1027374-85-1Relevant academic research and scientific papers
PHARMACEUTICAL COMPOSITIONS OF 6-(2-(2H-TETRAZOL-5-YL)ETHYL)-6-FLUORODECAHYDROISOQUINOLINE-3-CARBOXYLIC ACID AND ESTER DERIVATIVES THEREOF
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Paragraph 136, (2022/01/12)
6-(2-(2H-tetrazol-5-yl)ethyl)-6-fluorodecahydroisoquinoline-3-carboxylic acid and 6-(2-(2H-tetrazol-5-yl)ethyl)-6-fluorodecahydroisoquinoline-3-carboxylic acid hydrocarbyl ester derivatives of formula are disclosed, as are pharmaceutical compositions and methods for the treatment of pain, epilepsy, convulsions, and seizures employing those compositions.
GluK1 antagonists from 6-(carboxy)phenyl decahydroisoquinoline derivatives. SAR and evaluation of a prodrug strategy for oral efficacy in pain models
Martinez-Perez, Jose A.,Iyengar, Smriti,Shannon, Harlan E.,Bleakman, David,Alt, Andrew,Arnold, Brian M.,Bell, Michael G.,Bleisch, Thomas J.,Casta?o, Ana M.,Del Prado, Miriam,Dominguez, Esteban,Escribano, Ana M.,Filla, Sandra A.,Ho, Ken H.,Hudziak, Kevin J.,Jones, Carrie K.,Mateo, Ana,Mathes, Brian M.,Mattiuz, Edward L.,Ogden, Ann Marie L.,Simmons, Rosa Maria A.,Stack, Douglas R.,Stratford, Robert E.,Winter, Mark A.,Wu, Zhipei,Ornstein, Paul L.
, p. 6459 - 6462 (2013/11/19)
The synthesis and structure-activity relationship of decahydroisoquinoline derivatives with various benzoic acid substitutions as GluK1 antagonists are described. Potent and selective antagonists were selected for a tailored prodrug approach in order to f
Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain
Dominguez, Esteban,Iyengar, Smriti,Shannon, Harlan E.,Bleakman, David,Alt, Andrew,Arnold, Brian M.,Bell, Michael G.,Bleisch, Thomas J.,Buckmaster, Jennifer L.,Castano, Ana M.,Del Prado, Miriam,Escribano, Ana,Filla, Sandra A.,Ho, Ken H.,Hudziak, Kevin J.,Jones, Carrie K.,Martinez-Perez, Jose A.,Mateo, Ana,Mathes, Brian M.,Mattiuz, Edward L.,Ogden, Ann Marie L.,Simmons, Rosa Maria A.,Stack, Douglas R.,Stratford, Robert E.,Winter, Mark A.,Wu, Zhipei,Ornsteint, Paul L.
, p. 4200 - 4203 (2007/10/03)
Amino acids 5 and 7, two potent and selective competitive GluR5 KA receptor antagonists, exhibited high GluR5 receptor affinity over other glutamate receptors. Their ester prodrugs 6 and 8 were orally active in three models of pain: reversal of formalin-i
