51656-70-3Relevant articles and documents
MACROCYCLIC SULFONYLAMIDE DERIVATIVES USEFUL AS NLRP3 INHIBITORS
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Page/Page column 179; 247, (2021/02/26)
The present invention relates to macrocyclic compounds, such as macrocyclic sulfonyl amides. The present invention further relates to associated salts, solvates, prodrugs and pharmaceutical compositions, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3 inhibition.
C(sp3)?C(sp3) Bond Formation via Electrochemical Alkoxylation and Subsequent Lewis Acid Promoted Reactions
López, Enol,van Melis, Carlo,Martín, Raúl,Petti, Alessia,de la Hoz, Antonio,Díaz-Ortíz, ángel,Dobbs, Adrian P.,Lam, Kevin,Alcázar, Jesús
supporting information, p. 4521 - 4525 (2021/08/06)
A two-step transition metal-free methodology for the C(sp3)?C(sp3) functionalisation of saturated N-heterocyclic systems is disclosed. First, aminal derivatives are generated through the anodic oxidation of readily accessible carboxylic acids. Then, in the presence of BF3 ? OEt2, iminium ions are unmasked and rapidly alkylated by organozinc reagents under flow conditions. Secondary, tertiary and quaternary carbon centers have been successfully assembled using this methodology. Such an approach is especially relevant to drug discovery since it increases C(sp3)-functionalities rapidly within a molecular framework. As proof of concept, our methodology was applied to derivatization of peptides and an API. (Figure presented.).
DIFLUOROCYCLOHEXYL DERIVATIVES AS IL-17 MODULATORS
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Page/Page column 60, (2021/10/15)
A series of substituted 4,4-difluorocyclohexyl derivatives as defined herein, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.
DIFLUOROCYCLOHEXYL DERIVATIVES AS IL-17 MODULATORS
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Page/Page column 59, (2021/10/15)
A series of substituted 4,4-difluorocyclohexyl derivatives as defined herein, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.
Catalytic Asymmetric Fluorination of Copper Carbene Complexes: Preparative Advances and a Mechanistic Rationale
Buchsteiner, Michael,Fürstner, Alois,Jerabek, Paul,Lehmann, Christian W.,Martinez-Rodriguez, Luis,N?thling, Nils,Patzer, Michael,Pozo, Iago
supporting information, p. 2509 - 2515 (2020/02/26)
The Cu-catalyzed reaction of substituted α-diazoesters with fluoride gives α-fluoroesters with ee values of up to 95 %, provided that chiral indane-derived bis(oxazoline) ligands are used that carry bulky benzyl substituents at the bridge and moderately bulky isopropyl groups on their core. The apparently homogeneous solution of CsF in C6F6/hexafluoroisopropanol (HFIP) is the best reaction medium, but CsF in the biphasic mixture CH2Cl2/HFIP also provides good results. DFT studies suggest that fluoride initially attacks the Cu- rather than the C-atom of the transient donor/acceptor carbene intermediate. This unusual step is followed by 1,2-fluoride shift; for this migratory insertion to occur, the carbene must rotate about the Cu?C bond to ensure orbital overlap. The directionality of this rotatory movement within the C2-symmetric binding site determines the sense of induction. This model is in excellent accord with the absolute configuration of the resulting product as determined by X-ray diffraction using single crystals of this a priori wax-like material grown by capillary crystallization.
COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH NLRP ACTIVITY
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Page/Page column 332-334, (2020/06/10)
In one aspect, compounds of Formula A, or a pharmaceutically acceptable salt thereof, are featured (Formula A) or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.
NLRP3 INHIBITORS
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Page/Page column 130-131, (2020/06/10)
The present application relates to compounds with NLRP3inhibitory activity and to associated salts, solvates, prodrugs and pharmaceutical compositions. The present application further relates to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by NLRP3inhibition.
COMPOUND, RESIN, RESIST COMPOSITION AND PRODUCTION METHOD OF RESIST PATTERN
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Paragraph 0219, (2020/10/27)
PROBLEM TO BE SOLVED: To provide a compound from which a resist pattern with good line edge roughness (LER) can be produced. SOLUTION: The compound is represented by formula (I). In the formula, R1 represents an alkyl group having 1 to 6 carbon atoms, H, or a halogen atom; X1 represents a connecting group such as -COO-C6H5-COO-; A1 represents a single bond or the like; A3 represents an alkanediyl group having 1 to 6 carbon atoms; W represents a divalent alicyclic hydrocarbon group having 3 to 18 carbon atoms; and R2 represents a substituted/unsubstituted hydrocarbon group having 1 to 28 carbon atoms. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPO&INPIT
CYCLIN-DEPENDENT KINASE 2 BIOMARKERS AND USES THEREOF
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Page/Page column 123-124, (2020/08/28)
Biomarkers are provided that are predictive and/or indicative of a subject's responsiveness to a cyclin-dependent kinase 2 (CDK2) inhibitor. The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having, suspected of having, or at risk of developing a disease or disorder associated with CDK2 and for monitoring treatment.
SULFONYLAMIDE COMPOUNDS AS CDK2 INHIBITORS
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Page/Page column 108; 110, (2020/10/19)
The present application provides sulfonyl amide compounds of formula (I), which are inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.