1227210-32-3Relevant articles and documents
A concise synthesis of a tetrahydropyrazolopyrazine building block
Shu, Lianhe,Wang, Ping,Gu, Chen,Garofalo, Lisa,Alabanza, Lady Mae,Dong, Yan
, p. 1870 - 1873 (2012)
A concise synthesis of a tetrahydropyrazolopyrazine building block is described. 5-Methyl-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazin-2-ylamine was prepared in three steps and 80% yield from 5-nitro-2H-pyrazole-3-carboxylic acid. This compound was then coupled with 4-bromo-6-chloro-2-methyl-2H- pyridazin-3-one in the presence of sodium tert-pentoxide to give the target product in 87% yield. The process was successfully scaled up to a multihundred gram scale.
Focal adhesion kinase inhibitor and use
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, (2019/01/08)
The invention belongs to the field of medicines, relates to a focal adhesion kinase inhibitor and use, in particular relates to a novel focal adhesion kinase inhibitor compound, or stereoisomers, geometric isomers, tautomers, oxynitrides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, further relates to the use of the compound and pharmaceutical compositions as medicines, in particular the use of the compound and pharmaceutical compositions in manufacture of medicines for treatment or prevention of cancer, pulmonary hypertension, and pathological angiogenesis-related diseases.
Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability
Young, Wendy B.,Barbosa, James,Blomgren, Peter,Bremer, Meire C.,Crawford, James J.,Dambach, Donna,Eigenbrot, Charles,Gallion, Steve,Johnson, Adam R.,Kropf, Jeffrey E.,Lee, Seung H.,Liu, Lichuan,Lubach, Joseph W.,MacAluso, Jen,MacIejewski, Pat,Mitchell, Scott A.,Ortwine, Daniel F.,Di Paolo, Julie,Reif, Karin,Scheerens, Heleen,Schmitt, Aaron,Wang, Xiaojing,Wong, Harvey,Xiong, Jin-Ming,Xu, Jianjun,Yu, Christine,Zhao, Zhongdong,Currie, Kevin S.
supporting information, p. 575 - 579 (2016/01/09)
BTK inhibitor GDC-0834 (1) was found to be rapidly metabolized in human studies, resulting in a suspension of clinical trials. The primary route of metabolism was through cleavage of the acyclic amide bond connecting the terminal tetrahydrobenzothiophene
HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY
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Paragraph 0277; 0278, (2015/11/16)
Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
SUBSTITUTED PYRIMIDINE COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
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Paragraph 00088, (2015/03/13)
The present disclosure relates to pyrimidine compounds of formula (I), their stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs, solvates, and hydrates thereof. The present disclosure also relates to process of preparation of these pyrimidine compounds, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders mediated by epidermal growth factor receptor (EGFR) family kinases.
8-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS
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Paragraph 0389, (2013/05/21)
8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
BICYCLIC PIPERAZINE COMPOUNDS
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Paragraph 0376, (2013/05/21)
Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Page/Page column 94; 95, (2013/03/26)
This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with
PYRIDAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
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Page/Page column 57-58, (2012/03/26)
Pyridazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
PYRIDINONES/PYRAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
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Page/Page column 73, (2012/03/26)
Pyridone and pyrazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
