52605-99-9Relevant academic research and scientific papers
AZA-BENZOTHIOPHENE COMPOUNDS AS STING AGONISTS
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Page/Page column 45; 54-55, (2019/10/29)
Compounds of general formula (I), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R5, R6, R8, R9, A, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
D-AMINO ACID OXIDASE INHIBITORS AND THERAPEUTIC USES THEREOF
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, (2019/04/29)
The present invention relates to compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: each of A, B, C, D, and E, independently, is C, N, N—H, O, S, or absent is a single bond or a double bond; each of X, Y, and Z, independentl
Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units
Choi, Peter J.,Sutherland, Hamish S.,Tong, Amy S.T.,Blaser, Adrian,Franzblau, Scott G.,Cooper, Christopher B.,Lotlikar, Manisha U.,Upton, Anna M.,Guillemont, Jerome,Motte, Magali,Queguiner, Laurence,Andries, Koen,Van den Broeck, Walter,Denny, William A.,Palmer, Brian D.
supporting information, p. 5190 - 5196 (2017/11/01)
Analogues of bedaquiline where the phenyl B-unit was replaced with monocyclic heterocycles of widely differing lipophilicity (thiophenes, furans, pyridines) were synthesised and evaluated. While there was an expected broad positive correlation between lipophilicity and anti-TB activity, the 4-pyridyl derivatives appeared to have an additional contribution to antibacterial potency. The majority of the compounds were (desirably) more polar and had higher rates of clearance than bedaquiline, and showed acceptable oral bioavailability, but there was only limited (and unpredictable) improvement in their hERG liability.
THERAPEUTIC HYDROXYPYRIDINONES, HYDROXYPYRIMIDINONES AND HYDROXYPYRIDAZINONES
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Page/Page column 103-104, (2014/04/03)
The invention provides compounds of formula (I): and salts and prodrugs thereof wherein R4, X1 and X2 have any of the meanings defined in the specification, as well as pharmaceutical compositions comprising the compounds or salts and methods for their use in therapy. The compounds have useful antiviral properties.
FSH RECEPTOR ANTAGONISTS
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, (2013/04/10)
The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders
Antitumor agents 222. Synthesis and anti-androgen activity of new diarylheptanoids
Ohtsu, Hironori,Itokawa, Hideji,Xiao, Zhiyan,Su, Ching-Yuan,Shih, Charles C.-Y.,Chiang, Tzuying,Chang, Eugene,Lee, YiFen,Chiu, Shang-Yi,Chang, Chawnshang,Lee, Kuo-Hsiung
, p. 5083 - 5090 (2007/10/03)
Fifteen new diarylheptanoids were synthesized and evaluated for antagonistic activity against androgen receptor (AR)-mediated reporter gene transcription using DU145, PC-3, and LNCaP prostate cancer cell lines. Most compounds showed activity in a 5α-dihydrotestosterone (DHT)-induced reporter gene expression assay in DU145 cells transfected with wild-type AR. Ten compounds (5, 8, 10, 14-15, and 18-22) were equipotent with hydroxyflutamide (HF), the anti-androgen currently available for the treatment of prostate cancer. However, except for compounds 5 and 10, none of the tested compounds was significantly effective in attenuating DHT-induced reporter gene expression in LNCaP cells, which contain endogenous mutant AR.
