58584-63-7Relevant academic research and scientific papers
RET inhibitor, pharmaceutical composition and application thereof
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Paragraph 0423; 0424, (2021/03/31)
The invention belongs to the field of medicines, and relates to an RET inhibitor, a pharmaceutical composition and application thereof, specifically to a compound as shown in a formula (I), or a stereoisomer, a geometrical isomer, a tautomer, nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound as shown in the formula (I). The invention also relates to a pharmaceutical composition comprising the compound, and use of the compound and the pharmaceutical composition thereof in manufacture of medicine, wherein the medicine is particularly used for treatment and prevention of diseases and disorders associated with available RET, including cancers, irritable bowel syndrome and/or pain associated with irritable bowel syndrome.
RET Inhibitor. Pharmaceutical composition and use thereof
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Paragraph 0324-0325, (2021/11/26)
The invention belongs to the field of medicines, and relates to a novel RET inhibitor, a pharmaceutical composition and application thereof. , The present invention relates to a compound represented by formula (I), a stereoisomer, a geometric isomer, a tautomer, an oxynitride, a solvate, a metabolite, a pharmaceutically acceptable salt or prodrug thereof, I, and a pharmaceutical composition thereof in the manufacture of a medicament, in particular for the treatment and prevention and RET of diseases and disorders associated with irritable bowel syndrome.
GPR52 MODULATOR COMPOUNDS
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Page/Page column 54; 87; 91, (2021/05/15)
The disclosures herein relate to novel compounds of Formula (1): (1) and salts thereof, wherein R1, Q, X, Y and Z are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with GPR52 receptors.
Development of inhibitors against mycobacterium abscessus tRNA (m1G37) Methyltransferase (TrmD) Using Fragment-Based Approaches
Whitehouse, Andrew J.,Thomas, Sherine E.,Brown, Karen P.,Fanourakis, Alexander,Chan, Daniel S.-H.,Libardo, M. Daben J.,Mendes, Vitor,Boshoff, Helena I. M.,Floto, R. Andres,Abell, Chris,Blundell, Tom L.,Coyne, Anthony G.
supporting information, p. 7210 - 7232 (2019/08/20)
Mycobacterium abscessus (Mab) is a rapidly growing species of multidrug-resistant nontuberculous mycobacteria that has emerged as a growing threat to individuals with cystic fibrosis and other pre-existing chronic lung diseases. Mab pulmonary infections are difficult, or sometimes impossible, to treat and result in accelerated lung function decline and premature death. There is therefore an urgent need to develop novel antibiotics with improved efficacy. tRNA (m1G37) methyltransferase (TrmD) is a promising target for novel antibiotics. It is essential in Mab and other mycobacteria, improving reading frame maintenance on the ribosome to prevent frameshift errors. In this work, a fragment-based approach was employed with the merging of two fragments bound to the active site, followed by structure-guided elaboration to design potent nanomolar inhibitors against Mab TrmD. Several of these compounds exhibit promising activity against mycobacterial species, including Mycobacterium tuberculosis and Mycobacterium leprae in addition to Mab, supporting the use of TrmD as a target for the development of antimycobacterial compounds.
MUSCARINIC M1 RECEPTOR POSITIVE ALLOSTERIC MODULATORS
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Page/Page column 40-41, (2018/03/25)
The present invention relates to compounds of formula (I), or their isotopic forms, stereoisomers, tautomers or pharmaceutically acceptable salt (s) thereof as muscarinic M1 receptor positive allosteric modulators (M1 PAMs). The present invention describes the preparation, pharmaceutical composition and the use of compound formula (I).
Modular Route to Azaindanes
Huang, Qi,Zard, Samir Z.
supporting information, p. 3895 - 3898 (2017/07/26)
A convergent radical based route to azaindanes is described, relying on the degenerative addition transfer of various substituted S-(pyridylmethyl)-O-ethyl dithiocarbonates (xanthates) to functional alkenes followed by radical cyclization onto the pyridine ring activated by protonation with trifluoroacetic acid. In one case, a richly decorated cyclohepta[b]pyridine could be assembled swiftly by allowing the first adduct to N-phenylmaleimide to undergo addition to N-allylphthalimide prior to cyclization.
HETEROARYL SUBSTITUTED HETEROCYCLYL SULFONES
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Page/Page column 132, (2015/11/09)
The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Synthesis and reduction reactions of pyridones and 5-acyl-2-methoxypyridines
Bisset, Alexander A.,Dishington, Allan,Jones, Teyrnon,Clarkson, Guy J.,Wills, Martin
, p. 7207 - 7220 (2017/09/12)
The synthesis of a series of pyridones, from their 2-hydroxypyridine or 2-methoxypyridine precursors, is described, along with studies into their reductions to saturated heterocycles. A number of 5-acylpyridones were prepared and were evaluated as substrates for asymmetric transfer hydrogenation prior to conversion to saturated heterocycles. The enantioselective reduction of 5-acetyl-1-benzylpyrimidine-2,4(1H,3H)-dione is also described.
HETEROARYL INHIBITORS OF PDE4
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Paragraph 0808, (2014/05/24)
The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
Palladium-catalyzed arylation of aldehydes with bromo-substituted 1,3-diaryl-imidazoline carbene ligand
Yamamoto, Tetsuya,Furusawa, Takuma,Zhumagazin, Azamat,Yamakawa, Tetsu,Oe, Yohei,Ohta, Tetsuo
, p. 19 - 26 (2015/02/19)
The combination of 0 valent palladium precursor and bromo-substituted 1,3-diaryl-imidazoline carbene ligand precursor such as 1-(2-bromophenyl)-3-(2,6-diisopropylphenyl)-imidazolinium chloride 1a exhibited high catalytic activity for the 1,2-addition of arylboronic acids to aldehydes including aqueous formaldehyde.
