[EN] COLONY STIMULATING FACTOR-1 RECEPTOR (CSF-1R) INHIBITORS<br/>[FR] INHIBITEURS DU RÉCEPTEUR DE FACTEUR-1 DE STIMULATION DE COLONIES (CSF-1R)
申请人:GENZYME CORP
公开号:WO2017015267A1
公开(公告)日:2017-01-26
Compounds of the formulas I and XIII, which are useful as colony stimulating factor-1 receptor inhibitors ("CSF 1R inhibitors").
I和XIII式化合物,可用作促细胞增殖因子-1受体抑制剂("CSF 1R抑制剂")。
[EN] NOVEL COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS
申请人:CHIESI FARMA SPA
公开号:WO2014095700A1
公开(公告)日:2014-06-26
This invention relates to heterocyclic compounds, which are pyrimidinone derivatives having human neutrophil elastase inhibitory properties, and their use in therapy.
[EN] DECARBOXYLATIVE CONJUGATE ADDITIONS AND APPLICATIONS THEREOF<br/>[FR] ADDITIONS DE CONJUGUÉS AVEC DÉCARBOXYLATION ET APPLICATIONS ASSOCIÉES
申请人:UNIV PRINCETON
公开号:WO2016196931A1
公开(公告)日:2016-12-08
Synthetic methods are described herein operable to efficiently produce a wide variety of molecular species through conjugate additions via decarboxylative mechanisms. For example, methods of functionalization of peptide residues are described, including selective functionalization of peptide C-terminal residues. In one aspect, a method of peptide functionalization comprises providing a reaction mixture including a Michael acceptor and a peptide and coupling the Michael acceptor with the peptide via a mechanism including decarboxylation of a peptide reside.
[EN] PROCESS FOR THE SYNTHESIS OF ARFORMOTEROL<br/>[FR] PROCESSUS POUR LA SYNTHÈSE D'ARFORMOTÉROL
申请人:CIPLA LTD
公开号:WO2009147383A1
公开(公告)日:2009-12-10
The present invention provides a process for preparing a compound of formula (Vl) or a salt thereof, the process comprising: (i) reacting 4-methoxyphenyl acetone with an amine of formula (VIII) under conditions of reductive amination to produce a compound of formula (II) or a salt thereof, wherein there is no isolation of an imine intermediate formed during the reductive amination; (ii) condensing the compound (II) or the acid addition salt thereof with an α-haloketone of formula (III) to produce the compound of formula (IV); (iii) reducing the compound (IV) to a compound of formula (V); and (iv) reducing the compound (V) to the compound of formula (Vl), wherein the reduction is carried out in the presence of either (1 ) a hydrogen donating compound in the presence of a hydrogen transfer catalyst; or (2) ammonium formate using a hydrogenation catalyst, wherein: R1 and R2 are independently optionally substituted arylalkyl, and Hal is selected from chloro or bromo.
The present invention provides a process for preparing a compound of formula (VI) or a salt thereof, the process comprising: (i) reacting 4-methoxyphenyl acetone with an amine of formula (VIII) under conditions of reductive amination to produce a compound of formula (II) or a salt thereof, wherein there is no isolation of an imine intermediate formed during the reductive amination; (ii) condensing the compound (II) or the acid addition salt thereof with an α-haloketone of formula (III) to produce the compound of formula (IV); (iii) reducing the compound (IV) to a compound of formula (V); and (iv) reducing the compound (V) to the compound of formula (VI), wherein the reduction is carried out in the presence of either (1) a hydrogen donating compound in the presence of a hydrogen transfer catalyst; or (2) ammonium formate using a hydrogenation catalyst, wherein R
1
and R
2
are independently optionally substituted arylalkyl, and Hal is selected from chloro or bromo.