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filingDate 1981-01-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_828e9e1e9e474185b4bd4e97a305678c
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publicationDate 1981-08-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-0034259-A1
titleOfInvention Peptides, process for their preparation and medicaments or diagnostic agents containing them
abstract X für einen Acylrest einer N-Methylaminosäure oder einer in der a-Stellung eine Aminooxygruppe oder eine Hydroxygruppe aufweisenden aliphatischen Carbonsäure. jeweils in der L-Konfiguration im Falle eines asymmetrischen Kohlenstoffatomes, steht, Arg einen Rest von L-Arginin mit 1 gegenüber dem L-Arginin fehlenden Wasserstoffatom an einem Aminostickstoffatom außer dem Fehlen der Hydroxygruppe der Carboxylgruppe bedeutet. Val einen Rest von L-Valin mit 1 gegenüber dem L-Valin fehlenden Wasserstoffatom am Stickstoffatom außer dem Fehlen der Hydroxygruppe der Carboxylgruppe darstellt, , Tyr für einen Rest von L-Tyrosin mit 1 gegenüber dem L-Tyrosin fehlenden Wasserstoffatom am Stickstoffatom außer dem Fehlen der Hydroxygruppe der Carboxylgruppe steht, lle einen Rest von L-Isoleucin mit 1 gegenüber dem L-Isoleucin fehlenden Wasserstoffatom am Stickstoffatom außer dem Fehlen der Hydroxygruppe der Carboxylgruppe bedeutet, His einen Rest von L-Histidin mit 1 gegenüber dem L-Histidin fehlenden Wasserstoffatom an einem Aminostickstoffatom außer dem Fehlen der Hydroxygruppe der Carboxylgruppe darstellt, Pro für einen Rest von L-Prolin mit 1 gegenüber dem L-Prolin fehlenden Wasserstoffatom am Stickstoffatom außer dem Fehlen der Hydroxygruppe der Carboxylgruppe steht. Y einen Rest einer aliphatischen Aminosäure mit 1 gegenüber dieser Säure fehlenden Wasserstoffatom am Stickstoffatom beziehungsweise an einem Aminostickstoffatom außer dem Fehlen der Hydroxygruppe der Carboxylgruppe, jeweils in der L-Konfiguration im Falle eines asymmetrischen Kohlenstoffatomes, bedeutet und A einen Alkylrest mit 1 bis 5 Kohlenstoffatom(en) darstellt, ihre Säureadditionssalze und pharmazeutisch brauchbaren Komplexe, sowie ein Verfahren zu ihrer Herstellung. Diese Verbindungen können in Arzneimitteln auf dem Gebiet der Therapie und Diagnose, insbesondere zum Antagonisieren von Angiotensin und so zum Beispiel in Bezug auf hohen Blutdruck, verwendet werden. Octapeptide esters of the general formula wherein X represents an acyl radical of an N-methylamino acid or an aliphatic carboxylic acid having an aminooxy group or a hydroxyl group in the a position. each in the L configuration in the case of an asymmetric carbon atom, Arg is a residue of L-arginine with 1 hydrogen atom missing from the L-arginine on an amino nitrogen atom except for the absence of the hydroxyl group of the carboxyl group. Val represents a residue of L-valine with 1 hydrogen atom on the nitrogen atom missing from the L-valine, apart from the absence of the hydroxyl group of the carboxyl group, Tyr stands for a residue of L-tyrosine with 1 hydrogen atom on the nitrogen atom missing from the L-tyrosine, apart from the absence of the hydroxyl group of the carboxyl group, ll denotes a residue of L-isoleucine with 1 hydrogen atom on the nitrogen atom which is absent from the L-isoleucine, apart from the absence of the hydroxyl group of the carboxyl group, His represents a residue of L-histidine with 1 hydrogen atom missing from the L-histidine on an amino nitrogen atom, apart from the absence of the hydroxyl group of the carboxyl group, Pro stands for a residue of L-proline with 1 hydrogen atom on the nitrogen atom missing from the L-proline except for the absence of the hydroxyl group of the carboxyl group. Y is a residue of an aliphatic amino acid with 1 hydrogen atom missing from this acid on the nitrogen atom or on an amino nitrogen atom, apart from the absence of the hydroxyl group of the carboxyl group, in each case in the L configuration in the case of an asymmetric carbon atom, and A represents an alkyl radical with 1 to 5 carbon atoms, their acid addition salts and pharmaceutically acceptable complexes, and a process for their preparation. These compounds can be used in medicines in the field of therapy and diagnosis, in particular for antagonizing angiotensin and for example in relation to high blood pressure.
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