74290-66-7Relevant academic research and scientific papers
Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors
Barlaam, Bernard,Cosulich, Sabina,Fitzek, Martina,Germain, Hervé,Green, Stephen,Hanson, Lyndsey L.,Harris, Craig S.,Hancox, Urs,Hudson, Kevin,Lambert-van der Brempt, Christine,Lamorlette, Maryannick,Magnien, Fran?oise,Ouvry, Gilles,Page, Ken,Ruston, Linette,Ward, Lara,Delouvrié, Bénédicte
, p. 3030 - 3035 (2017)
We report the discovery of a novel aminopyrazine series of PI3Kα inhibitors, designed by hybridizing two known scaffolds of PI3K inhibitors. We describe the progress achieved from the first compounds plagued with poor general kinase selectivity to compounds showing high selectivity for PI3Kα over PI3Kβ and excellent general kinase selectivity. This effort culminated with the identification of compound 5 displaying high potency and selectivity, and suitable physiochemical and pharmacokinetic properties for oral administration. In vivo, compound 5 showed good inhibition of tumour growth (86% tumour growth inhibition at 50?mg/kg twice daily orally) in the MCF7 xenograft model in mice.
INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF
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Paragraph 00500, (2018/07/05)
The invention provides a class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
Compounds used as JAK inhibitor, and use of compounds
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Paragraph 0357; 0358; 0359; 0340, (2017/08/27)
The invention provides compounds used as a JAK inhibitor, and a use of the compounds, and concretely provides compounds (represented by formula (I)) with JAK inhibition activity or a stereoisomer, a geometric isomer, a tautomer, a racemate, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a medicinal composition including the compounds. The invention also discloses a use of the compounds or the medicinal composition thereof in the preparation of medicines used for treating autoimmune diseases or proliferative diseases.
SYK INHIBITORS
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Paragraph 0280, (2016/02/26)
The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease slates, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk. In certain embodiments, also disclosed are methods for treating a cancer in a subject (e.g., a human) in need thereof, comprising administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof, in combination with a vinca-alkaloid, or a pharmaceutically acceptable salt thereof.
TREATMENT OF CHRONIC GRAFT VERSUS HOST DISEASE WITH SYK INHIBITORS
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Page/Page column 33, (2016/11/17)
The present disclosure provides methods of utilizing Syk inhibiting compounds in the treatment for graft versus host disease (GVHD) in a human, including acute graft versus host disease (aGVHD) and chronic graft versus host disease (cGVHD), including the use of compounds selected from the group consisting of the formulas below: (I) and (II).
SYK INHIBITORS
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Paragraph 0242; 0244, (2015/07/02)
The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
SYK INHIBITORS
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Page/Page column 99, (2015/07/15)
The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.
Novel Heterocyclic Compounds and Uses Thereof
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Paragraph 0391, (2013/08/28)
New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
NOVEL HETEROCYCLIC COMPOUNDS AND USES THEROF
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Page/Page column 118, (2009/10/22)
New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
HETEROARYL COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Page/Page column 101, (2008/12/05)
Provided herein are Heteroaryl Compounds having the following structure: (I) wherein R1, R2, L, X, Y, Z, Q, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
