Patent SG-11201804210X-A (SG)
Title: Treatment of autoimmune disease
Inventor: NIESMAN MICHAEL
IPC: C07D491/00
Filed: 2016-11-14
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property - Organization International Bureau irst0) (43) International Publication Date ..... ..sr ,„../ 26 May 2017(26.05.2017) WIPO I PCT II (10) 11111111111111111111111 WO International Ell 2017/087318 Publication 1111111111111111111111111111111111111 Al Number In (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A01N 43/90 (2006.01) C07D 491/00 (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, DJ, DK, DM, PCT/US2016/061824 DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (22) International Filing Date: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, 14 November 2016 (14.11.2016) KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, (25) Filing Language: English OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, (26) Publication Language: English 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, (30) Priority Data: ZW. 62/258,190 20 November 2015 (20.11.2015) US (84) Designated States (unless otherwise indicated, for every (71) Applicant: MINGSIGHT PHARMACEUTICALS, INC. kind of regional protection available): ARIPO (BW, GH, [US/US]; P.O. Box 261208, San Diego, California 92196 GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, (US). TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, (72) Inventors: NIESMAN, Michael; P.O. Box 261208, San TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, Diego, California 92196 (US). ZHANG, Kai; P.O. Box DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, 261208, San Diego, California 92196 (US). 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, (74) Agent: CLARK, David; Wilson Sonsini Goodrich & Ros- GW, KM, ML, MR, NE, SN, TD, TG). ait, 650 Page Mill Road, Palo Alto, California 94304 (US). [Continued on next page] (54) Title: TREATMENT OF AUTOIMMUNE DISEASE : Provided herein (57) are compositions and methods r e T 5.0 for the treatment of autoimmune and alloimmune diseases and o a) 4.5 conditions, including rheumatoid arthritis, multiple sclerosis, O ° 4 0 co . — inflammatory bowel disease (IBD) (e.g., Crohn's disease, ul- neuritis, Neuromyelitis Optica, Sjo - cerative colitis), optic 2 3.5 ygren's Ankylosing syndrome, psoriasis, systemic scleroderma, in 3.0 . .r. Spondylitis, autoimmune hepatitis, Graft vs host disease _ = 2.5 .. t (GvHD), and organ transplant rejection. Said compositions a 2.0- useful for treating autoimmune diseases comprise - pyrro 73 0 E 1 . 5 lo-pyrazole PKC inhibitors. / — Eft m r) I n .e 0 - .. w 1.0 CO + c 1 —, ft • co 0.5 Z __,,gweitos...0 it! a 18 19 20 21 22 23 24 25 26 27 28 29 30 31 32 33 34 35 Study Day —o— Normal P0, BID (td29-35) —N— Vehicle Control (0.5% Methylcellulose) P0, BID —0— Dex (0.1 mg/kg) P0, BID (*d29-35) -- Compound A (60 mg/kg) P0, BID I'l —o— Compound A (90 mg/kg) P0, BID —In— Compound A (120 mg/kg) P0, BID (*d27, 35) .4 t n = 4Mormal & Dex GC n = 12ttreatment group & Vehicle Control Il \"7) < 0.05 ANOVA vs. Vehicle Control IN en tp <0.05 t-test vs. Vehicle Control (comparison to Normal) GC o FIG. 4 -..... N 1-1 0 ei o WO 2017/087318 Al MIDEDIMOREENDEFEDIMEIIIIIHEREVOIS Declarations under Rule 4.17: Published: — as to applicant's entitlement to apply for and be granted a patent (Rule 4.17(ii)) — with international search report (Art 21(3)) — as to the applicant's entitlement to claim the priority of the earlier application (Rule 4.17(iii))