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360575-29-7, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 360575-29-7, name is Methyl 4-bromobenzo[b]thiophene-2-carboxylate, introducing its new discovery.

KINASE INHIBITORS AND METHOD OF TREATING CANCER WITH SAME

The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are a pharmaceutical composition and method of use thereof.

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Benzothiophene – Wikipedia,
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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,
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Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as alpha7 nicotinic acetylcholine receptor agonists

A novel set of azabicyclic aryl amides have been identified as potent and selective agonists of the alpha7 nAChR. A two-pronged approach was taken to improve the potential hERG liability of previously disclosed alpha7 nAChR agonist, PNU-282,987, while maintaining the compound’s other desirable pharmacological properties. The first approach involved further exploration of the aryl carboxylic acid fragment of PNU-282,987, while the second approach focused on modification of the azabicyclic amine portion of PNU-282,987. The best compounds from each series are characterized by rapid brain penetration, good oral bioavailability in rat, and demonstrate in vivo efficacy in a rat P50 auditory sensory gating assay. At least one analog from each series (1h, 1o, 2a, 9a, and 18a) shows an improved hERG safety profile over PNU-282,987.

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Benzothiophene – Wikipedia,
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Synthesis of unprotected carboxy indazoles via Pd-catalyzed carbonylation

The first published synthesis of unprotected carboxy indazoles from the corresponding bromoindazoles is described. This is achieved via Pd(II)-catalyzed carbonylation and is demonstrated to work on a variety of indazoles.

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NOVEL 1H-INDAZOLE COMPOUND

The present invention provides a novel 1H-indazole compound having an excellent JNK inhibitory action. More specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein R1 is a C6-C14 aromatic cyclic hydrocarbon group etc.; R2, R4 and R5 each independently represent a hydrogen atom, a halogen atom, a cyano group etc.; L is a single bond, or a C1-C6 alkylene group etc.; X is a single bond, or a group represented by -CO-NH- or -NH-CO-, etc.; and Y is a C3-C8 cycloalkyl group, a C6-C14 aromatic cyclic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group etc.

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Rational drug design of indazole-based diarylurea derivatives as anticancer agents

A series of novel indazole-based diarylurea derivatives targeting c-kit were designed by structure-based drug design. The derivatives were prepared, and their antiproliferative activities were evaluated against human colon cancer HCT-116 cell line and hepatocellular carcinoma PLC/PRF/5 cell line. The antiproliferative activities demonstrated that six of nine compounds exhibited comparable activities with sorafenib against HCT-116. The structure?activity relationship (SAR) analysis indicated that the indazole ring part tolerated different kinds of substituents, and the N position of the central pyridine ring played key roles in antiproliferative activity. The SAR and interaction mechanisms were further explored using molecular docking method. Compound 1i with N-(2-(pyrrolidin-1-yl)ethyl)-carboxamide possessed improved solubility, 596.1?ng/ml and best activities, IC50 at 1.0?mum against HCT-116, and 3.48?mum against PLC/PRF/5. It is a promising anticancer agent for further development.

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Discovery of inhibitors of the mitotic kinase TTK based on N-(3-(3-sulfamoylphenyl)-1H-indazol-5-yl)-acetamides and carboxamides

TTK kinase was identified by in-house siRNA screen and pursued as a tractable, novel target for cancer treatment. A screening campaign and systematic optimization, supported by computer modeling led to an indazole core with key sulfamoylphenyl and acetamido moieties at positions 3 and 5, respectively, establishing a novel chemical class culminating in identification of 72 (CFI-400936). This potent inhibitor of TTK (IC50 = 3.6 nM) demonstrated good activity in cell based assay and selectivity against a panel of human kinases. A co-complex TTK X-ray crystal structure and results of a xenograft study with TTK inhibitors from this class are described.

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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.

SUBSTITUTED CONDENSED PYRIMIDINE COMPOUNDS

The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.

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Benzothiophene – Wikipedia,
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With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.360575-29-7,Methyl 4-bromobenzo[b]thiophene-2-carboxylate,as a common compound, the synthetic route is as follows.

12113] A mixture of 500 mg of methyl 4-bromobenzo[b] thiophene-2-carboxylate, 161 mg of methylboronic acid,g of potassium phosphate, 151 mg ofa [1,1?-bis(diphe- nylphosphino)ferrocene]palladium (II) dichloride dichloromethane adduct, 6 ml of 1,4-dioxane, and 0.1 ml of waterstirred for 3 hours at 100 C. under a nitrogen atmosphere. Afier being cooled to room temperature, the reaction mixture was concentrated under reduced pressure. Chloroform and water were added to the residues, and insoluble matter was separated by filtration. Tbe filtrate was extracted using chloroform, and the organic layer was washed with saturated saline, dried over magnesium sulfate, and then concentrated under reduced pressure. The residues were subjected to silica gel colunm chromatography, thereby obtaining 340 mg of methyl 4-methylbenzo[b]thiophene-2- carboxylate (hereinafier, described as a ?compound 22 ofpresent invention?).12114] Compound 22 of the Present InventionMe12115] ?H-NMR (CDC13) oe: 8.17-8.16 (m, 1H), 7.71-7.69(m, 1H), 7.37-7.35 (m, 1H), 7.20-7.18 (m, 1H), 3.95 (s, 3H),2.64 (s, 3H)., 360575-29-7

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Reference£º
Patent; SUMITOMO CHEMICAL COMPANY, LIMITED; Mukumoto, Fujio; Tamaki, Hiroaki; Kusaka, Shintaro; Iwakoshi, Mitsuhiko; US2015/282482; (2015); A1;,
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360575-29-7, Methyl 4-bromobenzo[b]thiophene-2-carboxylate is a benzothiophene compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

A mixture of methyl 4-bromobenzo[b]thiophene-2-carboxylate (101 g), sodium hydroxide (63 g), methanol (1200 ml) and water (600 ml) was stirred at ambient temperature for 16 hours, the methanol was removed in vacuo, and the resulting suspension was cooled to 0 C. and acidified by dropwise addition of concentrated hydrochloric acid. The mixture was stirred for 20 minutes and the resulting solid was collected by filtration, washed with water (3*250 ml) and dried in vacuo at 110-120 C. to give 4-bromobenzo[b]thiophene-2-carboxylic acid (62 g) as a cream solid which was used without further purification., 360575-29-7

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Reference£º
Patent; Doyle, Kevin James; Kerrigan, Frank; Watts, John Paul; US2003/166628; (2003); A1;,
Benzothiophene – Wikipedia
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