882679-89-2Relevant academic research and scientific papers
GLUCOSE SENSITIVE INSULIN DERIVATIVES
-
, (2020/10/20)
The present invention relates to novel insulin derivatives and their use in the treatment or prevention of medical conditions relating to diabetes. The insulin derivatives are glucose sensitive and display glucose-sensitive albumin binding. The invention
GLUCOSE-SENSITIVE ALBUMIN-BINDING DERIVATIVES
-
, (2019/05/30)
This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates. The diboron compounds are characterized by formula (I), which is: R1-X-R2, and wherein "X" is a mono- to multiatomic linker and where R1 and R2, which may be identical or different, each represents a group of Formula (lla) or (IIb) Also described are diboron conjugates represented by the general Formula (I'), which is: R1'-X'-R2', in which either the moeities R1' or R2' or X' carry a drug that is covalently attached to the diboron compound.
Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT
Kaitsiotou, Helena,Keul, Marina,Hardick, Julia,Mühlenberg, Thomas,Ketzer, Julia,Ehrt, Christiane,Krüll, Jasmin,Medda, Federico,Koch, Oliver,Giordanetto, Fabrizio,Bauer, Sebastian,Rauh, Daniel
, p. 8801 - 8815 (2017/11/15)
In modern cancer therapy, the use of small organic molecules against receptor tyrosine kinases (RTKs) has been shown to be a valuable strategy. The association of cancer cells with dysregulated signaling pathways linked to RTKs represents a key element in
BORON-CONTAINING DIACYLHYDRAZINES
-
, (2014/09/29)
The present disclosure provides boron-containing diacylhydrazines having Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, and R5 are defined as set forth in the specification. The present disclosure also provides the use of boron-containing diacylhydrazines is ecdysone receptor-based inducible gene expression systems. Thus, the present disclosure is useful for applications such as gene therapy, treatment of disease, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable.
New 7-phenyl-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives
-
, (2011/06/10)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), to pharmaceutical compositions comprising them, and to their use in therapy.
NEW 7-PHENYL-[1,2,4]TRIAZOLO[4,3-A]PYRIDIN-3(2H)-ONE DERIVATIVES
-
, (2011/06/16)
This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), to processes for their preparation, to pharmaceutical compositions comprising them, and to their use in therapy.
Indolin-2-one p38α inhibitors III: Bioisosteric amide replacement
Eastwood, Paul,González, Jacob,Gómez, Elena,Caturla, Francisco,Aguilar, Nuria,Mir, Marta,Aiguadé, Josep,Matassa, Victor,Balagué, Cristina,Orellana, Adelina,Domínguez, María
, p. 6253 - 6257 (2011/11/29)
Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38a inhibitors which showed general hydrolytic instability in human liver preparations. Triazole derivative 13 was found to have moderate bioavailability in the rat and demonstrated potent in-vivo activity in an acute model of inflammation.
3-Amino-7-phthalazinylbenzoisoxazoles as a novel class of potent, selective, and orally available inhibitors of p38α mitogen-activated protein kinase
Pettus, Liping H.,Xu, Shimin,Cao, Guo-Qiang,Chakrabarti, Partha P.,Rzasa, Robert M.,Sham, Kelvin,Wurz, Ryan P.,Zhang, Dawei,Middleton, Scott,Henkle, Bradley,Plant, Matthew H.,Saris, Christiaan J. M.,Sherman, Lisa,Lu, Min Wong,Powers, David A.,Tudor, Yanyan,Yu, Violeta,Lee, Matthew R.,Syed, Rashid,Hsieh, Faye,Tasker, Andrew S.
experimental part, p. 6280 - 6292 (2009/10/09)
The p38 mitogen-activated protein kinase (MAPK) is a central signaling molecule in many proinflammatory pathways, regulating the cellular response to a multitude of external stimuli including heat, ultraviolet radiation, osmotic shock, and a variety of cy
NITROGEN-CONTAINING BICYCLIC HETEROARYL COMPOUNDS AND METHODS OF USE
-
Page/Page column 77, (2008/06/13)
The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have Formula (I) wherein R1 is Formula (II), (III) or (IV) and A1, A2, A3, A4, X, Z, Z', R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
Phthalazine, aza- and diaza-phthalazine compounds and methods of use
-
Page/Page column 24; 25, (2008/06/13)
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
