922500-91-2Relevant academic research and scientific papers
Aryl alkylamine compound, preparation method thereof and application of aryl alkylamine compound in medicines
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Paragraph 0362-0368, (2021/07/17)
The invention relates to an aryl alkylamine compound, a preparation method thereof and application of the aryl alkylamine compound in medicines. Particularly, the compound disclosed by the invention is suitable for being used as a calcium-sensitive recept
Design and Identification of a GPR40 Full Agonist (SCO-267) Possessing a 2-Carbamoylphenyl Piperidine Moiety
Furukawa, Hideki,Miyamoto, Yasufumi,Hirata, Yasuhiro,Watanabe, Koji,Hitomi, Yuko,Yoshitomi, Yayoi,Aida, Jumpei,Noguchi, Naoyoshi,Takakura, Nobuyuki,Takami, Kazuaki,Miwatashi, Seiji,Hirozane, Yoshihiko,Hamada, Teruki,Ito, Ryo,Ookawara, Mitsugi,Moritoh, Yusuke,Watanabe, Masanori,Maekawa, Tsuyoshi
, p. 10352 - 10379 (2020/10/02)
GPR40/FFAR1 is a G-protein-coupled receptor expressed in pancreatic β-cells and enteroendocrine cells. GPR40 activation stimulates secretions of insulin and incretin, both of which are the pivotal regulators of glycemic control. Therefore, a GPR40 agonist
Synthesis of All-Carbon Quaternary Centers by Palladium-Catalyzed Olefin Dicarbofunctionalization
Koy, Maximilian,Bellotti, Peter,Katzenburg, Felix,Daniliuc, Constantin G.,Glorius, Frank
supporting information, p. 2375 - 2379 (2020/01/24)
The redox-neutral dicarbofunctionalization of tri- and tetrasubstituted olefins to form a variety of (hetero)cyclic compounds under photoinduced palladium catalysis is described. This cascade reaction process was used to couple styrenes or acryl amides with a broad range of highly decorated olefins tethered to aryl or alkyl bromides (>50 examples). This procedure enables one or two contiguous all-carbon quaternary centers to be formed in a single step. The products could be readily diversified and applied in the synthesis of a bioactive oxindole analogue.
Preparation method and application of 3-(substituted phenyl) oxetane-3-carboxylic acid and intermediate thereof
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Paragraph 0051-0054; 0065-0068; 0079-0082; 0092-0095; 0106, (2020/11/12)
The preparation method comprises the following steps: taking 3-oxetanone (compound II) as an initial raw material, and carrying out Wittig reaction on the initial raw material and triethyl phosphonotriacetate under an alkaline condition to obtain a compound III; carrying out coupling reaction on the compound III and a boric acid compound IV to obtain a compound V; reducing the ester group of the compound V to generate a compound VI; carrying out nucleophilic substitution reaction on hydroxyl of the compound VI and sulfonyl chloride/sulfonic anhydride to generate a compound VII; reacting hydroxyl of the compound VI with a halogenating reagent to generate a compound VIII; carrying out elimination reaction on the compound VII or the compound VIII to generate a compound IX; and finally, oxidizing the double bonds of the compound IX to generate 3-(substituted phenyl) oxetane-3-carboxylic acid (compound I). The method is easy and convenient to operate and high in yield, the total yield can reach 35%, and large-scale production can be achieved.
GPR40 receptor stimulant, and preparation method, pharmaceutical composition and application thereof
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Paragraph 0163; 0199; 0227-0229, (2019/10/15)
The invention discloses a GPR40 receptor stimulant, and a preparation method, a pharmaceutical composition and application thereof. The invention particularly discloses a GPR40 receptor stimulant shown in general formula (I) and pharmacologically acceptable salt thereof, a preparation process of the compound, a pharmaceutical composition containing the compound of general formula (I), and application of the compound and the pharmaceutical composition in anti-diabetes.
Macrocyclic MCL-1 inhibitors and methods of use
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Paragraph 0895, (2019/02/28)
The present disclosure provides for compounds of Formula (I) wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).
COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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Page/Page column 55; 74, (2018/11/22)
Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.
Synthesis method of 4-hydroxymethyl-dihydro-furan-2(3H)-ketone
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Paragraph 0021; 0022; 0023; 0024; 0025; 0026; 0027, (2017/08/28)
The invention belongs to the field of organic synthesis and drug synthesis, and particularly relates to a synthesis method of 4-hydroxymethyl-dihydro-furan-2(3H)-ketone. The synthesis method is carried out by a first step of mixing and stirring 3-oxetanone and ethoxyformyl methylidene triphenyl phosphorane solvent and obtaining an intermediate product 2-(oxetane-3-radical) ethyl acetate; a second step of hydrolyzing the intermediate product 2-(oxetane-3-radical) ethyl acetate through palladium carbon hydrogenation reduction under the alkali condition; meanwhile, completing rearrangement of reduction and oxygen heterocycles; obtaining 4-hydroxymethyl-dihydro-furan-2(3H)-ketone. The reaction condition of the synthesis method involved in the invention is easy to control, raw materials are low-price and easy to obtain; the operation and post treatment processes are simple; besides, the method is possessed of the industrial production value.
Synthesis of 6-Azaspiro[4.3]alkanes: Innovative Scaffolds for Drug Discovery
Chalyk, Bohdan A.,Isakov, Andrei A.,Butko, Maryna V.,Hrebeniuk, Kateryna V.,Savych, Olena V.,Kucher, Olexandr V.,Gavrilenko, Konstantin S.,Druzhenko, Tetiana V.,Yarmolchuk, Vladimir S.,Zozulya, Sergey,Mykhailiuk, Pavel K.
, p. 4530 - 4542 (2017/08/30)
New scaffolds for drug discovery, 6-azaspiro[4.3]alkanes, have been synthesized in two steps from four-membered-ring ketones: cyclobutanone, thienone, N-Boc-azetidinone (Boc = tert-butoxycarbonyl), etc. The key transformation was the reaction between electron-deficient exocyclic alkenes and an in-situ generated N-benzylazomethine ylide.
Discovery and optimisation of potent and highly subtype selective Nav1.8 inhibitors with reduced cardiovascular liabilities
Bagal, Sharan K.,Kemp, Mark I.,Bungay, Peter J.,Hay, Tanya L.,Murata, Yoshihisa,Payne, C. Elizabeth,Stevens, Edward B.,Brown, Alan,Blakemore, David C.,Corbett, Matthew S.,Miller, Duncan C.,Omoto, Kiyoyuki,Warmus, Joseph S.
supporting information, p. 1925 - 1931 (2016/10/22)
Voltage-gated sodium channels, in particular Nav1.8, can be targeted for the treatment of neuropathic and inflammatory pain. Herein, we describe the discovery and optimisation of a Nav1.8 inhibiting phenyl imidazole series that delivers chemical equity that possesses high potency and selectivity and is capable of demonstrating good oral pharmacokinetics.
