Properties and Exciting Facts About Benzo[b]thiophen-4-amine

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One method for the preparation of new […] (by machine translation)

The present invention provides a new method for preparing according to […], which belongs to the technical field of pharmaceutical and chemical synthesis. It solves the problem that the existing according to[…] of the preparation method of the impurity is high, the yield is low, the problem of serious pollution. This method, in order to 4-hydroxybenzene and thiophene as the starting material 4 is prepared by the step of reaction intermediates V, to 7-hydroxy-2-quinolone by 2 VII is prepared by the step of reaction intermediates, intermediate V and intermediates prepared by condensation VII clinical medicine […]according to. The raw materials of this invention is easy to obtain, the price is low, the operation is simple, mild reaction conditions, has excellent industrial application value. (by machine translation)

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Discovery of 26018-73-5

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SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa

In the search of Factor Xa (FXa) inhibitors structurally different from the pyrazole-based series, we identified a viable series of enantiopure cis-(1R,2S)-cycloalkyldiamine derivatives as potent and selective inhibitors of FXa. Among them, cyclohexyldiamide 7 and cyclopentyldiamide 9 were the most potent neutral compounds, and had good anticoagulant activity comparable to the pyrazole-based analogs. Crystal structures of 7-FXa and 9-FXa illustrate binding similarities and differences between the five- and the six-membered core systems, and provide rationales for the observed SAR of P1 and linker moieties.

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A new application about 20699-85-8

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BENZOTHIOPHENE DERIVATIVES

The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

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Awesome and Easy Science Experiments about 20532-28-9

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ACTIVATORS OF THE RETINOIC ACID INDUCIBLE GENE “RIG-I’ PATHWAY AND METHODS OF USE THEREOF

The present invention is directed to compounds of Formula (I), which are activators of the RIG-I pathway.

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Properties and Exciting Facts About 4-Chlorobenzo[b]thiophene

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 66490-33-3 is helpful to your research. Related Products of 66490-33-3

Related Products of 66490-33-3, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 66490-33-3, molcular formula is C8H5ClS, introducing its new discovery.

Substituted oxoazaheterocyclyl compounds

This invention is directed to oxoazaheterocycyl compounds which inhibit Factor Xa, to oxoazaheterocycyl compounds which inhibit both Factor Xa and Factor IIa, to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds, to a method of directly inhibiting Factor Xa and to a method of simultaneously directly inhibiting Factor Xa and Factor IIa..

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Awesome and Easy Science Experiments about 4923-87-9

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Covalent modification of 2?-deoxyuridine with two different molecular switches

Two different molecular switches, a spiropyran and a diarylethene, were attached synthetically to the 5-position of 2-de-oxyuridine. The diarylethene-modified nucleoside can be incorporated synthetically into DNA while preserving its characteristic photochromism. Georg Thieme Verlag Stuttgart ¡¤ New York.

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Brief introduction of Benzo[b]thiophen-5-ol

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Benzothiophene derivative compounds process of preparation and use thereof

This invention provides new benzothiophene derivatives of general formula (I) and a process for preparing them, the corresponding compositions and their use for manufacturing a medicine for the treatment of neurological disorders. These new compounds behave as serotonin reuptake inhibitors and show high affinity towards the 5-HT1A receptor.

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Awesome Chemistry Experiments For 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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Nonsteroidal estrogens bearing acyl azide functions: potential electrophilic and photoaffinity labeling agents for the estrogen receptor

In an effort to develop novel affinity labeling agents for the estrogen receptor, we have synthesized two nonsteroidal ligands, a 1-aroyl-2-aryl tetralin system (1) and a 2-aryl-3-aroylbenzothiophene system (2).These agents, patterned after the Lilly antiestrogens trioxifene and LY 117018, respectively, embody acyl azide functions as part of a benzoyl chromophore.The acyl azide group has weak acylating activity, suitable for electrophilic affinity labeling,but this function is also photoreactive and, in its particular embodiment within these ligands, it could provide an efficient photochemical route to the highly reactive singlet acyl nitrene.The tetralin system (1) was prepared nine steps from 6-methoxy-1-tetralone, and the benzothiophene system (2) was prepared in four steps from a known substituted benzothiophene precursor.In competitive binding assays, both compounds show reasonable binding affinity for the rat and lamb uterine estrogen receptor : estradiol = 100percent, 1 = 3percent, and 2 = 12percent.When assayed by indirect receptor consumption assays, both compounds appear to have substantial capacity for irreversible binding (electrophilic reaction) with the receptor.This reactivity, which suggests that acylation of the receptor has occurred, is photoreversible.The nature of this ligand-receptor interaction is being investigated further. keywords: estrogen receptor, affinity labeling, photoaffinity labeling, nonsteroidal estrogens, antiestrogens, steroids

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New explortion of 14315-11-8

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An improved synthesis of substituted benzo[b]thiophenes using microwave irradiation

An easy and high-yielding method for the synthesis of substituted benzo[b]thiophenes using microwave irradiation is described.

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Final Thoughts on Chemistry for Methyl 4-bromobenzo[b]thiophene-2-carboxylate

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Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5- carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT)

Potent, 1H-pyrazolo[3,4-b]pyridine-containing inhibitors of the human nicotinamide phosphoribosyltransferase (NAMPT) enzyme were identified using structure-based design techniques. Many of these compounds exhibited nanomolar antiproliferation activities against human tumor lines in in vitro cell culture experiments, and a representative example (compound 26) demonstrated encouraging in vivo efficacy in a mouse xenograft tumor model derived from the A2780 cell line. This molecule also exhibited reduced rat retinal exposures relative to a previously studied imidazo-pyridine-containing NAMPT inhibitor. Somewhat surprisingly, compound 26 was only weakly active in vitro against mouse and monkey tumor cell lines even though it was a potent inhibitor of NAMPT enzymes derived from these species. The compound also exhibited only minimal effects on in vivo NAD levels in mice, and these changes were considerably less profound than those produced by an imidazo-pyridine-containing NAMPT inhibitor. The crystal structures of compound 26 and the corresponding PRPP-derived ribose adduct in complex with NAMPT were also obtained.

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Benzothiophene – Wikipedia,
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