220731-04-4Relevant articles and documents
HETEROARYLAMINOISOQUINOLINES, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF
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, (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
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, (2016/08/17)
no abstract published
TYK2 INHIBITORS AND USES THEREOF
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, (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.
TRICYCLIC ALKYNES THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN
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, (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.
, 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
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, (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
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, (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
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, (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).
PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES AND THEIR USE IN CANCER THERAPY
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Page/Page column 54, (2011/02/15)
Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula I, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
Novel RGD peptidomimetics embedding 1,2,3-triazole as central scaffold; Synthesis and αvβ 3 integrin affinity
Ni, Ming Hong,Esposito, Emiliano,Castorina, Massimo,Pozzo, Alma Dal
scheme or table, p. 401 - 405 (2012/06/16)
Ten new RGD (Arginine-Glycine-Aspartic acid) peptidomimetics have been synthesized and screened for their affinity to αvβ 3 integrin receptor. Arginine and Aspartic acid mimetic subunits were connected through 1,2,3-triazole as central scaffold by click chemistry, affording the final products with good yields. Among them, compounds 3f-j exhibited high affinity to the receptor,with IC50 in the low nanomolar range, comparable to that of the reference compound Cilengitide.