- Trifluoromethylation reaction on dimethyl substituted heterocyclic compound
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The invention relates to a method for introducing a trifluoromethyl group through a trifluoromethylation reaction. A trifluoromethylation reagent used in the method is a Umemoto reagent, and a substrate is a wide dimethyl substituent-containing compound. The method has the advantages that the universality of the substrate is reflected, the reaction sites of the substrate acted by the Umemoto reagent in the past are always on the ring, and the site of the trifluoromethylation action is carbon on the dimethyl chain, which is a leap and breakthrough in the richness selection of the substrate andthe trifluoromethylation reaction.
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Paragraph 0044-0061
(2020/12/14)
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- PI3K INHIBITORS AND USES THEREOF
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The development of a new, targeted drug delivery paradigm coupled to improved PI3K inhibitors (e.g., PI3Kα inhibitors) represents a significant advance in cancer therapy. Provided herein are compounds, such as compounds of Formula (I) and (II), and pharmaceutically acceptable salts, hydrates, solvates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. The compounds provided herein are PI3K (e.g., PI3Kα) inhibitors and are therefore useful for the treatment and/or prevention of various diseases (e.g., proliferative diseases such as cancer). Also provided herein are nanoparticles and nanogels (e.g., P-selectin targeting nanoparticles) comprising PI3K inhibitors, such a compound described herein. In certain embodiments, a nanoparticle or nanogel described herein encapsulates a compound described herein for targeting delivery to cancer cells or tumors.
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- Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation
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Phosphatidylinositol-3-kinase α (PI3Kα) is a therapeutic target of high interest in anticancer drug research. On the basis of a binding model rationalizing the high selectivity and potency of a particular series of 2-aminothiazole compounds in inhibiting PI3Kα, a medicinal chemistry program has led to the discovery of the clinical candidate NVP-BYL719.
- Furet, Pascal,Guagnano, Vito,Fairhurst, Robin A.,Imbach-Weese, Patricia,Bruce, Ian,Knapp, Mark,Fritsch, Christine,Blasco, Francesca,Blanz, Joachim,Aichholz, Reiner,Hamon, Jacques,Fabbro, Doriano,Caravatti, Giorgio
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p. 3741 - 3748
(2013/07/27)
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- A CRYSTALLINE FORM OF (S)-PYRROLIDINE-1,2-DICARBOXYLIC ACID 2-AMIDE 1-(4 -METHYL-5-[2-(2,2,2-TRIFLUORO-1,1-DIMETHYL-ETHYL)-PYRIDIN-4-YL]-THIAZOL-2-YL)-AMIDE AND ITS USE AS PI3K INHIBITOR
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The present invention relates to specific solid forms of (S)-pyrrolidine-l,2-dicarboxylic acid 2-amide l-(4-methyI-5-[2-(2,2,2-trifluoro-l,l-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl)-amide, (I), and its hydrates and solvates. The present invention further relates to processes for preparing said solid forms, pharmaceutical compositions comprising said solid forms, and methods of using said solid forms and pharmaceutical compositions to treat disease.
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Page/Page column 33=34
(2012/02/15)
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- POLYMORPHS OF (S)-PYRROLIDINE-1,2-DICARBOXYLIC ACID 2-AMIDE 1-({4-METHYL-5-[2-(2,2,2-TRIFLUORO-1,1-DIMETHYL-ETHYL)-PYRIDIN-4-YL]-THIAZOL-2-YL}-AMIDE
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The present invention relates to specific solid forms of (S)-pyrrolidine-1,2- dicarboxylic acid 2-amide l-(4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4- yl]-thiazol-2-yl)-amide, and its solvates. The present invention further relates to processes for preparing said solid forms, pharmaceutical compositions comprising said solid forms, and methods of using said solid forms and pharmaceutical compositions to treat disease.
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Page/Page column 27
(2013/02/28)
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