280771-61-1Relevant academic research and scientific papers
MODIFIED PROTEINS AND PROTEIN DEGRADERS
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Paragraph 00450-00452, (2021/12/08)
Provided herein are compounds, pharmaceutical compositions, and methods for binding or degrading target proteins. Further provided herein are compounds having a DNA damage-binding protein 1 (DDB1) binding moiety. Some such embodiments include a linker. Some such embodiments include a target protein binding moiety. Further provided herein are ligand-DDB1 complexes. Further provided herein are in vivo modified DDB1 proteins.
URETHANES, UREAS, AMIDINES AND RELATED INHIBITORS OF FACTOR XA
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, (2011/10/03)
The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.
Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR
Zhang, Penglie,Bao, Liang,Fan, Jingmei,Jia, Zhaozhong J.,Sinha, Uma,Wong, Paul W.,Park, Gary,Hutchaleelaha, Athiwat,Scarborough, Robert M.,Zhu, Bing-Yan
experimental part, p. 2186 - 2189 (2010/02/28)
Anthranilamide-based benzamidine compound 4 and its N-substituted analogs were designed and examined as factor Xa inhibitors using substituted benzamidines as unconventional S4 binding element. A group of N,N-dialkylbenzamidines (11, 17 and 24) have been
Anthranilamide inhibitors of factor Xa
Mendel, David,Marquart, Angela L.,Joseph, Sajan,Waid, Philip,Yee, Ying K.,Tebbe, Anne Louise,Ratz, Andrew M.,Herron, David K.,Goodson, Theodore,Masters, John J.,Franciskovich, Jeffry B.,Tinsley, Jennifer M.,Wiley, Michael R.,Weir, Leonard C.,Kyle, Jeffrey A.,Klimkowski, Valentine J.,Smith, Gerald F.,Towner, Richard D.,Froelich, Larry L.,Buben, John,Craft, Trelia J.
, p. 4832 - 4836 (2008/02/11)
SAR about the B-ring of a series of N2-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1′ and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
AROMATIC ETHER DERIVATIVES USEFUL AS THROMBIN INHIBITORS
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Page/Page column 41, (2008/06/13)
This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a).
AROMATIC AMIDES
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, (2008/06/13)
This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
