Therapeutic 1,2,3,6-tetrahydropyrimidine-2-one compositions and methods therewith

作者: Edward T. Wei

DOI:

关键词:

摘要: A therapeutic composition is provided that comprises a 1-R1-phenyl, 4-R2-phenyl substituted 1,2,3,6-tetrahydropyrimidine-2-one cold receptor agonist in therapeutically effective amount and preferably further one or more pharmaceutically active drugs such as an anti-inflammatory glucocorticosteroid, sympathomimetic amine decongestant, anti-histamine, local anesthetic, menthol analog, mixtures thereof. The may be represented by the general formula 1-[R1-phenyl]-4-[R2-phenyl]-1,2,3,6-tetrahydropyrimidine-2-one wherein: R1 -hydroxy, -chloro, -fluoro, -alkyl, -acetoxy, -trifluoromethyl; R2 -nitro, -trifluoromethyl. Therapeutic compositions of invention elicit long-lasting cooling soothing, particularly when formulated for delivery to suppress sensations itch pain, inflamed skin, mucous membranes anogenital areas, enteric mucosa.

参考文章(14)
Sumi C. Chen, Chung-Ho Chen, Effective ophthalmic irrigation solution ,(1989)
Gedalya Mazor, Boris Baybikov, Moshe Trop, Avraham Kushelvesky, Sergay Popov, Cooling cylindrical device for therapeutic treatment of hemorrhoids. ,(1995)
William Jeffery Sandborn, Peter Rhodes, John Rhodes, Brian Kenneth Evans, Colonic delivery of nicotine to treat inflammatory bowel disease ,(1997)
Peter J. Barnes, Neurogenic inflammation in the airways. Respiration Physiology. ,vol. 125, pp. 145- 154 ,(2001) , 10.1016/S0034-5687(00)00210-3
David D. McKemy, Werner M. Neuhausser, David Julius, Identification of a cold receptor reveals a general role for TRP channels in thermosensation Nature. ,vol. 416, pp. 52- 58 ,(2002) , 10.1038/NATURE719
Eddie T. Wei, Chemical stimulants of shaking behaviour. Journal of Pharmacy and Pharmacology. ,vol. 28, pp. 722- 724 ,(2011) , 10.1111/J.2042-7158.1976.TB02849.X
Alexandru Babes, Bogdan Amuzescu, Ulrich Krause, Andreas Scholz, Maria-Luiza Flonta, Gordon Reid, Cooling inhibits capsaicin-induced currents in cultured rat dorsal root ganglion neurones. Neuroscience Letters. ,vol. 317, pp. 131- 134 ,(2002) , 10.1016/S0304-3940(01)02443-0
E. T. Wei, D. A. Seid, AG-3-5: a chemical producing sensations of cold. Journal of Pharmacy and Pharmacology. ,vol. 35, pp. 110- 112 ,(2011) , 10.1111/J.2042-7158.1983.TB04279.X