19967-57-8Relevant articles and documents
INHIBITORS OF LIN28 AND METHODS OF USE THEREOF
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Page/Page column 52; 56; 89, (2021/06/26)
The present disclosure relates to compounds of formula (I) and compositions comprising the same. The disclosure further relates to methods of treating cancers.
Ethylene oxide derivative and preparation method and application thereof to medicine
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Paragraph 0211; 0212; 0213; 0214; 0215, (2017/08/25)
The invention relates to an ethylene oxide derivative and a preparation method and application thereof to medicine, in particular to a compound shown in the general formula (I) or a stereisomer, hydrate, metabolite, solvate, pharmaceutically acceptable salt, co-crystal or a prodrug of the compound, preparation methods of the chemicals, and application of medicine compositions of the chemicals and a medicine composition of the compound to medicine, especially application as EGFR target spot inhibitors. Please see the formula (I) in the description. Definitions of substituent groups in the formula (I) are the same as the definitions of the description.
PYRROLO[1,2-A]PYRIMIDINYL CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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Paragraph 00326, (2017/11/04)
The invention provides substituted pyrrolo[1,2-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrrolo[1,2-a]pyrimidinyl carboxamide compounds described herein include substituted 2-heterocyclyl-4-alkyl-pyrrolo[1,2-a]pyrimidine-8-carboxarnide compounds and variants thereof.
Metabolism of the phytoalexins camalexins, their bioisosteres and analogues in the plant pathogenic fungus Alternaria brassicicola
Pedras, M. Soledade C.,Abdoli, Abbas
, p. 4541 - 4549 (2013/07/26)
The metabolism of the phytoalexins camalexin (1), 1-methylcamalexin (10) and 6-methoxycamalexin (11) by Alternaria brassicicola and their antifungal activity is reported. This work establishes that camalexins are slowly biotransformed (ca. six days) to the corresponding indole-3-thiocarboxamides, which are further transformed to the indole-3-carboxylic acids. These metabolites are substantially less inhibitory to A. brassicicola than the parent camalexins, indicating that these enzyme-mediated transformations are detoxifications. In addition, analyses of the metabolism of synthetic isomers and bioisosteres of camalexin (1) indicate that isomers of camalexin in the thiazole ring are not metabolized. Based on these results, the potential intermediates that lead to formation of indole-3-thiocarboxamides are proposed.
CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Page/Page column 30-31, (2012/10/08)
Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
PESTICIDES AND USES THEREOF
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Page/Page column 24, (2009/02/11)
The invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.
A convenient one-pot synthesis of thiazol-2-imines: application in the construction of pifithrin analogues
Murru, Siva,Singh,Kavala, Veerababurao,Patel, Bhisma K.
, p. 1931 - 1942 (2008/09/17)
For the first time a reaction intermediate has been isolated giving further insight into the mechanism of thiazol-2-imine formation. The first step of the reaction requires a basic medium, while the second step is an acid mediated E1 elimination reaction. An efficient one-pot synthesis of substituted thiazol-2-imines have been achieved by the condensation of carbonyl compounds with thioureas and 1,3-disubstituted thioureas using 1,1′-(ethane-1,2-diyl)dipyridinium bistribromide (EDPBT). Unsymmetrical 1,3-disubstituted thioureas give regioselective products with symmetrical ketones, which are mainly governed by the pKas of NH protons of thiourea, whereas symmetrical 1,3-disubstituted thioureas give regioselective products with symmetrical carbonyl compounds owing to the regioselective bromination of ketones. The methodology is extended to access novel neurodegenerative drug candidate pifithrin-α analogues in good yields in shorter reaction time. This method is simple, versatile and is applicable for different 1,3-disubstituted thioureas as well as a range of carbonyl compounds.
Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d] pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl- 4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrof
Gangjee, Aleem,Lin, Xin,Kisliuk, Roy L.,McGuire, John J.
, p. 7215 - 7222 (2007/10/03)
Two novel classical antifolates N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H- pyrrolo[2,3-d]-pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid 3 and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio] benzoyl}-L-glutamic acid 4 were d
THE MUKAIYAMA REACTION OF KETENE BIS(TRIMETHYLSILYL)ACETALS WITH α-HALO ACETALS - A CONVENIENT BUTENOLIDE SYNTHESIS
Demnitz, F. W. J.
, p. 6109 - 6112 (2007/10/02)
Ketene bis(trimethylsilyl) acetals were reacted with α-halo acetals giving β-alkoxy-γ-halo acids which were converted to butenolides by reaction with equivalents of base.This constitutes a novel and short butenolide synthesis.
