http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-761392-A

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D499-00
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D499-24
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D499-00
filingDate 1954-04-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1956-11-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-761392-A
titleOfInvention Improvements in or relating to diamino-2-butenes and penicillin salts thereof
abstract The invention comprises (1) the preparation of diamines of the formula R-NH-CH2-CH = CH-CH2-NH-R where R is alkyl, alkenyl, aralkyl, alicylic, partially unsaturated polyalicylic, heterocyclic-alkyl or alicyclic-alkyl, by reacting 1:4-diaminobut-2-ene with R-Hal; (2) the preparation of diamines as in (1) where R is alkyl, alkenyl, aralkyl, heterocyclic-alkyl or alicyclic-alkyl by reacting 1:4-diaminobut-2-ene or a salt thereof with the appropriate aldehyde and hydrogenating the product; and (3) penicillin salts of the diamines of (1) and their preparation by reacting the di-secondary diamine or a salt thereof with penicillin or a salt thereof. Examples are given of the preparation of 1:4-dibenzylaminobut - 2 - ene and 1:4 - didodecylaminobut - 2 - ene and hydrochloride and penicillin salts thereof. Other groups specified for R are dehydroabietyl, dihydroabietyl, tetrahydroabietyl, cinnamyl, decyl, undecyl, tetradecyl, hexadecyl, octadecyl, decenyl, undecenyl, dodecenyl, tetradecenyl, hexadecenyl, octadecenyl, thienylethyl, cyclohexyl, cyclohexylethyl and furfuryl. The penicillin used may be G, F, X, K, O or other biosynthetic penicillin.ALSO:Therapeutic compositions comprise penicillin salts of diamines of the formula R-NH-CH2-CH=CH-CH2-NH-R where R is alkyl, alkenyl, aralkyl, alicyclic, partially unsaturated polyalicylic (e.g. derived from resin amines), heterocyclic-alkyl or alicyclic-alkyl, suspended in a pharmaceutical carrier. The latter may comprise an aqueous solution of a wetting agent, buffer, bacteriostat and a suspending agent such as carboxymethyl-cellulose. An example is given of such a composition containing the benzylpenicillin salt of 1:4-dibenzylaminobut-2-ene, sodium citrate, a sorbitan mono-oleate polyglycol ether and methyl and propyl p-hydroxybenzoates. Many other groups are specified for R in the formula above. The penicillin may be G, F, X, K. O or other biosynthetic penicillin. It is also stated that the salts may be applied intramuscularly in a hydrocarbon oil or wax base, and that other penicillin salts may be present, e.g. of procaine or alkali metals.
priorityDate 1953-04-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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