146552-72-9Relevant articles and documents
Enantiodivergent synthesis of Wieland-Miescher ketone analog mediated by a chiral pyridinylmethyl-amine derivative
Honda, Shota,Inomata, Kohei,Endo, Yasuyuki
, p. 950 - 966 (2015)
A new enantiodivergent route to provide the Wieland-Miescher ketone analog (3b) bearing a 7-membered ring via the intramolecular aldol reaction of the trione (5) mediated by a single chiral pyridinylmethylamine derivative (13e) was established. Although the enantioselectivities of 3b were moderate, the complete inversion of the enantioselectivities was observed based on the amount of additional trifluoroacetic acid (TFA). The basicity of the nitrogen atom on the pyridine ring was very important for this enantiodivergent behavior.
LIBRARIES OF DIVERSE MACROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING THE SAME
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Paragraph 0330; 0366; 0367, (2019/06/07)
The present disclosure relates to novel macrocyclic compounds and libraries thereof that are useful as research tools for drug discovery efforts. This disclosure also relates to methods of preparing these compounds and libraries and methods of using these libraries, such as in high throughput screening. In particular, these libraries are useful for evaluation of bioactivity at existing and newly identified pharmacologically relevant targets, including G protein-coupled receptors, nuclear receptors, enzymes, ion channels, transporters, transcription factors, protein-protein interactions and nucleic acid-protein interactions. As such, these libraries can be applied to the search for new pharmaceutical agents for the treatment and prevention of a range of medical conditions.
NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
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Paragraph 1232; 1235; 1248, (2018/09/08)
An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.