65260-58-4Relevant academic research and scientific papers
CHDI-626, a PET Tracer Candidate for Imaging Mutant Huntingtin Aggregates with Reduced Binding to AD Pathological Proteins
Bard, Jonathan A.,Brown, Christopher J.,Chen, Xuemei,Clark-Frew, Daniel,Coe, Samuel,Conlon, Mike,Davis, Randall,Dominguez, Celia,Ensor, Samantha,Esposito, Simone,Gai, Xinjie,Green, Samantha,Greenaway, Catherine,Haber, James,Halldin, Christer,Hayes, Sarah,He?mann, Manuela,Herbst, Todd,Herrmann, Frank,Hsai, Ming Min,Johnson, Peter D.,Khetarpal, Vinod,Kotey, Adrian,Lee, Matthew R.,Liu, Longbin,Mangette, John E.,Mills, Matthew R.,Monteagudo, Edith,Moren, Anton Forsberg,Mrzljak, Ladislav,Munoz-Sanjuan, Ignacio,Nag, Sangram,Nibbio, Martina,Orsatti, Laura,Prime, Michael E.,Schaertl, Sabine,Scheich, Christoph,Sproston, Joanne,Stepanov, Vladimir,Varn?s, Katarina,Varrone, Andrea,Wityak, John
supporting information, p. 12003 - 12021 (2021/09/02)
The expanded polyglutamine-containing mutant huntingtin (mHTT) protein is implicated in neuronal degeneration of medium spiny neurons in Huntington's disease (HD) for which multiple therapeutic approaches are currently being evaluated to eliminate or redu
Triazolopyridazine derivative as well as preparation method, pharmaceutical composition and application thereof
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Paragraph 0471-0474, (2021/06/22)
The invention relates to triazolopyridazine derivatives as well as a preparation method, a pharmaceutical composition and application thereof. The invention provides a compound shown in a general formula (I), cis-trans isomers, enantiomers, diastereoisomers, racemes, solvates, hydrates or pharmaceutically acceptable salts or prodrugs of the compound, and a preparation method of the compound, the cis-trans isomers, the enantiomers, the diastereoisomers, the racemes, the solvates, the hydrates or the pharmaceutically acceptable salts or the prodrugs of the compound; preparation method thereof; pharmaceutical compositions containing the compounds, and the use of the compounds as alpha 5-GABAA receptor modulators, wherein R 1, R 2, and Z are as defined in the specification. pharmaceutical compositions containing the compounds and application of the compounds as alpha-5-GABAA receptor modulators, wherein R1, R2 and Z are as defined in the specification.
PROBES FOR IMAGING HUNTINGTIN PROTEIN
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Paragraph 0539; 0540, (2017/03/21)
Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.
HETEROCYCLIC COMPOUND
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Paragraph 1111, (2016/06/28)
A compound represented by the formula (I): wherein each symbol is as described in the SPECIFICATION, or a salt thereof has a PDE2A inhibitory action, and is useful as a prophylactic or therapeutic drug for schizophrenia, Alzheimer's disease and the like.
1,5-DIPHENYL-PYRROLIDIN-2-ONE COMPOUNDS AS CB-1 LIGANDS
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Page/Page column 21, (2009/12/05)
CB-1 receptor inverse agonist compounds of Formula (I) and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia.
Process for producing 2-substituted thiopyrimidine-4-carboxylate
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, (2008/06/13)
There is disclosed a process for producing a 2-substituted thiopyrimidine-4-carboxylate represented by the formula (3): wherein R2 represents a substituted or unsubstituted hydrocarbon group and R3 represents a hydrocarbon group, which comprises reacting an α-keto ester compound represented by the formula (1): R1OCH═CHCOCO2R2??(1) wherein R1 represents a substituted or unsubstituted hydrocarbon group, and R2 has the same meaning as defined above, with an isothiourea compound represented by the formula (2): wherein R3 has the same meaning as defined above.
Enantioselective synthesis of dihydropyrans. Catalysis of hetero Diels - Alder reactions by bis(oxazoline) copper(II) complexes
Evans, David A.,Johnson, Jeffrey S.,Olhava, Edward J.
, p. 1635 - 1649 (2007/10/03)
C2-symmetric bis(oxazoline) - Cu(II) complexes 1 and 2 catalyze the inverse electron demand hetero Diels - Alder reaction of α,β-unsaturated carbonyl compounds (heterodiene) with electron-rich olefins (heterodienophile) in high diastereo- and enantioselectivity, α,β- Unsaturated acyl phosphonates and β,γ-unsaturated α-keto esters and amides are effective heterodienes, while enol ethers and sulfides function as heterodienophiles. A range of substitution patterns is possible on the heterodiene: terminal alkyl, aryl, alkoxy, and thioether substituents are all tolerated. The enantioselective synthesis of dihydropyrans by this method has been shown to be straightforward: cycloadditions may be conducted with as little as 0.2 mol % of the chiral catalyst and are readily run on multigram scale. The reactions exhibit a favorable temperature - enantioselectivity profile, with selectivities exceeding 90% even at room temperature. A simple reaction protocol that employs a solid air-stable catalyst, convenient reaction temperatures, and low catalyst loadings is described. The utility of the derived cycloadducts in the preparation of chiral building blocks is demonstrated. Models for asymmetric induction are discussed considering product stereochemistry, X-ray crystallographic data for the solid catalysts, and mechanistic studies.
An improved dienophile-induced access to enantiopure 2,4-dideoxysugar lactones via hetero Diels-Alder reaction: Synthesis of the (+)-lactone moiety of compactin
Dujardin, Gilles,Rossignol, Sandrine,Brown, Eric
, p. 763 - 770 (2007/10/03)
Polystereocontrolled access to 4-type heterocycloadducts was consistently improved by using a new 4-oxy-substituted 1-oxabutadiene, methyl (E)-tert-butoxymethylenepyruvate (1c). Obtained in both enantiomeric forms with high diastereomerical purity, these adducts led to diprotected 2,4- dideoxyglucose 10 and -gluconolactone 12 in both L and D series in high yields. Epimerization of (-)-12 via intramolecular Mitsunobu inversion gave a straightforward access to the lactone moiety (+)-16 of compactin.
Highly Efficient Syntheses of Alkyl 3,3-Dialkoxypropanoates, Alkyl 4-Ethoxy-2-oxo-3-butenoates, and Monoprotected Malonaldehydes
Tietze, Lutz-F.,Meier, Heinrich,Voss, Edgar
, p. 274 - 277 (2007/10/02)
Haloform reaction of 4-alkoxy-1,1,1-trichloro-3-buten-2-ones, which can be obtained by acylation of enol ethers, gives 3,3-dialkoxypropanoic esters.Transacetalization of ethyl 3,3-diethoxypropanoate with 2,2-dimethyl-1,3-propanediol, followed by reduction and oxidation with DMSO/oxalyl chloride yields a monoprotected malonaldehyde. 4-Ethoxy-2-oxo-3-butenoates are synthesized either by acylation of enol ethers with alkoxalyl chlorides or by Claisen condensation of alkyl pyruvates with orthoesters.
