101010-74-6Relevant articles and documents
Aryl imidazole derivative and application thereof
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Paragraph 0286-0289, (2021/06/23)
The invention relates to an aryl imidazole derivative and application thereof. The aryl imidazole derivative is a compound shown as a formula (I) in the description or pharmaceutically acceptable salt thereof. The invention also discloses application of the aryl imidazole derivative in preparation of drugs for treating cancers. The invention further discloses application of the aryl imidazole derivative in preparation of drugs for treating diseases caused by EGFR mutation.
CRYSTAL OF COMPOUND HAVING JAK-INHIBITING ACTIVITY
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Paragraph 0173, (2019/02/24)
An object of the present invention is to provide a compound with an excellent JAK1 inhibitory activity. The compound of the invention has JAK1 inhibitory activity, and thus, immunosuppressive effect, anti-inflammatory effect, anti-proliferative effect and so on, and is useful in the treatment of the diseases, for example, rheumatoid arthritis, inflammatory bowel disease, psoriasis, vasculitis, bronchial asthma, chronic obstructive pulmonary disease, eosinophilic sinusitis and nasal polyp.
INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF
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Paragraph 00542, (2018/07/05)
The invention provides a class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
PYRAZOLOTHIAZOLE COMPOUND AND MEDICINE
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Paragraph 0119, (2017/07/31)
The invention provides a pyrazolothiazole compound of the formula [I], or a pharmaceutically acceptable salt thereof: The compound of the invention has JAK1 inhibitory activity, and thus, immunosuppressive effect, anti-inflammatory effect and anti-proliferative effect, and is useful in the treatment of the diseases, for example, rheumatoid arthritis, inflammatory bowel disease, psoriasis and vasculitis, bronchial asthma, chronic obstructive pulmonary disease and eosinophilic sinusitis, nasal polyp.
HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Paragraph 0174 - 0175, (2014/05/24)
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.
Discovery of novel quinolinone adenosine A2B antagonists
McGuinness, Brian F.,Ho, Koc-Kan,Stauffer, Tara M.,Rokosz, Laura L.,Mannava, Neelima,Kultgen, Steven G.,Saionz, Kurt,Klon, Anthony,Chen, Weiqing,Desai, Hema,Rogers, W. Lynn,Webb, Maria,Yin, Juxing,Jiang, Yan,Li, Tailong,Yan, Hao,Jing, Konghua,Zhang, Shengting,Majumdar, Kanak Kanti,Srivastava, Vikash,Saha, Samiran
scheme or table, p. 7414 - 7420 (2011/02/23)
A novel series of quinolinone-based adenosine A2B receptor antagonists was identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogs highlighted essential structural features of the initial hit. Optimization resulted in an A2B antagonist (2i) which exhibited potent activity in a cAMP accumulation assay (5.1 nM) and an IL-8 release assay (0.4 nM).
Reactions of 2-Halothiazoles with Ketone Enolates and Nitrile Carbanions
Dillender, Samuel C.,Greenwood, Thomas D.,Hendi, Mukta S.,Wolfe, James F.
, p. 1184 - 1188 (2007/10/02)
Photostimulated reactions of 2-chlorothiazole (1a), 2-chloro-4-methylthiazole (1b), and 2-chloro-5-methylthiazole (1c) with pinacolone potassium enolate (2a) in liquid NH3 lead to formation of mono- and bis-2-thiazolyl ketones 3a-c and 4a-c via the SRN1 mechanism.A similar reaction with 2-bromothiazole (1d) gave 3a but no 4a.Reaction of 1a with 2a in the dark, or with the potassium enolate of diisopropyl ketone (2b) under near-UV irradiation or in the dark, does not result in chloride displacement.Instead, carbinols 5a-b, derived from initial ionization of H5 of 1a followed by aldol-type condensation of the resulting carbanion (11) with neutral ketone, are produced in good yields.Carbanion 11 can also be produced in synthetically useful concentrations by metalation of 1a with KNH2, n-BuLi, and LDA, with the latter base being most effective.Carbanions derived from acetonitrile, propionitrile, and phenylacetonitrile react smoothly with 1a in liquid NH3 to give the corresponding monosubstitution products resulting from chloride displacement.However, these reactions appear to proceed by an addition-elimination (SNAr) mechanism rather than an SRN1 process.