1443331-82-5Relevant articles and documents
Effect of N-methyl deuteration on pharmacokinetics and pharmacodynamics of enzalutamide
Pang, Xuehai,Peng, Lingling,Chen, Yuanwei
, p. 401 - 409 (2017)
Enzalutamide, a second-generation antiandrogen, has been developed for the treatment of castration-resistance prostate cancer. We synthesized the deuterated analogues 6 and found that it showed higher drug exposure and thus stronger antitumor potency in preclinical settings. Compound 6 is being developed clinically for the potential to be differentiated from enzalutamide through reduced dosages and a higher safety margin.
METHOD FOR PREPARING DEUTERATED IMIDAZOLE DIKETONE COMPOUND
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, (2020/03/28)
A method for preparation of deuterated imidazole diketone compounds includes the following steps: (1) using compound of formula (I) and compounds of formula (II) as starting material, compounds of formula (III) can be obtained by a substitution reaction; (2) Compounds of formula (IV) can be prepared by esterification of carboxyl in compounds of formula (III); (3) Cyclization of compounds of formula (IV) and compound of formula (V) provides compounds of formula (VI); (4) Compounds of formula (VI) are deesterificated and react to produce compounds of formula (VII); (5) using compounds of formula (VII) and compounds of formula (VIII) as starting material, the deuterated imidazole diketone compounds of formula (IX) are obtained by the condensation reaction of amide.
IMIDAZOLIDINEDIONE COMPOUNDS AND THEIR USES
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Page/Page column, (2015/01/06)
Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds posses 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.
