26583-55-1Relevant academic research and scientific papers
GLYCOLATE OXIDASE INHIBITORS FOR THE TREATMENT OF DISEASE
-
Paragraph 001159; 001164; 001230; 001231, (2021/01/22)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with a defect in glyoxylate metabolism, for example a disease or disorder associated with the enzyme glycolate oxidase (GO) or alterations in oxalate metabolism. Such diseases or disorders include, for example, disorders of glyoxylate metabolism, including primary hyperoxaluria, that are associated with production of excessive amounts of oxalate.
Compound 1-[2-[4-(2-ethyl-6,8-dimethylimidazo[1,2-α]pyrazin-3-yl)phenyl]ethyl]-3-(p-tolylsulfonyl)urea as a prostaglandin EP4 receptor antagonist
-
Page/Page column 28-31, (2019/04/15)
The present invention describes novel compounds, or veterinary or pharmaceutically acceptable salts thereof, veterinary or pharmaceutical compositions thereof, and medical uses thereof. The compounds of the invention have activity as prostaglandin EP4 rec
Identification of N-Benzyl 3,5-Dinitrobenzamides Derived from PBTZ169 as Antitubercular Agents
Li, Linhu,Lv, Kai,Yang, Yupeng,Sun, Jingquan,Tao, Zeyu,Wang, Apeng,Wang, Bin,Wang, Hongjian,Geng, Yunhe,Liu, Mingliang,Guo, Huiyuan,Lu, Yu
supporting information, p. 741 - 745 (2018/07/05)
A series of benzamide scaffolds were designed and synthesized by the thiazinone ring opening of PBTZ169, and N-benzyl 3,5-dinitrobenzamides were finally identified as anti-TB agents in this work. 3,5-Dinitrobenzamides D5, 6, 7, and 12 exhibit excellent in vitro activity against the drug susceptive Mycobacterium tuberculosis H37Rv strain (MIC: 0.0625 μg/mL) and two clinically isolated multidrug-resistant strains (MIC 0.016-0.125 μg/mL). Compound D6 displays acceptable safety and better pharmacokinetic profiles than PBTZ169, suggesting its promising potential to be a lead compound for future antitubercular drug discovery.
LSD1 Inhibitors
-
Paragraph 0533, (2017/07/14)
The present invention relates to compounds that inhibit LSD1 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
Synthesis of modification material-triphenylamine derivative in perovskite solar cell and application thereof
-
, (2017/08/28)
The invention mainly relates to the design and synthesis of a triphenylamine derivative used as a modification material, and modifies an interface of a perovskite/electron transfer layer in an inverted structure. The specific method comprises the steps of increasing the stability of a perovskite layer by spin-coating of a layer of modification material on a perovskite film and by the use of the interaction among amidogen, I-ions in molecular structures and inorganic Pd in the perovskite layer, improving interfacial compatibility by the use of benzene ring and alkyl chain components in the molecular structures, reducing surface defect, and meanwhile introducing a dipole moment to adjust interfacial energy level, improve the injection efficiency of current carriers and achieve a high-performance solar cell eventually. The formula is shown in the description, and n=1-16.
Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives
Lv, Kai,Li, Linhu,Wang, Bo,Liu, Mingliang,Wang, Bin,Shen, Weiyi,Guo, Huiyuan,Lu, Yu
, p. 117 - 125 (2017/06/05)
We report herein the design and synthesis of “novel imidazo [1,2-a]pyridine-3-carboxamides (IPAs)” bearing a variety of different linkers, based on the structure of IMB-1402 discovered in our lab. Results reveal that 2,6-dimethyl-N-[2-(phenylamino)ethyl] IPAs with an electron-donating group on the benzene ring as a potent scaffold. Compounds 26g and 26h have considerable activity (MIC: 0.041–2.64 μM) against drug-sensitive/resistant MTB strains, and they have acceptable safety indices against MTB H37Rv with the SI values of 4395 and 1405, respectively. Moreover, N-[2-(piperazin-1-yl)ethyl] moiety was also identified as a potentially alternative linker (compound 31), opening a new direction for further SAR studies.
As opioid receptor antagonists or inverse agonists of the novel compounds
-
Paragraph 0467; 0468, (2016/10/08)
Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
Identification of N-(2-Phenoxyethyl)imidazo[1,2-a]pyridine-3-carboxamides as New Antituberculosis Agents
Wu, Zhaoyang,Lu, Yu,Li, Linhu,Zhao, Rui,Wang, Bin,Lv, Kai,Liu, Mingliang,You, Xuefu
supporting information, p. 1130 - 1133 (2016/12/16)
A series of imidazo[1,2-a]pyridine carboxamides (IPAs) bearing an N-(2-phenoxyethyl) moiety was designed and synthesized as new antitubercular agents. Seven 2,6-dimethyl IPAs demonstrated excellent in vitro activity (MIC: 0.025-0.054 μg/mL) against the drug susceptive H37Rv strain and two clinically isolated multidrug-resistant Mycobacterium tuberculosisstrains. Compound 10j displayed acceptable safety and pharmacokinetic properties, opening a new direction for further development.
NOVEL COMPOUNDS AS ANTAGONISTS OR INVERSE AGONISTS AT OPIOID RECEPTORS
-
, (2011/06/19)
Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.
METHOD OF TREATMENT USING NOVEL ANTAGONISTS OR INVERSE AGONISTS AT OPIOID RECEPTORS
-
, (2010/05/13)
A method of treatment using pharmaceutical compositions containing novel antagonists or inverse agonists at opioid receptors for the treatment of binge eating disorder, anorexia nervosa, bulimia nervosa, excess drug or alcohol use, or eating disorder not otherwise specified.
