10165-86-3Relevant academic research and scientific papers
Effect of substituent in pyridine-2-carbaldehydes on their heterocyclization to 1,2,4-triazines and 1,2,4-triazine 4-oxides
Krinochkin,Kopchuk,Chepchugov,Kovalev,Zyryanov,Rusinov,Chupakhin
, p. 963 - 970 (2017)
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.
MODULATORS OF THE INTEGRATED STRESS PATHWAY
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Page/Page column 541-542, (2019/05/22)
Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions.
A Simple, Mild and General Oxidation of Alcohols to Aldehydes or Ketones by SO2F2/K2CO3 Using DMSO as Solvent and Oxidant
Zha, Gao-Feng,Fang, Wan-Yin,Leng, Jing,Qin, Hua-Li
supporting information, p. 2262 - 2267 (2019/04/17)
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.).
A class of 2, 3 - dihydronaphth block pyrimidine analogs, its synthetic method, pharmaceutical composition and use thereof
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Paragraph 0234-0236, (2017/07/22)
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.
BTK INHIBITORS
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Page/Page column 70, (2016/07/27)
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.
BTK INHIBITORS
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Page/Page column 68, (2016/08/03)
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.
BTK INHIBITORS
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Page/Page column 126, (2014/08/07)
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.
BTK INHIBITORS
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Paragraph 0782, (2014/08/06)
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.
1H-2,3-Dihydroperimidine derivatives: A new class of potent protein Tyrosine Phosphatase 1B inhibitors
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
, p. 102 - 121 (2014/02/14)
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.
SMALL MOLECULE BRADYKININ B1 RECEPTOR ANTAGONISTS
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Page/Page column 86, (2009/04/25)
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.
