Detail of "211053-49-5"

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Preparation of azetidine derivatives as neurokinin receptor antagonists for treatment of gastrointestinal diseases

All Rights Reserved. Preparation of azetidine derivatives as neurokinin receptor antagonists for treatment of gastrointestinal diseases. Holmqvist, Sara; Johansson, Anders; Svensson, Arne; Von Unge, Sverker (Astrazeneca AB, Swed.). PCT Int. Appl. WO 2006137790 A1 28 Dec 2006, 53pp. 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. (English). (World Intellectual Property Organization). CODEN: PIXXD2. APPLICATION: WO 2006-SE759 21 Jun 2006. PRIORITY: SE 2005-1494 23 Jun 2005. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1, 25, 28 The title compds. with general formula I [wherein R2 = (un)substituted C1-4 alkyl; R3 = (CH2)nC(R6)(R7)OH, where n = 0-3; R6 and R7 = independently H or methyl; X = O or (un)substituted NH; Ar = substituted Ph, naphthyl, etc.] or pharmaceutically acceptable salts thereof are prepd. as neurokinin receptor antagonists for the treatment of gastrointestinal diseases. For example, the compd. II was prepd. in a multi-step synthesis. II showed antagonistic activity with pKB value of 8.1, 7.6, and 7.In this experiment, several chemicals are used like 211053-49-5 and 917572-10-2 1 against NK1, NK2, and NK3 receptors, resp. II also showed statistically significant CYP3A4 inhibitory activity with IC50 value of 19.2 mM. .