98298-66-9Relevant articles and documents
Anti-influenza virus compound as well as preparation method and application thereof
-
Paragraph 0131; 0134; 0136, (2021/05/01)
The invention provides an anti-influenza virus pharmaceutical compound, and a preparation method and application thereof. The compound provided by the invention is a prodrug, has remarkably improved bioavailability and antiviral activity compared with a parent drug, is suitable for treating/prepaid influenza virus infection related diseases, has improved pharmacokinetic characteristics, and is particularly suitable for being developed into an oral preparation.
Discovery of an Orally Available Diazabicyclooctane Inhibitor (ETX0282) of Class A, C, and D Serine β-Lactamases
Durand-Réville, Thomas F.,Comita-Prevoir, Janelle,Zhang, Jing,Wu, Xiaoyun,May-Dracka, Tricia L.,Romero, Jan Antoinette C.,Wu, Frank,Chen, April,Shapiro, Adam B.,Carter, Nicole M.,McLeod, Sarah M.,Giacobbe, Robert A.,Verheijen, Jeroen C.,Lahiri, Sushmita D.,Sacco, Michael D.,Chen, Yu,O'Donnell, John P.,Miller, Alita A.,Mueller, John P.,Tommasi, Rubén A.
supporting information, p. 12511 - 12525 (2020/12/17)
Multidrug resistant Gram-negative bacterial infections are an increasing public health threat due to rapidly rising resistance toward β-lactam antibiotics. The hydrolytic enzymes called β-lactamases are responsible for a large proportion of the resistance phenotype. β-Lactamase inhibitors (BLIs) can be administered in combination with β-lactam antibiotics to negate the action of the β-lactamases, thereby restoring activity of the β-lactam. Newly developed BLIs offer some advantage over older BLIs in terms of enzymatic spectrum but are limited to the intravenous route of administration. Reported here is a novel, orally bioavailable diazabicyclooctane (DBO) β-lactamase inhibitor. This new DBO, ETX1317, contains an endocyclic carbon-carbon double bond and a fluoroacetate activating group and exhibits broad spectrum activity against class A, C, and D serine β-lactamases. The ester prodrug of ETX1317, ETX0282, is orally bioavailable and, in combination with cefpodoxime proxetil, is currently in development as an oral therapy for multidrug resistant and carbapenem-resistant Enterobacterales infections.
Halogenated imidazole compound as well as preparation method and application thereof
-
Paragraph 0025-0031, (2020/01/25)
The invention discloses alogenated imidazole compounds as well as a preparation method and application thereof. The structure of the halogenated imidazole compounds is disclosed in the invention, wherein, C * in the formula is R-type chiral carbon, and R1 and R2 can be independently selected from H and C1-6 alkyl; R3 is a substituted or unsubstituted C1-18 saturated or unsaturated aliphatic hydrocarbon, the aliphatic hydrocarbon comprises linear, branched or cyclic aliphatic hydrocarbon groups; X is H or a halogen atom; Y is H or a halogen atom; and X and Y cannot be H at the same time. The compounds or pharmaceutically acceptable salts or solvates thereof almost have no corticoid inhibition effect, can generate a rapid reversible anesthetic effect, can be rapidly metabolized into inactivecarboxylic acid metabolites, and have good revival quality after drug withdrawal; the corticoid function of the body can be rapidly recovered after single administration or continuous administration,the occurrence rate of muscular tremor after administration is low, and the body is rapidly awakened after drug withdrawal. The compounds or the salt compounds thereof can be used for preparing central inhibitory drugs which have sedative-hypnotic and/or anesthetic effects on humans or animals.
