http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1000406-A

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D307-82
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D307-82
filingDate 1961-10-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1f708a728dd538097ee2bca9c3a7e93d
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_15dcf67914b783b3e7dd13ca03989580
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publicationDate 1965-08-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1000406-A
titleOfInvention Heterocyclic guanidine compounds
abstract The invention comprises pharmaceutically acceptable acid addition salts of guanidine derivatives of coumaran and indane, the corresponding free bases, which are unstable, having the formula <FORM:1000406/C2/1> wherein R1, R2, R3 and R4 are hydrogen, halogen or C1- 5 alkyl and X is O or CH2, except that where X is oxygen R1-R4 are not all hydrogen, and their preparation by reacting a salt of a 3-amino coumaran or indane with cyanamide in a solvent. Preferred products include salts of 5-chloro- and 5-, 6- and 7-methyl-, 3-guanidino-coumaran and 1-indanylguanidine. Specified anions include the chloride, bromide, iodide, sulphate, perchlorate, nitrate, phosphate and organic anions. The products may be obtained as d and l optical isomers and racemates. The guanidine derivatives may also be prepared by reacting the corresponding amine with dicyandiamide, an O-alkylisourea or thiourea in the presence of a desulphurizing agent, such as lead monoxide or iodine. Alternatively, in some cases a 3-halo-coumeran or indane may be reacted with guanidine. 5 - Chloro - and 7 - methyl - 3 - aminocoumarans are made by reducing the corresponding coumarone-oximes with sodium amalgam.ALSO:Pharmaceutical preparations having an adrenergic and nerve-blocking action, used for the treatment of hypertension, comprise the pharmaceutically acceptable acid addition salts of 3-guanidino-coumarans and indanes, whereof the free bases (which are unstable) have the formula <FORM:1000406/A5-A6/1> where R1, R2, R3 and R4 are hydrogen or halogen atoms or C1-5 alkyl groups and X is 0 or CH2, except that when X is oxygen R1-R4 are not all hydrogen (see Division C2), in association with a pharmaceutical carrier, preferably in a form suitable for oral or parenteral administration. Specified anions include the chloride, bromide, iodide, sulphate, perchlorate, nitrate, phosphate and organic anions. The preparations may be in liquid or solid form such as solutions, suspensions, emulsions, powders, encapsulated powders, tablets or lozenges and may contain, in addition to conventional diluents and solvents, adhesives, disintegrating agents, lubricants, sweetening agents, thickeners, emulsifying agents, buffering agents and preservatives. Liquid preparations for parenteral administration may also contain bactericides or bacteriostatics such as phenol, cresol, chlorbutol, chlorocresol and benzyl alcohol and antioxidants such as sodium sulphite, sodium metabisulphite and ascorbic acid.
priorityDate 1961-10-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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