The present invention provides AA targeting compounds which comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to treat disorders connected to abnormal angiogenesis.
The present invention provides GA targeting compounds which comprise GA targeting agent-linker conjugates linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to prevent or treat diabetes or diabetes-related conditions.
[EN] PROCESS FOR THE CATALYTIC DIRECTED CLEAVAGE OF AMIDE-CONTAINING COMPOUNDS<br/>[FR] PROCÉDÉ POUR LE CLIVAGE CATALYTIQUE DIRIGÉ DE COMPOSÉS CONTENANT UN AMIDE
申请人:UNIV ANTWERPEN
公开号:WO2017046133A1
公开(公告)日:2017-03-23
The present invention relates to a catalytic method for the conversion of amide-containing compouds by means of a build-in directing group and upon the action of a heteronucleophilic compound (in se an amine (RNH2 or RNHR') or an alcohol (ROH) or a thiol (RSH)) in the presence of a metal catalyst to respectively esters, thioesters, carbonates, thiocarbonates and to what is defined as amide-containing compounds (such as carboxamides, urea, carbamates, thiocarbamates). The present invention also relates to these amide-containing compounds having a build-in directing group (DG), as well as the use of such directing groups in the catalytic directed cleavage of N-DG amides with the use of heteronucleophiles (in se an amine (RNH2 or RNHR') or an alcohol (ROH) or thiol (RSH)).
Reversal of polarity by catalytic SET oxidation: synthesis of azabicyclo[<i>m</i>.<i>n</i>.0]alkanes <i>via</i> chemoselective reduction of amidines
作者:Kirana Devarahosahalli Veeranna、Kanak Kanti Das、Sundarababu Baskaran
DOI:10.1039/d1ob00416f
日期:——
A one-pot catalytic method has been developed for the stereoselective synthesis of cyclopropane-fused cyclic amidines using CuBr2/K2S2O8 as an efficient single electron transfer (SET) oxidative system. The generality of this mild method is demonstrated with a wide variety of substrates to furnish pharmaceutically important amidines containing aza-bicyclic and novel aza-tricyclic frameworks in very
使用CuBr 2 /K 2 S 2 O 8作为有效的单电子转移(SET)氧化体系,开发了一种用于立体选择性合成环丙烷稠合环脒的单锅催化方法。这种温和方法的普遍性通过多种底物得到证明,以非常好的收率提供含有氮杂-双环和新型氮杂-三环骨架的药学上重要的脒。将环脒化学选择性还原为 2-/3-氮杂双环[ m . n .0]烷烃和八氢吲哚已使用 NaBH 4 /I 2开发试剂系统。化学选择性还原脒官能团的合成范围已在基于亚氨基糖的 (±)-表喹酰胺类似物的立体选择性合成中得到例证。
[EN] 2-SULFANYL-BENZOIMIDAZOL-1-YL-ACETIC ACID DERIVATIVES AS CRTH2 ANTAGONISTS<br/>[FR] DERIVES DE L'ACIDE 2-SULFANYL-BENZOIMIDAZOL-1-YL-ACETIQUE EN TANT QU'ANTAGONISTES DE CRTH2
申请人:ACTELION PHARMACEUTICALS LTD
公开号:WO2006021418A1
公开(公告)日:2006-03-02
The invention relates to 2-sulfanyl-benzoimidazol-1-yl-acetic acid derivatives and their use as potent 'chemoattractant receptor-homologous molecule expressed on Th2 cells' antagonists in the treatment of prostaglandin mediated diseases, to pharmaceutical compositions containing these derivatives and to processes for their preparation.