- Effect of substituent in pyridine-2-carbaldehydes on their heterocyclization to 1,2,4-triazines and 1,2,4-triazine 4-oxides
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A series of substituted pyridine-2-carbaldehydes were brought into heterocyclization with isonitrosoacetophenone hydrazones, followed by aromatization by the action of oxidants or by dehydration in boiling acetic acid. As a result, substituted 3-(pyridin-2-yl)-1,2,4-triazines or 3-(pyridin-2-yl)-1,2,4-triazine 4-oxides were formed. 6-Formylpyridine-2-carbonitrile failed to undergo heterocyclization, 6-methylpyridine-2-carbaldehyde and methyl 6-formylpyridine-3-carboxylate can be converted to both 1,2,4-triazine and 1,2,4-triazine 4-oxide derivative, and only 1,2,4-triazine 4 oxides were obtained from 6-bromopyridine-2-carbaldehyde and 6-formyl-3-phenylpyridine-2-carbonitrile. Convenient procedures were proposed for the synthesis of some initial pyridinecarbaldehydes.
- Krinochkin,Kopchuk,Chepchugov,Kovalev,Zyryanov,Rusinov,Chupakhin
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Read Online
- MODULATORS OF THE INTEGRATED STRESS PATHWAY
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Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.
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Page/Page column 541-542
(2019/05/22)
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- A Simple, Mild and General Oxidation of Alcohols to Aldehydes or Ketones by SO2F2/K2CO3 Using DMSO as Solvent and Oxidant
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A practical, general and mild oxidation of primary and secondary alcohols to carbonyl compounds proceeds in yields of up to 99% using SO2F2 as electrophile in DMSO as both the oxidant and the solvent at ambient temperature. No moisture- and oxygen-free conditions are required. Stoichiometric amount of inexpensive K2CO3, which generates easy to separate by-products, is used as the base. Thus, 5-gram scale runs proceeded in nearly quantitative yields by a simple filtration as the work-up. The use of a polar solvent such as DMSO, which usually promotes competing Pummerer rearrangement, is also noteworthy. This protocol is compatible with a variety of common N-, O-, and S-functional groups on (hetero)arene, alkene and alkyne substrates (68 examples). The protocol was applied (99% yield) to a formal synthesis of the important cholesterol-lowering drug Rosuvastatin. (Figure presented.).
- Zha, Gao-Feng,Fang, Wan-Yin,Leng, Jing,Qin, Hua-Li
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supporting information
p. 2262 - 2267
(2019/04/17)
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- A class of 2, 3 - dihydronaphth block pyrimidine analogs, its synthetic method, pharmaceutical composition and use thereof
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The invention belongs to the technical field of medicines and relates to a 2,3-dihydronaphthalene-embedded m-diazabenzene analogue represented as the following general formula I and a preparation method thereof. The 2,3-dihydronaphthalene-embedded m-diazabenzene analogue has a function of inhibiting biological activities of different subtypes of a protein-tyrosine-phosphatase family (PTPases), can be used as a tool compound for researching a biological function correlation of the subtypes of the protein-tyrosine-phosphatase family (PTPases) in a cell signal transduction process, and provides a new approach for preventing and treating cancer, metabolic and immunological diseases, angiocardiopathy and neurological diseases.
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Paragraph 0234-0236
(2017/07/22)
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- BTK INHIBITORS
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Provided are Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
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Page/Page column 70
(2016/07/27)
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- BTK INHIBITORS
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The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
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Page/Page column 68
(2016/08/03)
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- BTK INHIBITORS
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The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
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Page/Page column 126
(2014/08/07)
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- BTK INHIBITORS
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The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
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Paragraph 0782
(2014/08/06)
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- 1H-2,3-Dihydroperimidine derivatives: A new class of potent protein Tyrosine Phosphatase 1B inhibitors
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A series of 1H-2,3-dihydroperimidine derivatives was designed, synthesized, and evaluated as a new class of inhibitors of protein tyrosine phosphatase 1B (PTP1B) with IC50 values in the micromolar range. Compounds 46 and 49 showed submicromolar inhibitory activity against PTP1B, and good selectivity (3.48-fold and 2.10-fold respectively) over T-cell protein tyrosine phosphatases (TCPTP). These results have provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.
- Wang, Wen-Long,Yang, Dong-Lin,Gao, Li-Xin,Tang, Chun-Lan,Ma, Wei-Ping,Ye, Hui-Hua,Zhang, Si-Qi,Zhao, Ya-Nan,Xu, Hao-Jie,Hu, Zhao,Chen, Xia,Fan, Wen-Hua,Chen, Hai-Jun,Li, Jing-Ya,Nan, Fa-Jun,Li, Jia,Feng, Bainian
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p. 102 - 121
(2014/02/14)
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- SMALL MOLECULE BRADYKININ B1 RECEPTOR ANTAGONISTS
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Disclosed are compounds of formula (I) which are bradykinin B1 receptor (B1R) antagonists. These compounds are useful to treat diseases or relieve adverse symptoms associated with inflammation and pain. The invention encompasses novel compounds and acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases involving inflammation and pain.
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Page/Page column 86
(2009/04/25)
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- Facile synthesis of 6-aryl-3-pyridyl-1,2,4-triazines as a key step toward highly fluorescent 5-substituted bipyridines and their Zn(II) and Ru(II) complexes
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A wide series of substituted bipyridines were obtained through the synthesis of 1,2,4-triazines and their aza Diels-Alder reactions. The reported method facilitates the synthesis of functionally diverse bipyridines that provides fine-tuning of photophysical properties of new ligands and their Zn(II) and Ru(II) complexes. Some of substituted bipyridines exhibit 'off-on' fluorescence response toward Zn2+ cations.
- Kozhevnikov, Valery N.,Shabunina, Olga V.,Kopchuk, Dmitry S.,Ustinova, Maria M.,K?nig, Burkhard,Kozhevnikov, Dmitry N.
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p. 8963 - 8973
(2008/12/22)
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- 5-Aryl-2,2′-bipyridines as tunable fluorophores
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Readily available 5-aryl-2,2′-bipyridines and their derivatives are a unique family of fine-tunable chromophores, where changes in the substitution patterns, solvation and coordination are translated into dramatic spectral changes. They exhibit sensitive and selective response to zinc ions with dramatic increases in emission intensity or significant red-shifts of emission maxima.
- Kozhevnikov, Dmitry N.,Shabunina, Olga V.,Kopchuk, Dmitry S.,Slepukhin, Pavel A.,Kozhevnikov, Valery N.
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p. 7025 - 7029
(2007/10/03)
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