- Pyrrolopyrazole derivative, preparation method and medical application thereof
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The invention relates to pyrrolopyrazole derivative, a preparation method and application thereof in medicines. Specifically, the invention relates to a new pyrrolopyrazole derivative as shown in a general formula (I), a preparation method and application of the pyrrolopyrazole derivative or a pharmaceutical composition containing the pyrrolopyrazole derivative as a therapeutic agent, particularlyas a gastric acid secretion inhibitor and potassium-competitive acid blockers (P-CABs) in biological medicines. Specifically, the substituents (R1, R2, R3 and R4) in the general formula (I) are the same as the definitions in the specification.
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Paragraph 0097-0098
(2021/02/24)
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- Pyrrolopyrazole derivatives and preparation method thereof, and application of pyrrolopyrazole derivatives in medicines
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The invention relates to pyrrolopyrazole derivatives and a preparation method thereof, and application of the pyrrolopyrazole derivatives in medicines. Specifically, the invention relates to novel pyrrolopyrazole derivatives as shown in a general formula (I) in the specification, the preparation method of the pyrrolopyrazole derivatives and application of the pyrrolopyrazole derivatives or pharmaceutical compositions containing the pyrrolopyrazole derivatives as therapeutic agents, particularly as gastric acid secretion inhibitors and potassium ion competitive acid blockers P-CABs) in biological medicines. All the substituents (R1, R2, R3 and R4) and groups (X and Y) in the general formula (I) are as defined in the specification.
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Paragraph 0089-0090
(2021/03/13)
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- Pyrrolopyrazole derivatives and preparation method thereof, and application of pyrrolopyrazole derivatives in medicines
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The invention relates to pyrrolopyrazole derivatives and a preparation method thereof, and application of the pyrrolopyrazole derivatives in medicines. Specifically, the invention relates to novel pyrrolopyrazole derivatives as shown in a general formula (I) in the specification, the preparation method of the pyrrolopyrazole derivatives and application of the pyrrolopyrazole derivatives or pharmaceutical compositions containing the pyrrolopyrazole derivatives as therapeutic agents, particularly as gastric acid secretion inhibitors and potassium ion competitive acid blockers (P-CABs) in biological medicines. All the substituents (R1, R2, R3 and R4) in the general formula (I) are as defined in the specification.
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Paragraph 0090-0091
(2021/03/13)
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- Homologation of Electron-Rich Benzyl Bromide Derivatives via Diazo C-C Bond Insertion
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The ability to manipulate C-C bonds for selective chemical transformations is challenging and represents a growing area of research. Here, we report a formal insertion of diazo compounds into the "unactivated"C-C bond of benzyl bromide derivatives catalyzed by a simple Lewis acid. The homologation reaction proceeds via the intermediacy of a phenonium ion, and the products contain benzylic quaternary centers and an alkyl bromide amenable to further derivatization. Computational analysis provides critical insight into the reaction mechanism, in particular the key selectivity-determining step.
- Alegre-Requena, Juan V.,De Lescure, Louis,Modak, Atanu,Paton, Robert S.,Race, Nicholas J.,Rynders, Kathryn J.
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supporting information
(2021/12/27)
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- COMPOUNDS
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A compound of formula (I), or a pharmaceutically acceptable salt thereof.
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Page/Page column 88-89
(2020/01/24)
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- Pyrrolopyrazole derivative and preparation method thereof, and applications of pyrrolopyrazole derivative in medicine
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The present invention relates to a pyrrolopyrazole derivative and a preparation method thereof, and applications of the pyrrolopyrazole derivative in medicine, particularly to a class of new pyrrolopyrazole derivatives represented by a general formula (I), and a preparation method thereof, and uses of the pyrrolopyrazole derivatives or pharmaceutical compositions containing the pyrrolopyrazole derivatives as treating agents, particularly as gastric acid secretion inhibitors and potassium ion competitive acid blockers (P-CABs) in biomedicine, wherein various substituents (R, R and R) and the groups (X, Y and Z) in the formula (I) are defined in the specification.
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Paragraph 0064
(2019/09/14)
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- Design, synthesis and biological evaluation of substituted aminopyridazin-3(2H)-ones as G0/G1-phase arresting agents with apoptosis-inducing activities
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A series of aminopyridazin-3(2H)-one derivatives has been designed and synthesized. Their antiproliferative activities were evaluated against three human cancer cell lines (SH-SY5Y human neuroblastoma, K562 human myelogenous leukemia and AGS gastric cancer cell lines) using the MTT assay. The preliminary activity test displayed that compound 8a exhibited comparable activities against all test cells with the positive control fluorouracil. Meanwhile compounds 8b, 8e and 9c-e displayed selective antiproliferative activities for SH-SY5Y cells. Furthermore, compounds 8a-b with low-micromole GI50 value for SH-SY5Y cells induced apoptosis with cell cycle arrest at G0/G1 phase in SH-SY5Y cells in a dose-dependent manner.
- Ge, Bing-Chen,Feng, Hong-Fang,Cheng, Yu-Fang,Wang, Hai-Tao,Xi, Bao-Ming,Yang, Xue-Mei,Xu, Jiang-Ping,Zhou, Zhong-Zhen
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supporting information
p. 440 - 445
(2017/10/17)
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- Nuclear versus side-chain bromination of 4-methoxy toluene by an electrochemical method
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GRAPHICAL ABSTRACT The electrochemical bromination of 4-methoxy toluene by two-phase electrolysis yields 3-bromo 4-methoxy toluene at first, which subsequently undergoes side-chain bromination to give 3-bromo 4-methoxy benzyl bromide as a final product in 86% yield. The two-phase electrolysis consists of 25-50% NaBr as aqueous electrolyte and CHCl3 containing aromatic compound as organic phase. The reaction temperature is maintained at 10-25 °C. The probable orientation of bromine atom in an alkyl aromatic compound (nuclear versus side chain) is explained from the experimental result.
- Kulangiappar,Anbukulandainathan,Raju
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p. 2494 - 2502
(2014/08/05)
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- Total synthesis of acerogenins E, G and K, and centrolobol
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The first total synthesis of the diarylheptanoid acerogenins E and K, isolated from Acer nikoense MAXIM., is described. Formation of the 13-membered m,m-cyclophane skeleton was successfully achieved on the basis of a domino process involving a Miyaura arylborylation-intramolecular Suzuki reaction. The cyclization precursor was prepared via a Wittig reaction and Claisen-Schmidt condensation, which proceeded in moderate yields. The total synthesis of acerogenin G and centrolobol was also achieved from a common synthetic intermediate.
- Ogura, Tetsuhiro,Usuki, Toyonobu
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supporting information
p. 2807 - 2815
(2013/03/28)
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- PYRAZOLE DERIVATIVES AS 5-LO INHIBITORS
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The invention relates to compounds of formula (I) processes for their preparation, their use as 5-lipoxygenase inhibitors and pharmaceutical compositions containing the same.
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Page/Page column 132
(2009/07/03)
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- Electrochemical method for the preparation of dibromomethyl, bis(bromomethyl), and bis(dibromomethyl) arenes
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Electrochemical bromination of alkyl aromatic compounds by two-phase electrolysis yields the corresponding α,α-dibrominated products. The reaction has been carried out in a single-compartment electrochemical cell using aqueous sodium bromide (40-50%), containing a catalytic amount of HBr as electrolyte, and chloroform, containing an alkyl aromatic compound, as the organic phase with a Pt plate as anode at 10-15C. Two-phase electrolysis results in high yields (70-90%) of dibromomethyl, bis(bromomethyl), and bis(dibromomethyl) arenes, depending upon the charge passed.
- Kulangiappar,Karthik,Kulandainathan, M. Anbu
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scheme or table
p. 2304 - 2309
(2009/12/06)
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- Quinolinone derivaties and uses thereof
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The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein m, p, q, r, A, E, X, Y, R1, R4, R5, R6, R7, R8, R9 and are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.
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Page/Page column 22
(2008/06/13)
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- Imidazopyridinone derivatives and their use as phosphodiesterase inhibitors
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A compound (Ia): wherein the variables are defined in the specification, its prodrug or a pharmaceutically acceptable salt thereof useful in the treatment of angina, hypertension etc.
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- Xanthine phosphodiesterase V inhibitors
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A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders: For example, a representative comp
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- Preparation of Novel 4-Substituted 6-Methoxy, 6,7-Dimethoxy-, and 6,7-(Methylenedioxy)isochroman-3-ones. 2
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The title compounds 20, 21, and 22 have been prepared in modest yields by a two-step reaction involving first the reaction of bromoarenes 3, 7, and 8 with lithioalkyl- and lithioarylacetonitriles under aryne-forming conditions.The cyano products 10, 14, and 16 so formed were then converted to the corresponding isochroman-3-ones by acidic hydrolysis.
- Khanapure, Subhash P.,Biehl, Edward R.
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p. 1471 - 1475
(2007/10/02)
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