发明名称 Antimicrobial compositions for treating microbial infections
摘要 The disclosure provides compounds and methods to treat a microbial or a bacterial pathogenesis, and demonstrates that the S. aureus pigment is a virulence factor and potential novel target for antimicrobial therapy.
申请公布号 US8778913(B2) 申请公布日期 2014.07.15
申请号 US201213364082 申请日期 2012.02.01
申请人 The Regents of the University of California 发明人 Nizet Victor;Liu George Y.;Oldfield Eric;Song Yongcheng
分类号 A61K31/67;A61K31/497;A61K31/415;A61K9/00;A01N25/34;A61K9/127;A61K31/662;A61K31/496;A61K31/4174 主分类号 A61K31/67
代理机构 Gavrilovich, Dodd & Linsey LLP 代理人 Einhorn Gregory P.;Gavrilovich, Dodd & Linsey LLP
主权项 1. An antimicrobial pharmaceutical formulation for topical administration comprising: (a) at least one squalene synthase inhibitor, (b) at least one antimicrobial; and (c) a pharmaceutically acceptable carrier, wherein the at least one squalene synthase inhibitor is or comprises a compound represented by formula I:wherein:m is 0, 1, 2 or 3;n is an integer between 1 and 10 inclusive;each D and E are each independently selected from the group consisting of: H, aryl, substituted aryl, alkyl, substituted alkyl, carboxyl, aminocarbonyl, alkylsulfonylaminocarboxyl, alkoxycarbonyl, and halo;M1, M2, and M3 are each independently selected from the group consisting of metals, ammonium and esters thereof;R1 is selected from the group consisting of: H, aryl, substituted aryl, alkyl, substituted alkyl, carboxyl, aminocarbonyl, alkylsulfonylaminocarboxyl, alkoxycarbonyl, and halo, or R1 and R2, together with the carbons to which they are bound, can be joined to form a 4 to 7 membered ring or a substituted 4 to 7 membered ring;R2 is selected from the group consisting of: H, aryl, substituted aryl, alkyl, substituted alkyl, carboxyl, aminocarbonyl, alkylsulfonylaminocarboxyl, alkoxycarbonyl, and halo, or R2 and R1, together with the carbons to which they are bound, can be joined to form a 4 to 7 membered ring or a substituted 4 to 7 membered ring, or R2 and R3, together with the carbons to which they are bound, can be joined to form a 4 to 7 membered ring or a substituted 4 to 7 membered ring;R3 is selected from the group consisting of: H, aryl, substituted aryl, alkyl, substituted alkyl, carboxyl, aminocarbonyl, alkylsulfonylaminocarboxyl, alkoxycarbonyl, and halo, or R3 and R2, together with the carbons to which they are bound, can be joined to form a 4 to 7 membered ring or a substituted 4 to 7 membered ring, or R3 and R4, together with the carbons to which they are bound, can be joined to form a 4 to 7 membered ring or a substituted 4 to 7 membered ring;R4 is selected from the group consisting of: H, aryl, substituted aryl, alkyl, substituted alkyl, carboxyl, aminocarbonyl, alkylsulfonylaminocarboxyl, alkoxycarbonyl, and halo, or R4 and R3, together with the carbons to which they are bound, can be joined to form a 4 to 7 membered ring or a substituted 4 to 7 membered ring;R5, R6, R7, R8, and R9 are each independently selected from the group consisting of: H, aryl, substituted aryl, alkyl, substituted alkyl, carboxyl, aminocarbonyl, alkylsulfonylaminocarboxyl, alkoxycarbonyl, and halo;L1 is —S—, —SO—, —SO2—, —O—, —N(R19)—, or —C(R20)(R21)—; wherein R19, R20 and R21 are each independently selected from the group consisting of: H, aryl, substituted aryl, alkyl, substituted alkyl, carboxyl, aminocarbonyl, alkylsulfonylaminocarboxyl, alkoxycarbonyl, and halo; and the antimicrobial pharmaceutical formulation is formulated for topical administration.
地址 Oakland CA US