186201-60-5Relevant academic research and scientific papers
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres
Sheffler, Douglas J.,Nedelovych, Michael T.,Williams, Richard,Turner, Stephen C.,Duerk, Brittany B.,Robbins, Megan R.,Jadhav, Sataya B.,Niswender, Colleen M.,Jones, Carrie K.,Conn, P. Jeffrey,Daniels, R. Nathan,Lindsley, Craig W.
, p. 1062 - 1066 (2014/03/21)
This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was observed, within this novel series and a number of other piperidine bioisosteric cores.
Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain
Beebe, Xenia,Yeung, Clinton M.,Darczak, Daria,Shekhar, Shashank,Vortherms, Timothy A.,Miller, Loan,Milicic, Ivan,Swensen, Andrew M.,Zhu, Chang Z.,Banfor, Patricia,Wetter, Jill M.,Marsh, Kennan C.,Jarvis, Michael F.,Scott, Victoria E.,Schrimpf, Michael R.,Lee, Chih-Hung
, p. 4857 - 4861 (2013/09/02)
A novel series of N-type calcium channel inhibitors have been discovered. Optimization of potency and HT-ADME properties provides 4- aminocyclopentapyrrolidines with analgesic efficacy after oral dosing.
Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca 2+ channel blockers with analgesic activity
Beebe, Xenia,Darczak, Daria,Henry, Rodger F.,Vortherms, Timothy,Janis, Richard,Namovic, Marian,Donnelly-Roberts, Diana,Kage, Karen L.,Surowy, Carol,Milicic, Ivan,Niforatos, Wende,Swensen, Andrew,Marsh, Kennan C.,Wetter, Jill M.,Franklin, Pamela,Baker, Scott,Zhong, Chengmin,Simler, Gricelda,Gomez, Erica,Boyce-Rustay, Janel M.,Zhu, Chang Z.,Stewart, Andrew O.,Jarvis, Michael F.,Scott, Victoria E.
, p. 4128 - 4139 (2012/09/22)
A novel 4-aminocyclopentapyrrolidine series of N-type Ca2+ channel blockers have been discovered. Enantioselective synthesis of the 4-aminocyclopentapyrrolidines was enabled using N-tert-butyl sulfinamide chemistry. SAR studies demonstrate selectivity over L-type Ca2+ channels. N-type Ca2+ channel blockade was confirmed using electrophysiological recording techniques. Compound 25 is an N-type Ca 2+ channel blocker that produces antinociception in inflammatory and nociceptive pain models without exhibiting cardiovascular or motor liabilities.
NOVEL SUBSTITUTED OCTAHYDROCYCLOPENTA[C]PYRROL-4-AMINES AS CALCIUM CHANNEL BLOCKERS
-
Page/Page column 83, (2010/06/14)
The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
ANTIBACTERIAL AGENTS
-
Page/Page column 19; 28, (2010/10/19)
Naphthalene, quinoline, quinoxaline and naphthyridine derivatives useful in the treatment bacterial infections in mammals, particularly humans, are disclosed herein.
