13024-16-3Relevant academic research and scientific papers
Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity
Tichenor, Mark S.,Wiener, John J. M.,Rao, Navin L.,Pooley Deckhut, Charlotte,Barbay, J. Kent,Kreutter, Kevin D.,Bacani, Genesis M.,Wei, Jianmei,Chang, Leon,Murrey, Heather E.,Wang, Weixue,Ahn, Kay,Huber, Michael,Rex, Elizabeth,Coe, Kevin J.,Wu, Jiejun,Seierstad, Mark,Bembenek, Scott D.,Leonard, Kristi A.,Lebsack, Alec D.,Venable, Jennifer D.,Edwards, James P.
, p. 782 - 790 (2021/05/04)
Bruton's tyrosine kinase (BTK) is a cytoplasmic tyrosine kinase that plays a critical role in the activation of B cells, macrophages, and osteoclasts. Given the key role of these cell types in the pathology of autoimmune disorders, BTK inhibitors have the
HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF EPILEPSY
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Paragraph 0135; 0143; 0144, (2020/06/19)
The present invention provides a novel heterocyclic compound represented by Formula [I] and a salt thereof: wherein the symbols are as defined in the specification, which is useful for treating, preventing and/or diagnosing seizure and the like in disease involving epileptic seizure or convulsive seizure (including multiple drug resistant seizure, refractory seizure, acute symptomatic seizure, febrile seizure and status epilepticus), as well as a medical use therefor.
INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
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, (2018/06/30)
The present disclosure is directed to compounds of Formula (I) and methods of their use and preparation, as well as compositions comprising compounds of Formula (I).
INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
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, (2018/06/30)
Compounds of formula (I') and methods of their use and preparation, as well as compositions comprising compounds of formula (I').
POLYCYCLIC COMPOUNDS AS INHIBITORS OF BRUTON'S TYROSINE KINASE
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, (2017/07/06)
The present disclosure is directed to compounds of Formula (I) as Bruton's kinase inhibitors and their preparation, as well as compositions comprising compounds of Formula (I).
INHIBITORS OF BRUTON'S TYROSINE KINASE AND METHODS OF THEIR USE
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, (2017/09/02)
The present disclosure is directed to compounds of formula I and methods of their use and preparation, as well as compositions comprising compounds of formula I.
TYROSINE KINASE INHIBITORS
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, (2017/04/19)
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
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Page/Page column 59; 60; 63; 75, (2015/06/25)
This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with ex
Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis
Akama, Tsutomu,Baker, Stephen J.,Zhang, Yong-Kang,Hernandez, Vincent,Zhou, Huchen,Sanders, Virginia,Freund, Yvonne,Kimura, Richard,Maples, Kirk R.,Plattner, Jacob J.
scheme or table, p. 2129 - 2132 (2009/12/07)
A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment of psoriasis and being pursued for the topical treatment of atopic dermatitis.
