发明名称 C-Linked Hydroxamic Acid Derivatives Useful As Antibacterial Agents
摘要 The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
申请公布号 US2014364398(A1) 申请公布日期 2014.12.11
申请号 US201414469657 申请日期 2014.08.27
申请人 Pfizer Inc. 发明人 Brown Matthew Frank;Marfat Anthony;Melnick Michael Joseph;Reilly Usa
分类号 C07C317/50;C07F9/09;C07D239/26;C07D231/12;C07D233/36;C07D213/30;C07D213/56;C07D261/08 主分类号 C07C317/50
代理机构 代理人
主权项 1. A compound of the formula:or a pharmaceutically acceptable salt thereof,in which: R1 is represented by C1-C3 alkyl; R2 is represented by hydrogen or C1-C3 alkyl; X is represented CH2, 0, NH, S or SO2, A is represented by phenyl or a 6-membered heteroaryl as depicted below: R3 is independently selected from the group consisting of hydrogen, halogen, nitro, cyano, hydroxy, amino, (C1-C6)alkyl, (C1-C6)alkoxy, trifluoromethyl, and trifluoromethoxy; L is absent, or is represented by S, SH, OH, —(CH2)p—O—(CH2)n, —(CH2)p—O—(CH2)z—O—(CH2)n—, S—(CH2)z, or (CH2)z—S; n is represented by an integer ranging from 0 to 3; p is represented by an integer ranging from 0 to 3; z is represented by an integer ranging from 1 to 3; D is absent, or is represented by a substituent selected from the group consisting of: i) (C3-C10)cycloalkyl, optionally substituted,ii) (C3—O10)cycloalkyl(C1-C6)alkyl, in which the alkyl and cycloalkyl moieties may each be optionally substituted,iii) (C6-C10)aryl optionally substituted,iv) (C6-C10)aryl(C1-C6)alkyl, in which the alkyl and aryl moieties may each be optionally substituted,v) heteroaryl, optionally substituted,vi) heteroaryl(C1-C6)alkyl, in which the heteroaryl and alkyl moieties may each be optionally substituted,vii) heterocyclic, optionally substituted,viii) heterocyclic(C1-C6)alkyl, in which the alkyl and heterocyclic moieties may each be substituted; T is absent, or is represented by —(CH2)z—, —(CH2)n—C(O)—(CH2)p—, O—(CH2)z—, —(CH2), —O—, or —O—(CH2)p—C(O)—(CH2)n— and; G is absent, or is represented by a substituent selected from the group consisting of: i) (C3-C10)cycloalkyl, optionally substituted; ii) (C6-C10)aryl optionally substituted; iii) heteroaryl, optionally substituted, or; iv) heterocyclic, optionally substituted; with the proviso that: a) at least one of D or L must be presentb) if D is absent, then T and G are also absent.
地址 New York NY US