- Development of a Robust Synthesis of Dactolisib on a Commercial Manufacturing Scale
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The development of the robust synthesis of 2-methyl-2-[4-[3-methyl-2-oxo-8-(quinolin-3-yl)-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl]-phenyl]propionitrile (dactolisib) on a commercial scale is described. The key step is a Pd-catalyzed Suzuki coupling of 2-[4-(8-bromo-3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinolin-1-yl)-phenyl]-2-methyl-propionitrile to 3-quinoline boronic acid. A special focus is placed on reducing the amount of Pd catalyst used in the Suzuki coupling and purifying the crude drug substance, including removing traces of Pd.
- Baenziger, Markus,Pachinger, Werner,Stauffer, Frédéric,Zaugg, Werner
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p. 1908 - 1917
(2019/09/30)
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- Acid-Promoted Cascade Reaction of N-(4-Chloroquinolin-3-yl)carbamates with Amines: One-Pot Assembly of Imidazo[4,5-c]quinolin-2-ones
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An acid-promoted cascade reaction of N-(4-chloroquinolin-3-yl)carbamates with amines is described. This method achieves the formation of two new C–N bonds through an intermolecular amination/intramolecular cyclization reaction sequence. In combination wit
- Lu, Xiao,Kim, Myunghoon,Orr, Meghan J.,Li, Hao,Huang, Wenwei
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p. 1572 - 1580
(2018/04/20)
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- COMPOUNDS AND METHOD FOR BLOCKING TRANSMISSION OF MALARIAL PARASITE
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Disclosed are compounds of formula (I) and formula (II): (I) (II) wherein R1, R2, A, and B are as defined herein. Also disclosed is a method of blocking transmission of a Plasmodium parasite and a method of treating or preventing mal
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- JAK PI3K/mTOR combination therapy
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Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.
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- JAK P13K/mTOR COMBINATION THERAPY
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Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PBK/mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.
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- SALTS AND CRYSTALL FORMS OF 2-METHYL-2-[4-(3-METHYL-2-OXO-8-QUINOLIN-3-YL-2,3-DIHYDRO-IMIDAZO[4,5-C]QUINOLIN-1-YL)-PHENYL]-PROPIONITRILE
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The invention relates to particular crystalline forms of 2-methyl-2-[4-(3-methyl-2-oxo-8-quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile, its hydrates and solvates, its salts and hydrates and solvates of its salts, certain processes for their preparation, pharmaceutical compositions containing these crystalline forms, and their use in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans.
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Page/Page column 15-16
(2008/12/05)
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- IMIDAZOQUINOLINES AS LIPID KINASE INHIBITORS
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The invention relates to novel organic compounds of formula (I) processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment of an inflammatory or obstructive airway disease, such as asthma, disorders commonly occurring in connection with transplantation, or a proliferative disease, such as a tumor disease.
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Page/Page column 51-52
(2008/06/13)
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