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SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS

The present invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 5676-60-8, help many people in the next few years.HPLC of Formula: C8H8N2O

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Palladium-catalyzed cross-coupling reaction of azides with isocyanides

An efficient palladium-catalyzed cross-coupling reaction of azides with isocyanides is developed, providing a general synthetic route to unsymmetric carbodiimides with excellent yields. This method shows a broad substrate scope, including not only aryl azides, but also unactivated benzyl and alkyl azides. Furthermore, from readily available substrates, Pd-catalyzed coupling with a tandem amine insertion cascade to obtain unsymmetric trisubstituted guanidines has been achieved in a one-pot fashion.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1

6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the discovery of 6-(4-fluorophenyl)-2-methyl-N-(2-methylbenzothiazol-5-yl)nicotinamide (32; SB-782443) which possesses an excellent overall profile and has been progressed into pre-clinical development.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Design, synthesis and biological evaluation of novel Pseudomonas aeruginosa DNA gyrase B inhibitors

In the present study, we attempted to develop a novel class of compounds active against Pseudomonas aeruginosa (Pa) by exploring the pharmaceutically well exploited enzyme targets. Since, lack of Pa gyrase B crystal structures, Thermus thermophilus gyrase B in complex with novobiocin (1KIJ) was used as template to generate model structure by performing homology modeling. Further the best model was validated and used for high-throughput virtual screening, docking and dynamics simulations using the in-house database for identification of Pa DNA gyrase B inhibitors. This study led to an identification of three lead molecules with IC50 values in range of 6.25?15.6 muM against Pa gyrase supercoiling assay. Lead-1 optimization and expansion resulted in 15 compounds. Among the synthesized compounds six compounds were shown good enzyme inhibition than Lead-1 (IC50 6.25 muM). Compound 13 emerged as the most potential compound exhibiting inhibition of Pa gyrase supercoiling with an IC50 of 2.2 muM; and in-vitro Pa activity with MIC of 8 mug/mL in presence of efflux pump inhibitor; hence could be further developed as novel inhibitor for Pa gyrase B.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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METHOD FOR THE PREPARATION OF FUSED HETEROCYCLIC SUCCINIMIDE COMPOUNDS AND ANALOGS THEREOF

Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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5676-60-8, Chemistry is traditionally divided into organic and inorganic chemistry. The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 5676-60-8

SUBSTITUTED IMIDAZO[1,5-A]PYRIMIDINES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS

The invention provides substituted imidazo[1,5-a]pyrimidines and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson’s disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted imidazo[1,5-a]pyrimidine compounds described herein include substituted 2,4-dimethyl-N-phenylimidazo[1,5-a]pyrimidine-8-carboxamide compounds and variants thereof.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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SUBSTITUTED PYRAZOLO(1,5-A)PYRIMIDINES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS

The invention provides substituted pyrazolo[l,5-a]pyrimidine and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson’s disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[l,5-a]pyrimidine compounds described herein include 5,7- dimethyl-N-phenylpyrazolo[l,5-a]pyrimidine-3-carboxamide compounds and variants thereof.

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Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

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Name is 2-Methylbenzo[d]oxazol-6-amine, as a common heterocyclic compound, it belongs to benzoxazole compound, and cas is 5676-60-8, its synthesis route is as follows.,5676-60-8

EXAMPLE 29- PREPARATION OF N-(2-METHYL-1,3-BENZODIOXOL-6-YL)-2,4- DIMETHYLIMIDAZO[1,5-a]PYRIMIDINE-8-CARBOXAMIDE To a stirred solution of 2,4-dimethylimidazo[1,5-a]pyrimidine-8-carboxylic acid 3 (50 mg, 0.262 mmol), 2-methyl-1,3-benzoxazol-6-amine (47 mg, 0.314 mmol) and HATU (149 g, 0.393 mmol) in DMF (1 mL) was added DIPEA (0.1 mL, 0.524 mmol), and the reaction mixture was stirred at room temperature for 16 hours until the reaction was complete. The suspension was diluted with H2O (3 mL), and the precipitated solid was collected by filtration, washed with minimum DCM and Et2O, and dried in vacuo to give the title compound (57 mg, 68%) as a white solid.1H NMR (400 MHz, DMSO-d6) delta 10.39 (s, 1H), 8.48 (s, 1H), 8.36 (s, 1H), 7.60 (s, 2H), 6.90 (d, J = 1.2 Hz, 1H), 2.71 (s, 3H), 2.61 (s, 3H), 2.60 (s, 3H). ES-MS m/z: 322.0 [M+H]+. HPLC Purity (214 nm): >98%; tR = 8.17 min.

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Reference£º
Patent; LYSOSOMAL THERAPEUTICS INC.; SKERLJ, Renato, T.; LANSBURY, Peter, T.; GOOD, Andrew, C.; BOURQUE, Elyse Marie, Josee; (134 pag.)WO2016/73889; (2016); A1;,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

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As a common heterocyclic compound, it belongs to quinuclidine compound,Quinuclidine-4-carboxylic acid hydrochloride,40117-63-3,Molecular formula: C8H14ClNO338,mainly used in chemical industry, its synthesis route is as follows.,5676-60-8

General procedure: To a solution of compound 3 (3.37 mmol) in DMF (10 mL), charged respective compound V (a-p) (4.04 mmol) and heated to 80 C. After3 h, TLC analysis showed complete conversion of starting materials. The reaction mixture was cooled to room temperature, charged water (30 mL) and extracted with EtOAc (2 ¡Á 20 mL). The combined organic layer was washed with water (20 mL) followed by brine and concentrated under reduced pressure to obtain gummy liquid. This crude material was triturated with MTBE to afford desired product as solid and which used as such in next step without any further purification.

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Reference£º
Article; Balraju, Vadla; Jogula, Sridhar; Krishna, Vagolu Siva; Meda, Nikhila; Sriram, Dharmarajan; Bioorganic Chemistry; vol. 100; (2020);,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem

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2-Methylbenzo[d]oxazol-6-amine, cas is 5676-60-8, it is a common heterocyclic compound, the benzoxazole compound, its synthesis route is as follows.,5676-60-8

General procedure: To a solution of compound 3 (3.37 mmol) in DMF (10 mL), charged respective compound V (a-p) (4.04 mmol) and heated to 80 C. After3 h, TLC analysis showed complete conversion of starting materials. The reaction mixture was cooled to room temperature, charged water (30 mL) and extracted with EtOAc (2 ¡Á 20 mL). The combined organic layer was washed with water (20 mL) followed by brine and concentrated under reduced pressure to obtain gummy liquid. This crude material was triturated with MTBE to afford desired product as solid and which used as such in next step without any further purification.

With the rapid development of chemical substances, we look forward to future research findings about 2-Methylbenzo[d]oxazol-6-amine

Reference£º
Article; Balraju, Vadla; Jogula, Sridhar; Krishna, Vagolu Siva; Meda, Nikhila; Sriram, Dharmarajan; Bioorganic Chemistry; vol. 100; (2020);,
Benzoxazole – Wikipedia
Benzoxazole | C7H5NO – PubChem