NEW BICYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND BETA-LACTAMASE INHIBITORS
申请人:Naeja Pharmaceutical Inc.
公开号:US20130225554A1
公开(公告)日:2013-08-29
A compound of formula (I):
wherein:
M is hydrogen or a pharmaceutically acceptable salt-forming cation;
Y is OR
1
or NR
2
R
3
,
and R
1
, R
2
, R
3
and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
[EN] NEW BICYCLIC COMPOUNDS AND THEIR USE AS ANTIBACTERIAL AGENTS AND &bgr;-LACTAMASE INHIBITORS<br/>[FR] NOUVEAUX COMPOSÉS BICYCLIQUES ET LEUR UTILISATION EN TANT QU'AGENTS ANTIBACTÉRIENS ET INHIBITEURS DE &Bgr;-LACTAMASE
申请人:NAEJA PHARMACEUTICAL INC
公开号:WO2014091268A1
公开(公告)日:2014-06-19
A compound of formula (I), wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1,R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.
[EN] HYDROXAMATE COMPOUNDS AS ANTAGONISTS OF THE ADENOSINE A2A RECEPTOR<br/>[FR] COMPOSÉS HYDROXAMATE EN TANT QU'ANTAGONISTES DU RÉCEPTEUR A2A DE L'ADÉNOSINE
申请人:ADORX THERAPEUTICS LTD
公开号:WO2020260857A1
公开(公告)日:2020-12-30
The present invention relates to compounds of formula I shown below: (I) wherein R1, R2 and R3 are each as defined in the application. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions in which adenosine A2a receptor activity is implicated, such as, for example, cancer.
The invention relates to compounds of formula (I) and salts thereof wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).
Discovery of a Tricyclic β-Lactam as a Potent Antimicrobial Agent against Carbapenem-Resistant Enterobacterales, Including Strains with Reduced Membrane Permeability and Four-Amino Acid Insertion into Penicillin-Binding Protein 3: Structure–Activity-Relationships and <i>In Vitro</i> and <i>In Vivo</i> Activities
clinical isolates with resistance mechanisms other than β-lactamase production. These mechanisms were the reduction of outer membrane permeability with the production of β-lactamases and the insertion of four amino acids into penicillin-binding protein 3. Here, we report the discovery of a potent compound that overcomes these resistance mechanisms by the conversion of the alkoxyimino moiety of the aminothiazole