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Pub. No.:    WO/2006/077501    International Application No.:    PCT/IB2006/001097
Publication Date: 27.07.2006 International Filing Date: 13.01.2006
C07H 17/08 (2006.01), A61K 31/7048 (2006.01)
Applicants: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. [HR/HR]; Prilaz Baruna Filipovica 29, 10000 Zagreb (HR) (For All Designated States Except US).
CULIC, Ognjen [HR/HR]; (HR) (For US Only).
BOSNAR, Martina [HR/HR]; (HR) (For US Only).
ALIHODZIC, Sulejman [HR/HR]; (HR) (For US Only).
LAZAREVSKI, Gorjana [HR/HR]; (HR) (For US Only).
ISTUK MARUSIC, Zorica [HR/HR]; (HR) (For US Only).
HUTINEC, Antun [HR/HR]; (HR) (For US Only).
VELA, Vanja [HR/HR]; (HR) (For US Only).
KRAGOL, Goran [HR/HR]; (HR) (For US Only)
Inventors: CULIC, Ognjen; (HR).
BOSNAR, Martina; (HR).
ALIHODZIC, Sulejman; (HR).
LAZAREVSKI, Gorjana; (HR).
HUTINEC, Antun; (HR).
VELA, Vanja; (HR).
KRAGOL, Goran; (HR)
Agent: CRAWLEY, Karen; GlaxoSmithKline, Corporate Intellectual Property, 980 Great West Road, Brentford, Middlesex TW8 9GS (GB)
Priority Data:
60/643,840 13.01.2005 US
Abstract: front page image
(EN)The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-&agr;, IL-1, IL-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.
(FR)La présente invention concerne des nouveaux macrolides semi-synthétiques présentant une activité anti-inflammatoire. Plus particulièrement, cette invention concerne des macrolides à 14 et 15 ramifications sans sucre de cladinose substitué à la position C-3, des dérivés pharmaceutiquement acceptables, des procédés et des produits intermédiaires permettant leur préparation, des compositions pharmaceutiques les contenant ainsi que leur activité et leur utilisation dans le traitement de maladies et affections inflammatoires chez des humains et des animaux, plus spécialement, des maladies associées à une sécrétion excessive de TNF-a, IL-1, IL-6, IL-8, IL-2 ou de IL-5; et/ou un inhibiteur de la prolifération excessive des lymphocites; et/ou de dégranulation excessive des granulocytes.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)