1558037-97-0Relevant academic research and scientific papers
Pyrimidine compounds and their uses
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Paragraph 0229-0234, (2022/01/20)
The present invention proposes pyrimidine compounds and their uses, in particular, the present invention proposes a new compound that effectively inhibits ATX, which is a compound shown in the formula below, or a tautomer of the compound of the following
Stereoselective Diboration of Spirocyclobutenes: A Platform for the Synthesis of Spirocycles with Orthogonal Exit Vectors
Nóvoa, Luis,Trulli, Laura,Parra, Alejandro,Tortosa, Mariola
, p. 11763 - 11768 (2021/04/26)
The diastereo- and enantioselective diboration of spirocyclobutenes provides a platform for the rapid preparation of a wide variety of chiral spirocyclic building blocks. The chemoselective functionalization of the carbon-boron bond in the products, including a stereospecific sp3-sp2 Suzuki–Miyaura cross-coupling reaction, provides a powerful tool to control the directionality and the nature of the exit vectors in the spirocyclic framework.
PYRAZOLYL DERIVATIVES USEFUL AS ANTI-CANCER AGENTS
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Page/Page column 191, (2021/06/26)
The present application provides a compound of formula (I) or a stereoisomer thereof, or an atropisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of a stereoisomer thereof, or a pharmaceutically acceptable salt of an atropisomer thereof; method for manufacturing said compound, and its therapeutic uses. The present application further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
PYRIMIDINYL GROUP-CONTAINING TRICYCLIC COMPOUND SERVING AS C-MET INHIBITOR
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Paragraph 0454-0456, (2021/12/18)
Disclosed are a pyrimidinyl group-containing tricyclic compound and applications thereof in preparing a cancer-treating medicament. Specifically disclosed are a compound as represented by formula (I), a pharmaceutically acceptable salt of same, or an isomer thereof.
Compound serving as IRARAK inhibitor as well as preparation method and application thereof (by machine translation)
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Paragraph 0114-0119; 0152-0157, (2020/10/30)
The present invention relates to compounds useful for treating cancer and inflammatory diseases associated with interleukin -1 receptor-related kinases (IRARAK), in particular compounds shown as IRARARARAK-4 inhibitors, stereoisomers thereof, racemates, t
SUBSTITUTED THIENOPYRROLES AS PAD4 INHIBITORS
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Paragraph 00159, (2020/03/02)
The present invention provides compounds of formula (I) useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
SULFINYLAMINOBENZAMIDE AND SULFONYLAMINOBENZAMIDE DERIVATIVES
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Paragraph 0695, (2019/12/06)
Provided is a compound of Formula (I): wherein the variable groups are defined herein.
Synthesis of Electron-Deficient Heteroaromatic 1,3-Substituted Cyclobutyls via Zinc Insertion/Negishi Coupling Sequence under Batch and Automated Flow Conditions
Tissot, Matthieu,Body, Nathalie,Petit, Sylvain,Claessens, Jehan,Genicot, Christophe,Pasau, Patrick
, p. 8022 - 8025 (2019/01/04)
Synthesis of 1,3-substituted cyclobutyls enabled by zinc insertion into functionalized iodocyclobutyl derivatives followed by Negishi coupling with halo-heteroaromatics is reported. Two distinct sets of conditions were developed; the first involved a two-step batch protocol using activated Rieke zinc, and the second involved a multistep continuous flow process. Both methods showed complementarity and allowed for rapid access to these medicinally relevant motifs, the possibility of scaling up, and automation for library synthesis.
TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
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Paragraph 1166, (2018/05/24)
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors with a Novel Monodentate Binding Interaction
Ahmed, Saleh,Ayscough, Andrew,Barker, Greg R.,Canning, Hannah E.,Davenport, Richard,Downham, Robert,Harrison, David,Jenkins, Kerry,Kinsella, Natasha,Livermore, David G.,Wright, Susanne,Ivetac, Anthony D.,Skene, Robert,Wilkens, Steven J.,Webster, Natalie A.,Hendrick, Alan G.
, p. 5663 - 5672 (2017/07/22)
Herein we describe the identification of 4-{[1,2,4]triazolo[1,5-a]pyridin-5-yl}benzonitrile-based inhibitors of the hypoxia-inducible factor prolylhydroxylase domain-1 (PHD-1) enzyme. These inhibitors were shown to possess a novel binding mode by X-ray crystallography, in which the triazolo N1 atom coordinates in a hitherto unreported monodentate interaction with the active site Fe2+ ion, while the benzonitrile group accepts a hydrogen-bonding interaction from the side chain residue of Asn315. Further optimization led to potent PHD-1 inhibitors with good physicochemical and pharmacokinetic properties.
