发明名称 ANTIMICROBIAL AGENTS
摘要 The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.;
申请公布号 US2015031694(A1) 申请公布日期 2015.01.29
申请号 US201314386718 申请日期 2013.03.21
申请人 Rutgers, the State University of New Jersey 发明人 LaVoie Edmond J.;Parhi Ajit;Zhang Yongzheng;Pilch Daniel S.;Kaul Malvika
分类号 C07D277/64;C07D417/12;C07D417/04;C07D263/56;C07D263/32;C07D513/04;C07D277/30 主分类号 C07D277/64
代理机构 代理人
主权项 1. A compound of formula (I):wherein: R1 is hydrogen or 1, 2 or 3 optional substituents; W is CRa, or N; Ra is absent, hydrogen, or an optional substituent, R2 is hydrogen, methyl, or fluoro, and R2′ is hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C3-C8)cycloalkyl, aryl, or 5-6 membered heterocyclyl, wherein each alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclyl may be optionally substituted with one or more Rb; or Ra and R2 taken together are —CH2—, —CH2—CH2—, —O—, —O—CH2—, —CH2O—, —O—CH2—CH2—, or —CH2—CH2—O—; or Ra is absent, hydrogen or an optional substituent, and R2′ taken together with R2 is cyclopropyl, cyclobutyl, azetidine, or ═CH—N(Rc)2; wherein the cyclopropyl, cyclobutyl, and azetidine can optionally be substituted with (C1-C6)alkyl; R3 is (Alk1)m-(Z)p-(Alk2)n-Q; Z is —O—, —S—, —S(O)—, —SO2—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(═O)—, —OC(═O)—, —C(═O)O—, or an optionally substituted divalent monocyclic carbocycle or heterocyclic radical having 3 to 6 ring atoms, or an optionally substituted divalent bicyclic heterocyclic radical having 5 to 10 ring atoms; Alk1 is optionally substituted (C1-C6)alkylene, (C2-C6)alkenylene, or (C1-C6)alkynylene radical, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —SO2—, —NH—, —N(CH3)—, —N(CH2CH3)—; Alk2 is optionally substituted (C1-C6)alkylene, (C2-C6)alkenylene, or (C1-C6)alkynylene radical, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —SO2—, —NH—, —N(CH3)—, —N(CH2CH3)—; Q is hydrogen, halo, cyano, or hydroxyl, or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 7 ring atoms, or an optionally substituted bicyclic heterocyclic radical having 5 to 10 ring atoms; the bond represented by ---- is a double bond, R4 is hydrogen or methyl, and R5 is absent; or the bond represented by ---- is a single double bond, R4 is H, optionally substituted monocyclic carbocycle, or heterocyclic radical having 3 to 6 ring atoms, and R5 is hydrogen; wherein each optionally substituted monocyclic carbocycle, or heterocyclic radical having 3 to 6 ring atoms of R4 is optionally substituted with one or more (e.g. 1, 2, or 3) substituents independently selected from (C1-C6)alkoxy, halo, hydroxy, cyano, nitro, amino, methylamino, dimethylamino, carboxy, (C1-C6)alkoxycarbonyl, aminocarbonyl, (C1-C6)alkanoylamino, or tetrazole; R6 and R7 are each independently hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, or a heterocyclic radical having 3 to 6 ring atoms, or R6 and R7 together with the nitrogen to which they are attached form a 5 or 6 membered heterocyclic ring, which ring is optionally substituted with one or more groups independently selected from (C1-C6)alkyl; wherein any (C1-C6)alkyl of R6 and R7 is optionally substituted with one or more (e.g. 1, 2, or 3) substituents independently selected from (C1-C6)alkoxy, halo, hydroxy, cyano, nitro, amino, methylamino, dimethylamino, oxo (═O), carboxy, (C1-C6)alkoxycarbonyl, aminocarbonyl, (C1-C6)alkanoylamino, aryl, or tetrazole; and wherein any aryl or heterocyclic radical having 3 to 6 ring atoms of R6 and R7 is optionally substituted with one or more (e.g. 1, 2, or 3) substituents independently selected from (C1-C6)alkyl, (C1-C6)alkoxy, halo, trifluoromethyl, trifluoromethoxy, hydroxy, cyano, nitro, tetrazole, carboxy, (C1-C6)alkoxycarbonyl, or a (C1-C4)alkyl that is optionally substituted with one or more (e.g. 1, 2, or 3) substituents independently selected from (C1-C6)alkoxy, halo, hydroxy, cyano, nitro, tetrazole, carboxy, (C1-C6)alkoxycarbonyl, amino, methylamino, dimethylamino, or oxo (═O); each Rb is independently Rf, ORe, —C(═O)Re, —OC(═O)Re, —C(═O)ORe, —N(Re), —NReC(═O)Rd, —C(═O)N(Re)2, —NReC(═O)ORd, —OC(═O)N(Re)2, —C(═O)N(Re)—N(Re)C(═O)Rd, —NHC(═O)NHRd, —NHS(O)0-2Rd, —S(O)0-2Rd, —OS(O)0-2Rd, —OP(═O)(ORe)2, or —P(═O)(ORe)2; each Re is independently H or (C1-C6)alkyl; each Rd is optionally substituted and is independently selected from (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, aryl, aryl(C1-C6)alkyl, 4-10 membered heterocyclyl and heterocyclyl(C1-C6)alkyl; each Re is independently selected from H, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, aryl, aryl(C1-C6)alkyl, 4-10 membered heterocyclyl and heterocyclyl(C1-C6)alkyl, wherein each (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, aryl, aryl(C1-C6)alkyl, 4-10 membered heterocyclyl and heterocyclyl(C1-C6)alkyl is optionally substituted; each Rf is optionally substituted and is independently selected from aryl and 4-10 membered heterocyclyl; and m, p, and n are each independently 0 or 1, provided that at least one of m, p, and n is 1; or a salt thereof.
地址 New Brunswick NJ US