307353-32-8Relevant academic research and scientific papers
Synthesis and evaluation of tiaprofenic acid-derived UCHL5 deubiquitinase inhibitors
Gurusingha Arachchige, Harshani S.,Herath Mudiyanselage, Poornima D.H.,VanHecke, Garrett C.,Patel, Kush,Cheaito, Hassan A.,Dou, Q. Ping,Ahn, Young-Hoon
supporting information, (2020/12/25)
The ubiquitin–proteasome system (UPS) plays an important role in maintaining protein homeostasis by degrading intracellular proteins. In the proteasome, poly-ubiquitinated proteins are deubiquitinated by three deubiquitinases (DUBs) associated with 19S re
BENZOPYRAZOLE COMPOUND USED AS RHO KINASE INHIBITOR
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Paragraph 0459-0462, (2021/02/25)
The invention relates to a benzopyrazole compound used as RHO kinase inhibitor, a pharmaceutical composition and uses thereof for preparing an RHO kinase inhibiting drug, and more specifically to said compound of formula (I-1), a pharmaceutically acceptable salt and isomer thereof.
Discovery of a potent class of PI3Kα inhibitors with unique binding mode via encoded library technology (ELT4)
Yang, Hongfang,Medeiros, Patricia F.,Raha, Kaushik,Elkins, Patricia,Lind, Kenneth E.,Lehr, Ruth,Adams, Nicholas D.,Burgess, Joelle L.,Schmidt, Stanley J.,Knight, Steven D.,Auger, Kurt R.,Schaber, Michael D.,Franklin, G. Joseph,Ding, Yun,Delorey, Jennifer L.,Centrella, Paolo A.,Mataruse, Sibongile,Skinner, Steven R.,Clark, Matthew A.,Cuozzo, John W.,Evindar, Ghotas
supporting information, p. 531 - 536 (2015/05/27)
In the search of PI3K p110α wild type and H1047R mutant selective small molecule leads, an encoded library technology (ELT) campaign against the desired target proteins was performed which led to the discovery of a selective chemotype for PI3K isoforms from a three-cycle DNA encoded library. An X-ray crystal structure of a representative inhibitor from this chemotype demonstrated a unique binding mode in the p110α protein.
Broad substrate specificity of the amide synthase in S. hygroscopicus -new 20-membered macrolactones derived from geldanamycin
Eichner, Simone,Eichner, Timo,Floss, Heinz G.,Fohrer, Joerg,Hofer, Edgar,Sasse, Florenz,Zeilinger, Carsten,Kirschning, Andreas
supporting information; experimental part, p. 1673 - 1679 (2012/03/12)
The amide synthase of the geldanamycin producer, Streptomyces hygroscopicus, shows a broader chemoselectivity than the corresponding amide synthase present in Actinosynnema pretiosum, the producer of the highly cytotoxic ansamycin antibiotics, the ansamit
AMIDE COMPOUNDS, COMPOSITIONS AND USES THEREOF
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Page/Page column 122-123, (2009/10/22)
Compounds are provided according to formula (1 ) : where A, B, W, X', L, R1, R3, R4b, and m' are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
NK-1 AND SEROTONIN TRANSPORTER INHIBITORS
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Page/Page column 85, (2010/11/28)
The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
QUINOXALINES AS B RAF INHIBITORS
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Page/Page column 81, (2010/11/08)
The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
QUINAZOLINONE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS
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Page/Page column 76, (2008/06/13)
The invention relates to chemical compounds of the formula (I): or pharmaceutically acceptable salts thereof, which possess B Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
PROCESS FOR PRODUCING 5-(3-CYANOPHENYL)-3-FORMYLBENZOIC ACID COMPOUND
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Page 8, (2008/06/13)
A 5-(3-cyanophenyl)-3-formylbenzoic acid compound of the formula (IV) is prepared by reacting a 5-bromo-3-(hydroxymethyl)benzoic acid compound of the formula (I) with manganese dioxide to provide a 5-bromo-3-formylbenzoic acid compound of the formula (II)
Cyanobiphenyl derivatives
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, (2008/06/13)
Intermediates represented by the following formula: (wherein R1is a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or the like; X is a carboxyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aralkoxycarbonyl group,
