Detail of "18542-42-2"

Reference

Preparation of pyrrole-2,5-dione derivatives as liver X receptor modulators

Preparation of pyrrole-2,5-dione derivatives as liver X receptor modulators. Bostroem, Jonas; Brickmann, Kay; Holm, Patrik; Sandberg, Pernilla; Swanson, Marianne; Westerlund, Christer (Astrazeneca AB, Swed.). PCT Int. Appl. WO 2005005417 A1 20 Jan 2005, 65 pp. 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, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: C07D405-06. ICS: C07D401-06; C07D207-416; A61K031-4439; A61K031-4025; A61P003-10; A61P025-28. APPLICATION: WO 2004-SE1114 8 Jul 2004. PRIORITY: GB 2003-16232 11 Jul 2003. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1, 63 The present invention relates to novel compds. I [R1 = (un)substituted phenylalkyl, heteroarylalkyl, alkyl; R2 = Ph; R3 = (un)substituted Ph, indolyl, benzofuranyl, etc.], to processes for prepg.Several substances with their cas registry numbers 18542-42-2 and 828931-83-5 may be metioned in this study. such compds., to their utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) a (NR1H3) and/or b (NR1H2) and in treating clin. conditions including cardiovascular diseases such as atherosclerosis, inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not assocd. with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compns. contg. them. Prepn. of twenty seven compds. I was described. Thus, reacting 3-chloro-1-(2-methoxyethyl)-4-phenyl-1H-pyrrole-2,5-dione with 4-methoxyaniline in DMF afforded 21% I [R1 = 2-methoxyethyl; R2 = Ph; R3 = 4-MeOC6H4]. The compds. I have an EC50 of < 50mM/L for LXRa and/or b in coactivator recruitment assays and/or reporter gene assays. .