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1. (WO2004052904) NOVEL SEMISYNTHETIC MACROLIDE ANTIBIOTICS OF THE AZALIDE SERIES
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2004/052904 International Application No.: PCT/HR2003/000062
Publication Date: 24.06.2004 International Filing Date: 10.12.2003
IPC:
A61K 31/70 (2006.01) ,A61P 31/04 (2006.01) ,C07H 17/00 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
70
Carbohydrates; Sugars; Derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
04
Antibacterial agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
17
Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
Applicants:
KUJUNDZIC, Nedjeljko [HR/HR]; HR (UsOnly)
BUKVIC KRAJACIC, Mirjana [HR/HR]; HR (UsOnly)
BRAJSA, Karmen [HR/HR]; HR (UsOnly)
PLIVA - ISTRAZIVACKI INSTITUT D.O.O. [HR/HR]; Prilaz baruna Filipovica 29 10000 Zagreb, HR (AllExceptUS)
Inventors:
KUJUNDZIC, Nedjeljko; HR
BUKVIC KRAJACIC, Mirjana; HR
BRAJSA, Karmen; HR
Priority Data:
P20020991A12.12.2002HR
Title (EN) NOVEL SEMISYNTHETIC MACROLIDE ANTIBIOTICS OF THE AZALIDE SERIES
(FR) DERIVES 9A-N-(N'-CARBAMOYL-$G(G)-AMINOPROPYLE), 9A-N-(N'- -THIOCARBAMOYL-$G(G)-AMINOPROPYLE), 9A-N-[N'-(($G(B)-CYANOETHYL)-N'-CARBAMOYL-$G(G)-AMINOPROPYLE] ET 9A-N-[N'-($G(B)-CYANOETHYL)-N'-THIOCARBAMOYL-$G(G)-AMINOPROPYLE] N'-SUBSTITUES DE 9-DEOXO-9-DIHYDRO-9A-AZA-9A-HOMOERYTHROMYCINE A ET 5-O-DESOSAMINYL-9-DEOXO-9- DIHYDR
Abstract:
(EN) The invention relates to N'-substituted 9a-N-(N'-carbamoyl-ϝ-aminopropyl), 9a--N-(N'-thiocarbamoyl-ϝ-aminopropyl), 9a-N-[N'-((&bgr;-cyanoethyl)-N'-carbamoyl-ϝ -aminopropyl] and 9a-N-[N'-((&bgr;-cyanoethyl)-N'-thiocarbamoyl-ϝ-aminopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, R1 represents H or (&bgr;-cyanoethyl moiety, R2 represents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, &bgr;-phenylethyl, ethoxycarbonylmethyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents 0 and S, and their acceptable addition salts thereof with inorganic or organic acids, to the process for preparation of their pharmaceutical compositions as well as the use their compositions in the treatment of bacterial infections.
(FR) L'invention concerne des dérivés 9a-N-(N'-carbamoyl-$g(g)-aminopropyle), 9a-N-(N'- -thiocarbamoyl-$g(g)-aminopropyle), 9a-N-[N'-(($g(b)-cyanoéthyl)-N'-carbamoyl-$g(g)-aminopropyle] et 9a-N-[N'-($g(b)-cyanoéthyl)-N'-thiocarbamoyl-$g(g)-aminopropyle] N'-substitués de 9-déoxo-9-dihydro-9a-aza-9a-homoérythromycine A, qui constituent de nouveaux antibiotiques semi-synthétiques de la série des azalides, de formule générale (1), dans laquelle R représente H ou une fraction cladinosyle, R1 représente H ou une fraction $g(b)-cyanoéthyle, R2 représente un groupe isopropyle, 1-naphtyle, 2-naphtyle, benzyle, 2-(trifluorométhyl)phényle, 3-phénylpropyle, $g(b)-phényléthyle, éthoxycarbonylméthyle, 1-(1-naphtyl)éthyle, 3,4,5-triméthoxyphényle et 2,4-dichlorophényle, et X représente O et S. L'invention concerne également les sels d'addition avec des acides inorganiques ou organiques, pharmaceutiquement acceptables, desdits dérivés. L'invention concerne en outre un procédé de préparation de compositions pharmaceutiques ainsi que l'utilisation de ces dernières pour le traitement d'infections bactériennes.
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, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (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)