218301-62-3Relevant academic research and scientific papers
SYK INHIBITOR AND USE METHOD THEREFOR
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Paragraph 0293-0294, (2020/05/07)
Provided are a Syk inhibitor and a use method therefor, and in particular, disclosed are quinolinone represented by formula (I) or quinazoline derivatives or pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition, and uses in preparing a medicament for treatment of Syk receptor related diseases.
Synthesis and Structural Investigation of Some Electron-Rich Nitroaromatics
White, Jonathan M.,Skene, Colin E.,Deadman, John,Epa, Ruwan,Foenander, Sarah,Hamer, Kyle,Fellowes, Thomas,Lim, Shea Fern,Marcuccio, Sebastian M.,Martin, Roger F.
, p. 311 - 327 (2019/02/07)
2,4-Difluoro-, 2,4,6-Trifluoro-, and 2,3,4,6,tetrafluoronitrobenzenes undergo nucleophilic aromatic substitution, once, twice, and three times with a variety of amine substituents with a high degree of regiochemical control to provide a range of electron-
Continuous Synthesis and Purification by Coupling a Multistep Flow Reaction with Centrifugal Partition Chromatography
?rkényi, Róbert,éles, János,Faigl, Ferenc,Vincze, Péter,Prechl, Anita,Szakács, Zoltán,Kóti, János,Greiner, István
supporting information, p. 8742 - 8745 (2017/07/17)
Continuous-flow multistep synthesis is combined with quasi-continuous final-product purification to produce pure products from crude reaction mixtures. In the nucleophilic aromatic substitution of 2,4-difluoronitrobenzene with morpholine followed by a het
Continuous synthesis and purification by direct coupling of a flow reactor with simulated moving-bed chromatography
O'Brien, Alexander G.,Horvath, Zoltan,Levesque, Francois,Lee, Ju Weon,Seidel-Morgenstern, Andreas,Seeberger, Peter H.
supporting information; experimental part, p. 7028 - 7030 (2012/10/08)
Continuous synthesis meets continuous purification to produce pure products from crude reaction mixtures. In the nucleophilic aromatic substitution of 2,4-difluoronitrobenzene with morpholine the desired monosubstituted product can be continuously separated from the byproducts in a purity of over 99 % by coupling a flow reactor to a simulated moving bed (SMB) chromatography module (see scheme). Copyright
Synthesis of 5-benzylidene-3-(3-fluoro-4-yl-morpholin-4-yl-phenylimino)- thiazolidin-4-one derivatives catalyzed by [BmIm]OH and their anti-microbial activity
Patil, Sudhakar G.,Bagul, Rahul R.,Swami, Mangesh S.,Kotharkar, Nandini,Darade, Kalpana
scheme or table, p. 883 - 886 (2012/01/11)
A series of novel 5-benzylidene-3-(3-fluoro-4-yl-morpholin-4-yl- phenylimino)thiazolidin-4-one derivatives were synthesized using [bmIm]OH as a catalyst and were tested for their antibacterial and antifungal activities. These compounds showed moderate in
NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
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Page/Page column 92, (2009/10/01)
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
Discovery of 1-(3′-aminobenzisoxazol-5′-yl)-3-trifluoromethyl- N-[2-fluoro-4-[(2′-dimethylaminomethyl)imidazol-1-yl]phenyl] -1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor
Quan, Mimi L.,Lam, Patrick Y. S.,Han, Qi,Pinto, Donald J. P.,He, Ming Y.,Li, Renhua,Ellis, Christopher D.,Clark, Charles G.,Teleha, Christopher A.,Sun, Jung-Hui,Alexander, Richard S.,Bai, Steve,Luettgen, Joseph M.,Knabb, Robert M.,Wong, Pancras C.,Wexler, Ruth R.
, p. 1729 - 1744 (2007/10/03)
Modification of a series of pyrazole factor Xa inhibitors to incorporate an aminobenzisoxazole as the P1 ligand resulted in compounds with improved selectivity for factor Xa relative to trypsin and plasma kallikrein. Further optimization of the P4 moiety led to compounds with enhanced permeability and reduced protein binding. The SAR and pharmacokinetic profile of this series of compounds is described herein. These efforts culminated in 1-(3′-aminobenzisoxazol-5′-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2′-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide (11d), a potent, selective, and orally bioavailable inhibitor of factor Xa. On the basis of its excellent in vitro potency and selectivity profile, high free fraction in human plasma, good oral bioavailability, and in vivo efficacy in antithrombotic models, the HCl salt of this compound was selected for clinical development as razaxaban (DPC 906, BMS-561389).
NOVEL GUANIDINE MIMICS AS FACTOR Xa INHIBITORS
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Page/Page column 46, (2010/02/13)
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt forms thereof, wherein rings D-E represent guanidine mimics, which are useful as inhibitors of factor Xa.
[Bmim]PF6 and BF4 ionic liquids as novel and recyclable reaction media for aromatic amination
Yadav,Reddy,Basak,Venkat Narsaiah
, p. 2217 - 2220 (2007/10/03)
Activated aryl halides undergo smooth nucleophilic substitution reactions with secondary amines in 1-butyl-3-methylimidazolium hexafluorophosphate ([bmim]PF6) or 1-butyl-3-methylimidazolium tetrafluoroborate ([bmim]BF4) ionic liquids (ILs) at room temperature to afford the corresponding arylamines in excellent yields under mild and neutral conditions.
Guanidine mimics as factor Xa inhibitors
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Page column 105, 106, (2010/02/04)
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein rings D—E represent guanidine mimics, which are useful as inhibitors of factor Xa.
