On January 21, 2010, Uchida, Hideharu; Ogawa, Shinichi; Makabe, Muneyoshi; Maeda, Yoshitaka published a patent.Related Products of 141940-37-6 The title of the patent was Preparation of heterocyclylidene-N-(heterocyclyl)acetamide derivatives as antagonists of transient receptor potential type I receptor (TRPV1). And the patent contained the following:
The title compounds [I; k, m, n, p = 0-2; j, q = 0-1; R1 = halo, H, heterocyclyl, alkoxy, alkoxycarbonyl, NH2, OH, CO2H, alkanoyl, cyano, NO2, etc.; R2 = halo, NH2, alkyl, aromatic heterocyclyl, oxo, etc.; X1 = O, NR3, or S(O)r; X2 = CH2, O, NR3, S(O)r (wherein r = 0-2; R3 = H, alkyl, heterocyclyl, etc.); W = CH2, CO, SO2; R7 = H, alkyl, heterocyclyl, etc.; R8 = H, halo, alkyl, heterocyclyl, etc.; a dashed line in the ring containing X1 and X2 means the fusion of two rings; L1, L2 = a single bond, (un)substituted CH2 or NH, S(O)t (t = 0-2); the “”Cycle”” moiety represents a 5-6 membered aryl or heteroaryl ring; a solid line and a dashed line between L1 and L2 mean the presence of a single bond and a double bond, resp.; and a wavy line means an E-form or Z-form], or salts thereof, or solvates of the compounds or the salts, useful as antagonists of transient receptor potential type I receptor (TRPV1), were prepared Thus, (E)-(8-trifluoromethyl-3,4-dihydro-2H-benzo[b]oxepin-5-ylidene)acetic acid was stirred with oxalyl chloride and one drop of DMF in CH2Cl2 at room temperature for 2 h, concentrated under reduced pressure, redissolved in CH2Cl2, and stirred with 6-amino-2,2-dimethyl-4H-benzo[1,4]oxazin-3-one at room temperature for 2 h to give (E)-2-(8-Trifluoromethyl-3,4-dihydrobenzo[b]oxepin-5(2H)-ylidene)-N-(2,2-dimethyl-3-oxo-2,3-dihydro-4H-benzo[1,4]oxazin-6-yl)ethanamide (II). II in vitro at <100 nM inhibited the capsaicin-induced cellular influx of calcium in CHO cells genetically transformed with human TRPV1. Pharmaceutical formulations, e.g. a tablet containing II, were described. The experimental process involved the reaction of tert-Butyl (4-(trifluoromethyl)phenyl)carbamate(cas: 141940-37-6).Related Products of 141940-37-6
The Article related to trpv1 antagonist heterocyclylideneheterocyclylacetamide preparation, heterocyclylideneheterocyclylacetamide preparation antagonist transient receptor potential type i receptor and other aspects.Related Products of 141940-37-6
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