1357476-69-7Relevant articles and documents
PI3K INHIBITORS AND USES THEREOF
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Paragraph 00430; 00438, (2020/05/15)
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.
Preparation process of Alpelisib
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Paragraph 0065-0066, (2020/04/17)
The invention relates to a preparation process of Alpelisib. The preparation process has the advantages of few reaction steps, simple process, mild reaction conditions, no extreme low-temperature reaction, simple purifying and low overall reaction difficulty, and is suitable for large-scale production.
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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Page/Page column 33=34, (2012/02/15)
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.