Category: 26018-73-5

New explortion of 6-Chlorobenzo[b]thiophene-2-carboxylic acid

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Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor

The blood coagulation enzyme factor Xa (FXa) is a particularly promising target for anticoagulant therapy, and identification of oral small-molecule inhibitors of FXa remains a research focus. On the basis of the X-ray crystal structure of FXa and its inhibitor rivaroxaban, we designed and synthesized a series of conformationally restricted mimics containing a novel [6,6,5] tricyclic fused oxazolidinone scaffold. Intensive structure-activity relationship (SAR) and structure-pharmacokinetic relationship (SPR) studies on this new series led to the discovery of compound 11a: a highly potent, selective, direct, and orally bioavailable FXa inhibitor with excellent in vivo antithrombotic efficacy and preferable pharmacokinetic profiles. Druggability evaluation of compound 11a was undertaken and elicited positive outcomes. All results indicate that compound 11a is a promising drug candidate for the prevention and treatment of thromboembolic diseases in venous and arterial systems.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Formula: C9H5ClO2S, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 26018-73-5, name is 6-Chlorobenzo[b]thiophene-2-carboxylic acid. In an article£¬Which mentioned a new discovery about 26018-73-5

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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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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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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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Related Products of 26018-73-5. In my other articles, you can also check out more blogs about 26018-73-5

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Synthesis of Antileukemic Indolylvinyl-1-benzofurans and -benzothiophenes

2-<2-(Indol-2-yl)vinyl>-1-benzofuran and -benzothiophene compounds 6-13 and 18-22 with terminal amidinium or imidazolinium groups were synthesized; in their antileukemic activity in mice they surpass the isosteric 2,2′-vinylenebis(1-benzofuran) and -(benzo-thiophene) compounds.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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26018-73-5, Name is 6-Chlorobenzo[b]thiophene-2-carboxylic acid, belongs to benzothiophene compound, is a common compound. Formula: C9H5ClO2SIn an article, once mentioned the new application about 26018-73-5.

(AZA)INDOLE-, BENZOTHIOPHENE-, AND BENZOFURAN-3-SULFONAMIDES

Disclosed are sulfonamide compounds with GPR17 modulating properties, which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating diseases or disorders.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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26018-73-5, Name is 6-Chlorobenzo[b]thiophene-2-carboxylic acid, belongs to benzothiophene compound, is a common compound. Recommanded Product: 6-Chlorobenzo[b]thiophene-2-carboxylic acidIn an article, once mentioned the new application about 26018-73-5.

METHOD FOR PROMOTING PLANT GROWTH

The present invention provides a method for promoting plant growth, which comprises treating a plant with at least one compound selected from a group consisting of a compound represented by the following Formula (1): and an agriculturally acceptable salt thereof, provided that a method for promoting plant growth which comprises treating plants with a compound corresponding to any one of the following (1) to (5) and an agriculturally acceptable salt thereof is excluded: (1) 4-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (2) 5-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (3) 6-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, (4) 7-(Trifluoromethyl)benzo[b]thiophene-2-carboxylic acid, and (5) Benzo[b]thiophene-2-carboxylic acid.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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GEMINAL SUBSTITUTED QUINUCLIDINE AMIDE COMPOUNDS AS AGONISTS OF ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTORS

The present invention relates to novel geminal substituted quinuclidine amide compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of alpha7- nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

The Absolute Best Science Experiment for 26018-73-5

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Reference of 26018-73-5, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.26018-73-5, Name is 6-Chlorobenzo[b]thiophene-2-carboxylic acid, molecular formula is C9H5ClO2S. In a Patent£¬once mentioned of 26018-73-5

Heteroaryl and benzyl amide compounds

Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Discovery of Novel Allosteric Inhibitors of Deoxyhypusine Synthase

Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for eIF5A activation, which, in turn, plays a key role in regulating protein translation of selected mRNA that are associated with the synthesis of oncoproteins, thereby enhancing tumor cell proliferation. Therefore, inhibition of DHPS is a promising therapeutic option for the treatment of cancer. To discover novel lead compounds that target DHPS, we conducted synthetic studies with a hit obtained via high-throughput screening. Optimization of the ring structures of the amide compound (2) led to bromobenzothiophene (11g) with potent inhibitory activity against DHPS. X-ray crystallographic analysis of 11g complexed with DHPS revealed a dramatic conformational change in DHPS, which suggests the presence of a novel allosteric site. These findings provide the basis for the development of novel therapy distinct from spermidine mimetic inhibitors.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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26018-73-5, 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, 26018-73-5, molcular formula is C9H5ClO2S, introducing its new discovery.

SUBSTITUTED (AMINOIMINOMETHYL OR AMINOMETHYL) BENZOHETEROARYL COMPOUNDS

This invention is directed to an (aminoiminomethyl or aminomethyl) benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem