108635-83-2Relevant academic research and scientific papers
Brain-penetrating 2-aminobenzimidazole H1-antihistamines for the treatment of insomnia
Coon, Timothy,Moree, Wilna J.,Li, Binfeng,Yu, Jinghua,Zamani-Kord, Said,Malany, Siobhan,Santos, Mark A.,Hernandez, Lisa M.,Petroski, Robert E.,Sun, Aixia,Wen, Jenny,Sullivan, Sue,Haelewyn, Jason,Hedrick, Michael,Hoare, Samuel J.,Bradbury, Margaret J.,Crowe, Paul D.,Beaton, Graham
scheme or table, p. 4380 - 4384 (2010/04/05)
The benzimidazole core of the selective non-brain-penetrating H1-antihistamine mizolastine was used to identify a series of brain-penetrating H1-antihistamines for the potential treatment of insomnia. Using cassette PK studies, brain
METHOD AND INTERMEDIA USED TO OBTAIN DERIVATIVES OF 1-(1H- BENZIMIDAZOLE-2-YL)-4-(2-AMINOPYRIMIDINE)PIPERIDINE
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Page 12-13, (2010/02/13)
The invention relates to a method of obtaining derivatives of 1-(1H-benzimidazole-2-il)-4-(2-aminopyrimidine)piperidine (IV), wherein - R1 represents hydrogen or 4-halobenzyl and R5 represents optionally-substituted hydrogen, alkyl or benzyl. The inventive method comprises the conversion of a 1-[1-(R1)-1H-benzimidazole-2-il]-4-(R2)(R3)-piperidine (I), wherein R2 or R3 represents optionally-protected hydroxy, or R2 and R3 represent, independently of each other, optionally-substituted alkoxy or benzyloxy, or R2 and R3 together form an optionally-substituted alkylenedioxy group, by means of hydrolysis and/or oxidation into a 1-[1-(R1)-1H-benzimidazole-2-il]-4-piperidone, which, by reductive amination (with optional separation of the intermediate imina formed) provides the corresponding amine which, by reaction with a pyrimidine, produces the above-mentioned derivative of 1-(1H-benzimidazole-2-il)-4-(2-aminopyrimidine) piperidine (IV).
BENZIMIDAZOLE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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, (2008/06/13)
Benzimidazole derivatives corresponding to the formula (1) STR1 in which X is CH or N,R 1 is either a hydrogen atom, or a benzyl radical which can bear 1 to 3 substituents chosen from halogen atoms and trifluoromethyl, (C 1-4)alkyl, (C 1-4)alkoxy, c
