52605-99-9Relevant articles and documents
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.
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.
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