[EN] TRICYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES TRICYCLIQUES UTILES EN TANT QU'INHIBITEURS DE L'INTÉGRASE DU VIH
申请人:MERCK SHARP & DOHME
公开号:WO2019209667A1
公开(公告)日:2019-10-31
The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, wherein R1, R2, R3, R4, R5, R6 and n are as defined herein. The present invention also relates to compositions comprising at least one Tricyclic Heterocycle Compound, and methods of using the Tricyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
[EN] DI-FLUORO AZEPANES AS HBV CAPSID ASSEMBLY MODULATORS<br/>[FR] AZÉPANES DI-FLUORÉS EN TANT QUE MODULATEURS DE L'ASSEMBLAGE DE LA CAPSIDE DU VHB
申请人:JANSSEN SCIENCES IRELAND UNLIMITED CO
公开号:WO2020239862A1
公开(公告)日:2020-12-03
Disclosed are compounds, compositions and methods for treating of diseases,syndromes, conditions, and disorders that are affected by the modulation of CAM1. Such compounds are represented by Formula (I) as follows: (I).Wherein R1a, R1b, R2, R3, R4, and X, are defined herein.
The application describes fused heterocycle derivative compounds, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases associated with HBV infection.
Total Syntheses of (−)-Scabronines G and A, and (−)-Episcabronine A
作者:Yu Kobayakawa、Masahisa Nakada
DOI:10.1002/anie.201303224
日期:2013.7.15
scab(ronine)s: The totalsynthesis of (−)‐scabronine G features a highlystereoselective oxidative dearomatization/intramolecular inverse‐electron‐demand Diels–Alder reaction cascade, and the first totalsynthesis of (−)‐scabronine A comprises a highlystereoselective oxa‐Michael/protonation/acetalization cascade. The first totalsynthesis of (−)‐episcabronine A includes another highlystereoselective cascade
A highlystereoselectivesynthesis of the hexahydrofuro[3,2-b]pyran core of (−)-dysiherbaine is described. The key step in this synthesis includes the stereocontrolled formation of the tetrahydrofuran ring using the formal [3+2] annulation of the isopropylidene-protected aldehydo-L-arabinose and the β-substituted allylsilane mediated by trifluoroborane etherate.
描述了(-)-dysiherbaine的六氢呋喃[3,2- b ]吡喃核的高度立体选择性合成。在该合成中的关键步骤包括使用异亚丙基保护的正规的[3 + 2]环四氢呋喃环的立体控制形成醛基-大号-arabinose和由三氟硼烷醚化物介导的β取代的烯丙基硅烷。