(WO/1998/046618) MORPHINE DERIVATIVES

(WO/1998/046618) MORPHINE DERIVATIVES

Latest bibliographic data on file with the International Bureau
Pub. No.:  WO/1998/046618   International Application No.:  PCT/GB1998/001071
Publication Date:22.10.1998 International Filing Date:14.04.1998
IPC: C07H 15/24 (2006.01)
Applicants:SALFORD ULTRAFINE CHEMICALS AND RESEARCH LTD. [GB/GB]; Synergy House, Guildhall Close, Manchester Science Park, Manchester M15 6SY (GB) (AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, CA, CF, CG, CH, CI, CM, CN, CU, CY, CZ, DE, DK, EE, ES, FI, FR, GA, GB, GE, GH, GM, GN, GR, GW, HU, ID, IE, IL, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MC, MD, MG, MK, ML, MN, MR, MW, MX, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, UA, UG, UZ, VN, YU, ZW only).
SCHEINMANN, Feodor [GB/GB]; (GB) (US Only).
STACHULSKI, Andrew, Valentine [GB/GB]; (GB) (US Only).
JOEL, Simon [GB/GB]; (GB) (US Only).
Inventors:SCHEINMANN, Feodor; (GB).
STACHULSKI, Andrew, Valentine; (GB).
JOEL, Simon; (GB).
Agent:QUEST, Barry et al.; Wilson Gunn M'Caw, 41-51 Royal Exchange, Cross Street, Manchester M2 7BD (GB).
Priority Data:
08/833,203 14.04.1997 US
9721137.9 07.10.1997 GB
Title: MORPHINE DERIVATIVES
Abstract: A new morphine derivative of formula (I) having enhanced activity in the treatment of pain is of the form 1-(morphine-6-yl)-$g(b)-D-glucopyrano siluronic acid, and acid addition and metal salts, wherein the usual ethylenic bond between the 7, 8 position of the morphine part of the molecule is modified by adducts and preferably the 7, 8 dihydromorphine derivatives is used. The compound may be formed by condensing morphine sulfate (with the 3-phenolic group protected by acylation) with D-glucuronolactone (with the hydroxyl and carboxylic acid groups protected) and then removing the protecting groups to give morphine-6-glucuronide; and at some stage the morphine-6-glucuronide is hydrogenated. In formula (I), positions 7, 8 is dihydro, dihydroxy-, hydroxyhalo-, epoxy-, dihalo-, hydrohalo-, hydrohydroxy-, or CXY (X, Y is halogen or hydrogen) adducts.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, GM, GW, HU, ID, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZW.
African Regional Intellectual Property Org. (ARIPO) (GH, GM, KE, LS, MW, SD, SZ, UG, ZW)
Eurasian Patent Organization (EAPO) (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (OAPI) (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG).
Publication Language:English (EN)
Filing Language:English (EN)

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