- Preparation method of alpelisib
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The invention provides a preparation method of alpelisib. 2-pyrrole methyl formate and N, N-carbonyldiimidazole which are used as raw materials are subjected to an amidation reaction, a suzuki reaction and an aminolysis reaction to obtain the compound apenelisib shown in the formula I. The method is mild in reaction condition, simple and convenient in treatment, environment-friendly, low in cost and suitable for industrial mass production.
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- Producing Method for 4,4′-oxydianiline from nitrochlorobenzene and nitrophenolate salt
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The present invention relates to a method for manufacturing 4,4′-oxydianiline, including: a first step of obtaining a reactant including dinitrodiphenyl ether by mixing and inducing a reaction of nitrochlorobenzene and a nitrophenolate salt under a hydrotalcite catalyst in which an organic acid is intercalated; a second step of obtaining a reaction product by hydrogenating the reactant including dinitrodiphenyl ether. The present invention proposes a novel manufacturing method related to mass production of 4,4′-oxydianiline as a raw material for polyimides, a high yield of dinitrodiphenyl ether as a raw material for 4,4′-oxydianiline, and the like.
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Paragraph 0034-0035
(2020/11/10)
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- Preparation method of alpelisib
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The invention discloses a preparation method of alpelisib (alpelisib). The preparation method comprises sequentially subjecting S-prolinamide as a raw material to acylation reaction, thiourea reaction, bromination cyclization and other basic unit reactions to obtain alpelisib. The preparation method has the advantages of easily available raw materials, simple process, economical property, environmental protection and suitability for industrial production.
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Paragraph 0034-0035
(2020/10/14)
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- Preparation process of Alpelisib
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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.
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- Novel synthesis method of PI3K inhibitor Alpelisib
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The invention relates to a novel synthesis method of a PI3K inhibitor Alpelisib. According to the synthesis method disclosed by the invention, the target molecule can be synthesized through four stepsof reactions including one-step substitution reaction of starting raw materials, amino protection group removal and two times of halogenation reaction, the total yield is high, the cost is low, and the HPLC purity of the product reaches 99.5% or above.
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Paragraph 0079-0089
(2020/05/05)
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- PHARMACEUTICAL COMBINATION COMPRISING THE PI3K INHIBITOR ALPELISIB AND THE B-RAF INHIBITOR DABRAFENIB; THE USE OF SUCH COMBINATION IN THE TREATMENT OR PREVENTION OF CANCER
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The present disclosure pertains to a pharmaceutical combination comprising (a) alpha- isoform specific PI3K inhibitor and (b) a B-RAF inhibitor; combined preparations and pharmaceutical compositions thereof; the uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.
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Page/Page column 23; 27
(2017/03/21)
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- A PHARMACEUTICAL COMBINATION COMPRISING THE PI3K INHIBITOR ALPELISIB AND THE CDK4/6 INHIBITOR RIBOCICLIB, AND THE USE THEREOF IN THE TREATMENT/PREVENTION OF CANCER
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The present disclosure pertains to a pharmaceutical combination comprising (a) an alpha- isoform specific PI3K inhibitor, (b) a cyclin dependent kinase 4/6 (CDK4/6) inhibitor, and (c) an antimetabolite antineoplastic agent; combined preparations and pharmaceutical compositions thereof; the uses of such a combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject comprising administering a therapeutically effective amount of such combination.
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Page/Page column 24; 25; 28; 29
(2017/03/28)
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- COMBINATION THERAPY
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The present disclosure pertains to a pharmaceutical combination comprising (a) alpha- isoform specific PI3K inhibitor and (b) an AKT inhibitor; combined preparations and pharmaceutical compositions thereof; the uses of such combination in the treatment or prevention of cancer; and methods of treating or preventing cancer in a subject in need thereof comprising administering a therapeutically effective amount of such combination. 43
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Page/Page column 24-25; 28
(2017/03/21)
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- COMBINATION THERAPY
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The present invention relates to a pharmaceutical combination comprising an alpha-isoform specific phosphatidylinositol 3-kinase inhibitor compound, such as (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), or pharmaceutically acceptable salt thereof, and an IGF1R inhibitor (e.g., the IGF1R inhibitor ANTIBODY A, or a variant or derivative thereof), a pharmaceutical composition comprising such combination, methods for treating cancer comprising administration of therapeutically effective amounts of such inhibitors to a subject in need thereof, and uses of such combination for the treatment of cancer.
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Paragraph 0120; 0121; 0136; 0137; 0138; 0139
(2014/02/16)
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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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- SYNTHESIS OF 2-CARBOXAMIDE CYCLOAMINO UREA DERIVATIVES
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Provided herein are processes and intermediate compounds useful for the preparation of 2-carboxamide cycloamino urea derivatives of formula (X), and useful intermediates therefore.
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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 27-28
(2013/02/28)
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- ORGANIC COMPOUNDS
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The present invention relates to a compound of formula (I) (I) or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.
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Page/Page column 55-56
(2010/04/06)
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