- Substituted aromatic fused ring derivative, composition containing same and application
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The invention provides a substituted aromatic fused ring derivative, a composition containing the compound and application. The substituted aromatic fused ring derivative is a compound shown in a formula (I) or a tautomer, a stereoisomer, a prodrug, a cry
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Paragraph 0471-0473
(2021/03/30)
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- PROCESSES FOR THE PREPARATION OF 4-{8-AMINO-3-[(2S)-1-(BUT-2-YNOYL)-PYRROLIDIN-2-YL]IMIDAZO[1,5-A]-PYRAZIN-1-YL}N-(PYRIDIN-2-YL)-BENZAMIDE
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The present disclosure relates, in general, to improved processes for the preparation of 4-{8-amino-3-[(2S)-1-(but-2-ynoyl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)-benzamide, particularly large-scale processes for manufacturing 4-{8-amino-3-[(2S)-1-(but-2-ynoyl)pyrrolidin-2-yl]imidazo[1,5-a]pyrazin-1-yl}-N-(pyridin-2-yl)benzamide and intermediates used in such processes.
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Paragraph 00232
(2020/03/23)
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- Method for preparing Acalabrutinib, in particular to method for preparing Acalabrutinib
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The invention relates to the field of chemical synthesis, in particular to a chemical synthesis method for preparing Acalabrutinib. The synthesis method of the compound 3 is optimized, wherein 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 material catalyst nickel is prevented from being adopted, and large-scale production is facilitated.In the preparation of the compound 15, water is used as a solvent, equivalent hydrogen peroxide is added to react the compound 13 with the compound 14 to prepare the compound 15, so that the method iseconomic and environment-friendly, the post-treatment is simple and convenient, and the reaction liquid is directly subjected to centrifugal operation; in addition, the yield is high and can reach 90% or above; and the compound 15 is high in purity and does not need to be further purified, so that the technology can satisfy the requirements of industrial production.
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Paragraph 0024-0027
(2020/07/24)
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- FUSED BICYCLIC COMPOUND FOR INHIBITING ACTIVITY OF TYROSINE KINASE
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A fused bicyclic compound having an effect in inhibition of the activity of a tyrosine kinase, and preparation and use thereof are disclosed. In particular, a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydr
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Paragraph 0166; 0167
(2019/06/12)
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- Alkynyl (hetero) aromatic ring compound for inhibiting activity of protein tyrosine kinase
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The present invention relates to an alkynyl (hetero) aromatic ring compound having protein tyrosine kinase inhibition effect, and a preparation method thereof, a pharmaceutical composition containingthe alkynyl (hetero) aromatic ring compound, and uses of
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Paragraph 0263; 0266; 0267; 0268
(2019/09/10)
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- A Manufacturing Process to an Intermediate in the Synthesis of Acalabrutinib
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Optimization and application of the reported synthesis of (3-chloropyrazin-2-yl)methanamine 3 have provided a high yielding, fully telescoped procedure to key intermediate 5 in the synthesis of acalabrutinib.
- Chen, Bo,Golden, Michael,Li, Zhonglian,Xu, Liwen,Xu, Zhaofu,Yao, Xiaolong
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p. 1458 - 1460
(2018/10/15)
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- The compounds of structure containing conjugated zincon, its pharmaceutical composition and use thereof (by machine translation)
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The present invention relates to compounds having a structure containing conjugated zincon, its pharmaceutical composition and use, and in particular relates to the general formula (I) or a salt thereof to the compound represented by the, pharmaceutical compositions thereof, and its as BTK inhibitors and/or B cell activation inhibitor, for the prevention or treatment B cell activity with abnormal and/or the use of the BTK-related diseases. The compounds of lymphoma, breast cancer, liver cancer, colon cancer, gastric cancer, such as lung cancer and cervical cancer cell has better lethal effect, note has potential for the treatment of cancer and self-immune diseases related to potential. (by machine translation)
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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 00361
(2017/07/27)
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- Compound used as Bruton tyrosine kinase inhibitor, and preparation method and application of compound
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The invention provides a compound with a structure shown as the formula (I), or an isomer, pharmaceutically acceptable solvate and salt thereof, which is used as the Bruton tyrosine kinase inhibitor. The Bruton tyrosine kinase inhibitor has higher inhibit
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- TYROSINE KINASE INHIBITORS
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The present disclosure provides compounds of formula (I) that are tyrosine kinase inhibitors, in particular Bruton tyrosine kinase ("BTK") inhibitors, and are therefore useful for the treatment of diseases treatable by inhibition of BTK such as cancer, au
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Page/Page column 72
(2017/04/19)
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- COMPOSITIONS AND METHODS FOR TREATING TOXOPLASMOSIS. CRYPTOSPORIDIOSIS AND OTHER APICOMPLEXAN PROTOZOAN RELATED DISEASES
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Compositions and methods for the treatment of toxoplasmosis-, caused by the infectious eukaryotic parasite Toxoplasma gondii (T, gondii) and for the treatment of ciyptosporidiosis, caused by the infectious eukaryotic parasites Cryptosporidium parvum (C parvuai) and Cnγtosporidium homimus (C. hominus) are described. In particular, the present disclosure is directed to compositions and methods for inhibiting either T. gondii calcium dependent protein kinases (TgCDPKs) or C. parvum and C. hominus calcium dependent protein kinases (CpDPKS) using pyrazolopyriinidine and/or imidazo[l,5-a]pyraziαe inhibitors, of the formula.(I), wherein the variables X. Y, Z, L. R1. and R3 are defined herein.
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- PREPARATION OF C-PYRAZINE-METHYLAMINES
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A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3- dichloropyrazine with a suitable diaryl imine followed by hydrolysis.
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Page/Page column 11-13
(2010/11/05)
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- Fused bicyclic mTOR inhibitors
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Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
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Page/Page column 61
(2008/06/13)
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- UNSATURATED mTOR INHIBITORS
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Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.
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Page/Page column 44-45
(2010/11/28)
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