- FURO[3,4-B]PYRROLE-CONTAINING BTK INHIBITOR
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The present application belongs to the field of pharmaceutical chemistry, and relates to a furo[3,4-b]pyrrole-containing BTK inhibitor, and in particular, to a compound of formula (I), a stereisomer or pharmacologically acceptable salt thereof, a preparation method therefor, a pharmaceutical composition containing the compound, and use thereof in treating BTK-related diseases.
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Paragraph 0090-0092
(2021/07/24)
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- Aminonorbornane derivative and preparation method and application thereof
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The invention discloses an aminonorbornane derivative and a preparation method and application thereof and relates to a compound having a structure represented by a formula I which is described in thespecification or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an ester, an optical isomer or a prodrug thereof, a pharmaceutical composition comprising the compound as shown in the formula I, and application of the compound and the pharmaceutical composition as highly selective Bruton's tyrosine kinase (BTK) inhibitors of BTK (C481S) mutants for preparation ofdrugs used for prevention or treatment of heteroimmune diseases, autoimmune diseases or cancer.
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Paragraph 0076-0078; 0085-0087
(2020/04/17)
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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 00206-00209
(2020/03/23)
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- PROCESSES TO PRODUCE ACALABRUTINIB
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The present invention relates to a method for preparing the compound of formula IV, compound of formula XI, and acalabrutinib, a new generation of bruton tyrosine kinase (BTK) inhibitor.
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Page/Page column 10
(2019/05/22)
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- Bruton's tyrosine kinase inhibitor
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The invention relates to a compound with a formula I and a pharmaceutically acceptable salt, a solvent compound, an active metabolite, a polycrystalline compound, an ester, an isomer or a prodrug thereof, a pharmaceutical composition containing the compound in the formula I, and application using the same as a selective Bruton's tyrosine kinase inhibitor to prepare a medicine for preventing or treating heterologous immunity diseases and self immunity diseases or cancers. The formula is shown in the specification.
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Paragraph 0099; 0100; 0101; 0102
(2017/08/29)
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- From arylureas to biarylamides to aminoquinazolines: Discovery of a novel, potent TRPV1 antagonist
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Bioisosteric replacement of piperazine with an aryl ring in lead VR1 antagonist 1 led to the biarylamide series. The development of B-ring SAR led to the conformationally constrained analog 70. The resulting aminoquinazoline 70 represents a novel VR1 anta
- Zheng, Xiaozhang,Hodgetts, Kevin J.,Brielmann, Harry,Hutchison, Alan,Burkamp, Frank,Brian Jones,Blurton, Peter,Clarkson, Robert,Chandrasekhar, Jayaraman,Bakthavatchalam, Rajagopal,De Lombaert, Stephane,Crandall, Marci,Cortright, Daniel,Blum, Charles A.
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p. 5217 - 5221
(2007/10/03)
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