[EN] ANTIVIRAL COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS ANTIVIRAUX ET LEURS UTILISATIONS
申请人:JANSSEN BIOPHARMA INC
公开号:WO2021198981A1
公开(公告)日:2021-10-07
Compounds for inhibiting replication of a respiratory syncytial virus (RSV) are provided. The compounds may find use as therapeutic agents for treating or preventing an RSV infection.
The synthesis of a new, suitably protected and activated binaphthalene building block representing the central structural element of all known natural dimeric naphthylisoquinoline alkaloids, is described. This functionalized fragment possesses organometallically robust O-isopropyl (instead of O-acetyl) protecting groups and bromo (instead of trifluoromethanesulfonyloxy) activation at the scheduled coupling positions. Starting from a biphenyl intermediate, the construction of the two `outer' naphthalene rings has been achieved by a Wittig reaction → cyclization sequence.
[EN] SUBSTITUTED AMINOPROPIONIC DERIVATIVES AS NEPRILYSIN INHIBITORS<br/>[FR] DÉRIVÉS AMINOPROPIONIQUES SUBSTITUÉS COMME INHIBITEURS DE NÉPRILYSINE
申请人:NOVARTIS AG
公开号:WO2010136493A1
公开(公告)日:2010-12-02
The present invention provides a compound of formula I' or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Synthesis of larreantin, a novel, cytotoxic naphthoquinone from Larrea tridentata
作者:Mark F. Comber、Melvyn V. Sargent
DOI:10.1039/c39910000190
日期:——
Larreantin, a biogenetically unique cytotoxicnaphthoquinone, has been synthesized by a convergent route which depends upon the selective functionalization of a naphthyldihydro-oxazole.
Method of preparing optically active homo-beta-amino acids
申请人:MONSANTO COMPANY
公开号:EP0561758A3
公开(公告)日:1995-04-05
The present invention is directed to synthesis of homo-β-amino acids of an optical purity sufficient to exhibit optical activity wherein Curtius rearrangement of 3-mono-substituted succinate acid half ester of an optical purity sufficient to exhibit optical activity is affected and the incipient isocyanate is trapped with a primary or secondary alcohol. The resulting carbamate-protected homo-β-amino esters are then saponified to produce the corresponding carbamate-protected homo-β-amino acids which are deprotected to yield homo-β-amino acids of an optical purity sufficient to exhibit optical activity.