Detail of "2629-72-3"

Reference

Preparation of pyrrolidine derivatives as histamine H3 antagonists or inverse agonists

All Rights Reserved. Preparation of pyrrolidine derivatives as histamine H3 antagonists or inverse agonists. Beavers, Lisa Selsam; Finley, Don Richard; Gadski, Robert Alan; Hipskind, Philip Arthur; Hornback, William Joseph; Jesudason, Cynthia Darshini; Pickard, Richard Todd; Takakuwa, Takako; Vaught, Grant Mathews (Eli Lilly and Company, USA). PCT Int. Appl. WO 2007005503 A1 11 Jan 2007, 65pp. 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-US25328 28 Jun 2006. PRIORITY: US 2005-696257P 1 Jul 2005. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1, 28 The title compds. I [R1 = -N-pyrrolidinyl (wherein the pyrrolidine is optionally substituted with R4), -N-morpholinyl, etc. 2629-72-3 and 919113-62-5 are cas registry numbers of chemicals which are used as reagents here.; R4 = Me, CF3, CN, etc.; R6 = H, (un)substituted alkyl; R7 = H, (un)substituted alkyl] are prepd. I are useful for the treatment of histamine H3 receptor-related diseases. Thus, [4-(2-pyrrolidin-1-ylethylamino)phenyl]-(2-(S)-pyrrolidin-1-ylmethylpyrroli din-1-yl)methanone was prepd. in 2 steps from (S)-(+)-1-(2-pyrrolidinylmethyl)pyrrolidine and 4-fluorobenzoyl chloride. In an assay for inhibition of [35S]GTPg[S] binding to H3R membranes in the presence of agonists, one compd. of this invention showed the Ki value of 11.7 nM. .