Heterocyclic Derivatives of 2-(3,5-Dimethylphenyl)tryptamine as GnRH Receptor Antagonists
摘要:
A series of heterocyclic 2-(3,5-dimethylphenyl)tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. The carbon tether length and heterocyclic ring attached to the amino group of 2-(3,5-dimethylphenyl)tryptamine were varied. Several of these derivatives were potent GnRH antagonists with the most potent compound having an IC50 of 16nM. (C) 2001 Elsevier Science Ltd. All rights reserved.
Substituted tetrahydropyridines as central nervous system agents
申请人:Warner-Lambert Co.
公开号:US05045550A1
公开(公告)日:1991-09-03
Substituted tetrahydropyridines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
Substituted tetrahydropyridines and their use as central nervous system
申请人:Warner-Lambert Company
公开号:US05187280A1
公开(公告)日:1993-02-16
Substituted tetrahydropyridines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
Process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates
申请人:RKYEK Omar
公开号:US20100261900A1
公开(公告)日:2010-10-14
A process for the palladium-catalyzed coupling of terminal alkynes with heteroaryl tosylates and heteroaryl benzenesulfonates
The present invention relates to a process for the regioselective synthesis of compounds of the formula (I),
wherein D, J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process of heteroaryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional heteroaryl-1-alkynes of the formula I.