Compounds and methods for modulation of estroglen receptors
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A technology for compounds and compositions, applied in the directions of active ingredients of heterocyclic compounds, drug combinations, organic chemistry, etc.
Inactive Publication Date: 2004-06-30
SIGNAL PHARMA LLC
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However, some of these results are controversial due to the method used to measure ER, the species used for the analysis (rat, mouse, human) and / or the differentiation state of the isolated primary cells
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Embodiment 1
[0133] 2-(4-Hydroxybenzylacetone)-5-methoxyphenol
[0134]
[0135] To 3-methoxyphenol (50g, 0.40mol), 4-hydroxyphenylacetic acid (71g, 0.46mol) and ZnCl 2 (174g, 1.28mol) was added with POCl 3 (100ml, 1.6mol). The mixture was stirred at 65°C for 2 hours, poured into ice water (2 L) and stirred until the ice melted. The clear supernatant was decanted, the residue was rinsed with water (1 L), and partitioned between EtOAc and water. The organic layer was washed with brine, dried (MgSO 4 ), filtered and concentrated. The resulting oil was purified by chromatography (SiO 2 , 20% EtOAc / n-Hexane) provided 2-(4-hydroxybenzylacetone)-5-methoxyphenol (34.1 g, 33% yield) as a white solid; mp 137-140°C.
[0139] To 2-(4-hydroxybenzylacetone)-5-methoxyphenol (10g, 0.038mole), NEt 3 (6ml, 0.042mole) in CH 2 Cl 2 (50ml) was added triisopropylsilyl chloride (9ml, 0.042mole). The mixture was stirred for 22 hours, concentrated, and the residue was dissolved in EtOAc and H 2 O distribution. The organic layer was washed with NaOH (1N), HCI (1N) and brine. The organic layer was dried (MgSO 4 ), filtered and concentrated. The residue was treated with n-hexane to give 2-(4-triisopropylsilyloxybenzylacetone)-5-methoxyphenol (6.2 g, 38% yield) as a white solid; mp 66-68°C .
[0143] To 2-(4-triisopropylsilyloxybenzylacetone)-5-methoxyphenol (4g, 9.6mmole), K 2 CO 3 (4g, 29mmoles) in CH 3 To the mixture in CN (50ml) was added phenylacetyl chloride (2.3ml, 14mmole). The mixture was stirred at reflux for 22 h, poured into H 2 O (0°C) (500ml), extracted with EtOAc (2x). The organic layer was dried (MgSO 4 ), filtered and concentrated. Residue and Et 2 With O stirring, the resulting solid was filtered and recrystallized (EtOH) to give 3-phenyl-4-(4-hydroxybenzyl)-7-methoxycoumarin (0.88 g, 15% yield) as a white solid; mp 235-236°C.
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Abstract
Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having structure I, as well as pharmaceutical compositions containing the same: wherein R1, R2, R3, n and p are as defined here. Methods are also disclosed for modulating ER in cells and / or tissues expressing the same, such as bone, breast, prostate, uterus, CNS or the cardiovascular system. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, and adverse reproductive effects associated with exposure to environmental chemicals or natural hormonal imbalances.
Description
technical field [0001] The present invention relates broadly to estrogen antagonists and agonists, cytokine inhibiting compounds, and related pharmaceutical compositions and methods. Background technique [0002] Estrogens have a wide range of effects on tissues in both females and males. Many of these biological effects are beneficial, including maintenance of bone density, cardiovascular protection, central nervous system (CNS) function, and protection of organ systems from the effects of aging. However, in addition to its positive effects, estrogen is also a potent growth factor that increases cancer risk in the breast and endometrium. [0003] To date, estrogen has been postulated to bind to a single intracellular estrogen receptor (ER). As discussed below, when a second ER (ER-β) was cloned (referring to the original ER as ER-α), and when cofactors regulating ER responses were discovered, this simple View. Ligands can bind two different ERs that bind estrogen-respon...
Claims
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