727736-69-8Relevant academic research and scientific papers
(PYRIDIN-2-YL)AMINE DERIVATIVES AS TGF-BETA R1 (ALK5) INHIBITORS FOR THE TREATMENT OF CANCER
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, (2020/07/15)
The present invention relates to pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment and/or prevention of a proliferation disorder associated with ΤGFβR1 activity, such as a cancer or fibrosis. The invention provides compounds of Formula (I) and Formula (II) as further described herein having an acidic moiety that enhances tissue specificity for targeted tissues and organs. The invention includes pharmaceutical compositions, pharmaceutical combinations, and methods of use of these compounds for treating conditions including cancer or fibrosis.
Method for synthesizing 3-hydroxy-2-picolinic acid and derivatives thereof
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, (2020/12/31)
The invention discloses an effective synthesis method of 3-hydroxy-2-picolinic acid and derivatives thereof. The method comprises an oxidation reaction, a cyanation reaction and a hydrolysis reaction.According to the oxidation reaction, 3-hydroxypyridine as shown in a formula I and derivatives thereof are used as substrates, and under the condition that an aqueous hydrogen peroxide solution is used as an oxidizing agent, the reaction is performed in glacial acetic acid at 60 DEG C in a nitrogen environment to obtain an oxidation product as shown in a structural general formula II. According to the cyanation reaction, the compound II and trimethylsilyl cyanide are taken as substrates and mixed with dimethylaminoformyl chloride in an ice bath, and then the reaction is conducted in dichloromethane at room temperature in the nitrogen environment to obtain a cyanation product as shown in a structural general formula III. According to the hydrolysis reaction, with the product as shown in the formula III as a substrate, the reaction is conducted in ethanol at a temperature of 80 DEG C under the condition of an aqueous sodium hydroxide solution to obtain the 3-hydroxy-2-picolinic acid asshown in the structural general formula IV and the derivatives thereof. The method is relatively economical, reaction universality is good, gram-level preparation is easy to carry out, the whole process can be industrialized, and reaction conditions are green.
FUSED FURAN COMPOUND
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Page/Page column 137, (2008/06/13)
The present invention provides a condensed furan compound of the formula (I): wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted cycloalkyl, an optionally substituted aryl, an optionally substituted saturated heterocyclic group, an optionally substituted unsaturated heterocyclic group; A is a single bond, lower alkylene, lower alkenylidene, lower alkenylene or an oxygen atom; R3 is hydrogen or the like; and , R4 is hydrogen, or the like, or pharmaceutically acceptable salts thereof, which is useful as a medicament, particularly, as an activated blood coagulation factor X inhibitor.
