105326-56-5Relevant academic research and scientific papers
NAPHTHALENE DERIVATIVE
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Paragraph 0616, (2013/06/27)
The present invention provides compounds which can regulate VCP activity. The present invention provides the compound of formula (I) (R is as defined in the description) or oxides, esters, prodrugs, pharmaceutically acceptable salts or solvates thereof. The compounds can regulate VCP activity, and thus are useful for treating VCP-mediated diseases such as neurodegenerative diseases.
2-quinolinyl methoxy compounds, medical uses and intermediates therefor
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, (2008/06/13)
The present invention relates to compounds of formula STR1 in which formula I X stands for O, S, STR2 R1 and R2 which can be the same or different stand for hydrogen, straight or branched, saturated or unsaturated, unsubstituted or substituted C1- C8 -alkyl, aryl or for ar-C1 -C4 -alkyl, aryl and ar being unsubstituted or substituted phenyl; R3, R4, R5, and R6 are the same or different and stand for hydrogen, halogen, pseudo halogen, cyano, nitro, amino, carboxy, hydroxy, alkyl, alkoxy; or R5 and R6 form an aromatic ring which is fused to the pyridyl ring, and which aromatic ring may substituted; provided that R1 and R2 cannot be hydrogen at the same time, and provided that when R5 and R6 both are chlorine and R1 is hydrogen, then R2 cannot be n-propyl; and salts and bioreversible derivatives thereof. The compounds of formula I are useful in the human and veterinary therapy, as they exert specific 5-lipoxygenase inhibition.
Pyridyl and quinoline derivatives
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, (2008/06/13)
The present invention relates to compounds of formula I STR1 in which formula I X stands for O, S, STR2 R1 and R2 which can be the same or different stand for hydrogen, straight or branched, saturated or unsaturated, unsubstituted or
Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters.
Musser,Kubrak,Chang,DiZio,Hite,Hand,Lewis
, p. 400 - 405 (2007/10/02)
A series of novel benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters has been prepared. These compounds were tested as inhibitors of rat polymorphonuclear leukocyte 5-lipoxgenase (LO) in vitro and as inhibitors of leukotriene D4 (LTD4) and ovalbumin (OA) induced bronchospasm in the guinea pig (GP) in vivo. In general, inhibitory activity against 5-LO, LTD4, and OA was broadest for benzthiazole-containing analogues (benzthiazole greater than benzimidazole much greater than benzoxazole, benzofuran). The most potent 5-LO inhibitor, 4-[[3-(2-benzthiazolylmethoxy)-phenyl]hydroxyamino]-4-oxobutanoic acid methyl ester (7), had an IC50 of 0.36 microM. Compound 7, however, was inactive vs. OA. The most potent compound in vivo, 4-[[3-[(1-methyl-2-benzimidazolyl)methoxy]phenyl]-amino] -4-oxobutanoic acid methyl ester 4, inhibited both LTD4- and OA-induced bronchospasm by 83% and 60%, respectively, at 50 mg/kg intraduodenally. Compound 4 was studied in the Ames assay employing five strains of bacteria (TA1535, TA1537, TA1538, TA98, and TA100) with and without S-9 rat liver enzyme metabolic activation, and there was no significant number of reversions noted.
