915949-00-7

Upstream product

• 124-40-3 dimethyl amine 
• 88625-23-4 5-chloropyrazine-2-carbonyl chloride 
• 506-59-2 N,N-dimethylammonium chloride 
• 36070-80-1 5-chloropyrazinoic acid 

Downstream Products

• 1020668-74-9 methyl 3-[5-(dimethylcarbamoyl)pyrazin-2-yl]oxy-5-hydroxy-benzoate 
• 1020668-62-5 5-[3-[(2S)-1-(difluoromethoxy)propan-2-yl]oxy-5-[(1-methylpyrazol-3-yl)carbamoyl]phenoxy]-N,N-dimethyl-pyrazine-2-carboxamide 
• 1020668-68-1 methyl 5-[(2S)-1-(difluoromethoxy)propan-2-yl]oxy-3-[5-(dimethylcarbamoyl)pyrazin-2-yl]oxy-benzoate 
• 1020668-71-6 methyl 3-[5-(dimethylcarbamoyl)pyrazin-2-yl]oxy-5-[(2S)-1-tripropan-2-ylsilyloxypropan-2-yl]oxy-benzoate 
• 1020668-59-0 5-[3-[(2S)-1-(difluoromethoxy)propan-2-yl]oxy-5-[(5-methylpyrazin-2-yl)carbamoyl]phenoxy]-N,N-dimethyl-pyrazine-2-carboxamide 
• 1020855-39-3 methyl 3-[5-(dimethylcarbamoyl)pyrazin-2-yl]oxy-5-[(3S)-1-methyl-2-oxo-pyrrolidin-3-yl]oxy-benzoate 
• 1352570-06-9 N,N-dimethyl-5-(3-(1-methyl-2-oxopyrrolidin-3-yloxy)-5-(6-oxo-1,6-dihydropyrimidin-yl)phenoxy)pyrazine-2-carboxamide 
• 1352571-64-2 C₂₈H₂₉N₅O₅ 
• 1352570-13-8 5-(3-isopropoxy-5-(6-oxo-1,6-dihydropyrimidin-2-yl)phenoxy)-N,N-dimethylpyrazine-2-carboxamide 
• 1352571-67-5 C₂₈H₂₉N₅O₆ 
• 1352570-02-5 (S)-5-(3-(1-hydroxypropan-2-yloxy)-5-(6-oxo-1,6-dihydropyrimidin-2-yl)phenoxy)-N,N-dimethylpyrazine-2-carboxamide 
• 915949-01-8 methyl 3-[5-(dimethylcarbamoyl)pyrazin-2-yl]oxy-5-[(2S)-1-methoxypropan-2-yl]oxy-benzoate 

Relevant academic research and scientific papers

SUBSTITUTED N-(METHYL-D3)PYRIDAZINE-3-CARBOXAMIDE OR N-(METHYL-D3)-NICOTINAMIDE COMPOUNDS AS IL-12, IL-23 AND/OR IFNALPHA MODULATORS

There are disclosed compounds of the following formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating inflammatory and autoimmune diseases or disorders.

HETEROCYCLIC COMPOUNDS COMPRISING PYRIDINE USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES

Compounds having the following formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

TYK2 INHIBITORS AND USES THEREOF

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.

Benzoxaborole Antimalarial Agents. Part 4. Discovery of Potent 6-(2-(Alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles

A series of 6-hetaryloxy benzoxaborole compounds was designed and synthesized for a structure-activity relationship (SAR) investigation to assess the changes in antimalarial activity which result from 6-aryloxy structural variation, substituent modification on the pyrazine ring, and optimization of the side chain ester group. This SAR study discovered highly potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles (9, 27-34) with IC50s = 0.2-22 nM against cultured Plasmodium falciparum W2 and 3D7 strains. Compound 9 also demonstrated excellent in vivo efficacy against P. berghei in infected mice (ED90 = 7.0 mg/kg).

IMIDAZOPYRIDAZINE COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES

Compounds having the following formula (I), or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of Type 2 diabetes mellitus

Glucokinase activators represent a promising potential treatment for patients with Type 2 diabetes. Herein, we report the identification and optimization of a series of novel indazole and pyrazolopyridine based activators leading to the identification of 4-(6-(azetidine-1-carbonyl)-5-fluoropyridin-3- yloxy)-2-ethyl-N-(5-methylpyrazin-2-yl)-2H-indazole-6-carboxamide (42) as a potent activator with favorable preclinical pharmacokinetic properties and in vivo efficacy.

2-(3,5-DISUBSTITUTEDPHENYL)PYRIMIDIN-4(3H)-ONE DERIVATIVES

O N NH R3 R2 O R1 168 ABSTRACT The present invention provides a 2-(3,5-disubstitutedphenyl)pyrimidin- 4(3H)-one compound of Formula (I) 5 (I) or a pharmaceutically acceptable salt thereof wherein R 1, R2 and R3 are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and 10 the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.

MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmacetical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.

SUBSTITUTED INDAZOLE AMIDES AND THEIR USE AS GLUCOKINASE ACTIVATORS

The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R4, R6, X, Y and Z are as defined herein. The compounds of Formula (I) have been found to act as glucokinase activators. Consequently, the compounds of Formula (I) and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucokinase.

Benzofuranyl Derivatives

The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.