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New Advances in Chemical Research in 2021. Catalysts allow a reaction to proceed that has a lower activation energy than the uncatalyzed reaction. In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. Computed Properties of C16H14O2S. Introducing a new discovery about 63675-74-1, Name is 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

The present invention relates to novel N-substituted azetidine derivatives < of the formula (I); wherein SERMF is a Selective Estrogen Receptor Modilator fragment; X is no atom, O, S, CH2, carbonyl, N-R5; R1 is H, (C1 -8)alkyl, (C3-8)cycloalkyl, (C3-6)heterocycloalkyl, (C2-6)alkenyl, (C2- 6)alkynyl, (C1 -4)alkylcarbonyl, (C1 -4)alkoxy(C2-4)alkyl, (C3-6)cycloalkyl(C1 -3)- alkyl, (C3-6)heterocycloalkyl(C1 -3)alkyl, each independently optionally substituted with one or more halogen, nitrile, hydroxyl or (C1 -2)alkyl; R5 is H, (C1 -3)alkyl, optionally substituted with one or more fluorine; R17, R18 and R19 are independently of each other H, fluorine, nitrile or (C1 -3)- alkyl, optionally substituted with one or more fluorine; or a prodrug, isotopically-labelled derivative or pharmaceutically acceptable salt thereof, > to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular to their use for the prevention or treatment of ovulatory dysfunction, uterine cancer, endometrium cancer, ovarian cancer, endometriosis, osteoporosis, prostate cancer, benign prostatic hypertrophy, and breast cancer, in particular ER-positive breast cancer, more in particular ER- positive, hormone treatment-resistant breast cancer. Said N-substituted azetidine derivatives have estrogen receptor alpha (ERa) antagonistic and – in certain embodiments – selective estrogen receptor downregulating (SERD) activity in ER-positive breast cancer cells.

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A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I wherein R1a is -H or -OR7a in which R7a is -H or a hydroxy protecting group; R2a is -H, halo, or -OR8a in which R8a is -H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 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, and further comprising administering to said woman an effective amount of estrogen.

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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. name: 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene, C16H14O2S. A document type is Patent, introducing its new discovery., name: 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

Mammary cancers are inhibited by administration of a combination of two drugs. The first compound is 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-pyrrolidinoethoxy)benzoyl]benzo[b]thiophene, and the second compound is tamoxifen.

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The present invention is directed to a new process for the synthesis of vinyl sulfenic acid derivatives. These compounds are useful for the synthesis of benzo b!thiophenes, in particular 2-aryl-benzo b!thiophenes.

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The present invention provides compounds with nitrogen, sulfur or carbon linked basic side chains of formula STR1 where R 1 and R. sup.2 are independently hydrogen, halo, hydroxy, alkoxy, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, arylcarbonyloxy, aryloxycarbonyloxy, or alkylsulfonyloxy; O–SO 2–(C 4-C 6 alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH 2 ; Y is–CH 2–,–NH–,–NMe–,–S–,–SO 2–; and R 3 and R. sup.4 are independently hydrogen, alkyl, alkylcarbonyl, alkylamino-carbonyl, or arylcarbonyl, or together with the nitrogen to which they are attached form 1-pyrrolidinyl, 1-piperidinyl, or a 5-or 6-membered imide or cyclic amide ring.

The present invention also provides pharmaceutical compositions containing the compounds optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for treating osteoporosis, aortal smooth muscle cell proliferation, (particularly restenosis), and estrogen-dependent cancer (particularly breast cancer).

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Breast cancer remains a significant cause of death in women, and few therapeutic options exist for estrogen receptor negative (ER (-)) cancers. Epigenetic reactivation of target genes using histone deacetylase (HDAC) inhibitors has been proposed in ER (-) cancers to resensitize to therapy using selective estrogen receptor modulators (SERMs) that are effective in ER (+) cancer treatment. Based upon preliminary studies in ER (+) and ER (-) breast cancer cells treated with combinations of HDAC inhibitors and SERMs, hybrid drugs, termed SERMostats, were designed with computational guidance. Assay for inhibition of four typea I HDAC isoforms and antagonism of estrogenic activity in two cell lines yielded a SERMostat with 1-3a muM potency across all targets. The superior hybrid caused significant cell death in ER (-) human breast cancer cells and elicited cell death at the same concentration as the parent SERM in combination treatment and at an earlier time point.

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Chemical Research Letters, May 2021. Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction.name: 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

The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): 1in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.

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Versatile, mild and high yielding methods for nucleophilic aromatic substitution of 2-dialkylamino-1-ethoxides and related nucleophiles on 3- aroyl-2-arylbenzothiophene nuclei are presented. A short synthesis of raloxifene is detailed.

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In an effort to identify selective for the estrogen receptor subtype ERbeta, a series of aryl benzthiophenes was synthesized. In a radioligand binding assay and reporter gene assat in HeLa and SH-SY5Y cells, compound were characterized as ERbeta-selective agonists. By targeting ERbeta in the brain, these compounds could lead to drugs able to separate the beneficial effects of estrogens on mood, learning, and memory from side effects such as the stimulation of edometrial and breast cancer.

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The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxyl)benzoyl]benzoyl]benzo[b]-thiophenes.

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