479226-58-9Relevant academic research and scientific papers
SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS INHIBITORS OF FGFR TYROSINE KINASES
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Paragraph 001380-001382, (2020/07/14)
Provided herein are compounds of the general Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which Ring A, Ring B, Ring C, R1, R2, L, Y, and W have the meanings given in the specification, which are inhibitors of FGFR1, FGFR2, FGFR3 and/or FGFR4 and are useful in the treatment and prevention of diseases which can be treated with an FGFR inhibitor, including diseases or disorders mediated by FGFR1, FGFR2, FGFR3 and/or FGFR4.
SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS
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Paragraph 001284; 001285; 001286, (2018/04/27)
Provided herein are compounds of the Formula I and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, X1, X2, X3, X4, Ring D, and E have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.
Use of small-molecule crystal structures to address solubility in a novel series of g protein coupled receptor 119 agonists: Optimization of a lead and in vivo evaluation
Scott, James S.,Birch, Alan M.,Brocklehurst, Katy J.,Broo, Anders,Brown, Hayley S.,Butlin, Roger J.,Clarke, David S.,Davidsson, ?jvind,Ertan, Anne,Goldberg, Kristin,Groombridge, Sam D.,Hudson, Julian A.,Laber, David,Leach, Andrew G.,MacFaul, Philip A.,McKerrecher, Darren,Pickup, Adrian,Schofield, Paul,Svensson, Per H.,S?rme, Pernilla,Teague, Joanne
supporting information; experimental part, p. 5361 - 5379 (2012/08/28)
G protein coupled receptor 119 (GPR119) is viewed as an attractive target for the treatment of type 2 diabetes and other elements of the metabolic syndrome. During a program toward discovering agonists of GPR119, we herein describe optimization of an initial lead compound, 2, into a development candidate, 42. A key challenge in this program of work was the insolubility of the lead compound. Small-molecule crystallography was utilized to understand the intermolecular interactions in the solid state and resulted in a switch from an aryl sulphone to a 3-cyanopyridyl motif. The compound was shown to be effective in wild-type but not knockout animals, confirming that the biological effects were due to GPR119 agonism.
PHENYLPYRIDINE CARBONYL PIPERAZINE DERIVATIVE
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Page 19-20, (2008/06/13)
The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (whereinR1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like,R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like,R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, andn: 0 or 1).
