- INHIBITORS OF LIN28 AND METHODS OF USE THEREOF
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The present disclosure relates to compounds of formula (I) and compositions comprising the same. The disclosure further relates to methods of treating cancers.
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Page/Page column 52; 56; 89
(2021/06/26)
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- PYRROLO[1,2-A]PYRIMIDINYL CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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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.
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Paragraph 00326
(2017/11/04)
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- Ethylene oxide derivative and preparation method and application thereof to medicine
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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.
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Paragraph 0211; 0212; 0213; 0214; 0215
(2017/08/25)
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- Metabolism of the phytoalexins camalexins, their bioisosteres and analogues in the plant pathogenic fungus Alternaria brassicicola
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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.
- Pedras, M. Soledade C.,Abdoli, Abbas
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p. 4541 - 4549
(2013/07/26)
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- CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR
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Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.
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Page/Page column 30-31
(2012/10/08)
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- PESTICIDES AND USES THEREOF
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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.
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Page/Page column 24
(2009/02/11)
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- A convenient one-pot synthesis of thiazol-2-imines: application in the construction of pifithrin analogues
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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.
- Murru, Siva,Singh,Kavala, Veerababurao,Patel, Bhisma K.
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p. 1931 - 1942
(2008/09/17)
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- 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
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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
- Gangjee, Aleem,Lin, Xin,Kisliuk, Roy L.,McGuire, John J.
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p. 7215 - 7222
(2007/10/03)
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- THE MUKAIYAMA REACTION OF KETENE BIS(TRIMETHYLSILYL)ACETALS WITH α-HALO ACETALS - A CONVENIENT BUTENOLIDE SYNTHESIS
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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.
- Demnitz, F. W. J.
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p. 6109 - 6112
(2007/10/02)
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- Process for preparing optically active carbonyl compounds
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A process is described for preparing optically active alpha-halogenated carbonyl compounds. This process consists of transforming the carbonyl compound into the corresponding acetal with tartaric acid or a derivative thereof, halogenating this acetal
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- A new furan annelation reaction by the palladium-catalyzed reaction of 2-alkynyl carbonates or 2-(1-alkynyl)oxiranes with β-keto esters
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A new furan annelation by the palladium-catalyzed reaction of 2-alkynyl carbonates with β-keto esters is described.The reaction proceeds under mild neutral conditions and hence unstable 3-alkylidene-2,3-dihydrofurans can be prepared in this way.Similarly,
- Minami, Ichiro,Yuhara, Masami,Watanabe, Hiroyuki,Tsuji, Jiro
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p. 225 - 242
(2007/10/02)
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- Process for preparing optically active carbonyl compounds
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A process is described for preparing optically active alpha--halogenated carbonyl compounds. This process consists of transforming the carbonyl compound into the corresponding acetal with tartaric acid or a derivative thereof, halogenating this acetal and
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- Reactions of Perfluoroalkanesulfonyl Bromide
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Perfluoroalkanesulfonyl bromides were readily prepared from the reaction of the corresponding sodium sulfinates with bromine in aqueous solution in excellent yield.Several reactions of these sulfonyl bromides were reported: 1.Spontaneous addition to olefin with the loss of sulfur dioxide to give the corresponding adducts in good yield. 2.Facile bromination of compounds containing active hydrogen. 3.Reaction with alcohol, amines and alkali.
- Huang, Wei-Yuan,Chen, Jian-Long,Hu, Li-Qing
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p. 881 - 884
(2007/10/02)
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- Rates of Acid- and Base-Catalyzed Enolization of trans-Hexahydrofluorenone. Concerning Stereoelectronic Control of Enolization
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Rates of both acid-catalyzed and base-catalyzed enolization of trans-hexahydrofluorenone (trans-HHF) have been measured and compared with those for a variety of other ketones.It was found that trans-HHF enolizes substantially faster than cyclohexyl phenyl ketone (CPK) in both acid (1800-fold) and base (2650-fold).This rate variation is thought to be due to two factors. (1) In trans-HHF the cleaving C-H bond is held rigidly parallel to the ? orbital of the ketone.About a factor of 25- to 60-fold is attributed to this stereoelectronic effect. (2) There are stericinteractions in the enol of CPK which decrease its rate of enolization by about 40- to 50-fold.
- Pollack, Ralph M.,Kayser, Robert H.,Cashen, Michael J.
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p. 3983 - 3987
(2007/10/02)
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- REACTION OF α-NITRO EPOXIDES WITH HYDROHALIC ACIDS AND THEIR SALTS
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The reaction of α-nitro epoxides of the aliphatic series with hydrohalic acids and their salts leads to the formation of the corresponding α-halogencarbonyl compounds.
- Sokolov, N. A.,Tishchenko, I. G.,Kovganko, N. V.
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p. 248 - 250
(2007/10/02)
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- α-CETOALDEHYDES A GROUPEMENT ALDEHYDIQUE OU CETONIQUE PROTEGE
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α-Ketoaldehydes with protected ketogroup 2 or protected aldehydrogroup 3 are obtained by reaction of thiophenol or methanol with α-chloro-α-(phenylthio)aldehydes 7.
- Duhamel, Lucette,Chauvin, Joe,Messier, Angela
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p. 4171 - 4174
(2007/10/02)
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- Effet d'engrenage. VIII. Extension a des derives fonctionnels de l'alanine
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The gear effect has been discovered and studied for the first time on molecules where the interacting groups were alkyl substituents.In order to be closer to biochemical models, this effect has now been studied where one interacting group is asymmetric and functional.For this purpose eighteen new compounds derived from alanine have been prepared and studied by nmr and dynamic nmr.The gear effect is operating, and it appears to be a suitable means to modulate the interaction of two active functions.
- Blaive, Bruno,Roussel, Christian,Metzger, Jacques,Sandstroem, Jan
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p. 2212 - 2220
(2007/10/02)
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- Reaction of 3-Substituted Imidazopyridines with Br+ and the Alleged 5-Bromo-Substituted Product
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The reaction of 3-methylimidazopyridine with NBS was reinvestigated and is shown to give products formed by apparent nucleophilic substitution at the 2-position.NBS in CHCl3 gave compounds 4 and 6, while NBS in CCl4 or Br2 in CHCl3 gave exclusively 4.Mechanisms and differences in product formation are discussed; evidence that the previously reported NBS product was in fact 3-bromo-5-methylimidazopyridine, rather than the alleged 5-bromo-3-methyl derivative 3, is presented.Compound 3 was prepared by diazotization of 5-amino-3-methylimidazopyridine in the presence of HBr and by condensation of 2-bromopropanal (or its acetal) with 2-amino-6-bromopyridine (12).This latter reaction of the weakly basic aminopyridine 12 is shown to follow the normal pattern in which the amino nitrogen condenses with the carbonyl carbon.Structures are established by infrared, mass, and 1H-NMR spectral analyses, mechanistic considerations, and diagnostic reactions.Experimental and computer-generated 1H-NMR spectra of compounds 3 and 13 are reproduced.
- Hand, E. Smakula,Paudler, William W.
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p. 3738 - 3745
(2007/10/02)
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