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2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents

Derivatives of 2-phenyl-3-aroylbenzothiophenes and 2-phenyl-3-aroylbenzothiophene-1-oxides are useful as antifertility agents. Certain of these compounds also are useful in suppressing the growth of mammary tumors.

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Inhibition of bone loss by 3-(4-acrylamidobenzoyl) benzo?b!-thiophenes

This invention relates to 3-(4-acrylamidobenzoyl)benzo?b! thiophenes, to the process for their preparation, to pharmaceutical compositions and to their use for modifying the balance between bone resorption and bone production in a mammal. The compounds useful in this invention are represented by the formula STR1 wherein R1 and R2 are independently hydrogen or lower alkyl containing 1-8 carbon atoms, or R1 and R2 together with the interposed nitrogen forms a 5-7 membered ring optionally containing an additional heteroatom selected from nitrogen, sulfur or oxygen.

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COMPOSITIONS AND METHODS FOR TREATING ESTROGEN-RELATED MEDICAL DISORDERS

Disclosed herein are methods for treatment of estrogen-related medical disorders. The methods of treatment may comprise administering to a subject in need of such treatment a composition comprising a therapeutically effective amount of at least one compound of formula (I) or a pharmaceutically acceptable salt thereof.

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Benzothiophene – Wikipedia,
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Description anti-mitotic agents which inhibit tubulin polymerization

Methoxy and ethoxy substituted 3-aroyl-2-arylbenzo[b]thiophenes and benzo[b]thiophene analogues are described for use in inhibiting tubulin polymerization. The compounds’ use for treating tumor cells is also described. Additional aspects described here are certain diaryl ether benzo[b]thiophene derivatives. Also described are particular analogs derived from dihydronaphthalene which have proven particularly effective. Certain new benzofuran analogs are described, as well as certain sulfur oxide benzo[b]thiophene analogs. Important compounds described herein include the first nitrogen-containing derivatives of combretastatin. These include nitro, amino and azide combrdtastatin derivatives.

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Antiestrogens. 2. Structure-Activity Studies in a Series of 3-Aroyl-2-arylbenzothiophene Derivatives Leading to <6-Hydroxy-2-(4-hydroxyphenyl)benzothien-3-yl><4-<2-(1-piperidinyl)ethoxy>phenyl>methanone Hydrochloride (LY156758), a Remarkably Effective Estrogen Antagonist with On…

In an effort to prepare nonsteroidal antiestrogens demonstrating greater antagonism and less intrinsic estrogenicity than those currently available, a series of 3-aroyl-2-arylbenzothiophene derivatives was synthesized.These compounds were prepared by Friedel-Crafts aroylation of appropriate O-protected 2-arylbenzothiophene nuclei with basic side-chain-bearing benzoyl chlorides followed by removal of the protective groups to provide the desired compounds containing both hydroxyl and basic side-chain functionality.A particularly useful method for the cleavage of aryl methoxy ethers without removal of (dialkylamino)ethoxy side chain functionality elsewhere in the molecule was found to be AlCl3/EtSH.The benzothiophene derivatives were tested for their ability to inhibit the growth-stimulating action of estradiol on the immature rat uterus.Seemingly minor changes in the side-chain amine moiety were found to have profound effects on the ability of the compounds to antagonize estradiol.Analogues having basic side chains containing cyclic (pyrrolidine, piperidine, and hexamethyleneamine) moieties were found to have less intrinsic estrogenicity and to antagonize estradiol action more completely than their noncyclic counterparts.The most effective antiestrogen in the series, compound 44, <6-hydroxy-2-(4-hydroxyphenyl)benzothien-3-yl><4-<2-(1-piperidinyl)ethoxy>phenyl>methanone, elicited a modest uterotropic activity that did not increase with increasing dose.In antagonism of estradiol, 44 exhibited a degree of inhibition surpassing that of tamoxifen at any dose tested.The new benzothiophene antiestrogen was also shown to have high affinity for rat uterine cycloplasmic estrogen receptor and to be an inhibitor of the growth of DMBA-induced rat mammary tumors.

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Benzothiophene – Wikipedia,
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Benzothiophene compounds, intermediates, processes, compositions, and methods

The invention provides benzothiophene compounds, of formula I, STR1 wherein R1, R2, R3, R4 and n are as defined in the specification, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions, including hyperlipidemia, and other cardiovascular pathologies.

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Glucopyranoside benzothiophenes

A compound of the formula STR1 or a pharmaceutically acceptable salt or solvate thereof. Also provided by the invention are methods of use of the above compounds, and processes for the preparation thereof.

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Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo

The synthesis of benzothiophenes containing a piperazine side chain and their binding affinities for estrogen receptors are described. These compounds bearing piperazine side chains were identified to be high-affinity ligands with high selectivity for ER alpha subtype. They were also potent agonists in bone tissue.

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Process for preparing benzo[b]thiophenes

The preparation of benzo[b]thiophenes by the acylation of alkoxy protected starting materials followed by demethylation using essentially odorless thiol compounds are provided herewith. Demethylation may be carried out in the same reaction vessel without isolation of the acylated, protected material.

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Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring.Application In Synthesis of 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 63675-74-1, Name is 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene, molecular formula is C16H14O2S

Process for preparing 2-substituted benzo[b]thiophene compounds and intermediates thereof

The present invention provides processes for preparing 2-substituted benzo[b]thiophene compounds, some of which are useful as intermediates for preparing pharmaceutically-active compounds and others which are useful, inter alia, for the treatment of osteoporosis in postmenopausal women.

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Benzothiophene – Wikipedia,
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