163209-96-9Relevant academic research and scientific papers
DEGRADATION OF BRUTON'S TYROSINE KINASE (BTK) BY CONJUGATION OF BTK INHIBITORS WITH E3 LIGASE LIGAND AND METHODS OF USE
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Paragraph 0567-0569, (2021/09/17)
Disclosed herein are novel bifunctional compounds formed by conjugating BTK inhibitor moieties with E3 ligase Ligand moieties, which function to recruit targeted proteins to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof.
RET INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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, (2020/07/05)
Provided herein are a RET inhibitor, a pharmaceutical composition thereof and uses thereof. In particular, provided is a compound having Formula (I) or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Provided is a pharmaceutical composition comprising the compound, and uses of the compound and pharmaceutical composition thereof for the preparation of a medicament, in particular for treatment and prevention of RET-related diseases and conditions, including cancer, irritable bowel syndrome, and/or pain associated with irritable bowel syndrome.
Preparation method for synthesizing 1-tert-butyloxycarbonyl -4-(4- carboxyphenyl) piperidine (by machine translation)
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Paragraph 0070-0072, (2020/05/05)
The preparation method 1 - of synthesizing)-tert-butyloxycarbonyl - 4 4 4 4 4-carboxyphenyl, piperidine comprises the following steps: reacting dibromobenzene or iodobromide as raw material, with N - Boc - 4 - piperidone to obtain the target product 2, with intermediate 3, and preparing intermediate 3 by hydrogenation or hydrogenation to obtain the target product through intermediate 4, preparation intermediate 3 and carrying out hydrogenation reaction with the carbon dioxide to obtain the target product, which is, suitable for industrial production 4, in large, scale 5. by using common reagent, raw material cost, and the reaction is carried out with carbon dioxide. (by machine translation)
INHIBITORS OF ACTIVIN RECEPTOR-LIKE KINASE
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Page/Page column 278; 279, (2017/11/10)
Described herein are compounds that inhibit ALK2 and its mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
METALLO-BETA-LACTAMASE INHIBITORS
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Paragraph 0336, (2016/12/01)
The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
METALLO-BETA-LACTAMASE INHIBITORS
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Page/Page column 56, (2017/04/04)
The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF
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Page/Page column 100, (2015/07/07)
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
METALLO-BETA-LACTAMASE INHIBITORS
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Page/Page column 53; 54, (2015/08/06)
The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.
HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS
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Page/Page column 85, (2014/01/18)
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
Imidazopyridine-based fatty acid synthase inhibitors that show anti-HCV activity and in vivo target modulation
Oslob, Johan D.,Johnson, Russell J.,Cai, Haiying,Feng, Shirley Q.,Hu, Lily,Kosaka, Yuko,Lai, Julie,Sivaraja, Mohanram,Tep, Samnang,Yang, Hanbiao,Zaharia, Cristiana A.,Evanchik, Marc J.,McDowell, Robert S.
supporting information, p. 113 - 117 (2013/02/26)
Potent imidazopyridine-based inhibitors of fatty acid synthase (FASN) are described. The compounds are shown to have antiviral (HCV replicon) activities that track with their biochemical activities. The most potent analogue (compound 19) also inhibits rat FASN and inhibits de novo palmitate synthesis in vitro (cell-based) as well as in vivo.
