[EN] POTENTIATORS OF BETA-LACTAM ANTIBIOTICS AND COMBINATION THERAPY<br/>[FR] POTENTIALISATEURS D'ANTIBIOTIQUES DE TYPE BÊTA-LACTAMES ET POLYTHÉRAPIE
申请人:UNIV NOTRE DAME DU LAC
公开号:WO2017106552A1
公开(公告)日:2017-06-22
Proteins of methicillin-resistant Staphylococcus aureus (MRSA), an antibiotic sensor/signal transducer, are phosphorylated on exposure to β-lactam antibiotics. This event is critical for the onset of the biochemical events that unleash induction of antibiotic resistance. The phosphorylation and the antibiotic-resistance phenotype can be abrogated in the presence of inhibitors described herein that restore susceptibility of the organism to β- lactam antibiotics. The invention thus provides compounds and methods for abrogating antibiotic resistance to β-lactam antibiotics and for treating infections causes by antibiotics prone to developing resistance by potentiating β-lactam antibiotics.
A class of pyrazole derivatives is described for use in treating p38 kinase medicated disorders. Compounds of particular interest are defined by Formula IA
wherein R
1
, R
2
, R
3
and R
4
are as described in the specification.
This invention provides a composition comprising Formula I, or salt thereof,
wherein X is either chlorine or bromine, Y is either hydrogen or an alkyl group having a carbon chain length from 1 to 5 carbon atoms, and R is an alkyl group having a carbon chain length from 1 to 5 carbon atoms, except that X is not chlorine when Y is hydrogen and R is an ethyl group. A method of preventing bone erosion in a patient and a method of reducing inflammation in a patient using the compositions of Formula I are disclosed.
本发明提供了一种由式 I 或其盐组成的组合物、
其中X为氯或溴,Y为氢或碳链长度为1至5个碳原子的烷基,R为碳链长度为1至5个碳原子的烷基,但当Y为氢和R为乙基时,X不是氯。本发明公开了一种使用式 I 组合物防止患者骨质侵蚀的方法和一种减轻患者炎症的方法。
Method For Inhibiting Osteoclast Development
申请人:Barnett John B.
公开号:US20130303621A1
公开(公告)日:2013-11-14
This invention provides a composition comprising Formula I, or salt thereof,
wherein X is either chlorine or bromine, Y is either hydrogen or an alkyl group having a carbon chain length from 1 to 5 carbon atoms, and R is an alkyl group having a carbon chain length from 1 to 5 carbon atoms, except that X is not chlorine when Y is hydrogen and R is an ethyl group. A method of preventing bone erosion in a patient and a method of reducing inflammation in a patient using the compositions of Formula I are disclosed.
Substituted Urea eIF2alpha Kinase Activators
申请人:THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
公开号:US20160318856A1
公开(公告)日:2016-11-03
This disclosure relates to substituted urea eIF2α kinase activators including methods of making and using the same. For example, such activators can include cycloalkyl aryl ureas, which activate at least one eIF2α kinase. These compounds may be useful for treatment of diseases such as, for example, cancer, hemolytic anemia not caused by infectious agents, Wolcott-Rallison syndrome, neurodegenerative disease, tuberous sclerosis complex, fragile-X syndrome, autism spectrum disorder, and ribosomal defect disease.