1638885-65-0Relevant articles and documents
Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles
Pang, Xuehai,Wang, Yingwei,Chen, Yuanwei
, p. 2803 - 2806 (2017)
A series of deuterated apalutamide were designed and prepared. Compared to its prototype compound 18, deuterated analogues 19 and 21 showed obviously higher plasma concentrations and better PK parameters after oral administration in mice. In rats, N-trideuteromethyl compound 19 displayed 1.8-fold peak concentration (Cmax), and nearly doubled its drug exposure in plasma (AUC0–∞) compared to compound 18. Unsurprisingly, compounds 18 and 19 had similar affinity for AR in vitro. In summary, the deuteration strategy could obviously improve PK parameters of apalutamide.
IMIDAZOLE DIKETONE COMPOUND AND USE THEREOF
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Paragraph 0113; 0118; 0119, (2016/06/28)
Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds possess androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.