PHOSPHONIUM ION CHANNEL BLOCKERS AND METHODS FOR USE
申请人:Nocion Therapeutics, Inc.
公开号:US20210128589A1
公开(公告)日:2021-05-06
The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof:
The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.
Stereoselective Synthesis of Fused Vinylcyclopropanes by Intramolecular Tsuji–Trost Cascade Cyclization
作者:John Braun、Maxim I. Ariëns、Bianca T. Matsuo、Steven de Vries、Ellen D. H. van Wordragen、Brecht D. Ellenbroek、Christophe M. L. Vande Velde、Romano V. A. Orru、Eelco Ruijter
DOI:10.1021/acs.orglett.8b02232
日期:2018.11.2
pendant β-ketoamide or related carbon nucleophile to give γ-lactam-fused vinylcyclopropanes is reported. In addition to two new rings, the products contain three new C-C stereocenters (two of which are quaternary) with a 9:1 dr. Moreover, the reaction proceeds in >94% enantiospecificity with optically enriched starting materials, using an inexpensive carbohydrate as the source of chirality.
Substituted imidazoles as dual histamine H1 and H3 agonists or antagonists
申请人:——
公开号:US20020086859A1
公开(公告)日:2002-07-04
The present invention discloses novel substituted imidazole compounds which have dual histamine-H
1
and H
3
receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.
Study on the selectivity in the electrophilic monofluorination of 2,3-allenoates with Selectfluor™: an efficient synthesis of 4-fluoro-2(5H)-furanones and 3-fluoro-4-oxo-2(E)-alkenoates
作者:Bo Lü、Chunling Fu、Shengming Ma
DOI:10.1039/b917793k
日期:——
Different from the reaction of 2,3-allenoic acids with Selectfluorâ¢, 4-fluoro-2(5H)-furanones and (E)-3-fluoro-4-oxo-2-alkenoates were highly selectively generated from 2,4-disubstituted 2,3-allenoates with Selectfluor⢠under different conditions in moderate yields. The reaction of 2,4,4-trisubstituted 2,3-allenoates afforded the corresponding 4-fluoro-2(5H)-furanones highly selectively with up to 95% yield under different conditions. The scope of the substrates has been carefully explored. Due to the more readily availability of 2,3-allenoates as compared to 2,3-allenoic acids, new 4-fluoro-2(5H)-furanones were prepared. Based on the isolation and characterization of the minor fluorohydroxylation product E-5m, a mechanism has been proposed.
butanol derivatives (6a—j, 12, 13, 15, 17, 24b,c, 26, 27a,b) were prepared from the readily available resorcinol derivatives 2a—f and 7‐hydroxy‐chroman (18). The products were tested for inhibitory activity on the LPS‐induced TNF‐α production in the plasma in comparison with that of cabenegrin A‐I (1a).