1229000-10-5Relevant articles and documents
SPECIFIC INHIBITORS OF METHIONYL-TRNA SYNTHETASE
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Paragraph 0198, (2016/03/13)
The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.
COMPOUNDS AS INHIBITORS OF RENIN
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Page/Page column 21, (2013/06/27)
The present invention relates to novel renin inhibitors of general formula (1), novel intermediates involved in their synthesis, their pharmaceutically acceptable salts and pharmaceutical compositions containing them. The present invention also relates to
Lead optimization of 2-(piperidin-3-yl)-1H-benzimidazoles: Identification of 2-morpholin- and 2-thiomorpholin-2-yl-1H-benzimidazoles as selective and CNS penetrating H1-antihistamines for insomnia
Ravula, Satheesh Babu,Yu, Jinghua,Tran, Joe A.,Arellano, Melissa,Tucci, Fabio C.,Moree, Wilna J.,Li, Bin-Feng,Petroski, Robert E.,Wen, Jianyun,Malany, Siobhan,Hoare, Samuel R.J.,Madan, Ajay,Crowe, Paul D.,Beaton, Graham
scheme or table, p. 421 - 426 (2012/02/04)
The structure-activity relationships of 2-(piperidin-3-yl)-1H- benzimidazoles, 2-morpholine and 2-thiomorpholin-2-yl-1H-benzimidazoles are described. In the lead optimization process, the pKa and/or log P of benzimidazole analogs were reduced e
The discovery and structure-activity relationships of 2-(piperidin-3-yl)-1H-benzimidazoles as selective, CNS penetrating H1-antihistamines for insomnia
Lavrador-Erb, Karine,Ravula, Satheesh Babu,Yu, Jinghua,Zamani-Kord, Said,Moree, Wilna J.,Petroski, Robert E.,Wen, Jianyun,Malany, Siobhan,Hoare, Samuel R.J.,Madan, Ajay,Crowe, Paul D.,Beaton, Graham
scheme or table, p. 2916 - 2919 (2010/08/05)
A series of 2-(3-aminopiperidine)-benzimidazoles were identified as selective H1-antihistamines for evaluation as potential sedative hypnotics. Representative compounds showed improved hERG selectivity over a previously identified 2-aminobenzimidazole series. While hERG activity could be modulated via manipulation of the benzimidazole N1 substituent, this approach led to a reduction in CNS exposure for the more selective compounds. One example, 9q, retained a suitable selectivity profile with CNS exposure equivalent to known centrally active H1-antihistamines.