[EN] OPSIN-BINDING LIGANDS, COMPOSITIONS AND METHODS OF USE<br/>[FR] LIGANDS DE LIAISON À UNE OPSINE, COMPOSITIONS ET PROCÉDÉS D'UTILISATION
申请人:BIKAM PHARMACEUTICALS INC
公开号:WO2013058809A1
公开(公告)日:2013-04-25
Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
The synthesis of diverse substituted indole structures on solidsupports is described. The immobilization of nitrobenzoic acid onto Merrifield resin and the subsequent treatment with alkenyl Grignard reagents delivered indole carboxylates bound to solidsupports. In contrast to results in the liquid phase, ortho,ortho-unsubstituted nitroarenes also delivered indole moieties in good yields. Subsequent
[EN] BENZIMIDAZOLE ANTIVIRAL AGENTS<br/>[FR] AGENTS ANTIVIRAUX À BASE DE BENZIMIDAZOLE
申请人:GLAXOSMITHKLINE LLC
公开号:WO2011097491A1
公开(公告)日:2011-08-11
Provided are compounds of Formula (I) and (II) and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the Flaviviridae family of viruses such as hepatitis C virus (HCV).
A Silver‐Catalyzed Modular Intermolecular Access to 6,6‐Spiroketals
作者:Alexander Ahrens、Niklas F. Heinrich、Simon R. Kohl、Martha Hokamp、Matthias Rudolph、Frank Rominger、A. Stephen K. Hashmi
DOI:10.1002/adsc.201900988
日期:2019.12.17
A modular synthesis of 6,6‐spiroketals via silver catalysis is reported. By combining an intermolecular Michael addition and a 6‐endo‐dig cyclization, this cascade reaction allows the modular preparation of highly substituted 6,6‐spiroketals by combining two substrate molecules. Established methods accessing this interesting substructure are complemented by this new transformation. The protocol tolerates
cobalt-bisoxazoline catalyst and afforded various α-alkyl-β,γ-unsaturated esters with excellent enantioselectivities and moderate to good yields (≤95% ee and ≤82% yields). The formal synthesis of the Californiaredscalepheromone using this method was investigated, and radical clock experiments were performed.