C−Harylation: Batch and continuous-flow protocols are developed for the first time for intramolecular Pd0-catalyzed C(sp3)−H activation/cyclization using a heterogeneousreusable palladium(II)-bis(N-heterocyclic carbene) catalyst.
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
2B
. 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.
FUSED TETRACYCLIC PYRIDO [4,3-B] INDOLE AND PYRIDO [3,4-B] INDOLE DERIVATIVES AND METHODS OF USE
申请人:Chakravarty Sarvajit
公开号:US20130210803A1
公开(公告)日:2013-08-15
This disclosure is directed to fused tetracyclic pyrido[4,3-b]indoles and pyrido[3,4-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.
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 antagonists of the adrenergic receptor α
2A
. The compounds may also bind to and are an antagonist of the adrenergic receptor α
2B
; or the compounds are not antagonists of the adrenergic receptor α
2B
and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.