125996-71-6Relevant articles and documents
THERAPEUTIC METHODS AND COMPOUNDS
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Page/Page column 20-22; 69, (2020/11/03)
The invention provides a compound of formula I: (I) or a pharmaceutically acceptable salt thereof, wherein R1-R5 Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful to treat malaria.
Continuous-Flow Synthesis of 2 H -Azirines and Their Diastereoselective Transformation to Aziridines
Baumann, Marcus,Baxendale, Ian R.
supporting information, p. 159 - 163 (2015/12/26)
Using continuous-flow techniques, a small collection of 2H-azirines was prepared from oxime precursors via mesylation and base-promoted cyclisation. The 2H-azirines were either isolated after in-line purification or derivatised into a selection of 2-subst
Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase
Walker, John K.,Selness, Shaun R.,Devraj, Rajesh V.,Hepperle, Michael E.,Naing, Win,Shieh, Huey,Kurambail, Ravi,Yang, Syaulan,Flynn, Daniel L.,Benson, Alan G.,Messing, Dean M.,Dice, Tom,Kim, Tina,Lindmark,Monahan, Joseph B.,Portanova, Joseph
scheme or table, p. 2634 - 2638 (2010/07/13)
Starting from an initial HTS screening lead, a novel series of C(5)-substituted diaryl pyrazoles were developed that showed potent inhibition of p38α kinase. Key to this outcome was the switch from a pyridyl to pyrimidine at the C(4)-position leading to analogs that were potent in human whole blood based cell assay as well as in a number of animal efficacy models for rheumatoid arthritis. Ultimately, we identified a clinical candidate from this substrate; SD-0006.
Synthesis and SAR of 2,3-diarylpyrrole inhibitors of parasite cGMP-dependent protein kinase as novel anticoccidial agents
Biftu, Tesfaye,Feng, Dennis,Ponpipom, Mitree,Girotra, Narindar,Liang, Gui-Bai,Qian, Xiaoxia,Bugianesi, Robert,Simeone, Joseph,Chang, Linda,Gurnett, Anne,Liberator, Paul,Dulski, Paula,Leavitt, Penny Sue,Crumley, Tami,Misura, Andrew,Murphy, Terence,Rattray, Sandra,Samaras, Samantha,Tamas, Tamas,Mathew, John,Brown, Christine,Thompson, Don,Schmatz, Dennis,Fisher, Michael,Wyvratt, Matthew
, p. 3296 - 3301 (2007/10/03)
Several analogs of 2,3-diaryl pyrroles were synthesized and evaluated as inhibitors of Eimeria tenella cGMP-dependent protein kinase and in in vivo anticoccidial assays. A 4-fluorophenyl group enhances both in vitro and in vivo activities. The most potent
Adenosine A3 receptor antagonists
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, (2008/06/13)
A pharmaceutical composition for antagonizing adenosine at adenosine A3receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophylactic and therapeutic agent for asthma, allergosis, inflammation, and so on.
Novel piperidine σ receptor ligands as potential antipsychotic drugs
Gilligan,Cain,Christos,Cook,Drummond,Johnson,Kergaye,McElroy,Rohrbach,Schmidt,Tam
, p. 4344 - 4361 (2007/10/02)
σ receptor ligands represent a new class of potential antipsychotic drugs. This paper presents the structure-activity relationships leading to novel disubstituted piperidine σ ligands, which have little or no affinity for dopamine D2 receptors. Selectivity for σ sites over dopamine D2 or serotonin 5-HT2 receptors appears to be governed by the chemical nature of the piperidine nitrogen substituent, its distance from the basic nitrogen, and its orientation relative to the other piperidine substituent. Several of these compounds have good oral potency in some animal models used to evaluate potential antipsychotic drugs. The N-cyclopropylmethyl ketones and ethers (e.g. 6i (DuP 734), 6q, 18a, and 18n) have the best in vivo potency. Compounds 6i (DuP 734) and 6q did not cause catalepsy in the rat, even at very high doses. On the basis of the pharmacology profiles of these σ ligands, we propose these compounds may be effective antipsychotic drugs, which do not induce extrapyramidal side effects or tardive dyskinesia.
Rate-equilibrium relationships for the deprotonation of 4-phenacylpyridines and 4-phenacylpyridinium cations
Stefanidis, Dimitrios,Bunting, John W.
, p. 3163 - 3168 (2007/10/02)
Substituent effects upon the equilibria and kinetics of enolate ion formation from eight 4-(X-phenacyl)pyridines (5), eight 1-methyl-4-(X-phenacyl)pyridinium cations (6), five 1-benzyl-4-(X-phenacyl)pyridinium cations (7), and eight 1-(X-benzyl)-4-phenacy