- Directing Group Enables Electrochemical Selectively Meta-Bromination of Pyridines under Mild Conditions
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Without the use of catalysts and oxidants, a facile and sustainable electrochemical bromination protocol was developed. By introducing the directing groups, the regioselectivity of pyridine derivatives could be controlled at themeta-position utilizing the inexpensive and safe bromine salts at room temperature. A variety of brominated pyridine derivatives were obtained in 28-95% yields, and the reaction could be readily performed at a gram scale. By combining the installation and removing the directing group, the concept ofmeta-bromination of pyridines could be verified.
- Wu, Yanwei,Xu, Shanghui,Wang, Hong,Shao, Dongxu,Qi, Qiqi,Lu, Yi,Ma, Li,Zhou, Jianhua,Hu, Wei,Gao, Wei,Chen, Jianbin
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p. 16144 - 16150
(2021/07/19)
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- Mono-N-methylation of anilines with methanol catalyzed by a manganese pincer-complex
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The selective mono-N-methylation of anilines derivatives was achieved under mild conditions using inexpensive methanol as C1 source. Under hydrogen borrowing conditions, using a tridentate PN3P manganese pre-catalyst (5?mol%), a catalytic amount of base (20?mol%), for 24?h at 120?°C, a large variety of anilines derivatives was methylated in good to excellent yield. Mechanistic investigations allowed us to isolate and characterize by X-ray diffraction studies a de-aromatized manganese intermediate.
- Bruneau-Voisine, Antoine,Wang, Ding,Dorcet, Vincent,Roisnel, Thierry,Darcel, Christophe,Sortais, Jean-Baptiste
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- Thiophene pyrimidines and preparation and its preparation method and application
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The invention discloses a pyrantel compound and preparation, as well as a preparation method and application of the pyrantel compound and preparation, belonging to the technical field of chemical medicines and preparations thereof. According to the pyrantel compound or pharmaceutically acceptable salt thereof, HDAC (histone deacetylase)/PI3K (phosphatidylinositide 3-kinase) double-target inhibitor is used for selectively inhibiting tumor cell messenger core protein kinase target PI3K and epigenetic target HDAC which are synergized, and is capable of destroying the network of tumor cell messengers, thus exerting a great killing effect on various tumor cells. In multiple blood and entity heterogenic transplanted tumor animal models, the inhibitor can be used for intensively effectively inhibiting tumor growth and especially has a remarkable effect on various blood B-cell malignant tumors, and safety evaluation tests indicate that the inhibitor has high safety and security. The pyrantel compound and preparation can be used for effectively treating patients with later reoccurrence of lymphoma, myeloma and lymphatic leukemia or drug resistance.
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Paragraph 0105; 0111; 0112; 0113
(2017/08/22)
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- IMIDAZOPYRIDAZINE COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES
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Compounds having the following formula (I), or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
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Page/Page column 87; 88
(2015/06/25)
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- OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION FOR COMBINATION THERAPY
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The present invention relates to combination therapy using compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein and an additional pharmaceutically active agent. The invention also relates to pharmaceutical compositions comprising these combinations, and methods of using these combinations in the treatment of various diseases and disorders.
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Paragraph 0292; 0293
(2013/08/14)
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- Tetrahydroquinoline Derivatives And Their Pharmaceutical Use
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Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 16
(2012/08/28)
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- TETRAHYDROQUINOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Tetrahydroquinoline compounds of Formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 40
(2011/06/11)
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- Methods of Treating Hepatitis C Virus with Oxoacetamide Compounds
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Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.
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- Identification and characterisation of 2-aminopyridine inhibitors of checkpoint kinase 2
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5-(Hetero)aryl-3-(4-carboxamidophenyl)-2-aminopyridine inhibitors of CHK2 were identified from high throughput screening of a kinase-focussed compound library. Rapid exploration of the hits through straightforward chemistry established structure-activity relationships and a proposed ATP-competitive binding mode which was verified by X-ray crystallography of several analogues bound to CHK2. Variation of the 5-(hetero)aryl substituent identified bicyclic dioxolane and dioxane groups which improved the affinity and the selectivity of the compounds for CHK2 versus CHK1. The 3-(4-carboxamidophenyl) substituent could be successfully replaced by acyclic ω-aminoalkylamides, which made additional polar interactions within the binding site and led to more potent inhibitors of CHK2. Compounds from this series showed activity in cell-based mechanistic assays for inhibition of CHK2.
- Hilton, Stephen,Naud, Sebastien,Caldwell, John J.,Boxall, Kathy,Burns, Samantha,Anderson, Victoria E.,Antoni, Laurent,Allen, Charlotte E.,Pearl, Laurence H.,Oliver, Antony W.,Wynne Aherne,Garrett, Michelle D.,Collins, Ian
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experimental part
p. 707 - 718
(2010/04/29)
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- NEW COMPOUNDS
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The present invention encompasses compounds of general formula (1), wherein R1 to R4 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use
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Page/Page column 16
(2010/04/03)
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- 2,4-SUBSTITUTED QUINAZOLINES AS LIPID KINASE INHIBITORS
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The invention relates to compounds of the formula (I), which are appropriate for the treatment of kinase, e.g. PI3K-related, diseases, such as proliferative diseases, inflammatory diseases, obstructive airways disorders and transplantation related disease
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Page/Page column 70
(2008/06/13)
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- CYTOKINE INHIBITORS
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The present invention provides low molecular weight compounds useful as cytokine inhibitors, and compositions thereof. In particular, compounds of the invention are useful as anti-inflammatory agents. There are further provided methods for the preparation of such agents and their use in preventing or treating conditions mediated by cytokines, such as for example arthritis, pain, cardiovascular disease and cancer.
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Page/Page column 127
(2008/12/07)
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- Acetylenyl-pyrazolo-pyrimidine derivatives
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The present invention relates to compounds of formula (I): wherein R1 to R3, A, M, L, E, G, and J are as defined in the description and claims. The invention also relates to a process for the manufacture of such compounds, pharmaceutical compositions containing them, and methods for treating CNS disorders.
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Page/Page column 31
(2008/06/13)
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- FAB I INHIBITORS
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Compounds of the formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.
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- Pyridinium N-,(2'-azinyl)aminides: Regioselective synthesis of 2- alkylaminoazines
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The regioselective alkylation of pyridinium-N-(2f'-azinil)aminides with alkyl halides under mild conditions is described. The alkylation, combined with a reduction of the N-N bond, allows an easy preparation of 2- alkylaminoazines. (C) 2000 Elsevier Science Ltd.
- Martínez-Barrasa, Valentín,Delgado, Francisca,Burgos, Carolina,Luis García-Navío,Luisa Izquierdo,Alvarez-Builla, Julio
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p. 2481 - 2490
(2007/10/03)
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- Synthetic Routes to Nitroamino Precursors of the Food Carcinogen 2-Amino-1-methyl-6-phenyl-1H-imidazopyridine and its 3-Methyl Isomer via Pd(0)-Catalysed Arylation
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The synthesis of the novel key intermediates 3-methylamino-2-nitro- and 2-methylamino-3-nitro-5-phenylpyridine, and some of their derivatives substituted in the benzene ring, from 5-bromonicotinic acid, 3-bromo-5-methoxypyridine, 2-chloro-3-nitropyridine, 2-amino-5-bromopyridine or 5-bromo-2-methoxypyridine is described.Palladium(0)-mediated arylation of bromopyridines with areneboronic acids was an essential step in the syntheses.
- Linstroem, Stefan,Eriksson, Mikael,Grivas, Spiros
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p. 805 - 812
(2007/10/02)
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