60964-09-2Relevant 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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, (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).
NOVEL THYROMIMETICS
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, (2020/09/19)
Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, X1, X2, Q, R1, R2 and n are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
DERIVATIVES OF SOBETIROME
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, (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.
DERIVATIVES OF SOBETIROME
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, (2017/12/15)
Disclosed are halo substituted derivative compounds of sobetirome with improved pharmacological characteristics relative to sobetirome, pharmaceutical compositions that include those compounds and methods of treating diseases such as neurodegenerative dis
Increasing Thyromimetic Potency through Halogen Substitution
Devereaux, Jordan,Ferrara, Skylar J.,Banerji, Tania,Placzek, Andrew T.,Scanlan, Thomas S.
, p. 2459 - 2465 (2016/11/13)
Sobetirome is one of the most studied thyroid hormone receptor β (TRβ)-selective thyromimetics in the field due to its excellent selectivity and potency. A small structural change—replacing the 3,5-dimethyl groups of sobetirome with either chlorine or bro
CYCLOHEXYLPYRAZOLE-LACTAM DERIVATIVES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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, (2009/05/29)
The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compound
OXADIAZOLE- AND OXAZOLE-SUBSTITUTED BENZIMIDAZOLE- AND INDOLE-DERIVATIVES AS DGAT1 INHIBITORS
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Page/Page column 100, (2009/05/29)
The present invention provides oxadiazolyl- substituted benzimidazole- and idole-derivates that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.
TETRACYCLIC INHIBITORS OF JANUS KINASES
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Page/Page column 106-107, (2008/06/13)
The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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Page/Page column 38-39, (2008/06/13)
The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
PIERIDINYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1
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Page/Page column 41, (2008/06/13)
ABSTRACT The present invention discloses novel compounds of Formula I: ( I ) having 11-Beta-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11-Beta-HSD type 1 activity. X-17433 PCT -1-