159217-95-5Relevant articles and documents
FUSED PYRIMIDINE PYRIDINONE COMPOUNDS AS JAK INHIBITORS
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Page/Page column 61-62, (2021/06/04)
The disclosure provides compounds of formula (I), or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The disclosure also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat gastrointestinal inflammatory diseases.
DIACYLGLYCEROL KINASE MODULATING COMPOUNDS
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Paragraph 1271, (2021/07/02)
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
NEW MALONITRILE DERIVATIVES
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Page/Page column 65-66, (2021/11/26)
The invention relates to a compound of formula (I) wherein R1-R4 and A1-A2 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability
Gandhi, Disha M.,Rosas, Ricardo,Greve, Eric,Kentala, Kaitlin,D.-R. Diby, N'Guessan,Snyder, Vladyslava A.,Stephans, Allison,Yeung, Teresa H.W.,Subramaniam, Saravanan,DiMilo, Elliot,Kurtenbach, Khia E.,Arnold, Leggy A.,Weiler, Hartmut,Dockendorff
supporting information, p. 3788 - 3796 (2019/07/17)
Novel analogs of the allosteric, biased PAR1 ligand ML161 (parmodulin 2, PM2) were prepared in order to identify potential anti-thrombotic and anti-inflammatory compounds of the parmodulin class with improved properties. Investigations of structure-activi
Synthesis and anti-parasitic activity of C-benzylated (N-arylcarbamoyl)alkylphosphonate esters
Adeyemi, Christiana M.,Isaacs, Michelle,Mnkandhla, Dumisani,Klein, Rosalyn,Hoppe, Heinrich C.,Krause, Rui W.M.,Lobb, Kevin A.,Kaye, Perry T.
, p. 1661 - 1667 (2017/03/08)
Unexpected substituent-dependent regioselectivty challenges in the synthesis of C-benzylated (N-arylcarbamoyl)phosphonate esters have been resolved. The C-benzylated N-furfurylcarbamoyl derivative showed low micromolar PfLDH inhibition, while one of the C-benzylated N-arylcarbamoyl analogues was active against Nagana Trypanosoma brucei parasites which are responsible for African trypanosomiasis in cattle.
OLIGONUCLEOTIDE HAVING NON-NATURAL NUCLEOTIDE AT 5'-TERMINAL THEREOF
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Paragraph 1567; 1568; 1569, (2018/01/19)
An oligonucleotide having a nucleotide residue or a nucleoside residue represented by formula (I) {wherein X1 is an oxygen atom or the like, R1 is formula (IIA) (wherein R5A is halogen or the like, and R6A is a hydrogen atom or the like), formula (IVA) (wherein Y3A is a nitrogen atom or the like, and Y4A is CH or the like), or the like, R2 is a hydrogen atom, hydroxy, halogen, or optionally substituted lower alkoxy, and R3 is a hydrogen atom or the like, or formula (VI) (wherein n2 is 1, 2 or 3)} at the 5′ end thereof, wherein the nucleotide residue or the nucleoside residue binds to an adjacent nucleotide residue through the oxygen atom at position 3, is provided.
NOVEL THERAPEUTIC COMPOUNDS
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Page/Page column 151, (2009/03/07)
Disclosed herein are novel compounds of Formula (I), wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases as well as proliferative disorders such as cancer.
Design, synthesis, and structure - Activity relationship of indole-3-glyoxylamide libraries possessing highly potent activity in a cell line model of prion disease
Thompson, Mark J.,Borsenberger, Vinciane,Louth, Jennifer C.,Judd, Katie E.,Chen, Beining
experimental part, p. 7503 - 7511 (2010/06/11)
Transmissible spongiform encephalopathies (TSEs) are a family of invariably fatal neurodegenerative disorders for which no effective curative therapy currently exists. We report here the synthesis of a library of indole-3-glyoxylamides and their evaluation as potential antiprion agents. A number of compounds demonstrated submicromolar activity in a cell line model of prion disease together with a defined structure-activity relationship, permitting the design of more potent compounds that effected clearance of scrapie in the low nanomolar range. Thus, the indole-3-glyoxylamides described herein constitute ideal candidates to progress to further development as potential therapeutics for the family of human prion disorders. 2009 American Chemical Society.
IMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABA-A RECEPTOR COMPLEX
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Page/Page column 15-16, (2008/06/13)
This invention relates to novel imidazole derivatives of formula (I), pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
BENZIMIDAZOLE DERIVATIVES AND THEIR USE FOR MODULATING THE GABAA RECEPTOR COMPLEX
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, (2008/06/13)
This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
