Category: 360575-29-7

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INHIBITORS OF BRUTON’S TYROSINE KINASE

Disclosed herein are reversible and irreversible inhibitors of Bruton’s tyrosine kinase (Btk). Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are describeded, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Related Products of 360575-29-7, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 360575-29-7, Name is Methyl 4-bromobenzo[b]thiophene-2-carboxylate, molecular formula is C10H7BrO2S. In a Article£¬once mentioned of 360575-29-7

Spirolactam-based acetyl-CoA carboxylase inhibitors: Toward improved metabolic stability of a chromanone lead structure

Acetyl-CoA carboxylase (ACC) catalyzes the rate-determining step in de novo lipogenesis and plays a crucial role in the regulation of fatty acid oxidation. Alterations in lipid metabolism are believed to contribute to insulin resistance; thus inhibition of ACC offers a promising option for intervention in type 2 diabetes mellitus. Herein we disclose a series of ACC inhibitors based on a spirocyclic pyrazololactam core. The lactam series has improved chemical and metabolic stability relative to our previously reported pyrazoloketone series, while retaining potent inhibition of ACC1 and ACC2. Optimization of the pyrazole and amide substituents led to quinoline amide 21, which was advanced to preclinical development.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. SDS of cas: 360575-29-7. Introducing a new discovery about 360575-29-7, Name is Methyl 4-bromobenzo[b]thiophene-2-carboxylate

NOVEL TETRAHYDROPYRIDOPYRIMIDINES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

The present invention provides novel compounds having the general formula (I) wherein R1, R2 and Z are as described herein, compositions including the compounds and methods of using the compounds.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Design, synthesis, and evaluation of acetylcholinesterase and butyrylcholinesterase dual-target inhibitors against Alzheimer?s diseases

A series of novel compounds 6a?h, 8i?1, 10s?v, and 16a?d were synthesized and evaluated, together with the known analogs 11a?f, for their inhibitory activities towards acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The inhibitory activities of AChE and BChE were evaluated in vitro by Ellman method. The results show that some compounds have good inhibitory activity against AChE and BChE. Among them, compound 8i showed the strongest inhibitory effect on both AChE (eeAChE IC50 = 0.39 muM) and BChE (eqBChE IC50 = 0.28 muM). Enzyme inhibition kinetics and molecular modeling studies have shown that compound 8i bind simultaneously to the peripheral anionic site (PAS) and the catalytic sites (CAS) of AChE and BChE. In addition, the cytotoxicity of compound 8i is lower than that of Tacrine, indicating its potential safety as anti-Alzheimer?s disease (anti-AD) agents. In summary, these data suggest that compound 8i is a promising multipotent agent for the treatment of AD.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. name: Methyl 4-bromobenzo[b]thiophene-2-carboxylate. Introducing a new discovery about 360575-29-7, Name is Methyl 4-bromobenzo[b]thiophene-2-carboxylate

HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK

Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Related Products of 360575-29-7, 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, 360575-29-7, molcular formula is C10H7BrO2S, introducing its new discovery.

Crystal structures, binding interactions, and ADME evaluation of brain penetrant N-substituted indazole-5-carboxamides as subnanomolar, selective monoamine oxidase B and dual MAO-A/B inhibitors

The pharmacological and physicochemical analysis of structurally optimized N-alkyl-substituted indazole-5-carboxamides, developed as potential drug and radioligand candidates for the treatment and diagnosis of Parkinson’s disease (PD) and other neurological disorders, is reported. Recent efforts have been focused on the development of subnanomolar potent, selective MAO-B (N1-alkyl-substituted compounds 12a?14a and 15) and dual active MAO-A/B (N2-methylated compounds 12b?14b) inhibitors with nanomolar potency towards MAO-B and moderately active against MAO-A enzyme, respectively. The most promising drug-like derivatives in both series were N-(3-chloro-4-fluorophenyl)-1-methyl-1H-indazole-5-carboxamide (13a, NTZ-1441, IC50hMAO-B 0.662?nM, >15000-fold selective versus MAO-A) and N-(3-chloro-4-fluorophenyl)-2-methyl-2H-indazole-5-carboxamide (13b, NTZ-1442, IC50hMAO-B 8.08?nM, IC50hMAO-A 0.56?muM, SI?=?70). Moreover, compounds 13a and 13b were predicted to cross both the gastrointestinal tract (at pH 2.0, 5.5, and 7,4) and the blood-brain barrier (BBB) in?vitro with appropriate drug-like properties required for CNS active drugs. Combined single X-ray/molecular modeling studies provided insights into the enzyme?inhibitor interactions within both MAO isoforms and the rationale for their inhibitory activity with controlled MAO-A/B selectivity ? despite their small structural differences. The binding modes of 12a,b and 13a,b confirmed that the major interactions with hMAO-B were established via the flexible carbonyl group of the carboxamide linkage and the electron-donating nitrogens N1 or N2 of the indazole moiety, allowing further exploration of the alkyl side chain for next step lead optimization efforts.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Scaffold oriented synthesis. Part 4: Design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions

We report the synthesis and biological evaluation of 5-substituted indazoles as kinase inhibitors. The compounds were synthesized in a parallel synthesis fashion from readily available starting materials employing heterocycle forming and multicomponent reactions and were evaluated against a panel of kinase assays. Potent inhibitors were identified for Gsk3beta, Rock2, and Egfr.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Synthetic Route of 360575-29-7, 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, 360575-29-7, molcular formula is C10H7BrO2S, introducing its new discovery.

Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening

The mediator complex-associated cyclin dependent kinase CDK8 regulates beta-catenin-dependent transcription following activation of WNT signaling. Multiple lines of evidence suggest CDK8 may act as an oncogene in the development of colorectal cancer. Here we describe the successful optimization of an imidazo-thiadiazole series of CDK8 inhibitors that was identified in a high-throughput screening campaign and further progressed by structure-based design. In several optimization cycles, we improved the microsomal stability, potency, and kinase selectivity. The initial imidazo-thiadiazole scaffold was replaced by a 3-methyl-1H-pyrazolo[3,4-b]-pyridine which resulted in compound 25 (MSC2530818) that displayed excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable. Furthermore, we demonstrated modulation of phospho-STAT1, a pharmacodynamic biomarker of CDK8 activity, and tumor growth inhibition in an APC mutant SW620 human colorectal carcinoma xenograft model after oral administration. Compound 25 demonstrated suitable potency and selectivity to progress into preclinical in vivo efficacy and safety studies.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

360575-29-7, Name is Methyl 4-bromobenzo[b]thiophene-2-carboxylate, belongs to benzothiophene compound, is a common compound. COA of Formula: C10H7BrO2SIn an article, once mentioned the new application about 360575-29-7.

Design, synthesis, in vitro and in vivo evaluation of benzylpiperidine-linked 1,3-dimethylbenzimidazolinones as cholinesterase inhibitors against Alzheimer?s disease

Cholinesterase inhibitor plays an important role in the treatment of patients with Alzheimer?s disease (AD). Herein, we report the medicinal chemistry efforts leading to a new series of 1,3-dimethylbenzimidazolinone derivatives. Among the synthesised compounds, 15b and 15j showed submicromolar IC50 values (15b, eeAChE IC50 = 0.39 ¡À 0.11 muM; 15j, eqBChE IC50 = 0.16 ¡À 0.04 muM) towards acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Kinetic and molecular modelling studies revealed that 15b and 15j act in a competitive manner. 15b and 15j showed neuroprotective effect against H2O2-induced oxidative damage on PC12 cells. This effect was further supported by their antioxidant activity determined in a DPPH assay in vitro. Morris water maze test confirmed the memory amelioration effect of the two compounds in a scopolamine-induced mouse model. Moreover, the hepatotoxicity of 15b and 15j was lower than tacrine. In summary, these data suggest 15b and 15j are promising multifunctional agents against AD.

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

 

As an important bridge between the micro and macro material world, chemistry is one of the main methods and means for humans to understand and transform the material world. 360575-29-7, name is Methyl 4-bromobenzo[b]thiophene-2-carboxylate. In an article£¬Which mentioned a new discovery about 360575-29-7, Recommanded Product: 360575-29-7.

A method for inhibiting ROCK compound and its application (by machine translation)

The present invention discloses a compound of the formula I as shown, or a stereoisomer thereof, or a pharmaceutically acceptable salt, or solvate thereof, or prodrug thereof, or its metabolic product. The test shows, the compounds of the invention has good ROCK inhibition activity, can be effectively used for ROCK activity with abnormal in the treatment of diseases. (by machine translation)

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Recommanded Product: 360575-29-7, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 360575-29-7, in my other articles.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem