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1. (WO2003077830) 9-DEXO-9A-AZA-9A-METHYL-9A-HOMOERYTHROMYCIN A DERIVATIVES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2003/077830    International Application No.:    PCT/IB2003/000987
Publication Date: 25.09.2003 International Filing Date: 18.03.2003
Chapter 2 Demand Filed:    16.10.2003    
IPC:
C07H 17/00 (2006.01), C07H 17/08 (2006.01)
Applicants: PLIVA - ISTRAZIVACKI INSTITUT d.o.o. [HR/HR]; Prilaz baruna Filipovica 29, 10000 Zagreb (HR)
Inventors: DUMIC, Miljenko; (HR).
VINKOVIC, Mladen; (HR).
ORESIC, Marina; (HR).
MESTROVIC, Ernest; (HR).
DANILOVSKI, Aleksandar; (HR).
DUMBOVIC, Alojz; (HR).
KNEZEVIC, Zdravka; (HR).
LAZAREVSKI, Gorjana; (HR).
CINCIC, Dominik; (HR).
FILIC, Darko; (HR).
LAZARIC, Katica; (HR).
BUCAR, Dejan-Kresimir; (HR)
Priority Data:
P20020231A 18.03.2002 HR
60/393,612 03.07.2002 US
60/394,705 08.07.2002 US
Title (EN) 9-DEXO-9A-AZA-9A-METHYL-9A-HOMOERYTHROMYCIN A DERIVATIVES
(FR) PSEUDOPOLYMORPHES ISOSTRUCTURAUX DE 9-DESOXO-9A-AZA-9A-METHYL-9A-HOMOERYTHROMYCINE A
Abstract: front page image
(EN)Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a- homo erythromycin A having the Formula I: wherein S is an organic solvent which is at least partially miscible with water, x is 1, 1.25, 1.5 or 2, y is 0, 0.5, or 1, the pseudopolymorph being characterized by the monoclinic space group P21 and average unit cell parameters comprising: crystal axis lengths of a = 15.5 - 17.0 Å, b = 15.5 - 17.0 Å, and c = 17.5 - 19.5 A, and angles between the crystal axes of &agr;. = ϝ = 90° and &bgr; = 106° - 112°. In addition, this disclosure is directed to processes for the preparation of the substantially pure isostructural pseudopolymorphs of Formula I; to pharmaceutical compositions containing substantially pure isostructural pseudopolymorphs of Formula I; and to a method for the treatment of bacterial and protozoan infections, and inflammation-related diseases by administration of a pharmaceutical composition containing the substantially pure isostructural pseudopolymorphs of Formula I.
(FR)L'invention concerne des pseudopolymorphes isostructuraux de 9-désoxo-9a-aza-9a-méthyl-9a-homoérythromycine A de formule (I), dans laquelle S est un solvant organique au moins partiellement miscible avec l'eau, x vaut 1, 1,25, 1,5 ou 2, et y vaut 0, 0,5 ou 1, le pseudopolymorphe étant caractérisé par le groupe d'espace monoclinique P21 et par des paramètres de motifs élémentaires moyens incluant les longueurs des axes cristallographiques, soit a = 15,5 17,0 Å, b = 15,5 17,0 Å, et c = 17,5 19,5 Å, ainsi que les angles entre les axes cristallographiques, soit $g(a) = $g(g) = 90° et $g(b) = 106° - 112°. En outre, l'invention concerne des procédés de préparation de pseudopolymorphes isostructuraux sensiblement purs de formule (I), des compositions pharmaceutiques contenant des pseudopolymorphes isostructuraux sensiblement purs de formule (I), ainsi qu'une méthode destinée à traiter des infections bactériennes et protozoaires et des maladies associées à une inflammation par administration d'une composition pharmaceutique contenant ces pseudopolymorphes isostructuraux sensiblement purs de formule (I).
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, OM, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, MZ, 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, IT, LU, MC, NL, 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)