- Preparation method of 6-chloro-4-hydroxypyridine-3-carbaldehyde
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The invention provides a preparation method of 6-chloro-4-hydroxypyridine-3-carbaldehyde. The final product, namely, 6-chloro-4-hydroxypyridine-3-carbaldehyde, is obtained through six-step reactions including ring closure, chlorination, etherification, reduction, oxidation and hydrolysis. The synthesis method is simple and easy to operate, a synthesis route is provided for product synthesis, theoretical and experimental bases are provided for industrial production, three wastes polluting the environment are not produced in the synthesis process, and the preparation method is very environment-friendly and suitable for large-scale industrial production. The synthesized product has high purity and yield and the production cost is low.
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Paragraph 0016; 0018; 0024; 0030
(2017/07/19)
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- A Facile Synthesis of New 4,6-Dichloropyridine Derivatives, Their Biological Evaluation for Antimicrobial and Antioxidant Activity, and Docking Studies
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A facile synthesis of new 4,6-dichloropyridine derivatives 5(a–f), 6(a–c), and 7(a–c) were synthesized using both conventional heating and solvent-free microwave irradiation techniques. The results revealed that the latter method is superior to the conventional heating method. The easy work-up of the products, rapid reaction, and mild conditions are noticeable features of this protocol. Structural elucidation of the synthesized compounds was made on the basis of various spectroscopic methods. The synthesized compounds were evaluated for their in vitro antimicrobial activity (minimum inhibitory concentration; MIC) against various microbial strains using the agar well-diffusion method. Among the compounds, 5c showed best antimicrobial activity against most of the employed strains, especially against Staphylococcus aureus, Escherichia coli, Rhizopus arrhizus, and Candida albicans. Compounds 5a, 6a, 6c, 7a, and 7c showed significant antioxidant activity when compared to the other compounds. In addition to this, theoretical docking studies were performed for the highly potent compounds 5a, 6a, 6c, 7a, and 7c against three different drug targets belonging to the oxidoreductase family, and the results were found to be highly satisfactory.
- Singaram, Kulathooran,Marimuthu, Dhamodaran,Baskaran, Selvakumar,Chinaga, Sureshkumar
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p. 758 - 769
(2016/10/04)
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- AZAINDAZOLE COMPOUNDS AS INHIBITORS OF T790M CONTAINING EGFR MUTANTS
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This invention relates to novel compounds of formula (I), which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.
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Page/Page column 40
(2015/01/16)
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- Structure-based design of substituted piperidines as a new class of highly efficacious oral direct renin inhibitors
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A cis-configured 3,5-disubstituted piperidine direct renin inhibitor, (syn,rac)-1, was discovered as a high-throughput screening hit from a target-family tailored library. Optimization of both the prime and the nonprime site residues flanking the central piperidine transition-state surrogate resulted in analogues with improved potency and pharmacokinetic (PK) properties, culminating in the identification of the 4-hydroxy-3,5-substituted piperidine 31. This compound showed high in vitro potency toward human renin with excellent off-target selectivity, 60% oral bioavailability in rat, and dose-dependent blood pressure lowering effects in the double-transgenic rat model.
- Ehara, Takeru,Irie, Osamu,Kosaka, Takatoshi,Kanazawa, Takanori,Breitenstein, Werner,Grosche, Philipp,Ostermann, Nils,Suzuki, Masaki,Kawakami, Shimpei,Konishi, Kazuhide,Hitomi, Yuko,Toyao, Atsushi,Gunji, Hiroki,Cumin, Frederic,Schiering, Nikolaus,Wagner, Trixie,Rigel, Dean F.,Webb, Randy L.,Maibaum, Jurgen,Yokokawa, Fumiaki
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supporting information
p. 787 - 792
(2014/08/05)
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- Diversity-oriented synthesis of 1-substituted 4-aryl-6-oxo-1,6- dihydropyridine-3-carboxamides.
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A simple five-step diversity-oriented synthesis of 1-substituted 4-aryl-6-oxo-1,6-dihydropyridine-3-carboxamides was developed. Treatment of dimethyl 2-((dimethylamino)methylidene)-3-oxopentanedioate with twenty primary amines gave 1-substituted methyl 4-hydroxy-6-oxo-1,6-dihydropyridine-3- carboxylates. Transformation into the corresponding 4-tosyloxy and 4-chloro derivatives, followed by Suzuki-Miyaura arylations gave a series of eleven N-substituted methyl 4-aryl-6-oxo-1,6-dihydropyridine-3-carboxylates. Combinatorial screening was employed to establish suitable reaction conditions for Suzuki-Miyaura arylation of N-alkylpyridones. Hydrolysis of the esters followed by parallel solution-phase amidation of the corresponding carboxylic acids with primary and secondary amines furnished a library of seventeen final products.
- Baskovc, Jernej,Dahmann, Georg,Golobic, Amalija,Groselj, Uros,Kocar, Drago,Stanovnik, Branko,Svete, Jurij
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p. 513 - 519
(2012/10/29)
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- 1,6- AND 1,8-NAPHTHYRIDINES
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Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
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Page/Page column 6; 17
(2012/07/28)
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- TRICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthama, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. (I)
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Page/Page column 98
(2012/09/10)
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- PYRIDINE DERIVATIVES USEFUL AS INHIBITORS OF PKC-THETA
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Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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Page/Page column 12
(2008/06/13)
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- 3-SUBSTITUTED-6-ARYL PYRIDINES
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3-substituted-6-aryl pyridines of Formula (I) are provided: Formula (I) wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula (I) bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
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- Process for preparing 2,4- dihydroxypyridine and 2,4- dihydroxy-3-nitropyridine
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The present invention is directed to a process for preparing 2,4-dihydroxy-pyridine comprising heating a compound of the formula A wherein R is H, alkyl or aralkyl and phosphoric acid where the ratio of phosphoric acid to water is not less than about 27 t
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- Sythesis of Substituted 3-Nitroso-2,4-pyridinediols for Use as Analytical Reagents
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The 5-bromo, 5-iodo, and 5-nitro derivatives of 6-methyl-3-nitroso-2,4-pyridinediol were synthesized and shown to produce colored complexes with a number of Group VIII metal ions.Also synthesized were the 1-pentyl and 1-octyl esters of 4,6-dihydroxy-5-nitrosopyridine-3-carboxylic acid.These compounds showed potential as solvent extraction reagents for certain Group VIII metals.
- Leard, Robert E.,Bedenbaugh, John H.,Bedenbaugh, Angela O.
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p. 1363 - 1366
(2007/10/02)
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