Discovery of an HIV integrase inhibitor with an excellent resistance profile
摘要:
在本文中,我们介绍了一系列 N-hydroxy-dihydronaphridthyinone HIV 整合酶抑制剂的 SAR 研究,该研究产生了一个候选化合物 PF-4776548,它具有很高的效力和出色的耐药性。由于 PF-4776548 的人体药代动力学预测存在不确定性,因此该化合物被纳入了一项人体微剂量研究,以确认其人体药代动力学,研究结果将在本文中介绍。
The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof:
which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
[EN] The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof, which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention. [FR] La présente invention concerne des composés de formule (I) ou des sels, esters ou promédicaments pharmaceutiquement acceptables de ceux-ci, lesquels présentent des propriétés antibactériennes. La présente invention concerne également des compositions pharmaceutiques comprenant les composés susmentionnés, destinées à être administrées à un sujet nécessitant une antibiothérapie. L'invention concerne également des procédés visant à traiter une infection bactérienne chez un sujet, consistant en l'administration d'une composition pharmaceutique comprenant les composés de la présente invention. Par ailleurs, des procédés de fabrication des composés selon cette invention sont également décrits.