- Oxalic amide ligands, and uses thereof in copper-catalyzed coupling reaction of aryl halides
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The present invention provides oxalic amide ligands and uses thereof in copper-catalyzed coupling reaction of aryl halides. Specifically, the present invention provides a use of a compound represented by formula I, wherein definitions of each group are described in the specification. The compound represented by formula I can be used as a ligand in copper-catalyzed coupling reaction of aryl halides for the formation of C—N, C—O and C—S bonds.
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Page/Page column 89-90
(2020/01/09)
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- Functionalized C-nucleosides as remarkable RNA binders: Targeting of prokaryotic ribosomal A-site RNA
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RNA represents an extremely promising and yet challenging therapeutic target. Here, we report the design of a series of C-nucleosides as original RNA binders. Some of them bind strongly and selectively to A-site prokaryotic ribosomal RNA.
- Joly, Jean-Patrick,Gaysinski, Marc,Zara, Lorena,Duca, Maria,Benhida, Rachid
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supporting information
p. 10432 - 10435
(2019/09/07)
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- NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF
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An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.
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Paragraph 0629; 0630
(2018/09/08)
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- VEGFR TYROSINE KINASE INHIBITORS
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Novel compounds, their prodrugs, and the pharmaceutically acceptable salts as pharmaceutical compositions containing such compounds useful in treating certain diseases modulated by the inhibition of vascular endothelial growth factors (VEGFs) receptor tyrosine kinases are provided. In particular, compounds and compositions and the methods for the prophylaxis, management and treatment of cancers through the inhibition of VEGF receptor tyrosine kinases are provided.
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Page/Page column 35
(2014/12/12)
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- ANTI-VIRAL COMPOUNDS
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Described herein are compounds and related compositions for the treatment of viral infections, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells,including compounds that can activate the RIG-I pathway.
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Paragraph 00292; 00293; 00294
(2018/09/18)
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- Mild and highly selective palladium-catalyzed monoarylation of ammonia enabled by the use of bulky biarylphosphine ligands and palladacycle precatalysts
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A method for the Pd-catalyzed arylation of ammonia with a wide range of aryl and heteroaryl halides, including challenging five-membered heterocyclic substrates, is described. Excellent selectivity for monoarylation of ammonia to primary arylamines was achieved under mild conditions or at rt by the use of bulky biarylphosphine ligands (L6, L7, and L4) as well as their corresponding aminobiphenyl palladacycle precatalysts (3a, 3b, and 3c). As this process requires neither the use of a glovebox nor high pressures of ammonia, it should be widely applicable.
- Cheung, Chi Wai,Surry, David S.,Buchwald, Stephen L.
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supporting information
p. 3734 - 3737
(2013/08/23)
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- HETEROAROMATIC UREAS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1)
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Compounds of formula (I): are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).
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Page/Page column 39
(2010/02/11)
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- NMR recognition studies of C·G base pairs by new easily accessible heterobicyclic systems
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Recognition of DNA duplexes by triplex forming oligonucleotides (TFO) is limited to DNA homopurine sequences. As a first step to overcome this limitation we report here NMR recognition studies of the C·G base pair by new heterocyclic systems, derived from benzimidazole and benzoxazole units bearing an urea donor moiety, designed to bound to the 4-amino group of the cytosine and the O4- and N7-atoms of the guanosine bases, respectively.
- Lecubin, Florence,Benhida, Rachid,Fourrey, Jean-Louis,Sun, Jian-Sheng
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p. 8085 - 8088
(2007/10/03)
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- Gould-Jacobs reaction of 5- and 6-amino-2-substituted benzoxazoles. I. Reaction with diethyl ethoxymethylenemalonate
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Reaction of 2-substituted 5- and 6-aminobenzoxazoles 1 and 2 with diethyl ethoxymethylenemalonate afforded the corresponding diethyl 3-N-(5- and 6-benzoxazolyl)aminomethylenemalonates 3 and 4. Under conditions of the Gould-Jacobs reaction, the compounds 3
- Ilavsky, Dusan,Heleyova, Katarina,Nadaska, Jana,Bobosik, Vladimir
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p. 268 - 275
(2007/10/03)
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- Gould-jacobs reaction of 5- and 6-amino-2-substituted benzoxazoles. II. Reaction with 3-ethoxymethylene-2,4-pentanedione and ethyl 2-ethoxymethylene-3-oxobutanoate
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Nucleophilic reaction of 5-amino- and 6-amino-2-substituted benzoxazoles 1 and 2 with 3-ethoxymethylene-2,4-pentanedione (3) gave compounds 5 and 6. Compounds 1 and 2 reacted with ethyl ethoxymethylene-3-oxobutanoate (4) under formation of compounds 7 and
- Heleyova, Katarina,Ilavsky, Dusan,Bobosik, Vladimir,Pronayova, Nad'a
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p. 371 - 380
(2007/10/03)
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