Reference

Preparation of phenoxyalkanoic acid derivatives for the treatment of diabetes

All Rights Reserved. Preparation of phenoxyalkanoic acid derivatives for the treatment of diabetes. Imoto, Hiroshi (Takeda Pharmaceutical Company Limited, Japan).In this study，615-83-8 is also used. PCT Int. Appl. WO 2007013694 A1 1 Feb 2007, 180pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IS, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (Japanese). (World Intellectual Property Organization). CODEN: PIXXD2. APPLICATION: WO 2006-JP315452 28 Jul 2006. PRIORITY: JP 2005-221627 29 Jul 2005. DOCUMENT TYPE: Patent CA Section: 25 (Benzene, Its Derivatives, and Condensed Benzenoid Compounds) Section cross-reference(s): 1, 28, 63 Title compds. I [A = (un)substituted cyclic group; B = bond or spacer; D = O or NR5; R5 = H or substituent; X = arom. ring which has optionally further substituent; E = CO, C(OR6)R7 or C:NR8; R6-R8 = H or substituent; G = (un)substituted divalent hydrocarbon; R = -OR9 or -NR10R11; R9 = H or (un)substituted hydrocarbon; R10, R11 = H, (un)substituted hydrocarbon or (un)substituted heterocycle; R10 and R11 may combine together with the adjacent nitrogen atom form a heterocycle; R1-R4 = H or substituent] and salts thereof were prepd. For example, reaction of (4-hydroxyphenyl)[4-methoxy-2-(methoxymethoxy)phenyl]methanone, e.g., prepd. from 4-bromophenol in 4 steps, with 4-(chloromethyl)-5-methyl-2-phenyl-1,3-oxazole followed by treatment with HCl, ethoxycarbonylmethylation and hydrolysis using LiOH×H2O afforded compd. II. Compd. II decreased the blood glucose level (54%) and the blood lipid level (44%) and showed the PPARg partial agonistic activity (EC50 = 100 nM). .