ISOSTRUCTURAL PSEUDOPOLYMORPHS OF 9- DEOXO-9A-AZA-9A-METHIL- 9A- HOMOERYTHROMYCIN A

• Main Authors: VINKOVIC MLADEN, BUCAR DEJAN-KRESIMIR, CIN IC DOMINIK, DUMBOVIC ALOJZ, DUMIC MILJENKO, DANILOVSKI ALEKSANDAR, FILIC DARKO, LAZARIC KATICA, LAZAREVSKI GORJANA, ORESIC MARINA, KNEZEVIC ZDRAVKA, MESTROVIC ERNEST
• Format: Patent
• Language: English; Serbian
• Published: 15.12.2006
• Edition: 7
• Subjects: CHEMISTRY; DERIVATIVES THEREOF; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; NUCLEIC ACIDS; NUCLEOSIDES; NUCLEOTIDES; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS; SUGARS

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 ?, b = 15.5 - 17.0 ?, and c = 17.5 - 19.5 A, and angles between the crystal axes of ?. = ? = 90ò and ? = 106ò - 112ò. 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. Stvarno čisti izostrukturni pseudopolimorfi 9-deoksi-9a-aza-9a-metil-9a-homoeritoromicina A koji imaju formulu I gde S je organski rastvarač koji je najmanje delimično mešljiv sa vodom, x je 1, 1,25, 1,5 ili 2, y je 0, 0,5 ili 1, poseudopolimorfi koji su okarakterisani kao monociklična prostorna grupa P21 i sa opsegom parametara ćelijske jedinice koji uključuju: dužine kristalnih osa od a=15,5-17,0 , b=15,5-17,0 i c=17,5-19,5 , i uglovima između kristalnih osa od α=-90° i á=106-112°. Dalje, ovo otkriće se odnosi na postupak za dobijanje stvarno čistih pseudopolimorfa formule I; farmaceutske kompozicije koje sadrže stvarno čiste izostrukturne pseudopolimorfe formule I; i na postupak za tretman bakterijskih i protozoičnih infekcija i oboljenja vezanih za zapaljenja sa uzimanjem farmaceutske kompozicije koja sadrži stvarno čiste izostrukturne pseudopolimorfe formule I.