[EN] AMINOACYLINDAZOLE IMMUNOMODULATORS FOR TREATMENT OF AUTOIMMUNE DISEASES [FR] IMMUNOMODULATEURS À BASE D'AMINOCYLINDAZOLE POUR LE TRAITEMENT DE MALADIES AUTO-IMMUNES
A novel photoinduced intermolecular 1,2-arylheteroarylation of alkenes and the efficient synthesis of valuable polyarylalkanes are reported. The reaction is operationally simple, proceeds under mild conditions and with no additional catalyst and reagents. The strategically designed radical cascade reaction is enabled by electron transfer, and involves cleavage of an inert C-C bond. The process features broad functional group compatibility as well as high product transformability.
COMPOUNDS AND METHODS FOR TREATMENT OF HYPERTENSION
申请人:Medivation Technologies, Inc.
公开号:US20150266884A1
公开(公告)日:2015-09-24
Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are adrenergic receptor α
2B
antagonists. The compounds may also bind to and antagonize adrenergic receptor α
1B
. The compounds may find use in therapy, e.g., to (i) reduce blood pressure and/or (ii) promote renal blood flow and/or (iii) decrease or inhibit sodium reabsorption. The compounds may also be used to treat diseases or conditions that are, or are expected to be, responsive to a decrease in blood pressure. Use of the compounds to treat cardiovascular and renal disorders is particularly described.
[EN] NEW TETRACYCLIC COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS TÉTRACYCLIQUES
申请人:MEDIVATION TECHNOLOGIES INC
公开号:WO2009055828A1
公开(公告)日:2009-04-30
This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3- b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
Four-Component Reactions for the Synthesis of Perfluoroalkyl Isoxazoles
作者:Yuanjin Chen、Liangkui Li、Xiao He、Zhiping Li
DOI:10.1021/acscatal.9b03189
日期:2019.10.4
A four-component strategy for the synthesis of the isoxazole skeleton is developed. The approach achieves the synthesis of perfluoroalkyl isoxazoles by using simple perfluoroalkyl reagents. In addition, the unprecedented 3-azido-5-arylisoxazole formation demonstrates Togni’s reagent as a C-1 unit to be used in the isoxazole formation. The advantages of the method include readily available starting
A functional group exchange reaction between allylamines and alkenes via nickel-catalyzed C-C bond cleavage and formation was developed. This reaction provides a novel protocol, which does not require the use of unstable imine substrates, for the synthesis of allylamines, which are widely used in the production of fine chemicals, pharmaceuticals, and agrochemicals.
开发了烯丙胺和烯烃之间通过镍催化的 CC 键断裂和形成的官能团交换反应。该反应为烯丙胺的合成提供了一种新方案,不需要使用不稳定的亚胺底物,烯丙胺广泛用于精细化学品、药物和农用化学品的生产。