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Pub. No.:    WO/2006/087644    International Application No.:    PCT/IB2006/001238
Publication Date: 24.08.2006 International Filing Date: 13.01.2006
C07H 17/00 (2006.01), C07H 17/08 (2006.01), A61K 31/7052 (2006.01), A61K 31/7048 (2006.01), A61P 29/00 (2006.01)
Applicants: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O. [HR/HR]; Prilaz baruna Filipovica 29, 10000 Zagreb (HR) (AE, AG, AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GW, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KM, KN, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, MG, MK, ML, MN, MR, MW, MX, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SI, SK, SL, SM, SN, SY, SZ, TD, TG, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, YU, ZA, ZM, ZW only).
CULIC, Ognjen [HR/HR]; (HR) (For US Only).
BOSNAR, Martina [HR/HR]; (HR) (For US Only).
MARJANOVIC, Nikola [HR/HR]; (HR) (For US Only).
JELIC, Dubravko [HR/HR]; (HR) (For US Only).
ALIHODZIC, Sulejman [HR/HR]; (HR) (For US Only).
VELA, Vanja [HR/HR]; (HR) (For US Only).
MARUSIC-ISTUK, Zorica [HR/HR]; (HR) (For US Only).
ERAKOVIC, Vesna [HR/HR]; (HR) (For US Only).
BOSNJAK, Berislav [HR/HR]; (HR) (For US Only).
HRVACIC, Boska [HR/HR]; (HR) (For US Only).
TOMASKOVIC, Marija [HR/HR]; (HR) (For US Only).
MUNIC, Vesna [HR/HR]; (HR) (For US Only).
IVETIC, Vanesa [HR/HR]; (HR) (For US Only).
HUTINEC, Antun [HR/HR]; (HR) (For US Only).
KRAGOL, Goran [HR/HR]; (HR) (For US Only).
LELJAK, Marija [HR/HR]; (HR) (For US Only)
Inventors: CULIC, Ognjen; (HR).
BOSNAR, Martina; (HR).
JELIC, Dubravko; (HR).
ALIHODZIC, Sulejman; (HR).
VELA, Vanja; (HR).
ERAKOVIC, Vesna; (HR).
BOSNJAK, Berislav; (HR).
HRVACIC, Boska; (HR).
MUNIC, Vesna; (HR).
IVETIC, Vanesa; (HR).
HUTINEC, Antun; (HR).
KRAGOL, Goran; (HR).
LELJAK, Marija; (HR)
Priority Data:
60/643,841 13.01.2005 US
60/715,828 09.09.2005 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 substituted at the 4' 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-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.
(FR)L'invention concerne de nouveaux macrolides semi-synthétiques qui présentent une activité anti-inflammatoire. D'une manière plus spécifique, l'invention concerne des macrolides à 14 ou 15 éléments substitués en position 4', leurs dérivés pharmaceutiquement acceptables, des processus et des intermédiaires pour leur préparation, des compositions pharmaceutiques contenant ces macrolides ainsi que leur activité et leur utilisation dans le traitement de maladies et d'états inflammatoires sur des humains et des animaux, notamment des maladies associées à une sécrétion excessive de TNF-a, IL-1, IL-8, IL-2 ou IL-5 ; et/ou à l'inhibition d'une prolifération lymphocytaire excessive ; et/ou à une 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)