220741-33-3Relevant academic research and scientific papers
TRIAZOLE DERIVATIVES WITH ANTIFUNGAL ACTIVITY
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Paragraph 00294, (2021/08/14)
Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, Q2, L1 and n are as defined herein. The compounds have antifungal properties and are useful in the treatment of fungal infections, including infections that are resistant to conventions anti-fungal agents. Q1 is selected from: (Formulae Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ii, Ij and Ik) wherein * indicates the point of attachment to L1.
Aniline derivatives as calcium channel blockers
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, (2008/06/13)
The present invention provides compounds that block calcium channels having formula (I). The present invention also provides methods of using the compounds of formula (I) to treat stroke, cerebral ischemia, head trauma, or epilepsy and to pharmaceutical compositions that contain the compounds of formula (I).
Heterocyclic substituted aniline calcium channel blockers
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, (2008/06/13)
The present invention provides compounds that block calcium channels having the Formula I shown below. STR1The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, epilepsy, asthma, amyotrophic lateral sclerosis, or pain and to pharmaceutical compositions that contain the compounds of Formula I.
The discovery of [1-(4-Dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethylbutyl)-phenyl]-(3-methyl-but-2-enyl)-amine, an N-type Ca+2 channel blocker with oral activity for analgesia
Hu, Lain-Yen,Ryder, Todd R.,Rafferty, Michael F.,Taylor, Charles P.,Feng, M. Rose,Kuo, Be-Sheng,Lotarski, Susan M.,Miljanich, George P.,Millerman, Elizabeth,Siebers, Krista M.,Szoke, Balazs G.
, p. 1203 - 1212 (2007/10/03)
Our drug discovery efforts for N-type calcium channel blockers in the 4-piperidinylaniline series led to the discovery of an orally active analgesic agent 26. 1-[4-Dimethylamino-benzyl)-piperidin-4-yl]-[4-(3,3-dimethyl-butyl)-phenyl]-(3-methyl-but-2-enyl)-amine (26) showed high affinity to functionally block N-type calcium channels (IC50=0.7 μM in the IMR32 assay) and exhibited high efficacy in the anti-writhing analgesia test with mice (ED50=12 mg/kg by po and 4 mg/kg by iv). In this report, the rationale for the design, synthesis, biological evaluation, and pharmacokinetics of this series of blockers is described. Copyright (C) 2000 Elsevier Science Ltd.
Synthesis of a series of 4-benzyloxyaniline analogues as neuronal N-type calcium channel blockers with improved anticonvulsant and analgesic properties
Hu, Lain-Yen,Ryder, Todd R.,Rafferty, Michael F.,Feng, M. Rose,Lotarski, Susan M.,Rock, David M.,Sinz, Michael,Stoehr, Sally J.,Taylor, Charles P.,Weber, Mark L.,Bowersox, S. Scott,Miljanich, George P.,Millerman, Elizabeth,Wang, Yong-Xiang,Szoke, Balazs G.
, p. 4239 - 4249 (2007/10/03)
In this article, the rationale for the design, synthesis, and biological evaluation of a series of N-type voltage-sensitive calcium channel (VSCC) blockers is described. N-Type VSCC blockers, such as ziconotide, have shown utility in several models of str
Structure-activity relationship at the proximal phenyl group in a series of non-peptidyl N-type calcium channel antagonists
Ryder, Todd R.,Hu, Lain-Yen,Rafferty, Michael F.,Lotarski, Susan M.,Rock, David M.,Stoehr, Sally J.,Taylor, Charles P.,Weber, Mark L.,Miljanich, George P.,Millerman, Elizabeth,Szoke, Balazs G.
, p. 2453 - 2458 (2007/10/03)
Selective N-Type Voltage Sensitive Calcium Channel (VSCC) antagonists have shown utility in several models of pain and ischemia. We report the structure-activity relationship at the proximal phenyl group in a series of non-peptidyl VSCC blockers.
