[EN] FLUORINATED CYCLOPROPANE ANALOGS OF GLUTAMIC ACID<br/>[FR] ANALOGUES CYCLOPROPANIQUES FLUORÉS DE L'ACIDE GLUTAMIQUE
申请人:INST NAT SCIENCES APPLIQ
公开号:WO2011009947A1
公开(公告)日:2011-01-27
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer or a mixture in all proportions of stereoisomers thereof, in particular a mixture of enantiomers, such as a racemic mixture, wherein R represents a (C1-C6)alkyl or (C1-C6)alkenyl group, optionally substituted by one or more groups chosen among an halogen atom, ORa, SRb, NRcRd, PO(ORe)(ORf), CO2Rg, SO2Rh SO3R1, P0(0H)(CH(0H)Rk), CN, N3 and NH- C(=NH)NH2, with Ra, Rb, Rc and Rd, representing, independently of each other, an hydrogen atom, a (C1-C6)alkyl group or a -CO-(C1-C6)alkyl group, Re, Rf, Rg, Rh and R1 representing, independently of each other, an hydrogen atom or a (C1-C6)alkyl group, and Rk representing an aryl or heteroaryl group, said group being optionally substituted by one or more groups selected from an halogen atom and NO2, as well as to the use thereof and to a process for preparing such a compound, to a pharmaceutical composition containing it and to synthesis intermediates.
本发明涉及一种具有式(I)的化合物或药学上可接受的盐,其立体异构体或其立体异构体的各种比例的混合物,特别是对映体的混合物,如消旋混合物,其中R代表(C1-C6)烷基或(C1-C6)烯基基团,可选地被一个或多个在卤素原子、ORa、SRb、NRcRd、PO(ORe)(ORf)、CO2Rg、SO2Rh、SO3R1、P0(0H)(CH(0H)Rk)、CN、N3和NH-C(=NH)NH2中选择的基团之一取代,其中Ra、Rb、Rc和Rd分别独立地表示氢原子、(C1-C6)烷基或-CO-(C1-C6)烷基基团,Re、Rf、Rg、Rh和R1分别独立地表示氢原子或(C1-C6)烷基基团,Rk表示芳基或杂环芳基基团,所述基团可选地被一个或多个从卤素原子和NO2中选择的基团取代,以及其用途、制备这种化合物的方法、含有它的药物组合物和合成中间体。