216257-25-9Relevant articles and documents
2-(2-ACRYLOYL-2,6-DIAZASPIRO[3.4]OCTAN-6-YL)-6-(1H-INDAZOL-4-YL)-BENZONITRILE DERIVATIVES AND RELATED COMPOUNDS AS INHIBITORS OF G12C MUTANT KRAS PROTEIN FOR INHIBITING TUMOR METASTASIS
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Page/Page column 137; 138, (2020/05/28)
The present invention provides e.g. 2-(2-acryloyl-2,6- diazaspiro[3.4]octan-6-yl)-6-(lH-indazol-4-yl)-benzonitrile and e.g. 2-(2-acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-6-(1H-indazol-4-yl)- benzonitrile derivatives and related compounds of formula (I) as inhibitors of G12C mutant KRAS protein for treating tumor metastasis. The present description discloses exemplary compounds (e.g. pages 53 to 90; table 1; compounds I-1 to I-141), pharmacological data (e.g. page 125 to 128; table 2; example 1) and synthesis thereof (e.g. pages 129 to 143; examples 2 to 7). Exemplary compounds are e.g. 2-(2-acryloyl-2,6- diazaspiro[3.4]octan-6-yl)-6-(5-methyl-1H-indazol-4-yl)-4- morpholinobenzonitrile (example 2; compound I-1) and 6-(2- acryloyl-2,7-diazaspiro[3.5]nonan-7-yl)-3-methoxy-2-(5-methyl-1H- indazol-4-yl)-4-morpholinobenzonitrile (example 7; compound I-84).
DERIVATIVES OF SOBETIROME
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Page/Page column 39; 40, (2019/09/04)
Compounds are provided that function as thyromimetics, which compounds have utility for treating diseases such as neurodegenerative disorders. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation. Such compounds have the structure of Formula (I) as shown herein, or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof.
INTEGRIN ANTAGONIST CONJUGATES FOR TARGETED DELIVERY TO CELLS EXPRESSING VLA-4
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Page/Page column 75, (2013/08/15)
The invention relates to compounds of formula I: wherein R1, R2, and n are defined in the detailed description and claims. In particular, the present invention relates to the compounds of formula I for use in the manufacture and delivery of conjugated moieties such as small molecules, peptides, nucleic acids, fluorescent moieties, and polymers which are linked to VLA-4 integrin antagonists to target cells expressing VLA-4.