403985-96-6Relevant academic research and scientific papers
Efficient Method for the Synthesis of Amino-1,3-Oxazines from Thioureas
Richardson, Jeffery,Lindsay-Scott, Peter J.,Larichev, Vladimir,Pocock, Emily
, p. 2853 - 2863 (2020/12/22)
The synthesis of a subtype-selective inhibitor BACE-1 inhibitor is presented. One of the key transformations in this sequence is the conversion of a thiourea to the bicyclic 1,3-aminooxazine. This article outlines the development and application of this method to the target molecule as well as further exploration of its scope and mechanism.
COMBINATION THERAPY OF BACE-1 INHIBITOR AND ANTI-N3PGLU ABETA ANTIBODY
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Page/Page column 19; 22, (2018/03/09)
The present invention provides a method of treating a cognitive or neurodegenerative disease, comprising administering to a patient in need of such treatment an effective amount of a compound of the formula or a pharmaceutically acceptable salt thereof in combination with an effective amount of an anti-N3pGlu Abeta antibody selected from the group consisting of hE8L, B12L, R17L, Antibody I, and Antibody II.
COMBINATION THERAPY
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Page/Page column 21; 24-25, (2018/05/16)
The present invention provides a method of treating a cognitive or neurodegenerative disease, comprising administering to a patient in need of such treatment an effective amount of a compound of the formula (I):or a pharmaceutically acceptable salt thereo
4,4A,5,7-TETRAHYDRO-3H-FURO[3,4-B]PYRIDINYL COMPOUNDS
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Page/Page column 45, (2018/05/24)
The present invention relates to 4,4a,5,7-tetrahydro-3H-furo[3,4-b]pyridinyl compound inhibitors of beta-site APP-cleaving enzyme having the structure shown in Formula (I) wherein the radicals are as defined in the specification. The invention is also dir
N-[3-[2-AMINO-5-(1,1-DIFLUOROETHYL)-4,4A,5,7-TETRAHYDROFURO[3,4-D][1,3]OXAZIN-7A-YL]-4-FLUORO-PHENYL]-5-(TRIFLUOROMETHYL)PYRIDINE-2-CARBOXAMIDE AND ITS (4AR,5S,7AS) ISOMER AS A SELECTIVE BACE1 INHIBITOR FOR TREATING E.G. ALZHEIMER'S DISEASE
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Page/Page column 17, (2017/12/16)
The present invention provides N-[3-[2-Amino-5-(1,1-difluoroethyl) -4,4a,5,7-tetrahydrofuro[3,4-d][1,3]oxazin-7a-yl]-4-fluoro-phenyl]-5- (trifluoromethyl)pyridine-2-carboxamide, i.e. the compound of Formula I: [Formula should be inserted here] or a pharma
TETRAHYDROFURANE-FUSED AMINOHYDROTHIAZINE DERIVATIVES WHICH ARE USEFUL IN THE TREATMENT OF ALZHEIMER'S DISEASE
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Page/Page column 13; 19; 20, (2016/11/17)
The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof.
SELECTIVE BACE1 INHIBITORS
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Paragraph 0046; 0047, (2016/09/26)
The present invention provides a compound of Formula II: or a pharmaceutically acceptable salt thereof.
FUSED AMINODIHYDRO-OXAZINE DERIVATIVES
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Page/Page column 88, (2011/02/24)
A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is -NReCO- or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
Synthesis and stereospecificity of 4,5-disubstituted oxazolidinone ligands binding to T-box riboswitch RNA
Orac, Crina M.,Zhou, Shu,Means, John A.,Boehm, David,Bergmeier, Stephen C.,Hines, Jennifer V.
scheme or table, p. 6786 - 6795 (2011/12/04)
The enantiomers and the cis isomers of two previously studied 4,5-disubstituted oxazolidinones have been synthesized, and their binding to the T-box riboswitch antiterminator model RNA has been investigated in detail. Characterization of ligand affinities and binding site localization indicates that there is little stereospecific discrimination for binding antiterminator RNA alone. This binding similarity between enantiomers is likely due to surface binding, which accommodates ligand conformations that result in comparable ligand-antiterminator contacts. These results have significant implications for T-box antiterminator-targeted drug discovery and, in general, for targeting other medicinally relevant RNA that do not present deep binding pockets.
Enantio- and regioselective iridium-catalyzed allylic hydroxylation
Gaertner, Martin,Mader, Steffen,Seehafer, Kai,Helmchen, Guenter
supporting information; experimental part, p. 2072 - 2075 (2011/04/16)
The first enantioselective allylic hydroxylation to prepare branched allylic alcohols directly is described. Bicarbonate was used as nucleophile in conjunction with new single component Ir-catalysts, which are stable to air and water. Excellent regio- and
