150559-94-7Relevant academic research and scientific papers
Divergent Palladium-Catalyzed Cross-Coupling of Nitropyrazoles with Terminal Alkynes
Ha, Hyeri,Shin, Changhoon,Bae, Seri,Joo, Jung Min
, p. 2645 - 2650 (2018)
Facile homo-coupling of terminal alkynes, which generates conjugated diynes, is an undesired pathway in the development of transition-metal-catalyzed oxidative C–H functionalization of (hetero)arenes with terminal alkynes. By incorporating this process into a catalytic cycle, we achieved regio- and stereoselective hydroarylation of nitropyrazoles with the resulting 1,3-diynes. A simple change in the stoichiometry and oxidant allowed direct C–H alkynylation of nitropyrazoles, producing the corresponding alkynyl pyrazoles.
HETEROCYCLIC COMPOUNDS AS TRIGGERING RECEPTOR EXPRESSED ON MYELOID CELLS 2 AGONISTS AND METHODS OF USE
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Page/Page column 497-498, (2021/11/13)
The present disclosure provides compounds of Formula (I), useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 ("TREM2"). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula (I).
CRYSTALLINE FORMS OF PLASMA KALLIKREIN INHIBITORS
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Paragraph 0169-0170, (2021/01/25)
Pure crystalline forms of 1-benzyl-N-(4-carbamimidoylbenzyl)-1H-pyrazole-4-carboxamide acetate, and an amorphous form, pharmaceutical compositions thereof, and methods for making the same, are disclosed.
PROCESSES FOR PREPARING PLASMA KALLIKREIN INHIBITORS
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Paragraph 0107, (2021/01/25)
A process for preparing and purifying a compound of Formula I is provided: or a salt thereof, wherein the subscript m is an integer of from 0 to 3;each Ra is independently selected from the group consisting of (C3-C8)cyclo
Design, synthesis, biological evaluation and in silico studies of pyrazole‐based nh2‐acyl oseltamivir analogues as potent neuraminidase inhibitors
Ye, Jiqing,Lin, Lin,Xu, Jinyi,Chan, Paul Kay-Sheung,Yang, Xiao,Ma, Cong
, (2021/05/05)
Oseltamivir represents one of the most successful neuraminidase (NA) inhibitors in the current anti‐influenza therapy. The 150‐cavity of NA was identified as an additional binding pocket, and novel NA inhibitors have been designed to occupy the 150‐cavity
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.
SUBSTITUTED BICYCLE HETEROCYCLIC DERIVATIVES USEFUL AS ROMK CHANNEL INHIBITORS
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Page/Page column 130, (2018/06/06)
Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is (II) or (III); each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3, L1, L2, R1a, R1b, R1c, and n are define herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Paragraph 0344; 0345, (2018/06/26)
The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton’ s tyrosine kinase (Btk), and for treating disorders mediated thereby.
Cu-catalysed pyrazole synthesis in continuous flow
Comas-Barceló, Júlia,Blanco-Ania, Daniel,Van Den Broek, Sebastiaan A. M. W.,Nieuwland, Pieter J.,Harrity, Joseph P. A.,Rutjes, Floris P. J. T.
, p. 4718 - 4723 (2016/07/07)
The synthesis of 1,4-disubstituted pyrazoles via the cycloaddition reaction of sydnones and terminal alkynes has been achieved employing silica-supported copper catalysts. Furthermore, this methodology has been successfully implemented in continuous flow
Cu-promoted sydnone cycloadditions of alkynes: Scope and mechanism studies
Comas-Barcel?3, Jffllia,Foster, Robert S.,Fiser, B??la,Gomez-Bengoa, Enrique,Harrity, Joseph P. A.
supporting information, p. 3257 - 3263 (2015/03/05)
Cu salts have been found to promote the cycloaddition reaction of sydnones and terminal alkynes, providing significant reduction in reaction times. Specifically, the use of Cu(OTf)2 is found to provide 1,3-disubstituted pyrazoles, whereas simpl
