76315-55-4Relevant articles and documents
NEW HETEROCYCLIC COMPOUNDS
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Page/Page column 67; 72-73, (2019/06/17)
The invention provides new heterocyclic compounds having the general formula (IA) wherein A, L, X, Y, m, n, R1 and R2 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
Substituted heterocyclic compounds and its application on the medicament (by machine translation)
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Paragraph 0200; 0201; 0202; 0203; 0292; 0293; 0294; 0295, (2017/06/02)
The invention relates to substituted heterocyclic compounds and its application on the medicament, in particular to a novel class of substituted heterocyclic compounds or its isomer, tautomer, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug, and their method of preparation. The invention also relates to the compounds of the invention pharmaceutical composition, and said compound or pharmaceutical compositions for the treatment5-HT6receptor-related diseases, in particular Alzheimer's disease in the use thereof. (by machine translation)
Synthesis and structure-activity relationships of novel histamine H 1 antagonists: Indolylpiperidinyl benzoic acid derivatives
Fonquerna, Silvia,Miralpeix, Montse,Pagès, Lluís,Puig, Carles,Cardús, Arantxa,Antón, Francisca,Cárdenas, álvaro,Vilella, Dolors,Aparici, Mónica,Calaf, Elena,Prieto, José,Gras, Jordi,Huerta, Josep M.,Warrellow, Graham,Beleta, Jorge,Ryder, Hamish
, p. 6326 - 6337 (2007/10/03)
A series of indolylpiperidinyl derivatives were prepared and evaluated for their activity as histamine H1 antagonists. Structure-activity relationship studies were directed toward improving in vivo activity and pharmacokinetic profile of our first lead (1). Substitution of fluorine in position 6 on the indolyl ring led to higher in vivo activity in the inhibition of histamine-induced cutaneous vascular permeability assay but lower selectivity toward 5HT2 receptor. Extensive optimization was carried out within this series and a number of histamine H1 antagonists showing potency and long duration of action in vivo and low brain penetration or cardiotoxic potential were identified. Within this novel series, indolylpiperidines 15, 20, 48, 51 and 52 exhibited a long half-life in rat and have been selected for further preclinical evaluation.