http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1419256-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a717ea5b2ac78ac329ab3a9659d834d2 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D499-54 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D205-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D277-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D499-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D265-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-43 |
| filingDate | 1972-12-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1975-12-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1419256-A |
| titleOfInvention | Penicillins and processes for the preparation of penicillins |
| abstract | 1419256 6 [(1-Amino-cycloalkyl)actamido]- penicillanic acids AMERICAN HOME PRO DUCTS CORP 13 Dec 1972 [16 Dec 1971] 57404/72 Heading C2C New penicillins of the general formula wherein R and R<SP>1</SP> are each H or C 1 -C 3 alkyl, Y is -CH 2 -, n is an integer from 1 to 5 and Z is an amino group optionally protected with a removable blocking group, are prepared by reacting a compound of Formula III wherein Z is an amino group or a group convertible thereto, an azido group or a nitro group with 6-aminopenicillanic acid or a functional derivative thereof followed, if necessary, by conversion of the group Z to an amino group by conventional methods. Alternatively, an N-carboxy amino acid anhydride of general formula or a 1-aminocycloalkaneacetic acid chloride hydrochloride of general formula where n, R, R<SP>1</SP> and Y have the above meanings may be reacted with the penicillanic acid compound which, in either case, may be a silyl derivative, a phosphorylated derivative or a 6-aminopenicillanamide in which the amide group is -CONXY wherein X and Y are electron-withdrawing groups or form, together with the N atom, a cyclic electron-withdrawing group followed by appropriate reactions to regenerate the carboxylic acid group of the penicillanic acid moiety. Alternatively, X and Y may be concatenated to form a saccharyl or substituted saccharyl group. The compound 6 - [2 - (1 - aminocyclohexyl) - acetamido]- penicillanic acid has been prepared in two different crystalline forms both of which, together with their preparations, are described. As illustrations of the preparation of the starting compounds of Formula III, there are prepared: (a) 1-aminocyclohexane acetic acid by treating 1-azospiro[3,5]nonane-2-one with concentrated HCl (1-amino-2,6-trans-dimethylcyclohexane acetic acid hydrate; 1-aminocyclobutaneacetic acid; 2-(1-aminocyclooctyl)-2-methyl acetic acid 1-aminocyclooctaneacetic acid and 1- aminocycloheptane acetic acid being made similarly), (b) 1-aminocyclopentane acetic acid (and other similar acetic acid derivatives similarly) by reacting cyclopentanone with malonic acid and ammonium acetate (or with ammonium malonate) and, (e) the N-carboxy anhydrides of such acetic acid derivatives by treatment thereof with phosgene. Pharmaceutical compositions comprise the new penicillins of the invention in which Z is NH 2 in association or conjunction with conventional pharmaceutical carriers and excipients. They may be in forms suitable for oral, parenteral and topical administration. |
| priorityDate | 1971-12-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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