477251-79-9

Upstream product

• 477251-78-8 1-(3-Bromophenyl)-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxylic Acid 
• 75-31-0 isopropylamine 
• 477251-77-7 ethyl 1-(3-bromophenyl)-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxylate 
• 701977-68-6 Ethyl 3-(3-Bromoanilino)-2-(2-Chloronicotinoyl) Acrylate 
• 220731-02-2 ethyl 3-(2-chloropyridin-3-yl)-3-oxopropionate 
• 591-19-5 m-Bromoaniline 
• 543-27-1 isobutyl chloroformate 

Downstream Products

• 477251-76-6 N-Isopropyl-1-[3-(3-acetylphenyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 
• 477252-06-5 N-Isopropyl-1-[3-(3-acetyl-4-hydroxyphenyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 
• 702640-76-4 N-Isopropyl-1-[3-(4,4,5,5,-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 
• 477252-07-6 N-isopropyl-1-[3-(5-carboethoxypyridin-3-yl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 
• 500355-51-1 N-isopropyl-1-[3-(3-hydroxy-3-phenylbut-1-ynyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 
• 500355-37-3 N-isopropyl-1-[(3-phenylethynyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 

Relevant academic research and scientific papers

Alternative Forms of the Phosphodiesterase-4 Inhibitor N-Cyclopropyl-1--4-Oxo-1,4-Dihydro-1,8-Naphthyridine-3-Carboxyamide

The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below:

Optimization and structure-activity relationship of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides: Identification of MK-0873, a potent and effective PDE4 inhibitor

A SAR study of a series of 1-phenyl-1,8-naphthyridin-4-one-3-carboxamides is described. Optimization of the series was based on in vitro potency against PDE4, inhibition of the LPS-induced production of TNF-α in human whole blood and minimizing affinity f

ALTERNATIVE FORMS OF THE PHOSPHODIESTERASE-4 INHIBITOR N-CYCLOPROPYL-1-{3-[(1-OXIDOPRYIDIN-3-YL)ETHYNYL]PHENYL}-4-OXO-1,4-DIHYDRO-1,8-NAPHTHYRIDINE-3-CARBOXYAMIDE

The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below: Compound IX

METHOD OF PREPARING INHIBITORS OF PHOSPHODIESTERASE-4

In one aspect, the present invention is directed to a one pot method of preparing intermediates of Formula V, which are useful in making inhibitors of phosphodiesterase-4: The present invention is also directed to a method of preparing phosphodiesterase inhibitors comprising the Formula

4-OXO-1-(3-SUBSTITUTED PHENYL-1,4-DIHYDRO-1,8-NAPHTHYRIDINE-3-CARBOXAMIDE PHOSPHODIESTERASE-4 INHIBITORS

Compounds represented by Formula (I):or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation and useful for the enhancement of cognition.

1-biaryl-1,8-naphthyridin-4-one phosphodiesterase-4 inhibitors

Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterrase 4 inhibitors useful in the treatment of asthma and inflammation.

Alkyne-aryl phosphodiesterase-4 inhibitors

Compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, are phosphodiesterase 4 inhibitors useful in the treatment of asthma and inflammation.