http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1497083-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0d6256baf554e46784d8daa478a2ddc6 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-03 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-096 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-02 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-03 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-096 |
| filingDate | 1975-01-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1978-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1497083-A |
| titleOfInvention | 1-substituted-4-(1,2-diphenylethyl)-piperazine derivatives and their salts and the preparation thereof |
| abstract | 1497083 1 - (1,2 - Diphenylethyl) - piperazines DAINIPPON PHARMACEUTICAL CO Ltd 22 Jan 1975 [23 Jan 1974 12 March 1974 14 March 1974] 2773/75 Heading C2C Novel 1 - (1,2 - diphenylethyl) - piperazines of the general formula wherein X is a hydroxy, methoxy, methyl or trifluoromethyl group and R is a C 6-8 monocycloalkyl or 2-methoxyphenyl group, provided that, when X is a hydroxy group, R is a cyclohexyl group and, when X is a trifluoromethyl group, R is a 2-methoxyphenyl group, and pharmaceutically acceptable acid addition salts thereof are prepared (a) by reacting a 1,2-diphenylethylamine of the general formula wherein Z is a residue of a reactive ester of an alcohol, or an acid addition salt thereof with an amine of the general formula R-NH 2 , (b) by reacting a 1,2-diphenylethylamine of the general formula with an amine of the general formula or a salt thereof, (c) when X is a methoxy, methyl or trifluoromethyl group, by reacting a nitrile and a Grignard reagent of the respective general formulae wherein Z<SP>1</SP> is a halogen atom and X<SP>1</SP> is a methoxy, methyl or trifluoromethyl group; and (d) when X is a hydroxy group, by subjecting an ether of the general formula wherein Y is a C 1-7 alkyl or benzyl group, or a salt thereof to cleavage of the ether linkage, followed optionally by salification of the product. 1,2 - Diphenylethylamines of the second general formula above wherein X is other than a hydroxy group are prepared by reacting 3 - (2 - hydroxyethyl) - 2 - phenyloxazolidine with a Grignard reagent of the general formula in an inert solvent and halogenating the resulting amino-alcohol of the general formula Nitriles of the sixth general formula above are prepared by heating a salt of piperazine of the general formula with benzaldehyde and NaCN or KCN in water or an aqueous solvent. Ethers of the eighth general formula above (isolated as acid addition salts) are prepared analogously to process (b) above. Pharmaceutical compositions having analgesic, antitussive and antiinflammatory activity comprise, as active ingredient, at least one 1-(1,2- diphenylethyl)piperazine of the first general formula above or a pharmaceutically acceptable acid addition salt thereof, together with a pharmaceutically acceptable carrier and/or diluient therefor. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0755680-A3 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6100280-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0755680-A2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-2138016-A |
| priorityDate | 1974-01-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 42.