613240-18-9Relevant academic research and scientific papers
Oxidize Amines to Nitrile Oxides: One Type of Amine Oxidation and Its Application to Directly Construct Isoxazoles and Isoxazolines
Zhang, Xiao-Wei,He, Xiao-Lin,Yan, Nan,Zheng, Hong-Xing,Hu, Xiang-Guo
, p. 15726 - 15735 (2020/11/30)
A facile oxidative heterocyclization of commercially available amines and tert-butyl nitrite with alkynes or alkenes leading to isoxazoles or isoxazolines is described. The unprecedented strategy of the oxidation of an amine directly to a nitrile oxide was used in this cyclization process. This reaction is highly efficient, regiospecific, operationally simple, mild, and tolerant of a variety of functional groups. Control experiments support a nitrile oxide intermediate mechanism for this novel class of oxidative cyclization reactions. Moreover, synthetic applications toward bioactive molecular skeletons and the late-stage modification of drugs were realized.
PIPERIDINE CXCR7 RECEPTOR MODULATORS
-
Page/Page column 132-133, (2018/02/28)
The present invention relates to piperidine derivatives of formula (I) wherein Ar1, Ar2, RAr1, R1, R2, and R3 are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as CXCR7 receptor modulators.
Synthesis and cellular bioactivities of novel isoxazole derivatives incorporating an arylpiperazine moiety as anticancer agents
?al??kan, Burcu,?bi?, Kübra,Banoglu, Erden,Sinoplu, Esra,Akhan Güzelcan, Ece,?etin Atalay, Rengül
, p. 1352 - 1361 (2018/11/21)
In our endeavour towards the development of effective anticancer therapeutics, a novel series of isoxazole-piperazine hybrids were synthesized and evaluated for their cytotoxic activities against human liver (Huh7 and Mahlavu) and breast (MCF-7) cancer ce
New FAAH inhibitors based on 3-carboxamido-5-aryl-isoxazole scaffold that protect against experimental colitis
Andrzejak, Virginie,Muccioli, Giulio G.,Body-Malapel, Mathilde,El Bakali, Jamal,Djouina, Madjid,Renault, Nicolas,Chavatte, Philippe,Desreumaux, Pierre,Lambert, Didier M.,Millet, Regis
experimental part, p. 3777 - 3786 (2011/08/03)
Growing evidence suggests a role for the endocannabinoid (EC) system, in intestinal inflammation and compounds inhibiting anandamide degradation offer a promising therapeutic option for the treatment of inflammatory bowel diseases. In this paper, we repor
Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists
Palin, Ronald,Abernethy, Lynn,Ansari, Nasrin,Cameron, Kenneth,Clarkson, Tom,Dempster, Maureen,Dunn, David,Easson, Anna-Marie,Edwards, Darren,MacLean, John,Everett, Katy,Feilden, Helen,Ho, Koc-Kan,Kultgen, Steve,Littlewood, Peter,McArthur, Duncan,McGregor, Deborah,McLuskey, Hazel,Neagu, Irina,Neale, Stuart,Nisbet, Lesley-Anne,Ohlmeyer, Michael,Pham, Quynhchi,Ratcliffe, Paul,Rong, Yajing,Roughton, Andrew,Sammons, Melanie,Swanson, Robert,Tracey, Heather,Walker, Glenn
scheme or table, p. 892 - 898 (2011/03/21)
Optimisation of a screening hit incorporating both TRPV1 activity and solubility was conducted. Substitution of the isoxazole-3-carboxamide with the bespoke 1S, 3R-3-aminocyclohexanol motif afforded the requisite balance of potency and solubility. Compounds 32 and 40 were found to have antihyperalgesic effects in the rat CFA Hg assay and induce a mechanism based hyperthermia.
Synthesis of 2,3 and 4,5-dihydro-hydroxy-isoxazoles and isoxazoles under different pH conditions
Andrzejak, Virginie,Millet, Regis,Bakali, Jamal El,Guelzim, Abdelhalim,Gluszok, Sebastien,Chavatte, Philippe,Bonte, Jean-Paul,Vaccher, Claude,Lipka, Emmanuelle
experimental part, p. 32 - 38 (2010/08/05)
Reaction between aryl 1,3-diketoesters 2a-e and hydroxylamine hydrochloride has been investigated under different experimental conditions. Whereas acid conditions gave principally 3,5-isoxazole esters (3a-e), reactions under neutral and basic conditions l
ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES
-
Page/Page column 41, (2010/08/18)
The present invention relates to isoxazole-3-carboxamide derivative having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide deriv
5-PHENYL-ISOXAZOLE-3-CARBOXAMIDE DERIVATIVES AS TRPV1 MODULATORS
-
Page/Page column 35-36, (2009/03/07)
The present invention relates to isoxazole-3-carboxamide derivative having the general Formula (I), or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of said isoxazole-3-carboxamide de
Synthesis and structure-activity relationships of thiadiazole-derivatives as potent and orally active peroxisome proliferator-activated receptors α/δ dual agonists
Shen, Lan,Zhang, Yan,Wang, Aihua,Sieber-McMaster, Ellen,Chen, Xiaoli,Pelton, Patricia,Xu, June Z.,Yang, Maria,Zhu, Peifang,Zhou, Lubing,Reuman, Michael,Hu, Zhiyong,Russell, Ronald,Gibbs, Alan C.,Ross, Hamish,Demarest, Keith,Murray, William V.,Kuo, Gee-Hong
, p. 3321 - 3341 (2008/09/19)
Replacement of the methyl-thiazole moiety of GW501516 (a PPARδ selective agonist) with [1,2,4]thiadiazole gave compound 21 which unexpectedly displayed submicromolar potency as a partial agonist at PPARα in addition to the high potency at PPARδ. A structu
ARYLACETATE DERIVATIVE HAVING ISOXAZOLE SKELETON
-
Page/Page column 111-112, (2008/06/13)
A compound of the formula (I): pharmaceutically acceptable salt or solvate thereof, wherein Y is a group of the formula: wherein Ring A is optionally substituted aryl or optionally substituted heteroaryl, X3 is COOR17 or the like Y i
