Reference

N-arylpiperazine derivatives as G-protein coupled receptor agonists and their preparation, pharmaceutical compositions, and use in the treatment of obesity and diabetes

All Rights Reserved. N-arylpiperazine derivatives as G-protein coupled receptor agonists and their preparation, pharmaceutical compositions, and use in the treatment of obesity and diabetes. Barba, Oscar; Bradley, Stuart Edward; Fyfe, Matthew Colin Thor; Bertram, Lisa Sarah; Gattrell, William; Procter, Martin James; Rasamison, Chrystelle Marie; Swain, Simon Andrew (Prosidion Limited, UK). PCT Int. Appl. WO 2007003964 A1 11 Jan 2007, 67pp. 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-GB50182 30 Jun 2006. PRIORITY: GB 2005-13276 30 Jun 2005; GB 2006-12897 29 Jun 2006. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 Compds. of formula I: or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes. Compds. of formula I wherein Z is (un)substituted (hetero)aryl and (un)substituted C1-4 alkyl(hetero)aryl; one of A1 and A2 is N and NO, and the other is CH, COH and N; d is 0, 1, 2, and 3; e is 1 and 2; k is 0, 1, 2, and 3; B is (un)substituted (un)branched C1-4 alkylene and (un)substituted (un)branched C1-4 alkenylene, etc.; G is CH-C1-3 alkyl and acylamino, sulfonylamino, ureido, etc.; R11 is H and OH; each R12 is independently OH, oxo, Me; or two R12 may form a methylene bridge; x is 0, 1, 2, and 3; y is 1, 2, 3, 4 and 5; and their pharmaceutically acceptable salts thereof, are claimed. Example compd.There are some commonly used reagents with their cas registry numbers 3685-22-1 and 23356-96-9 in this article. II was prepd. by redn. alkylation of 1-(4-methanesulfonylphenyl)piperazine with 4-formylpiperidine-1-carboxylic acid tert-Bu ester. All the invention compds. were evaluated for their G-protein couples receptor agonistic, antidiabetic, and antiobesity activity. .

Organocatalytic asymmetric Michael addition of 2,2-dimethyl-1,3-dioxan-5-one to nitro alkenes employing proline-based catalysts

All Rights Reserved. Several substances are used for example 64030-43-9 and 23356-96-9 which are their cas registry numbers. Organocatalytic asymmetric Michael addition of 2,2-dimethyl-1,3-dioxan-5-one to nitro alkenes employing proline-based catalysts. Enders, Dieter; Chow, Sharon (Institut fuer Organische Chemie, RWTH Aachen, Aachen 52074, Germany). European Journal of Organic Chemistry, (20), 4578-4584 (English) 2006 Wiley-VCH Verlag GmbH & Co. KGaA. CODEN: EJOCFK. ISSN: 1434-193X. DOCUMENT TYPE: Journal CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 27 The organocatalytic asym. Michael addn. of 2,2-dimethyl-1,3-dioxan-5-one to nitro alkenes using a no. of proline-based catalysts afforded polyfunctional nitro ketones. Reverse diastereoselectivity was obsd. with the diphenylprolinol catalyst. The best diastereo- and enantiomeric excesses were achieved with the sulfonamide catalyst (I). .