163083-48-5Relevant articles and documents
BENZIMIDAZOLE DERIVATIVES, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
-
Page/Page column 33-34, (2022/02/24)
The present disclosure relates to benzimidazole derivatives, a preparation method therefor and a medical use thereof. Specifically, the present disclosure relates to a benzimidazole derivative represented by the general formula (I), a preparation method therefor, a pharmaceutical composition containing the derivative, and its use as a therapeutic agent, in particular its use for the treatment of diseases related to P2X3 activity.
PROTEIN KINASE C INHIBITORS AND METHODS OF THEIR USE
-
Paragraph 0160, (2016/04/20)
PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absor
Synthesis of 2,5-thiazole butanoic acids as potent and selective αvβ3 integrin receptor antagonists with improved oral pharmacokinetic properties
Wendt, John A.,Wu, Hongwei,Stenmark, Heather G.,Boys, Mark L.,Downs, Victoria L.,Penning, Thomas D.,Chen, Barbara B.,Wang, Yaping,Duffin, Tiffany,Finn, Mary Beth,Keene, Jeffery L.,Engleman, V. Wayne,Freeman, Sandra K.,Hanneke, Melanie L.,Shannon, Kristen E.,Nickols, Maureen A.,Steininger, Christina N.,Westlin, Marissa,Klover, Jon A.,Westlin, William,Nickols, G. Allen,Russell, Mark A.
, p. 845 - 849 (2007/10/03)
We describe a series of 2,5 thiazole containing compounds, which are potent antagonists of the integrin αvβ3 and show selectivity relative to the other integrins, such as αIIbβ 3 and αvβ6. These analogs were demonstrated to have high bioavailability relative to other relative heterocyclic analogs.
Convergent, parallel synthesis of a series of β-substituted 1,2,4-oxadiazole butanoic acids as potent and selective α vβ3 receptor antagonists
Boys, Mark L.,Schretzman, Lori A.,Chandrakumar, Nizal S.,Tollefson, Michael B.,Mohler, Scott B.,Downs, Victoria L.,Penning, Thomas D.,Russell, Mark A.,Wendt, John A.,Chen, Barbara B.,Stenmark, Heather G.,Wu, Hongwei,Spangler, Dale P.,Clare, Michael,Desai, Bipin N.,Khanna, Ish K.,Nguyen, Maria N.,Duffin, Tiffany,Engleman, V. Wayne,Finn, Mary Beth,Freeman, Sandra K.,Hanneke, Melanie L.,Keene, Jeffery L.,Klover, Jon A.,Nickols, G. Allen,Nickols, Maureen A.,Steininger, Christina N.,Westlin, Marisa,Westlin, William,Yu, Yi X.,Wang, Yaping,Dalton, Christopher R.,Norring, Sarah A.
, p. 839 - 844 (2007/10/03)
We describe a series of 1,2,4-oxadiazoles, which are potent antagonists of the integrin αvβ3 and, in addition, show selectivity relative to the other β3 integrin αIIbβ3. In whole cells, the majority o
THIAZOLE COMPOUNDS AS INTEGRIN RECEPTOR ANTAGONISTS DERIVATIVES
-
Page 59, (2008/06/13)
The present invention relates to pharmaceutical compositions comprising compounds of the Formula (I), and methods of selectively inhibiting or antagonizing the ανβ3 and/or the ανβ5 integrin without significantly inhibiting the ανβ6 integrin.
Cycloalkyl alkanoic acids as integrin receptor antagonists derivatives
-
Page 87, (2010/02/07)
The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or αvβ5 integrin.
PYRAZOLE COMPOUNDS AS INTEGRIN RECEPTOR ANTAGONISTS DERIVATIVES
-
Page 52-53; 77, (2010/02/07)
The present invention relates to pharmaceutical compositions comprising compounds of the Formula (I), and methods of selectively inhibiting or antagonizing the αVβ3 and/or the α Vβ5 integrin without significantly inhibitin
IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS
-
Page/Page column 30, (2010/02/07)
A class of 1-phenylimidazo[4,5-b]pyridine derivatives, optionally substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, are selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety, convulsions and cognitive disorders.