3833-78-1Relevant academic research and scientific papers
Design, synthesis and biological evaluation of 2-aminoquinazolin-4(3H)-one derivatives as potential SARS-CoV-2 and MERS-CoV treatments
Lee, Jun Young,Shin, Young Sup,Jeon, Sangeun,Lee, Se In,Noh, Soojin,Cho, Jung-Eun,Jang, Min Seong,Kim, Seungtaek,Song, Jong Hwan,Kim, Hyoung Rae,Park, Chul Min
supporting information, (2021/03/15)
Despite the rising threat of fatal coronaviruses, there are no general proven effective antivirals to treat them. 2-Aminoquinazolin-4(3H)-one derivatives were newly designed, synthesized, and investigated to show the inhibitory effects on SARS-CoV-2 and MERS-CoV. Among the synthesized derivatives, 7-chloro-2-((3,5-dichlorophenyl)amino)quinazolin-4(3H)-one (9g) and 2-((3,5-dichlorophenyl)amino)-5-hydroxyquinazolin-4 (3H)-one (11e) showed the most potent anti-SARS-CoV-2 activities (IC50 50 50 > 25 μM). In addition, both compounds showed acceptable results in metabolic stabilities, hERG binding affinities, CYP inhibitions, and preliminary PK studies.
DIACYLGLYCEROL KINASE MODULATING COMPOUNDS
-
Paragraph 1252, (2021/07/02)
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
METHODS OF CULTURING AND/OR EXPANDING STEM CELLS AND/OR LINEAGE COMMITTED PROGENITOR CELLS USING AMIDO COMPOUNDS
-
Paragraph 0578, (2020/02/14)
Provided are methods for expanding stem cells and/or lineage committed progenitor cells, such as hematopoietic stems cells and/or lineage committed progenitor cells, at least in part, by using compounds that antagonize AhR. The compounds are represented by formulae (I) (II) (III) (IV), wherein the letters and symbols a, b, c, d, e, f, g, Z, R1b, R2a and R2b have the meanings provided in the specification. Also provided are compositions comprising stem cells and/or lineage committed progenitor cells expanded by methods disclosed herein and methods for the treatment of diseases treatable by same.
AMIDO COMPOUNDS AS AhR MODULATORS
-
Paragraph 0447, (2019/02/06)
Provided herein are compounds, compositions and methods of using the compounds and compositions for the treatment of diseases modulated, as least in part, by AhR. The compounds are represented by formulae Formula (I), (II), (III), (iv): wherein the letters and symbols a, b, c, d, e, f, g, Z, R1b, R2a and R2b have the meanings provided in the specification.
Facile and efficient synthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenation condensation
Wang, Peng-Xu,Wang, Ya-Nan,Lin, Zi-Yun,Li, Gang,Huang, Hai-Hong
, p. 1183 - 1189 (2018/04/02)
The heterocyclizations from various methyl (2-nitrobenzoyl)carbamates to substituted quinazoline-2,4(1H,3H)-diones under hydrogenation conditions were investigated in this study. In the presence of p-toluenesulfonic acid monohydrate in methanol, various q
BICYCLIC DERIVATIVE CONTAINING PYRIMIDINE RING, AND PREPARATION METHOD THEREFOR
-
Paragraph 0129; 0130, (2016/04/26)
The present invention provides: a bicyclic derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof; a preparation method therefor, a pharmaceutical composition comprising the same; and a use therefor. According to the present invention, the bicyclic compound derivative comprising a pyrimidine ring, or a pharmaceutically acceptable salt thereof acts as a 5-HT4 receptor agonist, and thus can be usefully applied to the prevention or treatment of dysfunction in gastrointestinal motility, for example, gastrointestinal diseases such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, diabetic gastric atony and the like.
A catalyst-free N-H insertion/Mannich-type reaction cascade of α-nitrodiazoesters
Yang, Ting,Zhuang, Hao,Lin, Xichen,Xiang, Jia-Ning,Elliott, John D.,Liu, Lianghui,Ren, Feng
supporting information, p. 4159 - 4163 (2013/07/26)
A catalyst-free N-H insertion/Mannich-type reaction cascade of α-nitrodiazoesters with anilines has been developed to afford a variety of α-amino-α-aryl esters in 60-83% yields and under mild reaction conditions (23 or 40 C).
Design and development of bioinspired guanine-based organic catalyst for asymmetric catalysis
Suez, Gal,Bloch, Victoria,Nisnevich, Gennady,Gandelman, Mark
, p. 2118 - 2122 (2012/06/01)
Design, preparation, and studies of a family of new organic catalysts are presented. The design of the catalysts is inspired by the ability of DNA nucleobases to develop precise and explicit hydrogen bonds. We have shown that this phenomenon can be used to create a useful organic catalyst that demonstrates a recognition pattern similar to those of common organic substrates. A selected bifunctional catalyst based on a guanine structure has been shown to catalyze the conjugate addition of 1,3-dicarbonyl compounds to various nitroalkenes, providing the products in good yields and enantioselectivities.
AMINOQUINAZOLINE COMPOUNDS FOR COMBATING INVERTEBRATE PESTS
-
Page/Page column 108, (2011/04/24)
The invention relates to aminoquinazoline compounds or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to me
AMINO-ETHYL-AMINO-ARYL (AEAA) COMPOUNDS AND THEIR USE
-
Page/Page column 123-124, (2009/10/06)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain amino-ethyl-amino-aryl (AEAA) compounds which, inter alia, inhibit protein kinase D (PKD) (e.g., PKD1, PKD2, PKD3). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PKD, and in the treatment of diseases and conditions that are mediated by PKD, that are ameliorated by the inhibition of PKD, etc., including proliferative conditions such as cancer, etc.
