- BENZODIOXOLE, BENZOFURAN, DIHYDROBENZOFURAN, AND BENZODIOXANE MELATONERGIC AGENTS
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Novel derivatives of benzodioxa alkylene ethers are provided which are useful as melatonergic agents.
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Page/Page column 18
(2010/02/09)
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- 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
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The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4fare defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
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- Aminoalkylindoles: Structure - Activity Relationships of Novel Cannabinoid Mimetics
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Aminoalkylindoles (AAIs) are a novel series of cannabinoid receptor ligands.In this report we disclose the structural features of AAIs which are important for binding to this receptor as measured by inhibition of binding of 3H>Win 55212-2 (5).Functional activity in the mouse vas deferens is also noted and used to distinguish agonists from potential antagonists.The key structural features for potent cannabinoid activity in this series are a bicyclic (naphthyl) substituent at the 3-position, a small (H) substituent at the 2-position, and an aminoethyl (morpholinoethyl) substituent at the 1-position.A 6-bromo analog, Win 54461 (31), has been identified as a potential cannabinoid receptor antagonist.Modeling experiments were done to develop a pharmacophore and also to compare AAI structures with those of classical cannabinoids.The fact that the cannabinoid AAIs arose out of work on a series of cyclooxygenase inhibitors makes sense now that an endogenous cannabinoid ligand has been identified which is a derivative of arachidonic acid.Because of their unique structures and physical properties, AAIs provide useful tools to study the structure and function of the cannabinoid receptor(s).
- Eissenstat, Michael A.,Bell, Malcolm R.,D'Ambra, Thomas E.,Alexander, E. John,Daum, Sol J.,et al.
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p. 3094 - 3105
(2007/10/02)
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- Benzo-furan derivative
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Novel benzo-furan(or -thiophene) derivative of the formula: STR1 wherein R1 is hydrogen atom, a lower alkyl group, a cycloalkyl group, a phenyl-lower alkyl group or a substituted or unsubstituted phenyl group, R2 is hydrogen atom, a lower alkyl group, an acyl group or phenyl group, R3 is hydrogen atom, a halogen atom, nitro group, a lower alkoxy group, amino group or an acylamino group, R4 is a group of the formula: STR2 A is a lower alkylene group optionally substituted with hydroxy group, B is single bond or a lower alkylene group, one of R5 and R6 is hydrogen atom or a lower alkyl group and the other is a lower alkyl group or a phenyl-lower alkyl group, or R5 and R6 combine together with adjacent nitrogen atom to form a heteromonocyclic group, R7 is a lower alkyl group, X is oxygen atom or sulfur atom, Y is oxygen atom, imino group, a lower alkylimino group or a phenyl-lower alkylimino group and a salt thereof are disclosed. Said compound (I) and a salt thereof have a potent inhibitory activity against reflective contraction of urinary bladder.
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