865712-53-4Relevant academic research and scientific papers
Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate
Ratcliffe, Paul,Adam, Julia M.,Baker, James,Bursi, Roberta,Campbell, Robert,Clark, John K.,Cottney, Jean E.,Deehan, Maureen,Easson, Anna-Marie,Ecker, Daniel,Edwards, Darren,Epemolu, Ola,Evans, Louise,Fields, Ruth,Francis, Stuart,Harradine, Paul,Jeremiah, Fiona,Kiyoi, Takao,McArthur, Duncan,Morrison, Angus,Passier, Paul,Pick, Jack,Schnabel, Peter G.,Schulz, Jurgen,Steinbrede, Heinz,Walker, Glenn,Westwood, Paul,Wishart, Grant,Haes, Joanna Udo De
, p. 2541 - 2546 (2011/06/17)
We report an expansion of the structure-activity relationship (SAR) of a novel series of indole-3-heterocyclic CB1 receptor agonists. Starting from the potent but poorly soluble lead, 1, a rational approach was taken in order to balance solubility, hERG a
Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor
Morrison, Angus J.,Adam, Julia M.,Baker, James A.,Campbell, Robert A.,Clark, John K.,Cottney, Jean E.,Deehan, Maureen,Easson, Anna-Marie,Fields, Ruth,Francis, Stuart,Jeremiah, Fiona,Keddie, Neil,Kiyoi, Takao,McArthur, Duncan R.,Meyer, Karsten,Ratcliffe, Paul D.,Schulz, Jurgen,Wishart, Grant,Yoshiizumi, Kazuya
scheme or table, p. 506 - 509 (2011/02/27)
Novel indole-3-heterocycles were designed and synthesized and found to be potent CB1 receptor agonists. Starting from a microsomally unstable lead 1, a bioisostere approach replacing a piperazine amide was undertaken. This was found to be a good strategy
(INDOL-3-YL)-HETEROCYCLE DERIVATIVES AS AGONISTS OF THE CANNABINOID CB1 RECEPTOR
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Page/Page column 31, (2010/11/26)
The invention relates to indole derivative having the general Formula (I) Wherein A, X1, X2, X3, Y, R1, R2, R3 and R4 are as defined in the claims, or a pharmaceutically acceptab
Indole derivatives
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Page/Page column 15, (2010/11/26)
Disclosed herein are indole derivatives of the formula (I) wherein each of the substitutents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the indole derivatives and use of
