Patent SG-11201408503Q-A (SG)
Title: Substituted bicyclic alkoxy pyrazole analogs as allosteric modulators of mglur5 receptors
Inventor: CONN P JEFFREY
IPC: A61K31/4985
Filed: 2013-06-19
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) CORRECTED VERSION (19) World Intellectual Property Organization International Bureau (43) International Publication Date 27 December 2013 (27.12.2013) WIPOIPCT (10) International Publication Number WO 2013/192346 A9 (51) International Patent Classification: A61K31/4985 (2006.01) C07D 471/04 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/US2013/046645 19 June 2013 (19.06.2013) English English (30) Priority Data: 61/662,300 20 June 2012 (20.06.2012) US (71) Applicant: VANDERBILT UNIVERSITY [US/US]; Center For Technology Transfer And, Commercialicatiion, 305 Kirkland Hall, 2201 West End Avenue, Nashville, TN 37240 (US). (72) Inventors: CONN, P., Jeffrey; 9012 Grey Point Ct., Brentwood, TN 37027 (US). LINDSLEY, Craig, W.; 401 Brierly Court, Brentwood, TN 37027 (US). STAUFFER, Shaun, R.; 9500 Wexcroft Drive, Brentwood, TN 37027 (US). BARTOLOME-NEBREDA, Jose, Manuel; Janssen Research And Development, Calle Jarama, 75, Po- ligono Industrial, E-45007 Toledo (ES). MACDONALD, Gregor, James; Janssen Pharmaceutica Nv, Turnhout- seweg 30, B-2340 Beerse (BE). CONDE-CEIDE, Susana; Janssen Research And Development, Calle Jarama, 75, Po- ligono Industrial, E-45007 Toledo (ES). TONG, Han, Min; Janssen Research And Development, Calle Jarama, 75, Poligono Industrial, E-45007 Toledo (ES). ALCAZ- AR-VACA, Manuel, Jesus; Janssen Research And Devel­ opment, Calle Jarama, 75, Poligono Industrial, E-45007 Toledo (ES). ANDRES-GIL, Jose Ignacio; Janssen Resarch and Development, Calle Jarama, 75, Poligono In­ dustrial, E-45007 Toledo (ES). PENA-PINON, Miguel, Angel; Novalix Pharma S.I., Calle Jarama, 75, Poligono In­ dustrial, E-TOLEDO E-45007 (ES). (74) Agents: SHORTELL, D., Brian et al.; Ballard Spahr LLP, 999 Peachtree Street, Suite 1000, Atlanta, GA 30309 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available)'. AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, [Continued on next page] (54) Title: SUBSTITUTED BICYCLIC ALKOXY PYRAZOLE ANALOGS AS ALLOSTERIC MODULATORS OF MGLUR5 RECEPTORS / \ , , I Zn /' \ v r ~) / •! s») / i PCP )\ V / \" - x i V ;' N ;V;: / \PAM \ f. Mg), ' KJ / \wA ^ / \ * : : 0\ < •t m CJ Ov NR1 J PI fX 1 rilJ, I (57) Abstract: In one aspect, the invention relates to substituted bicyclic alkoxy pyrazole analogs, de­ rivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the com­ pounds; pharmaceutical compositions comprising the compounds; and methods of treating neurolo­ gical and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. is intended as a scan­ ning tool for purposes of searching in the particu­ lar art and is not intended to be limiting of the present invention. WO 2013/192346 A91 lllll llllllll II llllll lllll III lllll lllll III III III lllll lllll lllll lllll llll llll lllllll llll llll DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available)'. ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) (48) Date of publication of this corrected version: 18 December 2014 (15) Information about Correction: see Notice of 18 December 2014