发明名称 ANTIMICROBIAL AGENTS
摘要 The invention provides compounds of formula (I):;;wherein R1-R3, n, 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 US2016367531(A1) 申请公布日期 2016.12.22
申请号 US201615253392 申请日期 2016.08.31
申请人 Rutgers, The State University of New Jersey ;Taxis Pharmaceuticals, Inc. 发明人 LaVoie Edmond J.;Parhi Ajit;Pilch Daniel S.;Zhang Yongzheng;Kaul Malvika
分类号 A61K31/428;A61K31/454;A61K31/166;A61K31/4439;A61K31/497;A61K31/437;A61K31/4545 主分类号 A61K31/428
代理机构 代理人
主权项 1. A method for treating a bacterial infection in a mammal comprising administering to the mammal an effective amount of a compound of formula (I):wherein: each R1 is independently selected from hydrogen, halo, cyano, nitro, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, (C1-C6)alkanoyloxy, aryl, heteroaryl, heterocycle, and NReRf, wherein each (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkanoyl, (Cr C6)alkoxycarbonyl, (C1-C6)alkanoyloxy, aryl, heteroaryl, and heterocycle is optionally substituted with one or more groups independently selected from halo, cyano, nitro, NReRf, —CRg(═N)N(Rg)2, —NRgC(═N)—N(Rg)2, —NRg—C(═NRg)Rg, (C1-C3)alkyl, (C1-C3)alkoxy, (C1-C3)alkanoyl, (C1-C3)alkoxycarbonyl, (C1-C3)alkanoyloxy, aryl, heteroaryl, and heterocycle; R2 is H or (C1-C6)alkyl that is optionally substituted with one or more groups independently selected from —ORk, halo, NReRf, NReRf, —CRg(═N)N(Rg)2, —NRgC(═N)—N(Rg)2, and —NRg—C(═NRg)Rg; R3 is:which is optionally substituted with one or more groups independently selected from trifluoromethyl, pentafluoroethyl, or 1-(trifluoromethyl)cyclopropyl; W is —NHCORa, —N(CORa)(CORb), —NRaCH2ORa, —NHC(═O)ORa, —NHC(═O)NRaRb, or —N(Ra)SOmRd; each Ra is independently selected from H, aryl, heteroaryl, heterocycle, (C3-C8)cycloalkyl, (C3-C8)cycloalkyl(C1-C6)alkyl and (C1-C6)alkyl that is optionally substituted with one or more groups independently selected from hydroxy, halo, cyano, (C1-C6)alkoxycarbonyl, aryl, heteroaryl, —NReRf, —CRg(═N)N(Rg)2, —NRgC(═N)—N(Rg)2, —NRg—C(═NRg)Rg and heterocycle; wherein any aryl, heteroaryl, heterocycle, and (C3-C8)cycloalkyl(C1-C6)alkyl of Ra is optionally substituted with one or more groups independently selected from hydroxy, halo, cyano, trifluoromethoxy, (C1-C6)alkyl, (C1-C6)alkoxy, halo(C1-C6)alkyl, —NReRf, —CRg(═N)N(Rg)2, —NRgC(═N)—N(Rg)2, —NRg—C(═NRg)Rg, and (C1-C6)alkoxycarbonyl; each Rb is independently selected from H and (C1-C6)alkyl that is optionally substituted with one or more groups independently selected from hydroxy, halo, cyano, (C1-C6)alkoxycarbonyl, aryl, heteroaryl, —NReRf, —CRg(═N)N(Rg)2, —NRgC(═N)—N(Rg)2, —NRg—C(═NRg)Rg, and heterocycle; each Rd is independently selected from OH, —NH2, —NReRf, aryl, heteroaryl, heterocycle, and (C1-C6)alkyl that is optionally substituted with one or more groups independently selected from hydroxy, halo, cyano, (C1-C6)alkoxycarbonyl, aryl, heteroaryl, —NReRf, —CH(═N)NH2, —NHC(═N)—NH2, —NH—C(═NH)R, and heterocycle; each Re is independently selected from H, aryl, heteroaryl, heterocycle, and (C1-C6)alkyl that is optionally substituted with one or more groups independently selected from hydroxy, halo, cyano, (C1-C6)alkoxycarbonyl, aryl, heteroaryl, and heterocycle; and each Rf is independently selected from H and (C1-C6)alkyl that is optionally substituted with one or more groups independently selected from hydroxyl, halo, cyano, (C1-C6)alkoxycarbonyl, aryl, heteroaryl, and heterocycle; or Re and Rf together with the nitrogen to which they are attached form a aziridino, azetidino, morpholino, piperazino, pyrrolidino or piperidino; each Rg is independently selected from H and (C1-C6)alkyl that is optionally substituted with one or more groups independently selected from halo; each Rk is independently selected from H or (C1-C6)alkyl that is optionally substituted with one or more groups independently selected from hydroxy, halo, oxo, carboxy, (C1-C6)alkoxy, (C1-C6)alkoxycarbonyl, and (C1-C6)alkanoyloxy; m is 0, 1, or 2; and n is 1, 2, 3, or 4; or a pharmaceutically acceptable salt thereof.
地址 New Brunswick NJ US