1822538-74-8Relevant articles and documents
Diastereoselective functionalizations of enecarbamates derived from pipecolic acid towards 5-guanidinopipecolates as arginine mimetics
Le Corre, Laurent,Kizirian, Jean-Claude,Levraud, Camille,Boucher, Jean-Luc,Bonnet, Veronique,Dhimane, Hamid
, p. 3388 - 3398 (2008)
Various substituents could be diastereoselectively introduced into the 5-position of pipecolic acid via electrophilic or free-radical-initiated addition to the carbon-carbon double bond of endocyclic enecarbamates derived from pipecolic acid. This study a
METHOD FOR PRODUCING AMINO ACID DERIVATIVES
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, (2022/01/04)
The present invention aims to provide a method for producing a (2S,5R)-5-(protected oxyamino)-piperidine-2-carboxylic acid derivative at a low cost that can be performed under mild reaction conditions not requiring a facility at an extremely low temperature, is safer, can control the quality of the desired product with ease, and shows good workability in the site of production. A method for producing a compound represented by the formula (2): wherein PG1 is an amino-protecting group, PG2 is an amino-protecting group, PG3 is a hydroxyl-protecting group, LG is a leaving group, and R is a hydrocarbon group having 1-8 carbon atoms and optionally having substituent(s), including a step of reacting a compound represented by the formula (1): wherein each symbol is as defined above, with a hydroxylamine derivative represented by the formula PG2NHOPG3 wherein each symbol is as defined above, in the presence of a base in a solvent.
Five-membered heteroaromatic derivative, preparation method and application thereof
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, (2021/07/08)
The invention belongs to the technical field of medicines, and particularly relates to a five-membered heteroaromatic compound, a composition, a preparation method and application thereof. The compound or the composition can be used as an inhibitor of a retinoid-related orphan receptor [gamma]t (ROR [gamma]t). The invention also relates to a method for preparing the compound and the composition, and application of the compound and the composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.
ROR [gamma]t inhibitor, preparation method and application thereof
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, (2021/07/08)
The invention relates to the technical field of medicines, in particular to an ROR [gamma]t inhibitor, a preparation method and application thereof. The invention also relates to a pharmaceutical composition containing the compound, a method for preparing the pharmaceutical composition, and application of the compound or the pharmaceutical composition in treatment or prevention of ROR [gamma]t-mediated cancers, inflammations or autoimmune diseases of mammals, especially human beings.
NLRP3 INFLAMMASOME INHIBITORS
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Paragraph 0770-0771, (2020/12/04)
The present invention relates to novel pyridazin-3-yl phenol compounds of Formula (I): wherein R1, R2, R3, R4, R5 and Z are defined herein, which inhibit NOD-like receptor protein 3 (NLRP3) inflammaso
RORγ ANTAGONIST AND APPLICATION THEREOF IN MEDICINE
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, (2020/02/06)
Provided herein are compounds as RORγ antagonist having Formula (I). The compounds or pharmaceutical composition thereof can be used for regulating Retinoid-related orphan receptor gamma t (RORγt). Also provided herein are methods of preparation of the compounds and composition thereof, and uses thereof in treating or preventing RORγt mediated inflammation or autoimmune diseases in mammals, particularly humans.
THERAPEUTIC METHODS
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Page/Page column 121-123, (2020/05/28)
The invention provides methods and compositions for delivering a nucleic acid to a cell or the cytosol of the target cell. The method includes contacting the cell with, 1) a membrane-destabilizing polymer; and 2) a nucleic acid conjugate. The nucleic acid conjugate includes a targeting ligand bound to an optional linker and a nucleic acid.
NEW BETA-LACTAMASE INHIBITORS TARGETING GRAM NEGATIVE BACTERIA
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, (2019/07/13)
The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, notably for use as β-lactamase inhibitors, notably in the treatment of a disease caused by gram negative bacteria, in particular enterobacteria, as well as pharmaceutical compositions containing such a compound and a process to prepare such a compound.
NEW ANTIBIOTICS TARGETING MYCOBACTERIA
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, (2019/07/13)
The present invention relates to a compound of the following formula (I) or a pharmaceutically acceptable salt and/or solvate thereof, notably for use as a drug, notably in the treatment of a disease caused by mycobacteria, as well as pharmaceutical compositions containing such a compound and a process to prepare such a compound.
METHODS FOR TREATING HEPATITIS B INFECTIONS
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Page/Page column 191, (2019/04/09)
Certain embodiments of the invention provide a method for identifying a patient that has a higher likelihood of responding to an HBV antigen inhibitor, such a method comprising detecting a hepatitis B virus (HBV) infected patient's genotype at one or more of the IL28B/A associated SNPs described herein, wherein the relevant genotype(s) described herein are indicative of a patient that has a higher likelihood of responding to an HBV antigen inhibitor as compared to an HBV infected patient having different genotypes at these locations.