915976-31-7Relevant academic research and scientific papers
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.
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.
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.
Recycling method of avibactam intermediate isomer
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, (2018/09/11)
The invention relates to a recycling method of an avibactam intermediate isomer, belonging to the technical fields of pharmaceutical synthesis and recycling. According to the pharmaceutical synthesis,the existing complex recycling problem is solved. The recycling method comprises the following steps: reacting by virtue of (2S,5S)-5-((benzyloxy)amino)piperidine-2-carboxylate and an amino protection group Boc2O in the presence of weakly alkaline substances, so as to generate an intermediate product; carrying out catalytic hydrogenation reduction reaction in the presence of a palladium-containing catalyst; carrying out oxidation reaction under the effect of an oxidant, so as to obtain a corresponding ketone intermediate product; and carrying out condensation reaction on a compound represented by a formula I (shown in the description) and benzyloxyamine hydrochloride in the presence of an acid-binding agent, and carrying out deprotection reaction, so as to obtain a final product, namely the compound of the formula I. The recycling method has the advantages that the recycling is efficient, the process route is simple, reaction conditions are mild, and the environmental pollution is low.
Synthesis of Avibactam Derivatives and Activity on β-Lactamases and Peptidoglycan Biosynthesis Enzymes of Mycobacteria
Edoo, Zainab,Iannazzo, Laura,Compain, Fabrice,Li de la Sierra Gallay, Inès,van Tilbeurgh, Herman,Fonvielle, Matthieu,Bouchet, Flavie,Le Run, Eva,Mainardi, Jean-Luc,Arthur, Michel,Ethève-Quelquejeu, Mélanie,Hugonnet, Jean-Emmanuel
, p. 8081 - 8086 (2018/05/30)
There is a renewed interest for β-lactams for treating infections due to Mycobacterium tuberculosis and M. abscessus because their β-lactamases are inhibited by classical (clavulanate) or new generation (avibactam) inhibitors, respectively. Here, access to an azido derivative of the diazabicyclooctane (DBO) scaffold of avibactam for functionalization by the Huisgen–Sharpless cycloaddition reaction is reported. The amoxicillin–DBO combinations were active, indicating that the triazole ring is compatible with drug penetration (minimal inhibitory concentration of 16 μg mL?1 for both species). Mechanistically, β-lactamase inhibition was not sufficient to account for the potentiation of amoxicillin by DBOs. Thus, the latter compounds were investigated as inhibitors of l,d-transpeptidases (Ldts), which are the main peptidoglycan polymerases in mycobacteria. The DBOs acted as slow-binding inhibitors of Ldts by S-carbamoylation indicating that optimization of DBOs for Ldt inhibition is an attractive strategy to obtain drugs selectively active on mycobacteria.
COMPOUNDS FOR USE IN THE TREATMENT OF KINETOPLASTID INFECTION
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, (2018/07/29)
The present invention relates to a class of novel heterocyclic compounds, to pharmaceutical compositions comprising the compounds and their use in the treatment of kinetoplastid infections.
AMINOPIPERIDINE QUINOLINES AND THEIR AZAISOSTERIC ANALOGUES WITH ANTIBACTERIAL ACTIVITY
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Page/Page column 59, (2008/06/13)
The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans.
