124236-38-0Relevant academic research and scientific papers
LOX ENZYME INHIBITING METHODS AND COMPOSITIONS
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Paragraph 248-249, (2021/10/30)
This invention relates to compounds, pharmaceutical compositions and their use for treating fibrotic disorders, proliferative disorders, cardiovascular diseases, acute and chronic inflammatory disorders, primary and metastatic cancer, pulmonary conditions, ocular diseases, or neurological and neuropsychiatric conditions. One particular aspect of the inventions relates to inhibitors of the family of lysyl oxidase enzymes and their use as therapeutics for fibrotic disorders.
[1,2,4]-TRIAZOLO [1,5-A]-PYRIMIDINYL DERIVATIVES SUBSTITUTED WITH PIPERIDINE, MORPHOLINE OR PIPERAZINE AS OGA INHIBITORS
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Page/Page column 87, (2018/09/19)
The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations.
Copper-mediated perfluoroalkylation of heteroaryl bromides with (phen)CuRF
Mormino, Michael G.,Fier, Patrick S.,Hartwig, John F.
, p. 1744 - 1747 (2014/04/17)
The attachment of perfluoroalkyl groups onto organic compounds has been a major synthetic goal over the past several decades. Previously, our group reported phenanthroline-ligated perfluoroalkyl copper reagents, (phen)CuR F, which react with aryl iodides and aryl boronates to form the corresponding benzotrifluorides. Herein the perfluoroalkylation of a series of heteroaryl bromides with (phen)CuCF3 and (phen)CuCF 2CF3 is reported. The mild reaction conditions allow the process to tolerate many common functional groups. Perfluoroethylation with (phen)CuCF2CF3 occurs in somewhat higher yields than trifluoromethylation with (phen)CuCF3, creating a method to generate fluoroalkyl heteroarenes that are less accessible from trifluoroacetic acid derivatives.
Highly selective trifluoromethylation of 1,3-disubstituted arenes through iridium-catalyzed arene borylation
Liu, Tianfei,Shao, Xinxin,Wu, Yaming,Shen, Qilong
, p. 540 - 543 (2012/03/11)
The old one two: A sequential iridium-catalyzed borylation and copper-catalyzed trifluoromethylation of arenes is described (see scheme; Pin=pinacol). The reaction is conducted under mild reaction conditions and tolerates a variety of functional groups. T
N-ACYL PYRIDINE BIARYL COMPOUNDS AND THEIR USES
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Page/Page column 165, (2012/08/08)
The present invention provides a compound of general formula:wherein Z2-Z6 include one or two nitrogen atoms as described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 208, (2012/08/08)
The present invention provides a compound of the general formula (1): wherein one of X and Y is N and the other is an optionally substituted carbon atom, and Z2-Z5 represent one or two nitrogen atoms, as further described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals and as components of pharmaceutical compositions. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds described herein or pharmaceutical compositions comprising such compounds.
PYRAZINYLPYRIDINES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES
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Page/Page column 90, (2011/04/14)
The present invention provides a compound of Formula (I) and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.
HETEROARYL COMPOUNDS AS KINASE INHIBITORS
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Page/Page column 91, (2011/04/14)
The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor
