Patent AU-2013201096-B2 (AU)
Title: Crystalline diacylhydrazine and the use thereof
Inventor: HORMANN ROBERT E
IPC: C12N5/10
Filed: 2012-09-07
Granted: 2015-04-02
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) I CORRECTED VERSION (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date W O 2013/036758 A8 14 March 2013 (14.03.2013) W I POI P CT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every C07C 243/18 (2006.01) C12N 5/10 (2006.01) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (21) International Application Number: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, PCT/US2012/054141 DO, DZ, EC, EE, EG, ES, Fl, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, 7 September 2012 (07.09.2012) KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, (25) Filing Language: English NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, (26) Publication Language: English 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, (30) Priority Data: ZM, ZW. 61/532,368 8 September 2011 (08.09.201 1) US (84) Designated States (unless otherwise indicated, for every (71) Applicant (for all designated States except US): IN- kind of regional protection available): ARIPO (BW, GH, TREXON CORPORATION [US/US]; 1750 Kraft Drive, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, Suite 1400, Blacksburg, VA 24060 (US). UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, (72) Inventors; and TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (75) Inventors/Applicants (for US only): HORMANN, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS , ST, L, LV, Robert, E. [US/US]; 1750 Kraft Drive, Suite 1400, MC, MK, MT, NL, NO, PL, PT, RO, GS, S, S , SM, Blacksburg, VA 24060 (US). SHULMAN, Inna [US/US]; TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, 1750 Kraft Drive, Suite 1400, Blacksburg, VA 24060 ML, MR, NE, SN, TD, TG). (US). RODEL, Eva [DE/US]; 1750 Kraft Drive, Suite Published: 1400, Blacksburg, VA 24060 (US). HILFIKER, Rolf _ with international search report (Art. 21(3)) [CH/US]; 1750 Kraft Drive, Suite 1400, Blacksburg, VA 24060 (US). DEPAUL, Susan, M. [US/US]; 1750 Kraft - with sequence listing part of description (Rule 5.2(a)) Drive, Suite 1400, Blacksburg, VA 24060 (US). (48) Date of publication of this corrected version: (74) Agents: ESMOND, Robert, W. et al.; Sterne, Kessler, 3 October 2013 Goldstein & Fox, P.L.L.C., 1100 New York Avenue, N.W., Washngto, D 2005-334 (S).(15) Information about Correction: Washington, DC 20005-3934 (US). see Notice of 3 October 2013 O (54) Title: CRYSTALLINE DIACYLHYDRAZINE AND THE USE THEREOF (57) Abstract: The present disclosure provides crystalline polymorphic and amorphous forms of (R)-3,5-dimethyl-benzoic acid N (1-tert-butyl-butyl)-N'-(2-ethyl-3-methoxy- benzoyl)-hydrazide (Compound 1) or (S)-3,5-dimethyl-benzoic acid N-(1-tert-butyl CA butyl)-N'-(2-ethyl-3-methoxy-benzoyl)-hydrazide (Compound 2). The present disclosure further provides compositions comprising crystalline polymorphic and amorphous forms of Compound 1 or Compound 2 and an excipient, methods of making crystalline polymorphic or amorphous forms of Compound 1 or Compound 2, and methods of using crystalline polymorphic or amorphous forms of Compound 1 or Compound 2 to regulate gene expression in a cell or in a subject.