198481-32-2 Usage
Uses
Bazedoxifene is an nonsteroidal selective estrogen receptor modulator (SERM). Bazedoxifene is used as an antiosteoporotic.
General Description
Bazedoxifene, 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol (Viviant), was declared to be “approvable” bythe FDA in 2007 for the prevention of postmenopausalosteoporosis. As of mid-2009, final approval in the UnitedStates is still pending. Bazedoxifene was approved inEurope in 2009 for the treatment of post–menopausalosteoporosis.
Clinical Use
Bazedoxifene is an indole-based SERM that is under investigation for the treatment and prevention of
postmenopausal osteoporosis. It also is being evaluated in combination with Premarin (conjugated
estrogens). Bazedoxifene displaces 17β-estradiol from estrogen receptors and has excellent binding affinity for
the receptor itself. Unlike raloxifene, this agent does not cause hot flashes at the doses required to have a
beneficial effect on bone. In addition, it does not cause uterine or mammary gland stimulation.
Enzyme inhibitor
This potent and selective estrogen receptor modulator, or SERM (FW =
530.65 g/mol; CAS 198481-33-3; Solubility: 00 mM in DMSO), also named
1-[[4-[2- (hexahydro-1H-azepin-1-yl) ethoxy]phenyl]methyl]-2- (4-
hydroxyphenyl) -3-methyl-1H-indol-5-ol, selectivity targets the extrogen
receptor ERα (IC50 = 26 nM), with weaker action against ERβ (IC50 = 99
nM), inhibiting 17β-estradiol-induced proliferation of MCF-7 cells.
Bazedoxifene represents a promising new treatment for osteoporosis, one
with a potential for less uterine and vasomotor effects than selective
estrogen receptor modulators now used clinically.
Check Digit Verification of cas no
The CAS Registry Mumber 198481-32-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,9,8,4,8 and 1 respectively; the second part has 2 digits, 3 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 198481-32:
(8*1)+(7*9)+(6*8)+(5*4)+(4*8)+(3*1)+(2*3)+(1*2)=182
182 % 10 = 2
So 198481-32-2 is a valid CAS Registry Number.
InChI:InChI=1/C30H34N2O3/c1-22-28-20-26(34)12-15-29(28)32(30(22)24-8-10-25(33)11-9-24)21-23-6-13-27(14-7-23)35-19-18-31-16-4-2-3-5-17-31/h6-15,20,33-34H,2-5,16-19,21H2,1H3
198481-32-2Relevant articles and documents
Preparation method of bazedoxifene acetate crystal form A
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Paragraph 0028-0031; 0044-0046, (2020/04/22)
The invention discloses a preparation method of a bazedoxifene acetate crystal form A. The method comprises the following steps: taking 1-(4-(2-(azepine-1-yl) ethoxy) benzyl)-5-(benzyloxy)-2-(4-(benzyloxy) phenyl)-3-methyl-1H-indole as a raw material; preparing bazedoxifene acetate free alkali, preparing a bazedoxifene acetate crude product, preparing a bazedoxifene acetate crystal form B, preparing a bazedoxifene acetate crystal form C and preparing the bazedoxifene acetate crystal form A. A mixed solvent is adopted in the hydrogenation process of the method; the rate and the activity of thepalladium-carbon reduction reaction are improved; an antioxidant is added, so that the stability of the bazedoxifene free alkali is improved, the conversion from the crystal form B to the crystal formC is increased in the middle, key parameters for converting the crystal form C into the crystal form A are found, the purity of the crystal form A in the next step is greatly improved, and the production cost for producing the bazedoxifene acetate crystal form A is effectively reduced.
METHODS OF PREPARINGBAZEDOXIFENE BY NEW INTERMEDIATES
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, (2019/12/25)
The present invention relates to a method for manufacturing novel bazedoxifene or a pharmaceutically acceptable salt thereof. A manufacturing method according to the present invention can provide high purity and high yield of bazedoxifene, and is economical in terms of time and cost and eco-friendly due to a relatively simple manufacturing process, thereby being able to be usefully applied to mass production.COPYRIGHT KIPO 2020
METHODS OF PREPARING BAZOEDOXIFENE
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, (2018/10/16)
The present invention relates to novel bazedoxifene or to a method for producing a pharmaceutically acceptable salt thereof. The production method according to the present invention can provide the bazedoxifene with high purity and high yield, and is economical and environmentally friendly in terms of time and cost due to a relatively simple manufacturing process to be usefully applied to mass production.COPYRIGHT KIPO 2018