发明名称 Acrylamide derivatives as Fab I inhibitors
摘要 In part, the present invention is directed to antibacterial compounds.
申请公布号 US8895545(B2) 申请公布日期 2014.11.25
申请号 US201213644351 申请日期 2012.10.04
申请人 Debiopharm International SA 发明人 Pauls Heinz W.;Ramnauth Jailall;Sampson Peter;Toro Andras
分类号 C07D471/04;C07D405/12;C07D409/12;C07D213/73;C07D401/12;C07D495/04;A61K31/4427;A61P31/04;C07D498/04;A01N43/90 主分类号 C07D471/04
代理机构 Goodwin Procter LLP 代理人 Goodwin Procter LLP
主权项 1. A compound of formula I: wherein, independently for each occurrence, A is a monocyclic ring of 4-7 atoms containing 0-2 heteroatoms, a bicyclic ring of 8-12 atoms containing 0-4 heteroatoms or a tricyclic ring of 8-12 atoms containing 0-6 heteroatoms wherein the rings are independently aliphatic, aromatic, heteroaryl or heterocyclic in nature, the heteroatoms are selected from the group consisting of N, S, and O, and the rings are optionally substituted with one or more groups selected from the group consisting of C1-4 alkyl, OR″, CN, OCF3, F, Cl, Br, and I; wherein R″ is selected from the group consisting of H, alkyl, aralkyl, and heteroaralkyl, wherein the heteroaryl group of the heteroaralkyl is a 3-10 membered ring structure containing 1-4 heteroatoms selected from the group consisting of N, S, and O; R′ is selected from the group consisting of H and alkyl; R is selected from the group consisting of: wherein, independently for each occurrence, R1 is OH;R2 is OH; andR3 is selected from the group consisting of H, alkyl, carbonyl, sulfonyl, or aryl; or a pharmaceutically acceptable salt thereof; wherein: carbonyl is —C(O)—X50—R55 or —X50—C(O)—R56, where X50 is a bond, oxygen, or sulfur; R55 and R56 are hydrogen, alkyl, alkenyl, or —(CH2)m—R61; R61 is aryl, c cloalkyl, cycloalkenyl, or heterocyclyl; and m is zero or an integer in the range of 1 to 8; and sulfonyl is —S(O)2—R58, where R58 is alkyl, alkenyl, alkenyl, cycloalkyl, heterocyclyl, aryl, or hetero aryl.
地址 Lausanne CH