- Preparation method capable of acalabrutinib being used for treating leukemia
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The invention relates to a preparation method of acalabrutinib capable of being used for treating leukemia. The synthesis method of the compound 3 is optimized, so that according to the method, the cyano compound 2 is reduced to obtain the compound 3 by adopting a method of generating borane in situ under the conditions of indium trichloride and sodium borohydride. The method is simple and convenient to operate, a special reaction container and hydrogen are not needed for reduction, a high-risk catalyst nickel is prevented from being adopted, and large-scale production is facilitated; in the preparation of the compound 8, under the condition of a catalyst, large-scale preparation is realized by adding an ammonia water closed system, so that a method of introducing ammonia gas at an extremely low temperature is avoided, and large-scale production is facilitated.
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Paragraph 0029-0032
(2020/07/24)
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- IMIDAZOPYRIDINAMINE PHENYL DERIVATIVE AND USE THEREOF
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The present invention relates to imidazopyridinamine phenyl derivatives, pharmaceutically acceptable salts and hydrates thereof, or metabolites thereof formed by any form of metabolism, and uses thereof in the preparation of medicaments for preventing and
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Paragraph 0038
(2019/05/16)
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- Imidazopyrazines as Selective BTK Inhibitors
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The invention relates to imidazopyrazine compounds as selective Bruton's tyrosine kinase (BTK) inhibitors. In particular, the invention discloses (S)-4-(8-amino-3-(1-(butyl-2-acetylenyl) pyrrolidine-2-yl) imidazo [1, 5-a] pyrazine-1-yl)-N-(pyridine-2-yl) benzamide and a deuterated compound of an optical isomer thereof, or a pharmaceutically acceptable salt or to a pharmaceutical composition containing the compound, and use thereof in the treatment of BTK-mediated diseases.
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Paragraph 0098-0102
(2019/12/25)
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- Imidazopyrazine compound, and preparation method and application thereof
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The invention belongs to the technical field of medicines and relates to an imidazopyrazine compound, and a preparation method and an application thereof. Specifically, the invention relates to a compound with a structure shown in a formula (I) defined in the specification, a pharmaceutically acceptable salt of the compound, a stereisomer of the compound or a prodrug of the compound, and an application of the compound, the pharmaceutically acceptable salt of the compound, the stereisomer of the compound or the prodrug of the compound to the preparation of drugs. The drugs are used for preventing and/or treating diseases and/or symptoms, related to the over-activity of Bruton's tyrosine kinases, of subjects. The invention furthermore relates to an application of the compound, pharmaceutically acceptable salts of the compound, the stereisomer of the compound or the prodrug of the compound to the preparation of preparations. The preparations are used for reducing or inhibiting the activity of the Bruton's tyrosine kinases in cells.
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Paragraph 0152; 0158; 0159
(2017/08/04)
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- HETEROAROMATIC NMDA RECEPTOR MODULATORS AND USES THEREOF
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Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated modulate the NMDA receptor.
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Paragraph 00352
(2017/07/27)
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- BTK INHIBITORS TO TREAT SOLID TUMORS THROUGH MODULATION OF THE TUMOR MICROENVIRONMENT
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In certain embodiments, the invention includes therapeutic methods of using a BTK inhibitor to treat solid tumor cancers by modulation of the tumor microenvironment, including macrophages, monocytes, mast cells, helper T cells, cytotoxic T cells, regulatory T cells, natural killer cells, myeloid-derived suppressor cells, regulatory B cells, neutrophils, dendritic cells, and fibroblasts.
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Paragraph 00207
(2016/02/29)
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- 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AND 4-IMIDAZOTRIAZIN-1-YL-BENZAMIDES BTK-INHIBITORS
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The present invention relates to 6-5 membered fused pyridine ring compounds of formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
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Page/Page column 25
(2013/03/26)
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- 4 - IMIDAZOPYRIDAZIN- 1 -YL-BENZAMIDES AND 4 - IMIDAZOTRIAZIN- 1 - YL - BENZAMIDES AS BTK- INHIBITORS
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The present invention relates to 6-5 membered fused pyridine ring compounds according to formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.
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Page/Page column 29-30
(2013/03/26)
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- 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
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The present invention provides 6-5 membered fused pyridine ring compounds according to Formula I or pharmaceutically acceptable salts thereof. or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
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Paragraph 0143
(2013/03/26)
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- Process to prepare substituted imidazopyrazine compounds
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A method of preparing wherein, X=Cl, Br, I, comprises the step of treating with N-chloro-, N-bromo-, or N-iodosuccinimide in a compatible solvent such as dimethylformamide (DMF) at 0-60° C. followed by halogenation.
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Page/Page column 5
(2008/06/13)
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