575474-26-9Relevant academic research and scientific papers
Synthesis, Biological Activity of Pyrimidine Linked with Morpholinophenyl Derivatives
Gorle, Sridevi,Maddila, Suresh,Chokkakula, Santosh,Lavanya, Palakondu,Singh, Moganavelli,Jonnalagadda, Sreekanth B.
, p. 1852 - 1858 (2016)
A new series of 5-fluoro-N4-(3-(4-substitutedbenzylamino)phenyl)-N2-(4-morpholinophenyl)pyrimidine-2,4-diamine derivatives (7a, 7b, 7c, 7d, 7e, 7f, 7g, 7h, 7i, 7j) are prepared from using an intermediate compound 5-fluoro-N4-(3-(aminophenyl)-N2-(4-morpholinophenyl)pyrimidine-2,4-diamine (5). The structures of the newly synthesized products are established from their spectral1H-NMR,13C-NMR,19F-NMR, ESI-MS, and analytical data. Here we report the synthesized compounds and larvicidal activity. All the compounds are screened for their significant larvicidal activity against third instar larvae at 24, 48, and 78-h time exposure, and values were compared with standard drug Malathion. The Compounds 7i, 7a, 7c, 7f, and 7j exhibited significant activity. However the compounds 7b, 7e, 7d, and 7h showed excellent activity when compared to the above compounds and to standard drug malathion too because of the presence of mild electron withdrawing groups such as trifluoro, fluorine, hydroxy, nitro, and methoxy derivatives which are attached to the benzyl ring.
BENZENESULFONAMIDE DERIVATIVES AND USES THEREOF
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Paragraph 00204; 00268, (2021/02/12)
Provided herein are benzenesulfonamide derivatives having Formula (III), pharmaceutical compositions comprising said compounds, and method for using said compounds for disrupting proteins/polypeptides, protein/polypeptide function, and for the treatment of diseases through the disruption of proteins or polypeptides involved in the etiology of the disease. Said compounds comprise fluorinated benzene sulfonamide structures.
PENTAFLUOROBENZENESULFONAMIDE DERIVATIVES AND USES THEREOF
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Paragraph 00288, (2021/05/29)
Provided herein are pentafluorobenzenesulfonamide compounds of Formula (I), pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases. These compounds are covalent small molecule inhibitors,
Design, synthesis and biological evaluation of novel dithiocarbamate-substituted diphenylaminopyrimidine derivatives as BTK inhibitors
Zhai, Zheng,Li, Ridong,Bai, Xinyu,Ning, Xianling,Lin, Zhiqiang,Zhao, Xuyang,Jin, Yan,Yin, Yuxin
, p. 4124 - 4142 (2019/08/07)
Bruton's tyrosine kinase (BTK) has emerged as an attractive target related to B-lymphocytes dysfunctions, especially hematologic malignancies and autoimmune diseases. In our study, a series of diphenylaminopyrimidine derivatives bearing dithiocarbamate moieties were designed and synthesized as novel BTK inhibitors for treatment of B-cell lymphoma. Among all these compounds, 30ab (IC50 = 1.15 ± 0.19 nM) displays similar or more potent inhibitory activity against BTK than spebrutinib (IC50 = 2.12 ± 0.32 nM) and FDA approved drug ibrutinib (IC50 = 3.89 ± 0.57 nM), which is attributed to close binding of 30ab with BTK predicted by molecular docking. In particular, 30ab exhibits enhanced anti-proliferative activity against B-lymphoma cell lines at the IC50 concentration of 0.357 ± 0.02 μM (Ramos) and 0.706 ± 0.05 μM (Raji), respectively, almost 10-fold better than ibrutinib and spebrutinib. In addition, 30ab displays stronger selectivity on B-cell lymphoma over other cancer cell lines than spebrutinib. Furthermore, 30ab efficiently blocks BTK downstream pathways and results in apoptosis of cancer cells. In vivo xenograft model evaluation demonstrates the significant efficacy and broad safety margin of 30ab in treatment of B-cell lymphoma. We propose that compound 30ab is a candidate for further study and development based on our current findings.
Dithiocarbamate type compound used as BTK (Bruton Tyrosine Kinase) inhibitor
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Paragraph 0086; 0087; 0088, (2019/04/27)
The invention aims at providing a dithiocarbamate type compound used as a BTK (Bruton Tyrosine Kinase) inhibitor and a pharmaceutical composition thereof, a preparation method and application. The compound provided by the invention has a structure shown as a general formula (I). The formula (I) is shown in the description.
HETEROARYL COMPOUNDS AND USES THEREOF
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Paragraph 0617, (2015/07/02)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
2,4-Pyrimidinediamine Compounds and Their Uses
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Paragraph 0451, (2015/11/10)
The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
HETEROARYL COMPOUNDS AND USES THEREOF
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Paragraph 0368; 0371, (2014/07/08)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
HETEROARYL COMPOUNDS AND USES THEREOF
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Page/Page column 244, (2010/01/30)
The present invention provides inhibitors of protein kinases of formula I-a and I-b, pharmaceutically acceptable compositions thereof, and methods of using the same.
