- SUBSTITUTED 1H-IMIDAZO[1, 2-B]PYRAZOLE-3-CARBOXAMIDE AS BRUTON TYROSINE KINASE INHIBITORS
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This invention relates to a series of compounds 1H-imidazo [1, 2-b] pyrazole-3-carboxamide substituted represented by formula I used as kinase inhibitors, in particular BTK inhibitors (Bruton tyrosine kinase), and the methods of manufacture and use thereof for the treatment of an autoimmune disease, inflammatory disease, cancer and potentially allergies.
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Page/Page column 92-93
(2022/01/24)
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- Nickel-Catalyzed Deaminative Cyanation: Nitriles and One-Carbon Homologation from Alkyl Amines
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A nickel-catalyzed deaminative cyanation of Katritzky pyridinium salts has been developed. When it is coupled with formation of the pyridinium salt from primary amines, this method enables alkyl amines to be converted to alkyl nitriles. A less toxic cyanide reagent, Zn(CN)2, is utilized, and diverse functional groups and heterocycles are tolerated. The method also enables a one-carbon homologation of alkyl amines via reduction of the nitrile products, in addition to many other potential transformations of the versatile nitrile group.
- Xu, Jianyu,Twitty, J. Cameron,Watson, Mary P.
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supporting information
p. 6242 - 6245
(2021/08/23)
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- Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton's tyrosine kinase
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BTK (Bruton's tyrosine kinase) inhibitors are the most promising drugs for the treatment of hematological tumors. A high selectivity of BTK inhibitors ensures reduced side effects from off-targeting. Accordingly, here, based on Zanubrutinib, we designed a
- Ding, Qingjie,He, Xing,Jiang, Yuqin,Li, Wei,Ma, Chunhua,Wang, Yue,Wu, Xiaofang,Xu, Guiqing,Yang, Shouning,Zhang, Dandan,Zhang, Shuting,Zhao, Jie
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supporting information
(2021/08/13)
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- TARGETING COMPOUNDS
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The disclosure provides, at least in part, liver, intestine and/or kidney-targeting compounds and their use in treating liver, intestine and/or kidney disorders, such as non-alcoholic steatohepatitis, alcoholic steatohepatitis, hepatocellular carcinoma, liver cirrhosis, and hepatitis B; and/or chronic kidney disease, glomerular disease such as IGA nephropathy, lupus nephritis, or polycystic kidney disease. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
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Paragraph 0115; 0116
(2019/07/19)
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- INDOLO SUBSTITUTED PIPERIDINE COMPOUND AS ESTROGEN RECEPTOR DEGRADING AGENT
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Disclosed in the present invention is a type of indole substituted piperidine compounds as an estrogen receptor degrading agent. Specifically disclosed are a compound as shown in formula (I), a pharmaceutically acceptable salt, hydrate or prodrug thereof, a preparation method therefor, a pharmaceutical composition thereof, and a use thereof as an estrogen receptor degrading agent in the treatment of estrogen receptor positive breast cancers.
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Paragraph 0041; 0044
(2019/11/19)
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- BENZYL SUBSTITUTED INDAZOLES
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Compounds of formula (I) and their use as pharmaceuticals.
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Page/Page column 254; 255
(2016/04/10)
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