1166819-48-2Relevant academic research and scientific papers
Discovery of AZD3514, a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer
Bradbury, Robert H.,Acton, David G.,Broadbent, Nicola L.,Brooks, A. Nigel,Carr, Gregory R.,Hatter, Glenn,Hayter, Barry R.,Hill, Kathryn J.,Howe, Nicholas J.,Jones, Rhys D.O.,Jude, David,Lamont, Scott G.,Loddick, Sarah A.,McFarland, Heather L.,Parveen, Zaieda,Rabow, Alfred A.,Sharma-Singh, Gorkhn,Stratton, Natalie C.,Thomason, Andrew G.,Trueman, Dawn,Walker, Graeme E.,Wells, Stuart L.,Wilson, Joanne,Wood, J. Matthew
, p. 1945 - 1948 (2013)
Removal of the basic piperazine nitrogen atom, introduction of a solubilising end group and partial reduction of the triazolopyridazine moiety in the previously-described lead androgen receptor downregulator 6-[4-(4-cyanobenzyl)piperazin-1-yl]-3-(trifluoromethyl)[1,2,4]triazolo[4,3-b] pyridazine (1) addressed hERG and physical property issues, and led to clinical candidate 6-(4-{4-[2-(4-acetylpiperazin-1-yl)ethoxy]phenyl}piperidin-1-yl)-3- (trifluoromethyl)-7,8-dihydro[1,2,4]triazolo[4,3-b]pyridazine (12), designated AZD3514, that is being evaluated in a Phase I clinical trial in patients with castrate-resistant prostate cancer.
TRIAZOLO [4,3-B] PYRIDAZINE DERIVATIVES AND THEIR USES FOR PROSTATE CANCER
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Page/Page column 135, (2010/09/03)
The invention concerns bicyclic compounds of Formula (I) wherein Formula (II), R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen- receptor associated conditions, particularly prostate cancer.
