Reference

Preparation of pyridine alkyne derivatives for treatment of pain

Preparation of pyridine alkyne derivatives for treatment of pain. Kyle, Donald J.; Sun, Qun; Zhou, Xiaoming (Euro-Celtique S. A., Belg.). PCT Int. Appl. WO 2005007641 A1 27 Jan 2005, 229 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).There are some reagents with their cas registry numbers 87120-72-7 and 5470-18-8 are used in this study. (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: C07D401-04. ICS: C07D295-185; C07D213-74; A61K031-4439; A61K031-444; A61K031-4545; A61P043-00. APPLICATION: WO 2004-US21246 1 Jul 2004. PRIORITY: US 2003-PV484881 3 Jul 2003. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1 The title compds. I [wherein R1 = halo, Me, CF3, NO2, CN, or H; Q = (un)substituted aminopiperidinyl, aminopyrrolidinyl, piperidinylamino, pyrrolidinylamino, etc.; A = CO or CH2; R2 = alkyl, cycloalkyl, Ph, naphthyl, etc.] or pharmaceutically acceptable salts thereof are prepd. for the treatment of pain. For example, the compd. II was prepd. in a multi-step synthesis. II showed inhibitory activity with IC50 of 109.7 nM against metabotropic glutamate receptor (mGluR5) in rat. I are useful for the treatment of pain, addictive disorder, Parkinson's disease, anxiety, Schizophrenia, etc. (no data). .