958488-72-7Relevant academic research and scientific papers
Synthesis of (S)-3-amino-benzo[b][1,4]oxazepin-4-one via Mitsunobu and SNAr reaction for a first-in-class RIP1 kinase inhibitor GSK2982772 in clinical trials
Jeong, Jae Uk,Harris, Philip A.,Kang, James,Leister, Lara,Lan, Yunfeng,Romano, Joseph,Dong, Xiaoyang,Marquis, Robert W.
, p. 2306 - 2308 (2017)
Two new synthetic routes were developed to prepare the RIP1 kinase inhibitor clinical candidate GSK2982772 involving a key (S)-3-amino-benzo[b][1,4]oxazepin-4-one intermediate prepared via Mitsunobu and SNAr cyclization reactions. Both routes are practical and cost effective compared to the initial medicinal chemistry route and are also applicable to kilogram scale-up to support on-going clinical studies.
FUSED RING HETEROARYL COMPOUNDS AS RIPK1 INHIBITORS
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Paragraph 0131, (2021/02/12)
The invention provides novel substituted heterocyclic compounds represented by Formula I, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided c
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer
Harris, Philip A.,Marinis, Jill M.,Lich, John D.,Berger, Scott B.,Chirala, Anirudh,Cox, Julie A.,Eidam, Patrick M.,Finger, Joshua N.,Gough, Peter J.,Jeong, Jae U.,Kang, James,Kasparcova, Viera,Leister, Lara K.,Mahajan, Mukesh K.,Miller, George,Nagilla, Rakesh,Ouellette, Michael T.,Reilly, Michael A.,Rendina, Alan R.,Rivera, Elizabeth J.,Sun, Helen H.,Thorpe, James H.,Totoritis, Rachel D.,Wang, Wei,Wu, Dongling,Zhang, Daohua,Bertin, John,Marquis, Robert W.
, p. 857 - 862 (2019/06/20)
RIP1 regulates cell death and inflammation and is believed to play an important role in contributing to a variety of human pathologies, including immune-mediated inflammatory diseases and cancer. While small-molecule inhibitors of RIP1 kinase have been ad
PROCESS AND INTERMEDIATES FOR PREPARING BENZOXAZEPINES
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Page/Page column 65, (2018/09/25)
Disclosed is a new process and intermediates for preparing benzoxazepines of Formula (I): (I) wherein Q is, and A, L, B, RA and m are as defined herein.
Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases
Harris, Philip A.,Berger, Scott B.,Jeong, Jae U.,Nagilla, Rakesh,Bandyopadhyay, Deepak,Campobasso, Nino,Capriotti, Carol A.,Cox, Julie A.,Dare, Lauren,Dong, Xiaoyang,Eidam, Patrick M.,Finger, Joshua N.,Hoffman, Sandra J.,Kang, James,Kasparcova, Viera,King, Bryan W.,Lehr, Ruth,Lan, Yunfeng,Leister, Lara K.,Lich, John D.,MacDonald, Thomas T.,Miller, Nathan A.,Ouellette, Michael T.,Pao, Christina S.,Rahman, Attiq,Reilly, Michael A.,Rendina, Alan R.,Rivera, Elizabeth J.,Schaeffer, Michelle C.,Sehon, Clark A.,Singhaus, Robert R.,Sun, Helen H.,Swift, Barbara A.,Totoritis, Rachel D.,Vossenk?mper, Anna,Ward, Paris,Wisnoski, David D.,Zhang, Daohua,Marquis, Robert W.,Gough, Peter J.,Bertin, John
, p. 1247 - 1261 (2017/03/08)
RIP1 regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including immune-mediated inflammatory diseases. Small-molecule inhibitors of RIP1 kinase that are suitable for advancement into
HETEROCYCLIC AMIDES AS KINASE INHIBITORS
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Page/Page column 110, (2014/09/03)
Disclosed are compounds having the formula (I) wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
DERIVATIVES OF 2-ALKOXY-3,4,5-TRIHYDROXY-ALKYL AMIDES, PREPARATION AND USE THEREOF, AND COMPOSITIONS CONTAINING THE SAME
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, (2009/04/24)
The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.
