1004294-58-9Relevant academic research and scientific papers
N-(PYRIDIN-2-YL)PYRIDINE-SULFONAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 69, (2020/08/22)
The invention relates to heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.
N-(PYRIDIN-2-YL)PYRIDINE-SULFONAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 122, (2018/03/25)
The invention relates to heterocyclic compounds of the formula (I) in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.
NEW 6-AMINO-QUINOLINONE COMPOUNDS AND DERIVATIVES AS BCL6 INHIBITORS
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Page/Page column 93, (2018/07/05)
The present invention encompasses compounds of formula (I), wherein the groups R1 to R5, X, Y and W have the meanings given in the claims and specification, their use as inhibitors of BCL6, pharmaceutical compositions which contain compounds of this kind and their use as medicaments, especially as agents for treatment and/or prevention of oncological diseases.
BENZENE SULFONAMIDES AS CCR9 INHIBITORS
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Page/Page column 102; 103, (2015/07/15)
The present invention relates to compounds useful as CCR9 modulators, to compositions containing them, to methods of making them, and to methods of using them. In particular, the present invention relates to compounds capable of modulating the function of the CCR9 receptor by acting as partial agonists, antagonists or inverse agonists. Such compounds may be useful to treat, prevent or ameliorate a disease or condition associated with CCR9 activation, including inflammatory and immune disorder diseases or conditions such as inflammatory bowel diseases (IBD).
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ? S-X) Interaction for Conformational Constraint
Pennington, Lewis D.,Bartberger, Michael D.,Croghan, Michael D.,Andrews, Kristin L.,Ashton, Kate S.,Bourbeau, Matthew P.,Chen, Jie,Chmait, Samer,Cupples, Rod,Fotsch, Christopher,Helmering, Joan,Hong, Fang-Tsao,Hungate, Randall W.,Jordan, Steven R.,Kong, Ke,Liu, Longbin,Michelsen, Klaus,Moyer, Carolyn,Nishimura, Nobuko,Norman, Mark H.,Reichelt, Andreas,Siegmund, Aaron C.,Sivits, Glenn,Tadesse, Seifu,Tegley, Christopher M.,Van, Gwyneth,Yang, Kevin C.,Yao, Guomin,Zhang, Jiandong,Lloyd, David J.,Hale, Clarence,St. Jean, David J.
supporting information, p. 9663 - 9679 (2016/01/12)
The HTS-based discovery and structure-guided optimization of a novel series of GKRP-selective GK-GKRP disrupters are revealed. Diarylmethanesulfonamide hit 6 (hGK-hGKRP IC50 = 1.2 μM) was optimized to lead compound 32 (AMG-0696; hGK-hGKRP IC50 = 0.0038 μM). A stabilizing interaction between a nitrogen atom lone pair and an aromatic sulfur system (nN → σ?S-X) in 32 was exploited to conformationally constrain a biaryl linkage and allow contact with key residues in GKRP. Lead compound 32 was shown to induce GK translocation from the nucleus to the cytoplasm in rats (IHC score = 0; 10 mg/kg po, 6 h) and blood glucose reduction in mice (POC = -45%; 100 mg/kg po, 3 h). X-ray analyses of 32 and several precursors bound to GKRP were also obtained. This novel disrupter of GK-GKRP binding enables further exploration of GKRP as a potential therapeutic target for type II diabetes and highlights the value of exploiting unconventional nonbonded interactions in drug design.
INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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Paragraph 00403, (2014/05/07)
The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provide
PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS
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Page/Page column 358, (2014/09/29)
Disclosed are compounds of Formula (IIa), wherein R1, R2, R3A, R3B, R3C, R3D, R3E, and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa)
BENZOTHIOPHENE SULFONAMIDES AND OTHER COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN
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Page/Page column 126-127, (2013/12/03)
The present invention relates to benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
N-ACYL PYRIDINE BIARYL COMPOUNDS AND THEIR USES
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Page/Page column 98, (2012/08/08)
The present invention provides a compound of general formula:wherein Z2-Z6 include one or two nitrogen atoms as described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds of Formula I and isomers thereof, and pharmaceutical compositions comprising such compounds.
N-ACYL PYRIMIDINE BIARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS
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Page/Page column 138, (2012/08/08)
The present invention provides a compound of the general formula (1): wherein one of X and Y is N and the other is an optionally substituted carbon atom, and Z2-Z5 represent one or two nitrogen atoms, as further described herein, including pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. These compounds inhibit the activity of CDK9 and are thus useful as pharmaceuticals and as components of pharmaceutical compositions. Also provided are methods of treating a disease or condition mediated by CDK9 using the compounds described herein or pharmaceutical compositions comprising such compounds.
