- Novel anticancer compound and usage thereof
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The invention provides a novel anticancer compound. The novel anticancer compound is a compound shown in chemical formula 1 in the description or pharmaceutically acceptable salt of the compound, andthe compound and the salt are active ingredients of a pharmaceutical composition for inhibiting the activity of hepatocyte growth factor receptor (c-Met) tyrosine kinase and pharmaceutical compositionfor preventing or curing excessive or abnormal proliferative diseases. The compound effectively inhibits the activity of the hepatocyte growth factor receptor tyrosine kinase, thereby being suitablefor treating the diseases with the characteristics of excessive or abnormal cell proliferation.
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Paragraph 0074; 0075; 0076; 0077
(2019/06/27)
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- Boronic acid derived salicylidenehydrazone complexes for wash-free fluorescence imaging of cellular organelles
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Wash-free fluorescence imaging process has intrinsic nature of monitoring biochemical process in real time fashion and enable us to get more insight on living organism. In this contribution, it was proved that boronic acid derived salicylidenehydrazone complexes (BSs) are suitable candidates for wash-free fluorescence labels. Through pre-installation of organelles' targeting group morpholine and triphenylphosphonium (TPP+) on phenyboronic acid and then assembly it with salicylidenehydrazone ligand by dehydration and dative N-B bond, Lyso-BS and Mito-BS were acquired, which were shown to selectively stain lysosomes and mitochondria with circumventing tedious wash-off procedures in Hela cells respectively, without inducing any appreciable cytotoxicity. Our findings indicate that BSs are potential candidates as wash-free fluorescent stains.
- Zhang, Boyu,Feng, Gang,Wang, Shichao,Zhang, Xuanjun
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p. 356 - 362
(2017/10/30)
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- CHEMICAL COMPOUNDS AS INHIBITORS OF KINASE ACTIVITY
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The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3- kinase activity.
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Page/Page column 129
(2017/09/05)
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- HETEROCYCLIC COMPOUND
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The present invention provides a compound having a superior JAK inhibitory action, which is useful as an agent for the prophylaxis or treatment of autoimmune diseases (rheumatoid arthritis, psoriasis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus, etc.), cancer (leukemia, uterine leiomyosarcoma, prostate cancer, multiple myeloma, cachexia, myelofibrosis, etc.) and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
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Paragraph 0843
(2015/04/15)
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- Efficient hydrolysis of organotrifluoroborates via silica gel and water
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(Chemical Equation Presented) A general, mild, and efficient method for the hydrolysis of organotrifluoroborates to unveil boronic acids using silica gel and H2O was developed. This method proved to be tolerant of a broad range of aryl-, heteroaryl-, alkenyl-, and alkyltrifluoroborates as well as structurally diverse aminomethylated organotrifluoroborates.As anticipated, electron-rich substrates provided the corresponding boronic acids more readily than electron-poor substrates, owing to the resonance-stabilized difluoroborane intermediate. The method developed was expanded further for the conversion of organotrifluoroborates to the corresponding boronate esters. 2009 American Chemical Society.
- Molander, Gary A.,Cavalcanti, Livia N.,Canturk, Belgin,Pan, Po-Shen,Kennedy, Lauren E.
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supporting information; experimental part
p. 7364 - 7369
(2010/01/16)
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- Pyrrolopyrimidines and Pyrrolopyridines
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Compounds of formula I in free or salt or solvate form, wherein X, T1, T3 and T4 have the meanings as indicated in the specification, are useful for treating diseases mediated by the ALK-5 and/or ALK-4 receptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
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Page/Page column 47
(2009/07/25)
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- Multistep synthesis of complex boronic acids from simple MIDA boronates
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Due to its sensitivity to most synthetic reagents, it is typically necessary to introduce the boronic acid functional group just prior to its utilization. Overcoming this important limitation, we herein report that air- and chromatographically stable MIDA boronates are compatible with a wide range of common reagents which enables the multistep synthesis of complex boronic acid building blocks from simple B-containing starting materials. X-ray and variable temperature NMR studies link the unique stability of MIDA boronates to a kinetic inaccessibility of the potentially reactive boron p-orbital and/or nitrogen lone pair. These findings were collectively harnessed to achieve a short and modular total synthesis of (+)-crocacin C via the iterative cross-coupling of a structurally complex, MIDA-protected haloboronic acid building block. Copyright
- Gillis, Eric P.,Burke, Martin D.
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supporting information; experimental part
p. 14084 - 14085
(2009/03/11)
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- NOVEL FUSED TRIAZOLONES AND THE USES THEREOF
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This invention relates to novel compounds having the structural diagram (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.
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Page 101-102
(2010/02/08)
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- Preparation and uses of conjugated solid supports for boronic acids
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The invention provides novel solid supports comprising dihydroxyalkyl aminoalkyl and dihydroxyalkylaminobenzyl groups, and methods for making and using them. The supports are particularly useful for immobilizing and derivatizing functionalized boronic acids for use in solid phase synthesis, such as those used in combinatorial chemistries. The compositions and methods of the invention are also useful as scavenger solid supports, e.g., in solution-phase parallel synthesis of small molecule libraries, and for use in resin-to-resin transfer reactions via phase transfer of solid supported boronic acids under both aqueous and anhydrous conditions. The methods of the invention provide convergent solid-phase synthesis of symmetrically or unsymmetrically functionalized compounds, such as biphenyl compounds. Also provided are synthesizer devices, e.g., semiautomated parallel synthesizers.
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- Universal solid-phase approach for the immobilization, derivatization, and resin-to-resin transfer reactions of boronic acids
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Boronic acid-containing molecules are employed in a broad range of biological, medicinal, and synthetic applications. These compounds, however, tend to be difficult to handle by solution-phase methods. Herein, this problem is addressed with the development of the first general solid-phase approach for the derivatization of functionalized boronic acids. This approach is based on the use of a diethanolamine resin anchor that facilitates boronic acid immobilization by avoiding the need for exhaustive removal of water in the esterification process. The immobilization of a wide variety of boronic acids onto N,N-diethanolaminomethyl polystyrene (DEAM-PS, 1) can be performed within minutes by simple stirring in anhydrous solvents at room temperature. Evidence for the formation of a bicyclic diethanolamine boronate with putative N-B coordination was shown by 1H NMR analysis of DEAM-PS-supported p-tolylboronic acid. The hydrolytic cleavage of the same model boronic acid from the DEAM-PS resin was studied by UV spectroscopy. Hydrolysis and attachment were shown to occur under a rapidly attained equilibrium, and a large excess of water (> 32 equiv) is required to effect a practically quantitative release of boronic acids from DEAM-PS. Despite their relative sensitivity to water and alcohols, DEAM-PS-bound arylboronic acids functionalized with a formyl, a bromomethyl, a carboxyl, or an amino group can be transformed in good to excellent yields into a wide variety of amines, amides, anilides, and ureas, respectively. Ugi multicomponent reactions on DEAM-PS-supported aminobenzeneboronic acids, derivatization of multifunctional arylboronic acids, and sequential reactions can also be carried out efficiently. These new DEAM-PS-supported arylboronic acids can be employed directly into resin-to-resin transfer reactions (RRTR). This type of multiresin process helps eliminate time-consuming cleavage and transfer operations, thereby considerably simplifying the outlook of combinatorial library synthesis by manual or automated means. This concept was illustrated by a set of optimized procedures for the Suzuki cross-coupling and the borono-Mannich reactions.
- Gravel, Michael,Thompson, Kim A.,Zak, Mark,Berube, Christian,Hall, Dennis G.
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