Supercharge Your Innovation With Domain-Expert AI Agents!
Compounds and methods for modulation of estrogen receptors
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
A compound and composition technology, applied in the field of compounds that selectively modulate estrogen beta-receptor activity, can solve problems such as side effects
Inactive Publication Date: 2006-10-25
SIGNAL PHARMA LLC
View PDF1 Cites 0 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
Problems solved by technology
For example, although estrogen replacement therapy has been associated with many beneficial effects (e.g., bone protection, cardiovascular effects, prevention of hot flashes, dementia, bone metabolism, etc.), this therapy also has side effects (e.g., breast and endometrial cancer, thrombosis Wait)
Method used
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
[0154] 2-(4-Hydroxybenzylacetone)-5-methoxyphenol
[0155]
[0156] To 3-methoxyphenol (50g, 0.40mol), 4-hydroxyphenylacetic acid (71g, 0.46mol) and ZnCl 2 (174g, 1.28mol) was added 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 and 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 provided chromatography (SiO 2 , 20% EtOAc / n-Hexane) to give 2-(4-hydroxyphenylacetone)-5-methoxyphenol (34.1 g, 33% yield) as a slightly white solid; mp 137-140°C.
[0160] To 2-(4-hydroxyphenylacetyl)-5-methoxyphenol (10g, 0.038mole), NEt 3 (6ml, 0.042mole) in CH 2 Cl 2 To the mixture in (50ml) was added triisopropylsilyl chloride (9ml, 0.042mole). The mixture was stirred for 22 h, concentrated and the residue was dissolved in EtOAc and H 2 O distribution. The organic layer was washed with NaOH (1N), HCl (1N) and brine. Dry the organic layer (MgSO 4 ), filtered and concentrated. The residue was treated with n-hexane to give 2-(4-triisopropylsilylbenzylacetone)-5-methoxyphenol (6.2 g, 38% yield) as a slightly white solid; mp 66-68°C.
[0164] To 2-(4-triisopropylsilylbenzylacetone)-5-methoxyphenol (4g, 9.6mmole), K 2 CO3 (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) and extracted with EtOAc (2x). Dry the organic layer (MgSO 4 ), filtered and concentrated. Residue and Et 2 O was stirred and the resulting solid was filtered and recrystallized (EtOH) to give 3-phenyl-4-(4-hydroxybenzyl)-7-methoxycoumarin (0.88 g, 15% yield) as White solid; mp235-236°C.
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
PUM
Login to View More
Abstract
Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having formula (I), as well as pharmaceutical compositions containing the same wherein R1, R2, R3, n and p are as defined here. In a specific embodiment, the compounds are selective modulators for ER- beta over ER- alpha . Methods are also disclosed for modulating ER- beta in cells and / or tissues expressing the same, including cells and / or tissues that preferentially express ER- beta . More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
Description
[0001] Cross-Referenced Related Applications [0002] This application claims priority to U.S. Provisional Application No. 60 / 114,472 (filed December 30, 1998), and is PCT / US99 / 31290 (filed December 30, 1999), U.S. Application No. 09 / 475,776 (filed December 30, 1999) , filed December 30, 2000) and US Application No. 09 / 492,939 (filed January 27, 2000) (each of which is hereby incorporated by reference in its entirety). technical field [0003] The present invention relates broadly to estrogen antagonists and agonists, and compounds that inhibit cytokines, and more specifically to compounds that selectively modulate the activity of estrogen β-receptors (ER-β), as well as their pharmaceutical compositions and about the method. Background of the invention [0004] Estrogens have a broad spectrum of effects on tissues in both females and males. Many of these biological effects are positive, including maintenance of bone density, cardiovascular protection, central nervous syste...
Claims
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to View More 
Login to View More