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The present invention provides a method of treating depression, mood swings, or Alzheimer’s disease in a patient in need of such treatment by administering a selective estrogen receptor modulating compound of the formula STR1 in which R 1 and R 2 are independently hydroxy and alkoxy of one to four carbon atoms; and R 3 and R 4 are independently methyl or ethyl, or R 3 and R 4, taken together with the nitrogen atom to which they are attached, form a pyrrolidino, methyl-pyrrolidino, dimethylpyrrolidino, piperidino, morpholino, or hexamethyleneimino ring.

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Reference:
Benzothiophene – Wikipedia,
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The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction. SDS of cas: 63675-74-1, 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

The boron trifluoride-etherate mediated cyclization of 2-arylthio- ketones 1a-h at ambient temperature gave 3-aryl-substituted benzothiophenes 2a-h in excellent yield. None of the rearranged 2-aryl-substituted benzothiophenes were observed.

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The present invention provides a novel process for preparing a compound of formula I STR1 wherein R1 and R2 combine to form C4 -C6 polymethylene, –CH2 CH(CH3)CH2 CH2 –, –CH2 C(CH3)2 CH2 CH2 –, or –CH2 CH2 OCH2 CH2 –; or a pharmaceutically acceptable salt or solvate thereof. Also provided intermediates of formulae II and IV STR2 wherein Z is a leaving group.

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Benzothiophene – Wikipedia,
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The present invention provides pharmaceutically active compounds of formula I STR1 wherein R1 is –H, –OH, –O(C1 -C4 alkyl), –OCOC6 H5, –OCO(C1 -C6 alkyl), or –OSO2 (C2 -C6 alkyl); R2 is –H, –OH, –O(C1 -C4 alkyl), –OCOC6 H5, –OCO(C1 -C6 alkyl), –OSO2 (C2 -C6 alkyl), or halo, providing when Z is –S–, R2 is not halo; R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and z is –O– or –S–; or a pharmaceutically acceptable salt thereof, for inhibiting restenosis.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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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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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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The invention relates to new furans and thiophenes with the general Formula 1, STR1 in which R1 and R2 independently of one another denote a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, a benzyl group, a group C(O)R4, where R4 is an alkyl or alkoxy group having 1 to 10 carbon atoms or a phenyl radical, or a carbamoyl group –C(O)NR5 R6, where R5 and R6 independently of one another are a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, and n denotes an integer from 0 to 12 if R3 is a hydrogen atom, or n denotes an integer from 4 to 12 if R3 is an amino group –NR7 R8, where R7 and R8 independently of one another represent a hydrogen atom or an alkyl group having 1 to 10 carbon atoms or R7 and R8 together represent an alkylene group –(CH2)m — or the group –(CH2)2 — or R3 denotes an amide group –C(O)NR7 R 8, where R7 and R8 have the abovementioned meanings, or R3 denotes a sulphinyl group –S(O)R3, where R9 is the radical –(CH2)m (CF2)o CF3 and m and o are 2, 3, 4, 5 or 6 and x denotes an oxygen or sulphur atom. These new compounds are strong and selective anti-oestrogens, and have therapeutic applications in the treatment of oestrogen-related illnesses.

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Benzothiophene – Wikipedia,
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The invention provides 2,3-aryl-benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.

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The invention provides novel benzothiophenes of the formula:wherein R1 is -H, -OH, -O(C1-C4 alkyl), -O-CO(C1-C6 alkyl), -OSO2(C4-C6 alkyl, or -OCOAr where Ar is optionally substituted phenyl; R2 is -H, -OH, -Cl, -Br, -O(C1-C4 alkyl), -OCO(C1-C6 alkyl), -OSO2(C4-C6 alkyl, or -OCOAr where Ar is optionally substituted phenyl; R3 is -H, -F, -Cl, -(C1-C4 alkyl), -CN, or -O(C1-C3 alkyl); R4 is -H, -F, -Cl, -(C1-C4 alkyl), -CN or -O(C1-C3 alkyl); R5 is -H, -F, -Cl, -(C1-C4 alkyl), or -O(C1-C3 alkyl); and R6 is -H, -F, -Cl, -(C1-C4 alkyl), or -O(C1-C3 alkyl); with the provisos that R3, R4, R5 and R6 can not all be hydrogen, and that when one of R3, R4, R5 or R6 is C1-C4 alkyl, no more than two of R3, R4, R5 and R6 can be hydrogen; Y is -CO-, -CHOH-, or -CH2-; R7 and R8 are independently C1-C4 alkyl or combine to form, with the nitrogen to which they are attached, 1-piperidinyl, 1-pyrrolidinyl, 1-hexamethyleneimino, or morpholino; or a pharmaceutically acceptable salt thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, optionally containing estrogen opr progestin, and the use of such compounds alone, or in combination with estrogen or progestin or alleviating the symptoms of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estroge

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Benzothiophene – Wikipedia,
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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem