Patent SG-11201903209T-A (SG)
Title: Structures and mechanism for the design of highly potent glucocorticoids
Inventor: XU HUAQIANG
IPC: A61M37/00
Filed: 2017-10-13
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property MD HIM 0 11101 010 11111 01 110 1 0 011101M 010 11111 HUHU° ill 011 Organization International Bureau (10) International Publication Number (43) International Publication Date .....0\"\" WO 2018/071736 Al 19 April 2018 (19.04.2018) WIP0 1 PCT (51) International Patent Classification: OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, A61M 37/00 (2006.01) A61P 37/06 (2006.01) SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, A61K 35/16 (2015.01) TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (21) International Application Number: (84) Designated States (unless otherwise indicated, for every PCT/US2017/056447 kind of regional protection available): ARIPO (BW, GH, (22) International Filing Date: GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, 13 October 2017 (13.10.2017) UG, TM), ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, (25) Filing Language: English EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, (26) Publication Language: English 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, (30) Priority Data: KM, ML, MR, NE, SN, TD, TG). 62/408,314 14 October 2016 (14.10.2016) US Published: (71) Applicant: VAN ANDEL RESEARCH INSTITUTE — [US/US]; 333 Bostwick Avenue NE, Grand Rapids, MI with international search report (Art. 21(3)) 49503 (US). — with amended claims (Art. 19(1)) (72) Inventors: XU, Huanqiang, Eric; 7145 Mooring Heights Court, S.E., Grand Rapids, MI 49546 (US). HE, Yuanzheng; 5337 Burton Court, S.E., Grand Rapids, MI 49525 (US). — = (74) Agent: SIEGEL, Douglas, H.; Honigman Miller Schwartz And Cohn LLP, 350 E. Michigan Ave., Suite 300, Kalama- = zoo, MI 49007 (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, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, _ KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, = MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, = = _ (54) Title: STRUCTURES AND MECHANISM FOR THE DESIGN OF HIGHLY POTENT GLUCOCORTICOIDS — = = = 50 = P.Ill Saline — = ••••••••••OVA + DIVISO 46 ...111...OVA. cat.e4(0,62125m6606 — ...op...OVA + cam • (0.125mctikg) a ...411..OVA +care 4 (0.0625M914) \" • klY , • OVA 1-e:ram .• (0,615625n-4CM = ....OVA -1. FF 6,,,125tagikgt # 3 ..411....OVA +CM.> 4 (0.03125m~ ,....... OVA. FF (0,0625thvy46 e 1:4 20 • •At • OVA ../API, P. 00.7215625mg( kg) P.m...OVA + FF (0.125rng(kg) „ , t ....o. OVA + FF — (0.0625Ingl614—____1 ' 4 ....e I 10 ....o.' .. .....;111 0 a , . El 0.25 0,5 N 2 4 L 0 0.55 0.5 1 2 4 M Acetylcholine IN. (taci)tt SW) IN 11 IN 00 Figure 15 1-1 0 \" (57) : The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and 0 uses thereof. P''