- Five-membered heterocyclic oxo carboxylic acid compound and medical application thereof
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The invention relates to a five-membered heterocyclic oxo carboxylic acid compound and a medical application thereof. Specifically, the invention relates to a compound, a pharmaceutical salt, a prodrug, a hydrate, a solvate or a crystal form as shown in a formula (I), and also relates to a preparation method of the compound, a pharmaceutical composition containing the compound and an application of the pharmaceutical composition as a secretion regulator of interferon type I, especially as an STING agonist in preparation of medicines for preventing and/or treating I-type interferon related diseases.
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Paragraph 0828-0832
(2021/05/01)
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- Palladium-metalated porous organic polymers as recyclable catalysts for chemoselective decarbonylation of aldehydes
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A novel palladium nanoparticle (NP)-metalated porous organic ligand (Pd NPs/POL-xantphos) has been prepared for the chemoselective decarbonylation of aldehydes. This heterogenous catalyst not only has excellent catalytic activity and chemoselectivity, but also holds high activity after 10 runs of reuse. The effective usage of this method is demonstrated through the synthesis of biofuels such as furfuryl alcohol (FFA) via the highly chemoselective decarbonylation of biomass-derived 5-hydroxy-methylfurfural (HMF) with a TON up to 1540. More importantly, 9-fluorenone could be obtained in one step through the decarbonylation of 2-bromobenzaldehyde by using this heterogeneous catalyst.
- Li, Wen-Hao,Li, Cun-Yao,Li, Yan,Tang, Hai-Tao,Wang, Heng-Shan,Pan, Ying-Ming,Ding, Yun-Jie
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supporting information
p. 8446 - 8449
(2018/08/28)
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- Metal free coupling of heteroaryl N-tosylhydrazones and thiols: Efficient synthesis of sulfides
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A metal free coupling of heteroaromatic N-tosylhydrazones with thiols is presented. A convenient synthetic route to synthesize heteroaryl N-tosylhydrazones is also showed. Valuable thioethers with pyrroles, pyridines, thieno[2,3-b]pyridines, imidazo[1,2-a]pyridines, and 6H-thieno[2,3-b]pyrroles derivatives were synthesized in good yields. This coupling reaction can be carried out in a one-pot fashion and scaled up to the gram scale by using heteroaryl aldehydes, without the need to isolate the N-tosylhydrazone.
- García-Carrillo, Mario Alfredo,Guzmán, ángel,Díaz, Eduardo
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supporting information
p. 1952 - 1956
(2017/04/27)
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- Discovery of (S)-1-(1-(Imidazo[1,2- a ]pyridin-6-yl)ethyl)-6-(1-methyl-1 H -pyrazol-4-yl)-1 H -[1,2,3]triazolo[4,5- b ]pyrazine (Volitinib) as a Highly Potent and Selective Mesenchymal-Epithelial Transition Factor (c-Met) Inhibitor in Clinical Development for Treatment of Cancer
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HGF/c-Met signaling has been implicated in human cancers. Herein we describe the invention of a series of novel triazolopyrazine c-Met inhibitors. The structure-activity relationship of these compounds was investigated, leading to the identification of compound 28, which demonstrated favorable pharmacokinetic properties in mice and good antitumor activities in the human glioma xenograft model in athymic nude mice.
- Jia, Hong,Dai, Guangxiu,Weng, Jianyang,Zhang, Zhulin,Wang, Qing,Zhou, Feng,Jiao, Longxian,Cui, Yumin,Ren, Yongxin,Fan, Shiming,Zhou, Jinghong,Qing, Weiguo,Gu, Yi,Wang, Jian,Sai, Yang,Su, Weiguo
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supporting information
p. 7577 - 7589
(2014/12/11)
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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 19
(2012/10/08)
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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 33
(2011/07/30)
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- Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
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The invention provides compounds of Formula I: 1where in W is 2These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful to treat diseases or conditions in which α7 is known to be involved.
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- Cascade radical reactions in synthesis: A new and general approach to condensed thiophenes
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A novel cascade radical sequence is described for the direct conversion of ketenedithioacetals into condensed thiophenes. A noteworthy feature of this approach is its generality with respect to substituents.
- Harrowven, David C.
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p. 2861 - 2862
(2007/10/02)
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- Thienopyridine derivatives and their pharmaceutical use
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Thienopyridine derivatives of the formula (I): STR1 wherein the ring A is an optionally substituted benzene ring; the ring B is an optionally substituted thiophene ring: X is a group of the formula: STR2 (wherein R1 is hydrogen, alkyl or alkoxy
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- Intramolecular Diels-Alder Reactions of 1,2,4-Triazines. A Facile Synthesis of Thienopyridines and 3,4-Dihydro-2H-thiopyranopyridines
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Thienepyridines and 3,4-dihydro-2H-thiopyranopyridines have been prepared in high overall yields via intramolecular Diels-Alder reactions of properly substituted 1,2,4-triazine derivatives.A one-pot synthesis of 2,3-dihydrothienopyrid
- Taylor, Edward C.,Macor, John E.
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p. 4280 - 4287
(2007/10/02)
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- A Versatile New Synthesis of Quinolines and Related Fused Pyridines. Part 9. Synthetic Application of the 2-Chloroquinoline-3-carbaldehydes
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The 2-chloro-groups of the title compounds have been replaced by H, I, OH, SR, Li, CO2H, CHO, Ph, piperidine, and N3 (giving a tetrazole).The aldehyde group has also been converted into oxime, hydrazone, and acrylic acid derivatives.From these and related
- Meth-Cohn, Otto,Narine, Bramha,Tarnowski, Brian,Hayes, Roy,Keyzad, Amitis,at al.
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p. 2509 - 2517
(2007/10/02)
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