- COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.
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Page/Page column 115-116; 141-142; 197; 203
(2020/07/06)
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- Discovery of 1,4-Benzodiazepine-2,5-dione (BZD) Derivatives as Dual Nucleotide Binding Oligomerization Domain Containing 1/2 (NOD1/NOD2) Antagonists Sensitizing Paclitaxel (PTX) to Suppress Lewis Lung Carcinoma (LLC) Growth in Vivo
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Nucleotide-binding oligomerization domain-like receptors (NLRs) are intracellular sensors of pathogen-Associated molecular patterns (PAMPs) and damage-Associated molecular patterns (DAMPs). Previously, we reported nucleotide-binding oligomerization domain-containing protein 1 (NOD1) antagonists (11, 12) and a NOD2 antagonist (9) that sensitized docetaxel (DTX) or paclitaxel (PTX) treatment for breast or lung cancer. In this article, we describe for the first time a 1,4-benzodiazepine-2,5-dione (BZD) derivative (26bh) that acts as a dual NOD1/NOD2 antagonist and inhibits both nuclear factor B (NF-B) and mitogen-Activated protein kinase (MAPK) inflammatory signaling, thereby sensitizing PTX to suppress Lewis lung carcinoma (LLC) growth. After investigation of the compound's cytotoxicity, a systematic structure-Activity relationship (SAR) was completed and revealed several key factors that were necessary to maintain antagonistic ability. This study establishes the possibility for using adjuvant treatment to combat cancer by antagonizing both NOD1 and NOD2 signaling.
- Wang, Suhua,Yang, Jingshu,Li, Xueyuan,Liu, Zijie,Wu, Youzhen,Si, Guangxu,Tao, Yiran,Zhao, Nan,Hu, Xiao,Ma, Yao,Liu, Gang
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supporting information
p. 5162 - 5192
(2017/06/28)
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- Substituted benzodiazepine ring compound and preparation method and application thereof
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The invention discloses a substituted benzodiazepine ring compound and a preparation method and application thereof and further relates to a pharmaceutical composition and application of the compound. According to the substituted benzodiazepine ring compound, the effect of preventing or treating an immune inflammatory disease or tumor is achieved through activation of a selectively antagonistic or collaboratively excited NOD1/2 signal transduction pathway; the substituted benzodiazepine ring compound has a polypeptidase stability and is not degraded by polypeptidase in the organism.
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Paragraph 0481-0483
(2017/07/22)
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- SUBSTITUTED TRICYCLIC COMPOUNDS AND METHODS OF USE THEREOF
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This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of disorders, particularly cancer.
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Page/Page column 94-95
(2009/04/25)
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- NEW SUBSTITUTED ARYLSULPHONYLGLYCINES, THE PREPARATION THEREOF AND THE USE THEREOF AS PHARMACEUTICAL COMPOSITIONS
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The present invention relates to substituted arylsulphonylglycines 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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- A convenient method of meta-directing nitration of 3-substituted phenol by lanthanide (III) nitrates
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Thirteen compounds of 3-substituted phenols were nitrated by lanthanide(III) nitrates in a solution of ethyl acetate. Whether the substituents were ortho-, para-directing groups or meta-directing groups, only one kind nitrated product, 3-substituted-5-nitropenol, and its intermediate were obtained respectively.
- Gu, Shangxiang,Jing, Huanwang,Wu, Jigui,Liang, Yongmin
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p. 2793 - 2797
(2007/10/03)
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