217172-22-0Relevant academic research and scientific papers
Heteroaryl alkyl alpha substituted peptidylamine 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. The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, asthma, amyotropic lateral sclerosis, or epilepsy and to pharmaceutical compositions that contain the compounds of Formula I.
Substituted peptidylamine calcium channel blockers
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, (2008/06/13)
PCT No. PCT/US98/10838 Sec. 371 Date Jan. 19, 1999 Sec. 102(e) Date Jan. 19, 1999 PCT Filed May 28, 1998 PCT Pub. No. WO98/54123 PCT Pub. Date Dec. 3, 1998The present invention provides compounds that block calcium channels having the Formula I shown belo
Structure-activity relationship of N-methyl-N-aralkylpeptidylamines as novel N-type calcium channel blockers
Hu, Lain-Yen,Ryder, Todd R.,Rafferty, Michael F.,Dooley, David J.,Geer, Joann J.,Lotarski, Susan M.,Miljanich, George P.,Millerman, Elizabeth,Rock, David M.,Stoehr, Sally J.,Szoke, Balazs G.,Taylor, Charles P.,Vartanian, Mark G.
, p. 2151 - 2156 (2007/10/03)
Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown efficacy in several animal models of stroke and pain. In the process of searching for small molecule N-type calcium channel blockers, we have identified a series of N-methyl-N-aralkyl-peptidylamines with potent functional activity at N-type VSCCs. The most active compound discovered in this series is PD 173212 (11, IC50 = 36 nM in the IMR32 assays). SAR and pharmacological evaluation of this series are described.
N,N-dialkyl-dipeptidylamines as novel N-type calcium channel blockers
Hu, Lain-Yen,Ryder, Todd R.,Rafferty, Michael F.,Cody, Wayne L.,Lotarski, Susan M.,Miljanich, George P.,Millerman, Elizabeth,Rock, David M.,Song, Yuntao,Stoehr, Sally J.,Taylor, Charles P.,Weber, Mark L.,Szoke, Balazs G.,Vartanian, Mark G.
, p. 907 - 912 (2007/10/03)
Selective N-type voltage sensitive calcium channel (VSCC) blockers have shown utility in several models of stroke and pain. We are especially interested in small molecule N-type calcium channel blockers for therapeutic use. Herein, we report a series of N,N-dialkyl-dipeptidylamines with potent functional activity at N-type VSCCs and in vivo efficacy. The synthesis, SAR, and pharmacological evaluation of this series are discussed.
