http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0048613-B1
Outgoing Links
Predicate | Object |
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classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07H15-224 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D207-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7036 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7034 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7028 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07H15-224 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07H15-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-70 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N63-02 |
filingDate | 1981-09-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 1985-01-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1985-01-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | EP-0048613-B1 |
titleOfInvention | 4-0-substituted -2-deoxystreptamine aminoglycoside derivatives, their preparation and formulations containing them |
abstract | Novel compounds are disclosed which are 2 min -N-acylated or 2 min -N-alkylated derivatives of a 4-O-substituted-2-deoxystreptamine aminoglycoside selected from the group consisting of: apramycin, alpha or beta -(C1 to C6 alkyl)aprosaminide, alpha or beta -(C2 to C6 hydroxyalkyl)aprosaminide, alpha or beta -(C2 to C6 aminoalkyl)aprosaminide, alpha or beta -(C2 to C6 protected aminoalkyl)aprosaminide, alpha or beta -(C3 to C6 aminohydroxyalkyl)aprosaminide, alpha or beta -(C3 to C6 (protected amino)hydroxyalkyl)aprosaminide, or a pharmaceutically-acceptable acid addition salt thereof; wherein the acyl or alkyl substituent group is selected from the group consisting of gamma -amino- alpha -hydroxybutyryl, gamma -protected amino- alpha -hydroxybutyryl, beta -amino- alpha -hydroxypropionyl, beta -protected amino- alpha -hydroxypropionyl, glycyl, N-protected glycyl, 3-hydroxypyrrolidine-3-carbonyl, N-protected 3-hydroxypyrrolidine-3-carbonyl, 3-hydroxyazetidine-3-carbonyl, N-protected 3-hydroxyazetidine-3-carbonyl, 2-hydroxy-2-(azetidin-3-yl)acetyl, N-protected 2-hydroxy-2-(azetidin-3-yl)acetyl, 4-amino-2-hydroxybulyl, 3-amino-2-hydroxypropyl, 2-aminoethyl, 3-hydroxypyrrolidine-3-methylene, 3-hydroxyazetidine-3-methylene, 2-hydroxy-2-(azetidin-3-yl)ethyl, C2 to C4 alkyl, C3 to C5 allyl, benzyl and substituted benzyl. They are useful for treating warm blooded animals suffering from bacterial diseases. They and 2 min -N-acylated and 2 min -N-alkylated derivatives of lividamine, paromamine and the 6 min -N-protected derivatives of nebramine, neamine, gentamine C1, gentamine C1a, gentamine C2, gentamine C2a, and gentamine C2b, and pharmaceutically-acceptable acid addition salts thereof can be prepared by reacting the corresponding aminoglycoside substrate with a nickel salt Ni (X2), X being C1 to C10 carboxylate, in water, diluting with a polar organic solvent, treating with an alkylating agent or acylating agent, optionally, deprotecting the amino or N-protected substituents, optionally, reducing carbonyl portions of an acyl group, and recovering as a free base or as a pharmaceutically-acceptable acid addition salt. |
priorityDate | 1980-09-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 76.