77039-78-2Relevant articles and documents
ANTAGONISTS OF THE TRPV1 RECEPTOR AND USES THEREOF
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Page/Page column 20, (2008/12/06)
The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.
NOVEL SULFONAMIDE SUBSTITUTED CHROMAN DERIVATIVES USEFUL AS BETA-3 ADRENORECEPTOR AGONISTS
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Page/Page column 32, (2008/12/07)
This invention relates to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
SUBSTITUTED AMINOMETHYLTETRALINS AND THEIR HETEROCYCLIC ANALOGUES
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, (2008/06/13)
For binding 5-HT 1 receptors and thereby treating central nervous system disorders, novel substituted aminomethyltetralins and their heterocyclic analogues of the formula STR1 in which Z--denotes a group of the formula STR2 R 1, E and F can be hydrogen or other radicals, or salts thereof.
Benzopyran fungicidal compositions and use
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, (2008/06/13)
The invention provides fungicidal compositions comprising as an active ingredient a compound having the general formula (I): STR1 or a stereoisomer thereof, wherein X is a methylene group and Y is an oxygen atom, or X is an oxygen atom and Y is a methylen
Pharmacomodulation d'adrenolytiques α en serie benzopyrannique
Mouysset, Genevieve,Payard, Marc,Grassy, Gerard,Tronche, Pierre,Dabire, Hubert,et al.
, p. 539 - 544 (2007/10/02)
Pharmacomodulation of α-adrenergic blocking agents by a series of benzopyrans.The N-methylpiperidine fragment was associated with four oxygenated heterocycles of the benzopyran ring system.Two different synthesis pathways were used in each case.Twenty intermediate derivatives and four aminomethylated derivatives whose structures were established by spectroscopic data are described.The pharmacological investigation demonstrates the interest of these compounds on the α-adrenergic receptors in light of their activities and selectivities. α1-adrenergic blocking agents / α2-adrenergic blocking agents / piperidinomethyl chromone, chromene and chromane
α-Adrenoreceptor Reagents. 2. Effects of Modification of the 1,4-Benzodioxan Ring System on α-Adrenoreceptor Activity
Chapleo, Christopher B.,Myers, Peter L.,Butler, Richard C. M.,Davis, John A.,Doxey, John C.,et al.
, p. 570 - 576 (2007/10/02)
Modification of the 1,4-benzodioxan ring present in RX 781094 (1) has not previously been considered.This paper describes a number of analogues of this ring system, including compounds in which one of the oxygen atoms has been replaced by a methylene group and also those in which the ring size has been changed to give, for example, furan and thiophene derivatives.The dihydroxybenzofuranylimidazoline compound 7 is the only analogue possesing presynaptic antagonist potency and selectivity comparable to that of 1.In view of this result, a number of derivatives was prepared to determine the structure-activity relationships within this series.Many derivatives, as well as the parent compound 7, were found to possess presynaptic α2-adrenoreceptor antagonist and postsynaptic α1-adrenoreceptor partial agonist properties.Two of the selective presynaptic antagonists,13 and 14, possess greater potency and selectivity than that possessed by 1.The 5-chloro derivative 25 is twice as potent as 1 after oral administration but only about half as potent when given intravenously.
Phenoxyalkylamines in Semi-rigid Conformation: Synthesis & Pharmacological Activity of N1-(4'-Chromanyl)-N4-arylpiperazines & N1-(2'-Chromanylmethyl)-N4-arylpiperazines
Pratap, Ram,Gupta, R. C.,Anand, Nitya
, p. 1063 - 1067 (2007/10/02)
Synthesis and pharmacological activity of N1-(4'-chromanyl)-N4-arylpiperazines and N1-(chromanylmethyl)-N4-arylpiperazines, cyclic congeners of N1-aryloxyalkyl-N4-arylpiperazines, are reported.None of the compounds of this series shows any significant pharmacological activity.