115891-09-3Relevant articles and documents
FUSED CYCLIC UREA DERIVATIVES AS CRHR2 ANTAGONIST
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Paragraph 0525, (2019/11/04)
The present invention relates to fused cyclic urea derivatives which have antagonistic activities against CRHR1 and/or CRHR2, and which are useful in the treatment or prevention of disorders and diseases in which CRHR1 and/or CRHR2 is involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CRHR1 and/or CRHR2 is involved.
Potential Anticancer Benzo-naphthyridones with Fused Rings: a Theoretical Model for Predicting Orientation in the Cyclization of Intermediates
Mefetah, Hafid,Brouant, Pierre,Galy, Anne-Marie,Galy, Jean-Pierre,Barbe, Jacques
, p. 522 - 533 (2007/10/03)
Synthesis of benzo[b]-1,8-naphthyridine-5-ones with fused ring from halonicotinic acids and amino-substituted benzoheterocycles, leads either to an isomeric mixture or to single isomers. MO calculations conducted on the starting amino-substituted benzoheterocycles, allow predictions of the derivative(s) to be obtained. Some selected compounds belonging to this series were screened in vitro against several human tumor cell lines.
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.
Naphthyridine and pyridopyrazine compounds and pharmaceutical usage thereof
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, (2008/06/13)
Certain substituted 1,8-naphthyridines and 1,5,8-azanaphthyridines of formula I are disclosed which are useful for treating allergy or inflammation in mammals. A preferred use is the treatment of chronic obstructive lung disease in mammals. The compounds have the formula, wherein X is CH or N;, R1 represents alkenyl, alkynyl, cycloalkyl, cycloalkenyl, 2-, 3- or 4- pyridinyl, 2-, 4- or 5- pyrimidinyl, 2- or 3- thienyl, 2- or 3-furanyl, alkyl carbonyl, phenyl carbonyl or alkyl, each of which may be substituted with -COOH, hydroxy, halogen, alkoxy phenyl, 2-, 3-, or 4- pyridinyl, 2-, 4- or 5-pyrimidinyl, 2- or 3-thienyl, 2- or 3- furanyl, alkyl carbonyl, phenyl carbonyl, cycloalkyl, formyloxy, alkyl carbonyloxy, or phenyl carbonyloxy;, R2 represents hydrogen, hydroxyalkyl, dihydroxyalkyl, hydroxyalkoxyalkyl, a cation, alkenyl having, R aR bN(CH2) n-(wherein R aand R bare hydrogen or alkyl and n is an integer from 2 to 6), alkynyl or a group of the general formula: where Z = 0 or 1; p is an integer of 0 to 5, R3 and R4 are each alkyl or R3 and R4 together form a cycloalkyl up to 6 carbon atoms, and M is H or where Y1, Y2 and Y3 represent hydrogen, hydroxy, halogen, alkyl, alkoxy, halogenated alkyl; and, A is 2-, 3- or 4-biphenyl, 1- or 2-naphthylenyl, 4- or 5-indenyl, 4- or 5- indanyl, 2-, 3-, 4-, 5-, 6-, 7-or 8-quinolinyl, 1-, 3-, 4-, 5-, 6-, 7- or 8-isoquinolinyl, 2-, 3- or 4-pyridinyl, 2-, 4- or 5-pyrimidinyl, 2-pyrazinyl, 3- or 4-pyridazinyl, 3-, 5- or 6-(1,2,4-triazinyl), 2- or 3-furanyl, 2- or 3-thienyl, 2-, 3-, 4-, 5-, 6- or 7-benzofuranyl, 3- 4- or 5-pyrazolyl, 3- or 5-(1,2,4-triazolyl) each of which may be substituted with one or more of hydroxy, alkyl, halogen, nitro, alkoxy, trifluoromethyl or cyano.
