- BTK Inhibitors and uses thereof
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The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
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Paragraph 1771; 1777-1779
(2020/05/02)
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- Aza-Wittig Reaction with Nitriles: How Carbonyl Function Switches from Reacting to Activating
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Transformations of α-EWG-substituted (electron-withdrawing group, EWG) γ-azidobutyronitriles proceeding via unusual aza-Wittig reactions between the phosphazene and nitrile functions and affording pyrrole-derived iminophosphazenes were developed. α-EWGs w
- Tukhtaev, Hamidulla B.,Ivanov, Konstantin L.,Bezzubov, Stanislav I.,Cheshkov, Dmitry A.,Melnikov, Mikhail Ya.,Budynina, Ekaterina M.
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supporting information
p. 1087 - 1092
(2019/02/19)
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- Palladium(II)-Catalyzed highly enantioselective C-H arylation of cyclopropylmethylamines
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C-H arylation via a Pd(II)/Pd(IV) catalytic cycle has been one of the most extensively studied C-H activation reactions since the 1990s. Despite the rapid development of this reaction in the past two decades, an enantioselective version has not been reported to date. Herein, we report a Pd(II)-catalyzed highly enantioselective (up to 99.5% ee) arylation of cyclopropyl C-H bonds with aryl iodides using mono-N-protected amino acid (MPAA) ligands, providing a new route for the preparation of chiral cis-aryl-cyclopropylmethylamines. The enantiocontrol is also shown to override the diastereoselectivity of chiral substrates.
- Chan, Kelvin S. L.,Fu, Hai-Yan,Yu, Jin-Quan
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supporting information
p. 2042 - 2046
(2015/03/04)
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- NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVES AND METHOD FOR PREPARING THE SAME
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The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).
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Paragraph 0347; 0349; 0350
(2014/09/16)
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- NOVEL ANTIVIRAL PYRROLOPYRIDINE DERIVATIVE AND A PRODUCTION METHOD FOR SAME
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The present invention relates to a pyrrolopyridine derivative represented by the Chemical Formula I, and a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and relates to an antiviral composition including the same as an active ingredient. The compound of the Chemical Formula I has excellent antiviral activity and selectivity for wild type and resistant HIV-1, and thereby is useful as a therapeutic agent for acquired immune deficiency syndrome (AIDS).
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Paragraph 0328; 0330; 0331
(2014/12/09)
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- PHENYL-HETEROARYL AMINE COMPOUNDS AND THEIR USES
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The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I, and pharmaceutical compositions comprising such compounds
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Page/Page column 72
(2012/06/01)
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- 3-(AMINOARYL)-PYRIDINE COMPOUNDS
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The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are pharmaceutical compositions containing these compounds and methods of treating a disease or condition mediated by CDK9 using these compounds and compositions.
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Page/Page column 78-79
(2012/06/01)
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- PYRIDINE BIARYL AMINE COMPOUNDS AND THEIR USES
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The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
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Page/Page column 87
(2012/08/08)
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- PYRIMIDINE BIARYL AMINE COMPOUNDS AND THEIR USES
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The present invention provides a pyrimidine compound of formula (I): wherein one of X and Y but not both is N, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tantomers, diastereomers, deuterated versions, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds
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Page/Page column 76-77
(2012/08/08)
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- POLO-LIKE KINASE INHIBITORS
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Compounds of the following formula are provided for use with kinases, wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful
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Page/Page column 268
(2009/06/27)
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- Preparation and structure of β-peptides consisting of geminally disubstituted β2,2- and β3,3-amino acids: A turn motif for β- peptides
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We report on the synthesis of new and previously described β-peptides (1-6), consisting of up to twelve β2,2- or β3,3-geminally disubstituted β-amino acids which do not fit into any of the secondary structural patterns of β-peptides, hitherto disclosed. The required 2,2- and 3,3-dimethyl derivatives of 3-aminopropanoic acid are readily obtained from 3-methylbut-2-enoic acid and ammonia (Scheme 1) and from Boc-protected methyl 3-aminopropanoate by enolate methylation (Scheme 2). Protected (Boc for solution-, Fmoc for solid-phase syntheses) 1- (aminomethyl)cycloalkanecarboxylic-acid derivatives (with cyclopropane, cyclobutane, cyclopentane, and cyclohexane rings) are obtained from 1- cyanocycloalkanecarboxylates and the corresponding dihaloalkanes (Scheme 3). Fully 13C- and 15N-labeled 3-amino-2,2-dimethylpropanoic-acid derivatives were prepared from the corresponding labeled precursors (see asterixed formula numbers and Scheme 4). Coupling of these amino acids was achieved by methods which we had previously employed for other β-peptide syntheses (intermediates 18-23). Crystal structures of Boc-protected geminally disubstituted amino acids (16a-d) and of the corresponding tripeptide (23a), as well as NMR and IR spectra of an isotopically labeled β-hexapeptide (2a*) are presented (Figs. 1-4) and discussed. The tripeptide structure contains a ten-membered H-bonded ring which is proposed to be a turn-forming motif for β-peptides (Fig. 2).
- Seebach, Dieter,Abele, Stefan,Sifferlen, Thierry,Haenggi, Martin,Gruner, Sibylle,Seiler, Paul
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p. 2218 - 2243
(2007/10/03)
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- Practical large scale preparation of activated cyclopropanes
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Simple and practical experimental conditions for the large scale preparation of activated cyclopropanes by K2CO3 promoted cycloalkylation of malonate precursors with 1,2-dibromoethane are described.
- Lavoisier, Tania,Rodriguez, Jean
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p. 525 - 530
(2007/10/03)
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- A Facile Synthesis of Dialkyl Cyclopropane-1,1-dicarboxylates and Alkyl 1-Cyanocyclopropanecarboxylates by Phase-Transfer Alkylation
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The efficient syntheses of dialkyl cyclopropane-1,1-dicarboxylates and alkyl 1-cyanocyclopropanecarboxylates by alkylation of dialkyl malonates and alkyl cyanoacetates with 1,2-dihaloethanes are described.The importance of a certain amount of water under the solid-liquid phase-transfer conditions is demonstrated in the reactions.
- Heiszman, Jozsef,Bitter, Istvan,Harsanyi, Kalman,Toeke,, Laszlo
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p. 738 - 739
(2007/10/02)
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