948581-62-2Relevant 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
scheme or table, 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
17 BETA HSD TYPE 5 INHIBITOR
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Page/Page column 20, (2008/12/08)
To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17βHSD type 5. It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17βHSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone; and the present invention has thus been completed.
