850697-56-2Relevant academic research and scientific papers
BENZIMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 46, (2008/12/08)
The present invention relates to compounds of formula (I); compositions comprising the compounds, and methods of using the compounds to treat or prevent pain, diabetes, a diabetic complication, impaired glucose tolerance (IGT) or impaired fasting glucose
Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties
Bridges, Thomas M.,Brady, Ashley E.,Phillip Kennedy,Nathan Daniels,Miller, Nicole R.,Kim, Kwango,Breininger, Micah L.,Gentry, Patrick R.,Brogan, John T.,Jones, Carrie K.,Jeffrey Conn,Lindsley, Craig W.
scheme or table, p. 5439 - 5442 (2009/06/02)
This Letter describes the first account of the synthesis and SAR, developed through an iterative analogue library approach, of analogues of the highly selective M1 allosteric agonist TBPB. With slight structural changes, mAChR selectivity was maintained, but the degree of partial M1 agonism varied considerably.
BENZIMIDAZOLONES WHICH HAVE ACTIVITY AT Ml RECEPTOR
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Page/Page column 40, (2008/06/13)
Compounds of formula (I) and salts and solvates are provided: wherein R6 is selected from hydrogen, halogen, C1-6alkyl, C1-6alkyl substituted with one or more fluorine atoms, C3-6cycloalkyl, C3-6cycloalkyl substituted with one or more fluorine atoms, C1-6 alkoxy, C1-6 alkoxy substituted with one or more fluorine atoms, and cyano, and Q is hydrogen or C1-6alkyl. The compounds are M1 agonists and are useful for therapy, for example in the treatment of psychotic disorders and cognitive impairment.
Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: Optimization of the 4-substituted piperidine
Burgey, Christopher S.,Stump, Craig A.,Nguyen, Diem N.,Deng, James Z.,Quigley, Amy G.,Norton, Beth R.,Bell, Ian M.,Mosser, Scott D.,Salvatore, Christopher A.,Rutledge, Ruth Z.,Kane, Stefanie A.,Koblan, Kenneth S.,Vacca, Joseph P.,Graham, Samuel L.,Williams, Theresa M.
, p. 5052 - 5056 (2007/10/03)
In our continuing effort to identify CGRP receptor antagonists for the acute treatment of migraine, we have undertaken a study to evaluate alternative 4-substituted piperidines to the lead dihydroquinazolinone 1. In this regard, we have identified the piperidinyl-azabenzimidazolone and phenylimidazolinone structures which, when incorporated into the benzodiazepine core, afford potent CGRP receptor antagonists (e.g., 18 and 29). These studies produced a potent analog (18) which overcomes the instability issues associated with the lead structure 1. A general pharmacophore for the 4-substituted piperidine component of these CGRP receptor antagonists is also presented.
Discovery and SAR studies of a novel series of noncovalent cathepsin S inhibitors
Gustin, Darin J.,Sehon, Clark A.,Wei, Jianmei,Cai, Hui,Meduna, Steven P.,Khatuya, Haripada,Sun, Siquan,Gu, Yin,Jiang, Wen,Thurmond, Robin L.,Karlsson, Lars,Edwards, James P.
, p. 1687 - 1691 (2007/10/03)
A novel series of competitive, reversible cathepsin S (CatS) inhibitors was discovered and optimized. The 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety was found to be an effective replacement for the 4-arylpiperazin-1-yl group found in our earlier series of CatS inhibitors. This replacement imparted improved PK properties as well as decreased off-target activity. Optimization of the ketobenzimidazole moiety led to the discovery of the lead compound JNJ 10329670, which represents a novel class of selective, noncovalent, reversible, and orally bioavailable inhibitors of cathepsin S.
