161117-88-0Relevant articles and documents
Discovery of novel heterocyclic factor VIIa inhibitors
Rai, Roopa,Kolesnikov, Aleksandr,Sprengeler, Paul A.,Torkelson, Steven,Ton, Tony,Katz, Bradley A.,Yu, Christine,Hendrix, John,Shrader, William D.,Stephens, Robin,Cabuslay, Ronnell,Sanford, Ellen,Young, Wendy B.
, p. 2270 - 2273 (2006)
Structure-activity relationships and binding mode of novel heterocyclic factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2-b]pyridine sca
HETEROARYLAMINOISOQUINOLINES, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF
-
Page/Page column 103; 104, (2016/08/23)
The application is directed to compounds of formula (IA) : and specifically compounds of formula (I) and their salts and solvates, wherein R1, R11, R12, R13, R4, R5, n, A1, A2, and A3 are as set forth in the specification, as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of conditions associated with the alteration of the activity of β-galactosidase, specially galactosidase beta-1 or GLB1, including GM1 gangliosidoses and Morquio syndrome, type B.
PLATELET ADP RECEPTOR INHIBITORS
-
Paragraph 0132, (2016/08/17)
no abstract published
TYK2 INHIBITORS AND USES THEREOF
-
Paragraph 001167; 001168, (2015/09/28)
The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
Azonia Aromatic Cations by Ring-Closing Metathesis: Synthesis of Azaquinolizinium Cations
Abeng?zar, Alberto,Abarca, Beatriz,Cuadro, Ana M.,Sucunza, David,álvarez-Builla, Julio,Vaquero, Juan J.
, p. 4214 - 4223 (2015/06/30)
A strategy based on a ring-closing metathesis (RCM) reaction of pyridinium azadienes in the presence of the second generation Grubbs catalyst was employed as a new approach to synthesize the 1-azaquinolizinium (pyrido[1,2-a]pyrimidin-5-ium) heterocycle and some simple derivatives. This method was also successfully applied to the first reported synthesis of the benzo-1-azaquinolizinium (pyrimido[2,1-a]isoquinolinium) cation by using the Hoveyda-Grubbs catalyst in Cl2CHCHCl2 at 130 C.
TRICYCLIC ALKYNES THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN
-
Page/Page column 68, (2014/03/25)
The present invention relates to tricyclic alkyne compounds of formula I 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 gluco
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N′-arylpiperazine series
Nishimura, Nobuko,Norman, Mark H.,Liu, Longbin,Yang, Kevin C.,Ashton, Kate S.,Bartberger, Michael D.,Chmait, Samer,Chen, Jie,Cupples, Rod,Fotsch, Christopher,Helmering, Joan,Jordan, Steven R.,Kunz, Roxanne K.,Pennington, Lewis D.,Poon, Steve F.,Siegmund, Aaron,Sivits, Glenn,Lloyd, David J.,Hale, Clarence,St. Jean, David J.
supporting information, p. 3094 - 3116 (2014/05/06)
We have recently reported a novel approach to increase cytosolic glucokinase (GK) levels through the binding of a small molecule to its endogenous inhibitor, glucokinase regulatory protein (GKRP) these initial investigations culminated in the identification of 2-(4-((2S)-4-((6-amino-3- pyridinyl)sulfonyl)-2-(1-propyn-1-yl)-1-piperazinyl)phenyl)-1,1,1,3,3, 3-hexafluoro-2-propanol (1, AMG-3969), a compound that effectively enhanced GK translocation and reduced blood glucose levels in diabetic animals. Herein we report the results of our expanded SAR investigations that focused on modifications to the aryl carbinol group of this series. Guided by the X-ray cocrystal structure of compound 1 bound to hGKRP, we identified several potent GK-GKRP disruptors bearing a diverse set of functionalities in the aryl carbinol region. Among them, sulfoximine and pyridinyl derivatives 24 and 29 possessed excellent potency as well as favorable PK properties. When dosed orally in db/db mice, both compounds significantly lowered fed blood glucose levels (up to 58%).
SULFONYL COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN
-
Page/Page column 59; 60, (2013/08/28)
The present invention relates to sulfonyl 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.
Imidazopyridine derivatives as PI3K inhibitors
-
Page/Page column 41, (2012/11/13)
New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)
IMIDAZOPYRIDINE DERIVATIVES AS PI3K INHIBITORS
-
Page/Page column 95, (2012/11/13)
New imidazopyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).