161581-95-9Relevant academic research and scientific papers
INDUCTION OF ESTROGEN RECEPTOR BETA BY CHOLESTEROL BIOSYNTHESIS INHIBITORS AND METHODS OF TREATMENT OF CANCER
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Paragraph 00197, (2014/01/17)
Disclosed herein are methods and compositions related to the discovery that cholesterol inhibitors induce the anti-proliferative protein, estrogen receptor beta (ERβ), in both ERα- positive and ERα-negative breast cancer cell lines, including triple negat
CHEMICAL COMPOUNDS
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Page/Page column 94, (2008/06/13)
The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation.
Oxidosqualene cyclase (OSC) inhibitors for the treatment of dyslipidemia
Dehmlow, Henrietta,Ackermann, Jean,Aebi, Johannes,Blum-Kaelin, Denise,Chucholowski, Alexander,Coassolo, Philippe,Hartman, Peter,Kansy, Manfred,Maerki, Hans Peter,Morand, Olivier,Von Der Mark, Elisabeth,Panday, Narendra,Ruf, Armin,Thoma, Ralf,Schulz-Gasch, Tanja
, p. 72 - 76 (2007/10/03)
Novel inhibitors of oxidosqualene cyclase (OSC) for the treatment of dyslipidemia are reported. Starting point for the chemistry program was a set of compounds derived from a fungicide project which, in addition to high affinity for OSC from Candida albicans, also showed high affinity for the human enzyme (hOSC). Here the evaluation process of different scaffolds is outlined for two representative series, the phenyl substituted benzo[d]isothiazoles and the aminocyclohexanes. The most promising compounds derived from the latter series were further profiled in vivo and showed promising properties with respect to modulation of lipid parameters. Schweizerische Chemische Gesellschaft.
Synthesis and structure-activity studies of novel orally active non-terpenoic 2,3-oxidosqualene cyclase inhibitors
Dehmlow, Henrietta,Aebi, Johannes D.,Jolidon, Synèse,Ji, Yu-Hua,Von der Mark, Elisabeth M.,Himber, Jacques,Morand, Olivier H.
, p. 3354 - 3370 (2007/10/03)
New orally active non-terpenoic inhibitors of human 2,3-oxidosqualene cyclase (hOSC) are reported. The starting point for the optimization process was a set of compounds derived from a fungicide project, which in addition to showing high affinity for OSC from Candida albicans showed also high affinity for human OSC. Common structural elements of these inhibitors are an amine residue and an electrophilic carbonyl C atom embedded in a benzophenone system, which are at a distance of about 10.7 ?. Considering that the keto moiety is in a potentially labile position, modifications of the substitution pattern at the benzophenone as well as annelated heteroaryl systems were explored. Our approach combined testing of the compounds first for increased binding affinity and for increased stability in vitro. Most promising compounds were then evaluated for their efficacy in lowering plasma total cholesterol (TC) and plasma low-density lipoprotein cholesterol (LDL-C) in hyperlipidemic hamsters. In this respect, the most promising compounds are the benzophenone derivative 1·fumarate and the benzo[d]-isothiazol 24·fumarate, which lowered TC by 40% and 33%, respectively.
Amino alkenyloxybenzene derivatives
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, (2008/06/13)
A method of lowering cholesterol which comprises administering to a host requiring such treatment an effective amount of a compound of the formula STR1 wherein one of R1 and R2 is C1-7 -alkyl and the other is C1-7 -alkyl or C2-6 -alkenyl-methyl; L is C1-11 -alkylene or C2-11 -alkenylene optionally bonded to the phenyl group via an O atom or L is 1,4-phenylene; n is 0 or, when L contains an O atom, n is 0 or 1; Q is C1-7 -alkyl, C2-10 -alkenyl or a group of formula STR2 wherein R is H, halogen, CF3, CN or NO2 ; R3 and R4 are H, C1-4 -alkyl or halogen; and R5 is H or, when R is H, R5 is H or halogen; or a pharmaceutically acceptable acid addition salt thereof, as well as certain compounds of formula I, are described.
