89660-14-0Relevant academic research and scientific papers
COMBINATIONS COMPRISING BENZODIOXOL AS GLP-1R AGONISTS FOR USE IN THE TREATMENT OF NASH/NAFLD AND RELATED DISEASES
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Page/Page column 149; 150, (2020/12/07)
In part, the invention provides a new combination comprising (1) a GLP-1R agonist and (2) an ACC inhibitor or a DGAT2 inhibitor, or a KHK inhibitor or FXR agonist. The invention further provides new methods for treating diseases and disorders, for example, fatty liver, nonalcoholic fatty liver disease, nonalcoholic steatohepatitis, nonalcoholic steatohepatitis with liver fibrosis, nonalcoholic steatohepotitis with cirrhosis, and nonalcoholic steatohepatitis with cirrhosis and with hepatocellular carcinoma or with a metabolic-related disease, obesity, and type 2 diabetes, for example, using the new combination described herein.
GLP-1 Receptor Agonists and Uses Thereof
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Paragraph 0493; 0495, (2020/01/04)
Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
GLP-1 RECEPTOR AGONISTS AND USES THEREOF
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Page/Page column 86, (2020/01/08)
Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza- benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
GLP-1 Agonists and Uses Thereof
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Paragraph 0443, (2018/07/05)
Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, 7-aza- and 4,7-diaza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
NEW IMIDAZO[4,5-B]PYRIDINE DERIVATIVES AS DUAL DYRK1/CLK1 INHIBITORS
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Page/Page column 31, (2017/05/07)
(Formula I) Compounds of formula (I) usefull for the treatment of cancer, neurodegenerative disorders and metabolic disorders.
Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis
Layton, Mark E.,Reif, Alexander J.,Hartingh, Timothy J.,Rodzinak, Kevin,Dudkin, Vadim,Wang, Cheng,Arrington, Ken,Kelly, Michael J.,Garbaccio, Robert M.,O'Brien, Julie A.,Magliaro, Brian C.,Uslaner, Jason M.,Huszar, Sarah L.,Fillgrove, Kerry L.,Tang, Cuyue,Kuo, Yuhsin,Jacobson, Marlene A.
supporting information, p. 1260 - 1264 (2016/02/23)
Optimization of a benzimidazolone template for potency and physical properties revealed 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as a key template on which to develop a new series of mGlu2 positive allosteric modulators (PAMs). Systematic invest
Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI
Pero, Joseph E.,Rossi, Michael A.,Kelly, Michael J.,Lehman, Hannah D. G. F.,Layton, Mark E.,Garbaccio, Robert M.,O'Brien, Julie A.,Magliaro, Brian C.,Uslaner, Jason M.,Huszar, Sarah L.,Fillgrove, Kerry L.,Tang, Cuyue,Kuo, Yuhsin,Joyce, Leo A.,Sherer, Edward C.,Jacobson, Marlene A.
supporting information, p. 312 - 317 (2016/03/22)
Investigation of a novel amino-aza-benzimidazolone structural class of positive allosteric modulators (PAMs) of metabotropic glutamate receptor 2 (mGluR2) identified [2.2.2]-bicyclic amine 12 as an intriguing lead structure due to its promising physicochemical properties and lipophilic ligand efficiency (LLE). Further optimization led to chiral amide 18, which exhibited strong in vitro activity and attractive pharmacokinetic (PK) properties. Hypothesis-driven target design identified compound 21 as a potent, highly selective, orally bioavailable mGluR2 PAM, which addressed a CYP time-dependent inhibition (TDI) liability of 18, while maintaining excellent drug-like properties with robust in vivo activity in a clinically validated model of antipsychotic potential.
PRMT5 INHIBITORS AND USES THEREOF
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Paragraph 00395, (2014/07/08)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described
Pyrazolopyrrolidine Derivatives and their Use in the Treatment of Disease
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Paragraph 0952; 0953; 1015; 1016, (2014/12/09)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
PYRAZOLOPYRROLIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF DISEASE
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Page/Page column 193; 194; 209, (2014/12/12)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
