102625-91-2

Upstream product

• 35392-66-6 5-methoxy-2-methylpyridine-1-oxide 
• 1121-78-4 5-Hydroxy-2-methylpyridine 
• 55270-47-8 5-methoxy-2-picoline 
• 124-41-4 sodium methylate 
• 113209-88-4 5-fluoro-2-methyl-4-nitropyridine 1-oxide 

Downstream Products

• 1448870-51-6 4-bromo-5-methoxy-2-methyl-pyridine 1-oxide 
• 1256804-48-4 4-bromo-5-methoxy-2-methyl-pyridine 
• 62885-49-8 4,5-Dimethoxy-2-hydroxymethylpyridin 

Relevant academic research and scientific papers

CHROMEN-4-ONE DERIVATIVES, SUCH AS E.G. FLAVONES, FOR USE AS CK2 INHIBITORS FOR THE TREATMENT OF NEUROINFLAMMATION

Chromen-4-one derivatives, such as e.g. flavone derivatives and pharmaceutical compositions thereof are disclosed. In some instances, the compounds have increased aqueous solubility, bioavailability, and ability to cross the blood-brain-barrier. The compounds may be used to inhibit casein kinase 2 (CK2) activity and/or to treat diseases and conditions mediated at least in part by CK2 enzyme, such as e.g. inflammation, in particular neuroinflammation, or other diseases, such as e.g. cancer, cardiac hypertrophy, cystic fibrosis, a neurodegenerative disease, bipolar disorder, depression, a viral infection, obesity, diabetes mellitus, atherosclerosis, epilepsy, or any combination thereof.

NEW 6-MEMBERED HETEROAROMATIC SUBSTITUTED CYANOINDOLINE DERIVATIVES AS NIK INHIBITORS

The present invention relates to pharmaceutical agents of formula (I), useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-KB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

IMIDAZOPYRROLIDINONE COMPOUNDS

The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.

PYRROLOPYRROLIDINONE COMPOUNDS

The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.

(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate

[(Pyridylmethyl)sulfinyl]benzimidazoles 1 (PSBs) are a class of highly potent antisecretory (H+,K+)-ATPase inhibitors which need to be activated by acid to form their active principle, the cyclic sulfenamide 4. Selective inhibitors of the (H+,K+)-ATPase in vivo give rise to the nonselective thiophile 4 solely at low pH, thus avoiding interaction with other thiol groups in the body. The propensity to undergo the acid-catalyzed transformation is dependent on the nucleophilic/electrophilic properties of the functional groups involved in the formation of 2 since this step is both rate-determining and pH-dependent. The aim of this study was to identify compounds with high (H+,K+)-ATPase inhibitory activity in stimulated gastric glands possessing acidic pH, but low reactivity (high chemical stability) at neutral pH as reflected by in vitro (Na+,K+)-ATPase inhibitory activity. The critical influence of substituents flanking the pyridine 4-methoxy substituent present in all derivatives was carefully studied. The introduction of a 3-methoxy group gave inhibitors possessing a combination of high potency, similar to omeprazole and lansoprazole, but increased stability. As a result of these studies, compound 1a (INN pantoprazole) was selected as a candidate drug and is currently undergoing phase III clinical studies.

Fluoroalkoxy substituted benzimidazoles useful as gastric acid secretion inhibitors

Dialkoxypyridines of formula I STR1 wherein R1 is 1-3C-alkyl which is completely or predominantly substituted by fluorine, or a chlorodifluoromethyl radical and R1' is hydrogen, halo, trifluoromethyl, 1-3C-alkyl, or 1-3C-alkoxy which is optionally completely or predominantly substituted by fluorine, or R1 and R1', together with the oxygen atom to which R1 is bonded, are 1-2C-alkylenedioxy, which is optionally completely or partly substituted by fluorine, or chlorotrifluoroethylenedioxy, R3 is 1-3C-alkoxy, one of R2 and R4 is 1-3C-alkoxy and the other is a hydrogen atom or 1-3C-alkyl and n is 0 or 1, and salts thereof are new compounds with a pronounced protective action on the stomach. Processes for preparing these compounds, medicaments containing them and their use, as well as intermediate compounds and their use for preparing the subject dialkoxypyridines, are disclosed.

Picoline derivative useful as gastric acid secretion inhibitors

Picoline derivatives of the formula I STR1 wherein the substituents have the meanings given in the description, and their salts are new compounds having a pronounced protective action on the stomach.