851179-06-1Relevant academic research and scientific papers
Synthesis and biological investigation of triazolopyridinone derivatives as potential multireceptor atypical antipsychotics
Shi, Wenqiang,Wang, Yu,Wu, Chunhui,Yang, Feipu,Zheng, Wei,Wu, Song,Liu, Yongjian,Wang, Zhen,He, Yang,Shen, Jingshan
, (2020)
A series of triazolopyridinone derivatives originating from the antidepressant trazodone was designed and pharmacologically evaluated. Most of the compounds with a multireceptor functional profile exhibited high potency at the D2, 5-HT1A, and 5-HT2A receptors. Compounds S1, S3, S9 and S12 were selected for further evaluation of druggable potential. Among these compounds, S1, as a D2 receptor partial agonist, demonstrated very potent inhibition of quipazine-induced head-twitch response, which validated its 5-HT2A receptor antagonistic efficacy in vivo. S1 also demonstrated a dose-dependent effect on PCP-induced hyperactivity when administered orally. Thus, S1 endowed with a triazolopyridinone scaffold represents a valuable lead for the development of novel atypical antipsychotics.
SUBSTITUTED HYDANTOINAMIDES AS ADAMTS7 ANTAGONISTS
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Page/Page column 245, (2021/05/21)
The application relates to substituted hydantoinamides of formula (I) as ADAMTS7 antagonists, to processes for their preparation, their use alone or in combination for the treatment or prophylaxis of diseases, in particular of cardiovascular diseases, including atherosclerosis, coronary artery disease (CAD), peripheral vascular disease (PAD), arterial occlusive disease or restenosis after angioplasty. R1 is hydrogen, alkyl, cycloalkyl, heterocycloalkyl, 5- to 6-membered heteroaryl or phenyl; R2 is hydrogen or alkyl; A is 5-membered heteroaryl; Z is 6- to 10-membered aryl or 5- to 10-membered heteroaryl; all groups being optionally substituted.
A O-carboxamide benzamide derivatives, preparation method thereof and a pesticide (by machine translation)
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Paragraph 0086, (2017/08/25)
The present invention provides a kind of formula (I) the structure shown as the O-carboxamide benzamide derivatives. In order to its preparation of insecticide, agricultural, forestry and other common pest with broad-spectrum, high activity, long lasting period and the like, in addition to preventing bollworm, Diamondback moth, Lepidoptera beet pest have very good effect the outer, thereof for the aphid and Homoptera pest also having very good application prospects, therefore in the pest control in the process, can be used as active ingredients used alone, without the need for other insecticides. (by machine translation)
HETEROCYCLIC COMPOUNDS AS PESTICIDES
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, (2015/09/23)
The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.
Novel triazolopyridylbenzamides as potent and selective p38α inhibitors
Aiguadé, Josep,Balagué, Cristina,Carranco, Inés,Caturla, Francisco,Domínguez, María,Eastwood, Paul,Esteve, Cristina,González, Jacob,Lumeras, Wenceslao,Orellana, Adelina,Preciado, Sara,Roca, Ramón,Vidal, Laura,Vidal, Bernat
experimental part, p. 3431 - 3436 (2012/06/18)
A new class of p38α inhibitors based on a biaryl-triazolopyridine scaffold was investigated. X-ray crystallographic data of the initial lead compound cocrystallised with p38α was crucial in order to uncover a unique binding mode of the inhibitor to the hinge region via a pair of water molecules. Synthesis and SAR was directed towards the improvement of binding affinity, as well as ADME properties for this new class of p38α inhibitors and ultimately afforded compounds showing good in vivo efficacy.
PYRAZOLYL-AMINO-SUBSTITUTED PYRIMIDINES AND THEIR USE FOR THE TREATMENT OF CANCER
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Page/Page column 86, (2008/12/08)
The present invention relates to compounds of Formula (I) and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.
NEW 3-([1,2,4]TRIAZOLO[4,3-A]PYRIDIN-7-YL)BENZAMIDE DERIVATIVES
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Page/Page column 54, (2008/12/07)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
Process for preparing 2-aminopyridine derivatives
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Page/Page column 3, (2008/06/13)
A method for preparing 2-aminopyridine derivatives, which comprises substituting of fluorine for hydrazine moiety and reducing with hydrogen using 3-substituted-2,5,6-trifluoropyridine as a starting material, provides 2-aminopyridine derivatives having a purity over 98% under a mild reaction condition.
Removal of fluorine from and introduction of fluorine into polyhalopyridines: An exercise in nucleophilic hetarenic substitution
Bobbio, Carla,Rausis, Thierry,Schlosser, Manfred
, p. 1903 - 1910 (2007/10/03)
Starting from six industrially available fluorinated pyridines, an expedient access to all three tetrafluoropyridines (2-4), all six trifluoropyridines (5-10), and the five non-commercial difluoropyridines (11-14 and 16) was developed. The methods employed for the selective removal of fluorine from polyfluoropyridines were the reduction by metals or complex hydrides and the site-selective replacement by hydrazine followed by dehydrogenation-dediazotation or dehydrochlorination-dediazotation. To introduce an extra fluorine atom, a suitable precursor was metalated and chlorinated before being subjected to a chlorine/ fluorine displacement process.
