67354-35-2Relevant academic research and scientific papers
GPR52 MODULATOR COMPOUNDS
-
Page/Page column 54; 59-60, (2021/05/15)
The disclosures herein relate to novel compounds of Formula (1): (1) and salts thereof, wherein R1, Q, X, Y and Z are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with GPR52 receptors.
HETEROCYCLIC COMPOUND
-
Paragraph 0539, (2018/09/14)
The present invention provides a heterocyclic compound having an RIP1 kinase inhibitory action, which is useful for the prophylaxis or treatment of Gaucher's disease, Niemann-Pick disease, inflammatory bowel disease, multiple sclerosis, chronic kidney disease, acute kidney injury, acute hepatic failure, autoimmune hepatitis, hepatitis B, hepatitis C, alcohol steatohepatitis, non-alcohol steatohepatitis and the like. The present invention relates to a compound represented by the following formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
Synthesis of Substituted 3(2H)-Furanones Using Alkylative Intramolecular Cyclization of Sulfonium Salts
Inagaki, Sho,Ukaku, Mika,Chiba, Akira,Takahashi, Fumi,Yoshimi, Yasuharu,Morita, Toshio,Kawano, Tomikazu
, p. 8363 - 8369 (2016/09/28)
The facile alkylative intramolecular cyclization of 3-alkoxycarbonyl-2-oxopropyldiphenylsulfonium salts is described. This simple method can be readily applied to the synthesis of a novel family of 4-alkylated 3(2H)-furanones in moderate to high yields under mild conditions via a one-pot process.
Synthesis and Antifungal Activity of Novel Furan-2,4-dione Derivatives Containing Substituted Phenylhydrazine Moiety
Hu, Ying,Zhang, Li-Zhi,Ren, Zheng-Jiao,Zhao, Zheng,Xu, Wen-Qin,Yang, Chun-Long
, p. 495 - 500 (2015/06/23)
A series of novel 3-(2-(substituted phenyl)hydrazinylmethylidene)furan-2,4(3H,5H)-diones were designed and synthesized with ethyl 4-chloroacetoacetate as the starting material. Their structures were confirmed by FT-IR, 1H NMR, 13C NMR, EI-MS and elemental analysis. Bioassay data demonstrated that these compounds exhibited remarkable antifungal activity against Fusarium graminearum, Botrytis cinerea, Rhizoctonia cerealis and Colletotrichum capsici. Compound 3-(2-(4-bromophenyl)hydrazinylmethylidene)furan-2,4(3H,5H)-dione (5g) had excellent bioactivity against Botrytis cinerea with an EC50 value of 0.18 μg/mL - markedly lower than the 0.24 μg/mL of the commercial fungicide procymidone. The result revealed that introducing the halogenated phenylhydrazine at the 3-position of furan-2,4(3H, 5H)-dione was an effective way to design new tetronic acid derivatives as new fungicides. A series of novel furan-2,4-dione derivatives containing a substituted phenylhydrazine moiety were designed and synthesized. These compounds exhibited remarkable antifungal activity against Fusarium graminearum, Botrytis cinerea, Rhizoctonia cerealis and Colletotrichum capsici. Compound 5g showed significantly better bioactivity than the control fungicides.
3,4-DISUBSTITUTED 1 H-PYRAZOLE AND 4,5-DISUBSTITUTED THIAZOLE INHIBITORS OF SYK
-
Page/Page column 91, (2014/05/24)
The present invention relates to the use of novel compounds of formula (I), wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.
Synthesis, characterization, antifungal evaluation and 3D-QSAR study of phenylhydrazine substituted tetronic acid derivatives
Hu, Ying,Wang, Junjun,Lu, Aimin,Yang, Chunlong
supporting information, p. 3772 - 3776 (2014/09/17)
A series of 3-(1-(2-(substituted phenyl)hydrazinyl)alkylidene)furan-2,4(3H, 5H)-diones were designed and prepared using two synthetic routes. Their structures were confirmed by FT-IR, 1H NMR, 13C NMR, MS, elemental analysis and single-crystal X-ray diffraction. Their bioactivity was evaluated against Botrytis cinerea in vitro. Most target compounds exhibited remarkable antifungal activity. Two compounds 7f and 7h were highly effective and their EC50 values were 0.241 μg/mL and 0.167 μg/mL, respectively, close to that of the control drug procymidone. 3D-QSAR studies of CoMFA and CoMSIA were carried out. Models with good predictive ability were generated with the cross validated q2 values for CoMFA and CoMSIA being 0.565 and 0.823. Conventional r2 values were 0.983 and 0.945, respectively. The results provided a practical tool for guiding the design and synthesis of novel and more potent tetronic acid derivatives containing substituted phenylhydrazine moiety.
4-tert-butoxy-1-ethoxy-1,3-bis(trimethylsilyloxy)-1,3-butadiene. A new diene and its application to the synthesis of γ-alkylidenetetronic acids
Van Nguyen, Thi Hong,Cam, Bui Duy,Ahmed, Zafar,Langer, Peter
, p. 836 - 840 (2013/08/23)
A new approach to γ-alkylidenetetronic acids is reported which is based on Me3SiOTf-catalyzed [3+2] cyclization of 4-tert-butoxy-1,3- bis(trimethylsilyloxy)-1,3-butadiene with oxalyl chloride, orthogonal protection of the α-hydroxy group by benzylation and subsequent deprotection of the β-hydroxy group.
Biomimetic synthesis, antibacterial activity and structure-activity properties of the pyroglutamate core of oxazolomycin
Angelov, Plamen,Chau, Yui Kwan Sonia,Fryer, Paul J.,Moloney, Mark G.,Thompson, Amber L.,Trippier, Paul C.
supporting information; experimental part, p. 3472 - 3485 (2012/06/01)
Biomimetic intramolecular aldol reactions on oxazolidine templates derived from serine may be used to generate densely functionalised pyroglutamates, which are simpler mimics of the right hand side of oxazolomycin. Some of the compounds from this sequence exhibit in vivo activity against S. aureus and E. coli, suggesting that pyroglutamate scaffolds may be useful templates for the development of novel antibacterials, and cheminformatic analysis has been used to provide some structure-activity data.
Ru-catalyzed asymmetric hydrogenation of γ-heteroatom substituted β-keto esters
Fan, Weizheng,Li, Wanfang,Ma, Xin,Tao, Xiaoming,Li, Xiaoming,Yao, Ying,Xie, Xiaomin,Zhang, Zhaoguo
experimental part, p. 9444 - 9451 (2012/01/13)
A series of enantiomerically pure γ-heteroatom substituted β-hydroxy esters were synthesized with high enantioselectivities (up to 99.1% ee) by hydrogenation of γ-heteroatom substituted β-keto esters in the presence of Ru-(S)-SunPhos catalyst. These asymmetric hydrogenations provide key building blocks for a variety of naturally occurring and biologically active compounds.
LIGAND-DIRECTED COVALENT MODIFICATION OF PROTEIN
-
Page/Page column, (2013/03/26)
The present invention relates to enzyme inhibitors. More specifically, the present invention relates to ligand-directed covalent modification of proteins; method of designing same; pharmaceutical formulation of same; and method of use.
