1127-29-3Relevant academic research and scientific papers
NOVEL CYP17 INHIBITORS/ANTIANDROGENS
-
Page/Page column 32, (2015/01/07)
Compounds of formula (I), wherein R1 to R8 A, B, Z1 and Z2 are as defined in the claims and pharmaceutically acceptable salts and esters thereof are disclosed. The compounds of formula (I) possess utility as androgen receptor antagonists (inhibitors) and/or cytochrome P450 monooxygenase 17a-hydroxylase/17,20-lyase (CYP17) inhibitors. The compounds are useful as medicaments in the treatment of cancer, particularly prostate cancer, and other androgen dependent conditions and diseases where androgen antagonism is desired.
Imines and Derivatives. Part 21. A Study of Structural and Mechanistic Aspects of the Synthesis of Imine, Imine Oxide, and Oxime Derivatives of 2,2,4,4-Tetramethylcyclobutane-1,3-Dione by X-Ray Crystalography and Nuclear Magnetic Resonance and Ultraviolet Spectroscopy
Boyd, A. John,Boyd, Derek R.,Burnett, Michael G.,Malone, John F.,Jennings, W. Brian
, p. 2093 - 2098 (2007/10/02)
The dinitrone derivatives (5a, b) of 2,2,4,4-tetramethylcyclobutane-1,3-dione were synthesised by peroxyacid oxidation of the corresponding di-imines (3a, b).X-ray crystallographic analysis of diimine (3a) and the hydroxyimino nitrone isomers (6a, b) indicate a marked buttressing effect leading to an exclusive preference for the trans geometry in di-imine (3a) and dinitrone (5a).Thermal elimination reactions of the N-But substituted nitrones (5a), (6a), and (8a) to yield oximes and 2-methylpropene have been investigated bu u.v. kinetic studies.The results areconsistent with a concerted mechanism involving a five-membered cyclic transition state.
