115891-34-4Relevant academic research and scientific papers
Naphthyridinone derivatives
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, (2008/06/13)
Compounds of formula I STR1 including pharmaceutically acceptable salts thereof in which R1 represents a phenyl C1-6 alkyl group (in which the phenyl ring is optionally substituted by one or more of the following: halo, a C1-4 alkyl group, a C1-4 alkoxy group, hydroxy or trifluoromethyl) and the alkyl chain is optionally substituted by one or more C1-2 alkyl groups; R2 represents a C2-6 alkoxycarbonyl group; and R3 represents hydrogen or halo are disclosed, which are antirheumatic agents and are useful as modulators of cytokine synthesis, immunomodulatory agents, antiinflammatory agents and anti-allergic agents. Compositions containing these compounds and processes to make these compounds are also disclosed.
Antiallergy Agents. 1. Substituted 1,8-Naphthyridin-2(1H)-ones as Inhibitors of SRS-A Release
Sherlock, Margaret H.,Kaminski, James J.,Tom, Wing C.,Lee, Joe F.,Wong, Shing-Chun,et al.
, p. 2108 - 2121 (2007/10/02)
A novel class of antiallergy agents, the substituted 1,8-naphthyridin-2(1H)-ones, is described.The present compounds are orally active, potent inhibitors of allergic and nonallergic bronchospasm in animal models.Structure-activity studies of the lead compound in this sereis, 1-phenyl-3-n-butyl-4-hydroxynaphthyridin-2(1H)-one (11), identified three compounds of interest, 1-phenyl-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one (12), 1-(3'-chlorophenyl)-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one (87), and 1-(3'-methoxyphenyl)-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one (89).The mechanism of antiallergy activity may involve inhibition of the release of the sulfidopeptide leukotrienes. 1-Phenyl-3-(2-propenyl)-4-acetoxy-1,8-naphthyridin-2(1H)-one, Sch 33303 (12), was selected for preclinical development as an antiallergy agent.
