122957-08-8Relevant academic research and scientific papers
1,4-DIHYDROPYRIDINE DERIVATIVES
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, (2008/06/13)
A 1,4-dihydropyridine derivative having the formula (I): wherein, R1represents a substituted or unsubstituted phenyl or heterocyclic group, R2represents a C1to C5lower alkyl group, R3represents a substituted or unsubstituted C2to C8alkyl, alkenyl, alkynyl or substituted or unsubstituted cycloalkyl group, R4represents -A-R5, wherein A represents a C2to C8alkylene group or a substituted or unsubstituted C2to C8alkenylene group, and R5represents a substituted or unsubstituted pyridyl, pyridylcarbonyl or piperadinyl group and a drug for overcoming resistance to an anti-cancer drug or a drug increasing the effect of an anti-cancer drug containing as an effective ingredient the derivative or its pharmacologically acceptable salt or hydrate.
Dihydropyridine antiallergy agents
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, (2008/06/13)
STR1 Platelet activating factor antagonists of formula (I), in which R2 is optionally substituted phenyl, R1 is H, alkyl or arylalkyl, Het is an optionally substituted N-containing heterocyclic group optionally fused to a phenyl or a
1,4-dihydropyridines useful as pharmaceuticals
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, (2008/06/13)
The invention provides compounds of the formula: STR1 The variables are defined in the specification. The compounds are useful e.g. for the curative or prophylactic treatment of allergic conditions.
Dihydropyrimidine antiallergy agents
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, (2008/06/13)
STR1 A compound of formula (I), where Ar is optionally substituted phenyl or methylenedioxyphenyl or benzothienyl, R1 is alkyl, R2 is selected from hydroxy, alkoxy, alkylthio, alkyl and optionally substituted phenyl or amino, and "He
1,4-Dihydropyridines as Antagonists of Platelet Activating Factor. 1. Synthesis and Structure-Activity Relationships of 2-(4-Heterocyclyl)phenyl Derivatives
Cooper, Kelvin,Fray, M. Jonathan,Parry, M. John,Richardson, Kenneth,Steele, John
, p. 3115 - 3129 (2007/10/02)
A novel class of 2-(4-heterocyclylphenyl)-1,4-dihydropyridines (2-38) possessing antagonist activity against platelet activating factor (PAF) was prepared by the Hantzsch synthesis from a variety of ethyl 4'-heterocyclic-substituted benzoylacetates, aryl or heteroaryl aldehydes, and substituted 3-aminocrotonamides or 3-aminocrotonate esters.Structure-activity relationships were evaluated where PAF antagonist activity was measured in vitro by determining the concentration of compound (IC50) required to inhibit the PAF-induced aggregation of rabbit washed platelets,and in vivo by determining the oral dose (ED50) which protected mice from a lethal injection of PAF.The nature of the substituent at the dihydropyridine 2-position was found to be important for both in vitro and in vivo activity, whereas there was greater flexibility for structural variation at the 4- and 5-positions.The most potent compound was 4-(2-chlorophenyl)-1,4-dihydro-3-(ethoxycarbonyl)-6-methyl-2-pyrid-1-yl)phenyl>-5-pyridine (17, UK-74,505), IC50 = 4.3 nM, ED50 = 0.26 mg/kg po, which was found to be approximately 33 times more potent in vitro (rabbit platelet aggregation) and about 8 times more potent in vivo (murine lethality) than WEB2086.Compound 17 also exhibited a long duration of action in the dog (inhibition of PAF-induced whole blood aggregation ex vivo was maintained for > 24 h following a single oral dose of 75 μg/kg) and was highly selective as a PAF antagonist, showing only weak affinity (IC50 = 6600 nM) for the nitrendipine binding site.As a result of its high oral potency, selectivity, and duration of action, UK-74,505 has been selected for clinical evaluation.
Diazepine antiallergy agents
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, (2008/06/13)
Platelet activating factor antagonists of formula (I), (II) or (III): STR1 where A is optionally substituted benzene, pyridine, naphthalene, quinoline, thiophene, benzothiophene, pyrazole or isothiazole, X is O, S or NH Y is 1,4 phenylene or a group of formula STR2 R1 is H or optionally substituted C1 -C4 alkyl, R2 and R3 are H or C1 -C4 alkyl, B is an optionally fused 5- or 6-membered ring containing nitrogen atoms, Het is an optionally substituted 5-membered heterocyclic ring containing nitrogen or a pyridine ring, the ring optionally being fused to benzene or nitrogen-containing heterocyclic ring.
1,4-dihydropyridine derivatives
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, (2008/06/13)
The invention provides compounds of the formula STR1 and pharmaceutically acceptable salts thereof, wherein R is phenyl substituted by halo; R1 is C1 -C4 alkyl; is hydrogen, C5 -C7 cycloalkyl, benzyl
