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filingDate 1973-07-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1975-03-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1386206-A
titleOfInvention Oxyacetic ether derivatives of orthothymotic esters their prepa ration and their applications
abstract 1386206 Ortho thymotic acid esters CENTRE D'ETUDES POUR L'INDUSTRIE PHARMACEUTIQUE 13 July 1973 [20 July 1972] 33576/73 Heading C2C Novel compounds of formula in which R<SP>1</SP> is an amino radical or an OR group in which R represents a lower alkyl radical having 1-4 carbon atoms, n is an integer from 1 to 4, R 2 considered individually in each radical -(CHR<SP>2</SP>)- is hydrogen or an alkyl radical having 1-6 carbon atoms; R<SP>3</SP> and R<SP>4</SP>, which may be the same or different, are hydrogen or an alkyl radical having 1-6 carbon atoms or,together with the nitrogen atom to which they are attached, form a heterocyclic ring optionally containing another hetero-atom, X and Y are hydrogen, a nitro radical, an amino radical or halogen, and their acid addition salts and their quaternary ammonium derivatives are prepared by reacting a compound of formula in which X and Y are as defined above with an esterifying agent of the formula A(R) a in which R is as defined in claim 1, A is an anion and a is the valence of said anion, to give the derivative of the Formula (II): in which R<SP>1</SP> is OR and, if desired, converting group OR to an NH 2 group, and then reacting derivative (II) with a lower alkyl halogenoacetate Z-CH 2 -COO-Alk in which Z is halogen and Alk is a lower alkyl group, to give the esterified oxyacetic derivative of the formula: in which R<SP>5</SP> is a lower alkoxy group, hydrolysing group COR<SP>5</SP> to a carboxyl group, esterifying same with an aminoalcohol of the formula in which R<SP>2</SP>, R<SP>3</SP>, R<SP>4</SP> and n are as defined in claim 1 and, if desired, salifying resulting derivative (I). Pharmaceutical compositions in conventional forms for oral, rectal or parenteral administration and having vaso and coronary dilatory activity, local anaesthetic and antitussive activity comprise an above novel compound and a carrier or diluent.
priorityDate 1972-07-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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Total number of triples: 36.