123723-93-3Relevant academic research and scientific papers
CYANOMETHYLPYRIDINE DERIVATIVES
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, (2008/06/13)
The present invention relates to new cyanomethylpyridine dervatives of formula I wherein Y represents N or CH;R1 represents hydrogen, fluoro, chloro, difluoro or dichloro; R2 represents hydrogen or C1-4alkyl;n is 0 or 1; p is 0 or 1; A represents a covalent bond or a group of formula -CONHC-H(Ar)-, -NHCH(Ar)-, -S02NHCH(Ar)-,NHCONHCH(Ar) or OCONHCH(Ar),and when p is 1,A can also represent CH(Ar)NH; and AT represents phenyl or phenyl substituted with halogen,C M alkyl, C1-4 alkoxy or trifluoromethyl. These compounds are PAF antagonist and/or 5-lipoxygenase inhibitors.
ARYL AND HETEROARYLMETHOXYPHENYL INHIBITORS OF LEUKOTRIENE BIOSYNTHESIS
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, (2008/06/13)
The present invention relates to a compound of the formula or a pharmaceutically acceptable salt thereof wherein W is selected from optionally substituted pyridyl, naphthyl, and quinolyl; which inhibits lipoxygenase enzyme activity and leukotriene biosynt
(Quinolin-2-yl-methoxy)phenylacetic acid derivatives containing cyclic substituents
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, (2008/06/13)
For inhibiting lipoxygenzce, (quinolin-2-yl-methoxy) phenylacetic acid derivatives containing cyclic substituents of the formula STR1 in which A, Q, D, E, G, T and M are hydrogen or various radicals, R3 is halogen or an alkyl or phenyl radical,
N- Carboxylic Acids, Hydroxamic Acids, Tetrazoles, and Sulfonyl Carboxamides. Potent Orally Active Leukotriene D4 Antagonists of Novel Structure
Musser, John H.,Kreft, Anthony F.,Bender, Reinhold H. W.,Kubrak, Dennis M.,Grimes, David,et al.
, p. 240 - 245 (2007/10/02)
Four series of N- compounds were prepared as leukotriene D4 (LTD4) antagonists.In the hydroxamic acid series, methyl 3-(2-quinolinylmethoxy)benzeneacetohydroxamate (Wy-48,422, 20) was the most potent inhibitor of LTD4-induced bronchoconstriction with an oral ED50 of 7.9 mg/kg.Compound 20 was also orally inhibited ovalbumin-induced bronchoconstriction in the guinea pig with an ED50 of 3.6 mg/kg.In vitro, against LTD4-induced contraction of isolated guinea pig trachea pretreated with indomethacin and 1-cysteine, 20 produced a pKB value of 6.08.In the sulfonyl carboxamide series, N--3-(2-quinolinylmethoxy)-benzamide (Wy-49,353, 30) was the most potent antagonist.Compound 30 orally inhibited both LTD4- and ovalbumin-induced bronchoconstriction with ED50s of 0.4 and 20.2 mg/kg, respectively.In vitro, against LTD4-induced contraction of isolated guinea pig trachea, 30 produced a pKB value of 7.78.In the carboxylic acid series, which served as intermediates for the above two series, 3-(2-quinolinylmethoxy)benzeneacetic acid (Wy-46,016, 5) was the most potent inhibitor of LTD4-induced bronchoconstriction (99percent at 25 mg/kg, intraduodenally); however, the pKB for this compound was disappointing (5.79).In the tetrazole series, the most potent inhibitor was 2-methyl>quinoline (Wy-49,451, 41).The respective inhibitory ED50s were 3.0 mg/kg versus LTD4 and 17.5 mg/kg versus ovalbumin.In the isolated guinea pig trachea, 41 produced a pKB value of 6.70.
α-substituted 4-(quinolin-2-yl-methoxy)phenylacetic acids and esters and lipoxygenase inhibition therewith
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, (2008/06/13)
As lipoxygenase inhibitors, the novel α-substituted 4-(quinolin-2-yl-methoxy)phenyl-acetic acid and esters thereof of the formula STR1 in which R1 - stands for hydrogen, alkyl, arylalkyl, aryl or - for a group of the formula where R3 - stands for hydrogen, alkyl, arylalkyl or aryl and R2 - stands for hydrogen, alkyl, alkenyl or alkinyl, and salts thereof.
Substituted 4-(quinolin-2-yl-methoxy)phenyl-acetic acid derivatives and anti-allergic use thereof
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, (2008/06/13)
Leucotriene synthesis inhibiting substituted 4-(quinolin-2-yl-methoxy)phenyl-acetic acid derivatives of the formula STR1 R1 --represents a group of the formula STR2 wherein Y--represents a group of the formula STR3 Z--represents norbornyl, or represents a group of the formula STR4 and A and B are identical or different and denote hydrogen, lower alkyl or halogen, and salts thereof.
