95926-99-1Relevant articles and documents
DEUTERATED MGL-3196 COMPOUND AND USE THEREOF
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Paragraph 0051; 0054, (2021/09/26)
Disclosed are a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, prodrugs, hydrates or solvates thereof, wherein R1-R10 are independently selected from H and D, respectively, and not all are H. Compared to the undeuterated control compound MGL3 196, the compound of formula (I) or the optical isomers, pharmaceutically acceptable salts, prodrugs, hydrates or solvates thereof has/have better agonistic activity on thyroid hormone receptor p (THR-p), has/have a longer half-life and a lower clearance rate, has/have better metabolic stability and pharmacokinetic properties, and has/have excellent application prospects in the preparation of THR-p agonists and drugs for treating indications to which THR-p agonists are applicable, including dyslipidemia, hypercholesterolemia, nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD).
Substituted pyridazinone compound
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Paragraph 0140; 0143; 0149-0150, (2019/04/17)
The invention provides a pharmaceutical composition of a substituted pyridazinone compound, and application thereof. The substituted pyridazinone compound is a compound as shown in formula (I), or a pharmaceutically acceptable salt, prodrug, hydrate or solvent compound, crystalline form, stereoisomer or isotopic variant thereof. The compound, namely a THR-beta agonist, can be used for treating and/or preventing diseases regulated by thyroid hormone analogs.
COMPOUNDS AS NUCLEAR TRANSPORT MODULATORS AND USES THEREOF
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Page/Page column 96-97, (2019/12/28)
Provided are compounds of Formula I'-III', as well as their preparation and uses, and pharmaceutical compositions comprising these compounds and their uses as nuclear transport modulators. Provided are also uses of the compounds or pharmaceutical compositions in treating or preventing certain neurological disorders and diseases as well as certain types of cancer in humans.
Synthesis of Bicyclo[n.1.0]alkanes by a Cobalt-Catalyzed Multiple C(sp3)?H Activation Strategy
Zhang, Zhuo-Zhuo,Han, Ye-Qiang,Zhan, Bei-Bei,Wang, Sai,Shi, Bing-Feng
supporting information, p. 13145 - 13149 (2017/09/28)
A cobalt-catalyzed dual C(sp3)?H activation strategy has been developed and it provides a novel strategy for the synthesis of bicyclo[4.1.0]heptanes and bicyclo[3.1.0]hexanes. A key to the success of this reaction is the conformation-induced methylene C(sp3)?H activation of the resulting cobaltabicyclo[4.n.1] intermediate. In addition, the synthesis of bicyclo[3.1.0]hexane from pivalamide, by a triple C(sp3)?H activation, has also been demonstrated.
Destabilized Carbenium Ions: α-Carbomethoxy-α,α-dimethyl-methyl Cations
Wolf, Rainer,Gruetzmacher, Hans-Fr.
, p. 398 - 404 (2007/10/02)
Tertiary α-carbomethoxy-α,α-dimethyl-methyl cations a have been generated by electron impact induced fragmentation from the appropriately α-substituted methyl isobutyrates 1-4.The destabilized carbenium ions a can be distinguished from their more stable isomers protonated methyl methacrylate c and protonated methyl crotonate d by MIKE and CA spectra.The loss of I. and Br. from the molecular ions of 1 and 2, respectively, predominantly gives rise to the destabilized ions a, whereas loss of Cl. from +. results in a mixture of ions a and c.The loss of CH3. from +. favours skeletal rearrangement leading to ions d.The characteristic reactions of the destabilized ions a are the loss of CO and elimination of methanol.The loss of CO is associated by a very large KER and non-statistical kinetic energy release (T50 = 920 meV).Specific deuterium labelling experiments indicate that the α-carbomethoxy-α,α-dimethyl-methyl cations a rearrange via a 1,4-H shift into the carbonyl protonated methyl methacrylate c and eventually into the alkyl-O protonated methyl methacrylate before the loss of methanol.The hydrogen rearrangements exhibit a deuterium isotope effect indicating substantial energy barriers between the + isomers.Thus the destabilized carbenium ion a exists as a kinetically stable species within a potential energy well.
Collision-induced Dissociations of Carboxylate Negative Ions from 2-Ethylbutanoic, 2-Methylpropanoic, and Pivalic Acids. An Isotopic Labelling Study
Stringer, Michael B.,Bowie, John H.,Eichinger, Peter C. H.,Currie, Graeme J.
, p. 385 - 390 (2007/10/02)
Deprotonation of Et2CHCO2H yields Et2CHCO21-.On collisional activation this ion forms CO2-., CH2=CH-, and MeCH=CH-.In addition, elimination of H. and Et. yield Et(R)C=CO2-. (R=Et and H, respectively).The elimination of Et. is not a simple cleavage but occurs by loss of H. from a methyl group followed by loss of ethene.The carboxylate ion also rearranges to ; this species decomposes to OH-, , and also eliminates the elements of C3H8 and CH4.All fragmentations have been studied using 2H and 13C labelling: for example it is proposed that loss of CH4 from occurs by a six-centre stepwise process in which the first step (formation of an incipient methyl anion) is rate determining.The collisional activation mass spectra of Et2CHCO2-, Me2CHCO2-, and Me3CCO2- are different, all showing characteristic decompositions.For example, all three ions eliminate methane; the mechanism is different in each case.
ON THE MECHANISM OF THE DECARBOXYLATIVE REARRANGEMENT OF THIOHYDROXAMIC ESTERS
Barton, Derek H.R.,Crich, David,Potier, Pierre
, p. 5943 - 5946 (2007/10/02)
The thermal and photochemical decomposition of a typical thiohydroxamic ester (mixed anhydride) doubly labelled with deuterium has shown the photochemical reaction to be a radical chain process, whereas about 20percent of the thermal reaction involves a cage mechanism.An improved route to 1-hydroxy-5-phenylthiazolin-2-thione is reported.
