107618-14-4Relevant articles and documents
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.
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.
Piperidines
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, (2008/06/13)
Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-dependent sodium channels. More particularly, the invention provides substituted piperidines, and compositions containing these compounds. Also provided are methods using the compounds of the invention for the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrance of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a channel that includes a PN3 subunit.