Patent SG-194767-A1 (SG)
Title: L-proline and citric acid co-crystals of (2s, 3r, 4r, 5s, 6r )- 2- (3- ((5- (4-fluorophenyl)thiophen-2-yl) methyl) -4-methylphenyl)-6- (hydroxymethyl)tetrahydro-2h-pyran-3,4,5-triol
Inventor: NGUYEN MINH
Filed: 2012-05-09
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT)(19) World Intellectual Property OrganizationInternational Bureau(43) International Publication Date 15 November 2012 (15.11.2012) WIPO I PCT (10) International Publication NumberWO 2012/154812 Al (51) International Patent Classification:CO7D 409/10 (2006.01) CO7H 7/04 (2006.01)A61K 31/70 (2006.01)International Application Number: PCT/US2012/037062International Filing Date: 9 May 2012 (09.05.2012)Filing Language: EnglishPublication Language: English(30) Priority Data:61/483,887 9 May 2011 (09.05.2011) USApplicant all designated States except US): JANSSEN PHARMACEUTICA NV [BE/BE]; Turnhout seweg 30, B-2340 Beerse (BE).Inventors; and(75) Inventors/Applicants (for US only): NGUYEN, Minh [US/US]; 18 Bearse Avenue, Apt. 3, Dorchester, MA 02124 (US). COLLIER, Edwin, A. [GB/US]; C/o Janssen Research & Development, Llc, 1000 Route 202, Raritan, NJ 08669 (US).(74) Agents: JOHNSON, Philip S. et al.; Johnson & Johnson, One Johnson & Johnson Plaza, New Brunswick, NJ 08933 (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, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, Fl, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, 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, 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, Fl, 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, ML, MR, NE, SN, TD, TG).Declarations under Rule 4.17:as to the identity of the inventor (Rule 4.170)as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii))as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii))Published:— with international search report (Art. 21(3)) (54) Title: L-PROLINE AND CITRIC ACID CO-CRYSTALS OF (2S, 3R, 4R, 5S, 6R )- 2- (3- ((5- (4- FLUOROPHENYL)THIOPHEN-2-YL) METHYL) -4-METHYLPHENYL)-6- (HYDROXYMETHYL)TETRAHYDRO-2H PYRAN-3,4,5-TRIOL(57) Abstract: The present invention is directed to L-proline and citric acid co-crystals of (2S,3R,4R,5S,6R)-2-(345-(4- fluorophenyl)thiophen-2-y1)methyl)-4- methylpheny1)-6-(hydrox3rmethyptetrahydro-2H-pyran-3,4,5-triol, pharmaceutical composi tions containing said co-crystals and their use in the treatment glucose-related disorders such as Type 2 diabetes mellitus and S3rn - drome X.