106791-93-9Relevant academic research and scientific papers
TRIAZOLE COMPOUNDS AS ADENOSINE RECEPTOR ANTAGONISTS
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, (2021/08/13)
Described herein are triazole compounds of Formula (I): and pharmaceutically acceptable salts thereof. Methods of making and using compounds of Formula (I) are also described. Compounds of Formula (I) and pharmaceutically acceptable salts thereof can be useful as adenosine receptor antagonists, for example in the treatment of diseases or conditions mediated by the adenosine receptor, such as cancer, movement disorders, or attention disorders.
Triazolopyrimidine derivative, preparation method thereof, and application thereof in medicines
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Paragraph 0266; 0268-0272, (2019/04/10)
The invention relates to a triazolopyrimidine derivative, a preparation method thereof, and an application thereof in medicines. In particular, the invention relates to the triazolopyrimidine derivative represented as the general formula (I), a preparation method thereof, a medicine composition containing the derivative, and an application of the derivative as a treatment agent, especially an application as an A2a receptor antagonist, and an application in preparation of a medicine for relieving symptoms and diseases by inhibiting the A2a receptor; wherein the substituent groups in the generalformula (I) are defined as the specification.
HETEROARYL[4,3-C]PYRIMIDINE-5-AMINE DERIVATIVE, PREPARATION METHOD THEREFOR, AND MEDICAL USES THEREOF
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Paragraph 0114; 0115, (2019/12/15)
A heteroaryl[4,3-c]pyrimidin-5-amine derivative, a preparation method therefor, and medical uses thereof. Specifically, a heteroarylo[4,3-c]pyrimidin-5-amine derivative represented by a general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and uses thereof as therapeutic agents, in particular, a use as a A2a receptor antagonist and A use in preparation of a medicament for treatment of conditions or symptoms that are ameliorated by inhibiting the A2a receptor; various substituent groups in the general formula (I) have the identical meanings as those in the specification.
Structural studies on bioactive compounds. Part 29: Palladium catalysed arylations and alkynylations of sterically hindered immunomodulatory 2-amino- 5-halo-4,6-(disubstituted)pyrimidines
Hannah, Duncan R.,Sherer, Edward C.,Davies, Roy V.,Titman, Roger B.,Laughton, Charles A.,Stevens, Malcolm F. G.
, p. 739 - 750 (2007/10/03)
The immunological agent bropirimine 5 is a tetra-substituted pyrimidine with anticancer and interferon-inducing properties. Synthetic routes to novel 5-aryl analogues of bropirimine have been developed and their potential molecular recognition properties analysed by molecular modelling methods. Sterically challenged 2-amino-5-halo-6-phenylpyrimidin-4-ones (halo=Br or I) are poor substrates for palladium catalysed Suzuki cross-coupling reactions with benzeneboronic acid because the basic conditions of the reaction converts the amphoteric pyrimidinones to their unreactive enolic forms. Palladium-mediated reductive dehalogenation of the pyrimidinone substrates effectively competes with cross-coupling. 2-Amino-5-halo-4-methoxy-6- phenylpyrimidines can be converted to a range of 5-aryl derivatives with the 5-iodopyrimidines being the most efficient substrates. Hydrolysis of the 2- amino-5-aryl-4-methoxy-6-phenylpyrimidines affords the required pyrimidin-4- ones in high yields. Semi-empirical quantum mechanical calculations show how the nature of the 5-substituent influences the equilibrium between the 1H- and 3H-tautomeric forms, and the rotational freedom about the bond connecting the 6-phenyl group and the pyrimidine ring. Both of these factors may influence the biological properties of these compounds. (C) 2000 Elsevier Science Ltd.
4-substituted-6-aryl-pyrimidine compounds
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, (2008/06/13)
This invention describes the synthesis and anti-neoplastic use of 4-aziridyl-5-substituted/unsubstituted 6-aryl-pyrimidine compounds of Formula IA STR1 as well as N'-[2-(1-aziridyl)ethyl]-6-aryl-2,4-pyrimidinediamines of Formula IB STR2 and 4-chloro or bromo-5-substituted/unstubstituted-6-aryl-pyrimidines.
