Reference

Preparation of novel polysubstituted 1,1-pyridinyl aminocyclopropanamines as selective a4b2 nicotinic receptor ligands and their pharmaceutical compositions for treatment of memory assocd

All Rights Reserved. Preparation of novel polysubstituted 1,1-pyridinyl aminocyclopropanamines as selective a4b2 nicotinic receptor ligands and their pharmaceutical compositions for treatment of memory assocd. diseases. Goldstein, Solo; Guillonneau, Claude; Charton, Yves; Lockhart, Brian; Lestage, Pierre (Les Laboratoires Servier, Fr.). PCT Int. Appl. WO 2007012761 A1 1 Feb 2007, 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. (French). (World Intellectual Property Organization). CODEN: PIXXD2. APPLICATION: WO 2006-FR1831 27 Jul 2006. PRIORITY: FR 2005-8032 28 Jul 2005. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1, 24, 63 Title compds. I [X = (CH2)n; n = 1-6; R1-R2, R7 = independently H, alkyl, (un)substituted arylalkyl; R3, R4 = independently H, alkyl; R5, R6 = independently H, alkyl, halo, OH, alkoxy, CN, acyl, etc.Several substances like 5350-93-6 may be metioned in this study.; and their enantiomers, diastereomers, and their pharmaceutically acceptable acid or base addn. salts] were prepd. as selective a4b2 nicotinic receptor ligands for treatment of memory assocd. diseases. Thus, reductive alkylation 3-aminopyridine with tert-Bu N-[1-(formyl)cyclopropyl]-N-methylcarbamate (prepn. given), reaction of the secondary amine with carbonyldiimidazole and formic acid n DMF, redn. of the formyl intermediate with borane Me sulfide complex in THF/Boc-deprotection, and acidulation of II with an ethereal HCl soln. gave II·2HCl. I, at 10 mM concn., were highly selective for binding to a4b2 nicotinic receptors (Ki = 1.5x10-8 M for II·2HCl) over muscle (Ki > 10-5 M), ganglionic (Ki > 10-5 M) and a7 (Ki = 8.3x10-6 M for II·2HCl) subtype nicotinic receptors, and muscarinic receptors (Ki > 10-5 M). .

Lysergic acid amides

Lysergic acid amides. Hauth, Hartmut (Sandoz Ltd., Switz.). Swiss CH 579080 31 Aug 1976, 4 pp.Chemical with cas number 5350-93-6 also plays role. (Unavailable). (Switzerland). CODEN: SWXXAS. CLASS: IC: C07D457-06. APPLICATION: CH 72-17822 7 Dec 1972. DOCUMENT TYPE: Patent CA Section: 31 (Alkaloids) Section cross-reference(s): 27 Ergolinecarboxamides I (R = R1; R2 = H, R3 = H, MeO; R4 = H, Cl, MeO, BuO; R2 = Me, R3 = H, R4 = MeO) and their salts (8 compds.) were prepd. by treating I (R = Cl) with R1H. Thus, lysergic acid in DMF-MeCN at -30.degree. was treated with (COCl)2 and I (R = Cl) treated with R1H (R2 - R4 = H) at -30.degree. followed by storing for 2 hr at 0.degree. to give I (R = R1, R2-R4 = H). .