C6-C10) aryl, unsubstituted 5 to 10 membered heteroaryl comprising 1, 2, 3, or 4 heteroatoms independently selected from O, S, or N, substituted 5 to 10 membered heteroaryl comprising 1, 2, 3, or 4 heteroatoms independently selected from O, S, or N, unsubstituted 5 to 10 membered heterocyclyl comprising 1, 2, 3 or 4 heteroatoms independently selected from O, S, or N, substituted 5 to 10 membered heterocyclyl comprising 1, 2, 3, or 4 heteroatoms independently selected from O, S, or N, unsubstituted 3 or 4 membered heterocyclyl comprising 1 heteroatom selected from O, S, or N, substituted 3 or 4 membered heterocyclyl comprising 1 heteroatom selected from O, S, or N, or unsubstituted (C3-C7)cycloalkyl, wherein, the substituted (C6-C10) aryl, the substituted 5 to 10 membered heteroaryl, the substituted 5 to 10 membered heterocyclyl, and the 3 or 4 membered heterocyclyl are substituted with 1, 2, or 3 substituents independently selected from —F, —Cl, —Br, —I, —C≡N, —NO2, —C(═NH)—NH2, —OH, —O—(C1-C6)alkyl, —SH, —S—(C1-C6)alkyl, —OCF3, —OCHF2, —CH2CHF2, —CF3, —(C1-C6)alkyl, —NH2, —NH((C1-C4)alkyl), —N((C1-C4)alkyl)2, —NHSO2—(C1-C6)alkyl, —NHC(═O)—(C1-C6)alkyl, —C(═O)NH2, —C(═O)NH((C1-C6)alkyl), —C(═O)N((C1-C6)alkyl)2, —C(═O)NH—OH, —C(═O)NH—O—(C1-C6)alkyl, —C(═O)—(C1-C6)alkyl, —CO2H, —C(═O)—O—(C1-C6)alkyl, —SO2NH2, —SO2NH((C1-C6)alkyl), —SO2N((C1-C6)alkyl)2, —SO2—(C1-C6)alkyl, —SO—(C1-C6)alkyl, —(C1-C4)alkylene-OH, or —(C1-C4)alkylene-O—(C1-C6)alkyl, and further wherein the substituted 5 to 10 membered heterocyclyl and the 3 or 4 membered heterocyclyl may also be substituted with a ═O.
地址 Thousand Oaks CA US