15506-18-0

Upstream product

• 124-41-4 sodium methylate 
• 74-88-4 methyl iodide 
• 609-71-2 2-hydroxy-3-carboxypyridine 
• 74-83-9 methyl bromide 
• 10128-91-3 methyl-2-oxo-1,2-dihydro-3-pyridinecarbonitrile 
• 609-71-2 1,2-dihydro-2-oxonicotinic acid 
• 67367-27-5 methyl 1-methyl-2-oxo-1,2-dihydropyridine-3-carboxylate 
• 98-92-0 nicotinamide 
• 6456-44-6 N-methylnicotineamide iodide 
• 61856-47-1 3-formyl-1-methyl-2(1H)-pyridinethione 
• 769-09-5 1-methyl-2-oxopyridine-3-carboxamide 
• 13362-27-1 2-imino-1-methyl-1,2-dihydro-pyridine-3-carboxylic acid 

Downstream Products

• 84854-00-2 1-Methyl-2-oxo-1,2-dihydro-pyridine-3-carbonyl chloride 
• 863395-25-9 1,1'-dimethyl-3,3'-(N-benzyliminodicarbonyl)di-2-pyridone 

Relevant academic research and scientific papers

Rhodium-Catalyzed C4-Selective C-H Alkenylation of 2-Pyridones by Traceless Directing Group Strategy

A rhodium-catalyzed C4-selective C-H alkenylation of 3-carboxy-2-pyridones with styrenes has been developed. The carboxylic group at the C3 position works as the traceless directing group, and the corresponding C4-alkenylated 2-pyridones are obtained exclusively with concomitant decarboxylation. Unlike the reported procedures, the exclusive C4 selectivity is uniformly observed even in the presence of potentially more reactive C-H bonds at the C5 and C6 positions. By using this strategy, the multiply substituted 2-pyridone can be prepared via sequential C-H functionalization reactions.

IMMUNOMODULATORY COMPOUNDS

Disclosed are immunomodulatory compounds, pharmaceutical compositions containing them, and methods of making and using the compounds to treat diseases and disorders characterized by aberrant protein activity that can be targeted by cereblon.

USE OF MORPHINAN DERIVATIVES FOR TREATMENT OF OPIOID RECEPTOR AGONIST-RELATED DISEASES

The present invention relates to a pharmaceutical composition comprising a morphinan derivative that exhibits an opioid δ receptor agonist activity. By administering the pharmaceutical composition provided by the present invention, opioid δ receptor-related diseases (for example, headache) can be treated or prevented.

MORPHINAN DERIVATIVE

A morphinan derivative represented by the following general formula (I): (wherein R1 represents hydrogen, C1-10 alkyl, cycloalkylalkyl where the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms, etc., R2 represents heterocyclic ring containing 1 to 4 heteroatoms selected from N, O and S and at least one carbon atom as ring-constituting atoms, containing at least one set of adjacent ring-constituting atoms bound by a double bond, and further substituted with at least one oxo group, Y binds to a carbon atom as a ring-constituting atom of R2, R3, R4, and R5 represent hydrogen; hydroxy, etc., R6a and R6b represent hydrogen, etc., R7 and R8 represent hydrogen, etc., R9 and R10, which are the same or different, represent hydrogen, etc., X represents O or CH2, and Y represents C(=O)), a tautomer or stereoisomer of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof is used as an anxiolytic drug, antidepressant, etc.

ARYLHYDRAZIDES CONTAINING A 2-PYRIDONE MOIETY AS SELECTIVE ANTIBACTERIAL AGENTS

The present invention belongs to the field of antibacterial agents, more specifically to antibacterials for treating Acinetobacter baumannii infections. The invention provides arylhydrazides containing a 2-pyridone moiety, according to formula (I), which

Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor

Bioisosteric replacement of acylureido moiety in 6-acylureido-3- pyrrolylmethylidene-2-oxoindoline derivatives resulted in a series of malonamido derivatives with indolin-2-one scaffold (11-14). Further conformational restrictions of the malonamido moiety led to 2-oxo-1,2-dihydropyridine (21-25) or a 4-oxo-1,4-dihydropyridine derivatives (31-36). 4-Oxo-1,4-dihydropyridine derivatives were more potent Aurora B inhibitors than their 2-oxo-1,2- dihydropyridine counterparts and demonstrated cytotoxicities against A549 and HepG2 cells in the submicromolar range. In A549 cells, 31h decreased phosphorylation of histone H3, triggered polyploidy, induced expression of pro-apoptotic Fas and FasL with subsequent activation of caspase 8, resulting into apoptosis. In a Huh7-xenograft mouse model, 31h demonstrated potent in vivo efficacy with a daily dose of 5 mg/kg.

MODULATORS OF C3A RECEPTOR AND METHODS OF USE THEREOF

Provided are compounds that are modulators of C3a receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, the compounds are pyridones. In certain embodiments, provided are methods for treatment or amelioration of diseases associated with modulation of C3a receptor activity.

Heterobicyclic thiophene compounds and methods of use

Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

Heterobicyclic pyrazole compounds and methods of use

Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

NOVEL DIAZASPIROALKANES AND THEIR USE FOR TREATMENT OF CCR8 MEDIATED DISEASES

The invention provides compounds of general formula (I) wherein A, B, p, w, x, y, and z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.