专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:EP-2173747-B1 优先权日:2007-06-26 标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS 权利人:SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:US-7105617-B2 优先权日:2003-02-06 标题:Metal 8-hydroxyquinoline-functionalized polymers and related materials and methods of making and using the same 发明人:WECK MARCUS; MEYERS AMY 权利人:GEORGIA TECH RES INST 摘要:This invention relates to the synthesis of Mq n -containing monomeric compounds, comprising a polymerizable moiety, an Mq n -moiety, and an optional chemical spacer therebetween, wherein q, in each instance, comprises an 8-hydroxyquinoline residue, M is a metal such as Mg, Zn, Al, Ga, or In, and n is 2 or 3 as the valence of the metal requires. For example, the polymerization of Znq 2 - or Alq 3 -containing monomers, in the presence or absence of a co-monomer, provided a Znq 2 - or Alq 3 -containing polymer, which retained the optical properties of Znq 2 or Alq 3 in solution, respectively. The Mq n -containing polymers may be used in, among other things, the fabrication of light-emitting diodes (LEDs).
专利号:US-10287265-B2 优先权日:2015-03-09 标 题 :Enantiomers of 8-hydroxyquinoline derivatives and the synthesis thereof 发明人:Puskás László; Kanizsai István; PILLOT THIERRY; GYURIS Márió; Szabó András; Takács Ferenc; Hackler László 权利人:AVIDIN CO LTD; SONEAS RES CO LTD; SYNAGING SAS 摘要:Our invention relates to novel enantiomer derivatives of 8-hydroxyquinoline derivatives with general formula (I) and (II) and the synthesis thereof and pharmaceutically acceptable salts and metal complexes thereof, and the medicinal and/or pharmaceutical compositions comprising these compounds. n n n n n n n n n n The essence of the subject matter of the invention relates to the fact that prior art discloses the biological effect and characteristics only of the racemic products, the novel enantiomer derivatives according to the invention appear in our application for the first. n The subject matter of the invention furthermore relates to a novel, stereoselective synthesis for the preparation of the novel enantiomer derivatives according to the invention. The novel medicinal and/or pharmaceutical compositions comprising these enantiomers are suitable for the treatment of the named diseases, and the enanatiomers are used for manufacture of these compositions. These applications for manufacture of the compositions are also the subject matters of the invention. The compounds according to the invention can be used preferably as cytoprotective, neuroprotective, cardioprotective, anxiolytic and antidepressant agent for treatment of neuropsychiatric and neurologic diseases and diseases in connections with transplantations and with ischemia and reperfusion injuries thereof, and inhibition of organ, advantageously skin graft rejection. According to our studies the R-enantiomer has either sole or high biological effect in some cases.
专利号:WO-0032619-A1 优先权日:1998-11-30 标题:Methods and compositions for identification of inhibitors of ribosome assembly 发明人:DAMMEL CAROL S; WATSON JULIE C 权利人:RIBOGENE INC 摘要:The invention provides a means for identifying novel antibiotics by screening for compounds that inhibit bacterial ribosome assembly and ribosomal protein synthesis, which comprises the screening of test compounds to identify those that inhibit the activity of a bacterial ribosomal protein. The in vitro and in vivo assays detect (a) increased translation of a reporter mRNA that is normally repressed in the presence of a ribosomal protein, (b) increased growth in cells that over-express ribosomal protein, and (c) decreased binding of the ribosomal protein to its target RNA. The invention encompasses the (a) methods of screening and testing compounds by the above methods, (b) compounds that are identified in the assay which inhibit ribosome assembly and protein synthesis and (c) methods for treatment using said compounds.
专利号:US-2010261909-A1 优先权日:2007-06-26 标题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
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合成参考文献
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