http://rdf.ncbi.nlm.nih.gov/pubchem/patent/IE-41697-B1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_df4e72183c5ee38a234212562dca6570 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C03C17-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D501-20 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C03C17-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-546 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-06 |
| filingDate | 1975-09-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1980-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | IE-41697-B1 |
| titleOfInvention | New cephalosporin derivatives their preparation and compositions containing them |
| abstract | 1481779 7 - [α - Amino - (5,6 - dihydro - 1,4- dithiin- and oxathiin-2-yl)acetamido]cephalo- Sporins RHONE-POULENC INDUSTRIES 26 Sept 1975 [27 Sept 1974 21 July 1975] 39589/75 Heading C2C Novel 7 - [α - amino - (5,6 - dihydro - 1,4- dithiin- and oxathiin-2-yl)acetamido]cephalosporins of the general Formula I wherein A is O or S, R 1 is H or acetoxy and R 2 is - COOH or -COOCHR 3 OCOR 4 , in which -CHR 3 OCOR 4 is a radical which can be easily removed enzymatically and in which R 3 is H or straight- or branched-chain C 1-4 alkyl and R 4 is straight- or branched-chain C 1-4 alkyl or cyclohexyl, which may be in diastereomeric forms or mixtures thereof, and pharmaceutically acceptable acid addition salts thereof and, when R 2 is -COOH, pharmaceutically acceptable non- toxic metal salts thereof and addition salts thereof with N-containing bases other than ammonia are prepared (a) by reacting an acid of the general Formula IV which is in racemic or optically active form and in which the amino group is protected, or a reactive derivative thereof with an amine of the general Formula V in which the carboxy group may be protected and removing the protecting group(s) from the resulting protected cephalosporin; and (b) when R 2 is -COOCHR 3 OCOR 4 , by esterifying the corresponding compound in which R 2 is - COOH, in amino-protected form, and removing the protecting group ; and optionally salifying the product. Amino-protected acids of the general Formula IV are prepared by reacting HA-CH 2 CH 2 -SH with X-CH 2 COC(=NOH)COOR 5 , in which X is halogen and R 5 is C 1-4 alkyl, cyclizing the resulting alkyl 2 - hydroxylimino - 4 - mercapto- 3-oxo-butyrate, reducing the resulting oxime of the general Formula VII saponifying the resulting ester of the general Formula VI and N-protecting the resulting acid (the racemic form of which can be resolved using (+)- camphorsulphonic acid). Pharmaceutical compositions having antibacterial activity comprise, as active ingredient, at least one 7-[α-amino-(5,6-dihydro-1,4-dithiin- or oxathiin-2-yl)acetamido]cephalosporin (I) or salt thereof as defined above, in association with a pharmaceutically acceptable carrier, diluent or adjuvant. |
| priorityDate | 1974-09-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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