- SYK INHIBITOR AND USE METHOD THEREFOR
-
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.
- -
-
Paragraph 0293; 0295
(2020/05/07)
-
- Continuous Synthesis and Purification by Coupling a Multistep Flow Reaction with Centrifugal Partition Chromatography
-
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
- ?rkényi, Róbert,éles, János,Faigl, Ferenc,Vincze, Péter,Prechl, Anita,Szakács, Zoltán,Kóti, János,Greiner, István
-
supporting information
p. 8742 - 8745
(2017/07/17)
-
- Hydrazine-mediated reduction of nitro and azide functionalities catalyzed by highly active and reusable magnetic iron oxide nanocrystals
-
Iron oxide (Fe3O4) nanocrystals generated in situ from an inexpensive and readily available iron source catalyze the reduction of nitroarenes to anilines with unparalleled efficiency. The procedure is chemoselective, avoids the use of precious metals, and can be applied under mild reflux conditions (65 or 80 C) or using sealed vessel microwave heating in an elevated temperature regime (150 C). Utilizing microwave conditions, a variety of functionalized anilines have been prepared in nearly quantitative yields within 2-8 min at 150 C, in a procedure also successfully applied to the reduction of aliphatic nitro compounds and azides. The iron oxide nanoparticles are generated in a colloidal form, resulting in homogeneous solutions suitable for continuous flow processing. Selected examples of anilines of industrial importance have been prepared in a continuous regime using this protocol.
- Cantillo, David,Moghaddam, Mojtaba Mirhosseini,Kappe, C. Oliver
-
p. 4530 - 4542
(2013/06/05)
-
- 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
-
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
- Patil, Sudhakar G.,Bagul, Rahul R.,Swami, Mangesh S.,Kotharkar, Nandini,Darade, Kalpana
-
scheme or table
p. 883 - 886
(2012/01/11)
-
- NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
-
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.
- -
-
Page/Page column 92
(2009/10/01)
-
- 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
-
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).
- 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)
-
- NOVEL GUANIDINE MIMICS AS FACTOR Xa INHIBITORS
-
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.
- -
-
Page/Page column 46
(2010/02/13)
-
- Guanidine mimics as factor Xa inhibitors
-
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.
- -
-
Page column 105-106
(2010/02/04)
-
- Nitrogen containing heteroaromatics as factor Xa inhibitors
-
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.
- -
-
-