http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-416516-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-1005 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K7-16 |
classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K7-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-103 |
filingDate | 1973-07-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1976-03-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | ES-416516-A1 |
titleOfInvention | A PROCEDURE FOR THE PREPARATION OF NONAPEPTIDES. |
abstract | A procedure for the preparation of nonapeptides that constitute active ingredients in pharmaceutical compositions with natriuretic properties, of the general formula **(See formula)** in which Q means the radical of arginine or lysine, Mpr means the beta-mercaptopropionyl group and all amino acids with an asymmetric carbon atom have the L configuration, and their non-toxic and pharmaceutically usable acid addition salts, the process of which comprises a) dissociate the protecting groups of a peptide of the general formula **(See formula)** in which R1 means a hydrogen atom or an amide protecting group and Q'means a grouping of the formula -NH-CH [- (CH2) 3-NH-C (= NH) -NHR2] -CO- or -NH-CH [- (CH2) 4-NH-R3] -CO, where R2 means a hydrogen atom or a guanidine radical protecting group and R3 means a hydrogen atom or a protecting group from the lysine epsilon-amine group, provided that at least one of the radicals R1 and R2 or R3 signifies a protecting group and where all amino acids with an asymmetric carbon atom have L-configuration, and convert, if desired, the obtained free peptide, by reaction with an organic or inorganic acid, into a pharmaceutically usable non-toxic acid addition salt, or b) oxidizing a peptide of the general formula **(See formula)** in which Q has the meaning attributed to it in claim 1 and, R4 and R5 each represent a hydrogen atom or a sulfhydryl protecting group, and where all amino acids with an asymmetric carbon atom have an L configuration, with simultaneous or preliminary dissociation of any protecting group that may be present and convert the product obtained, if desired, by reaction with an organic or inorganic acid, in a pharmaceutically usable non-toxic acid addition salt, O well c) oxidizing a peptide of the general formula **(See formula)** in which R1 means a hydrogen atom or an amide protecting group, Q'means a grouping of the formula -NH-CH [- (CH2) 3-NH- C (= NH) -NHR2] -CO- or -NH-CH [- (CH2) 4-NH-R3] -C0- where R2 means a hydrogen atom or a guanidine radical protecting group and R3 means a hydrogen atom or a protecting group from the lysine epsilon-amine group, provided that at least one of the radicals R1 and R2 or R3 represents a protecting group and R4 and R5 each represent a hydrogen atom or a protecting group and where all amino acids with an asymmetric carbon atom have an L configuration, with simultaneous dissociation of the protecting group or groups, and convert the product obtained, if desired, by reaction with an organic or inorganic acid, in a pharmaceutically usable non-toxic acid addition salt, or d) amidating a peptide of the general formula **(See formula)** in which means the radical of lysine or arginine, Mpr means the beta-mercaptopropionyl group and R6 means a hydroxy group or a carboxylic group activating radical, O well e) reacting a hexapeptide of the general formula **(See formula)** with a tripeptide of the general formula H-Pro-Q-Gly-NH2 0 react a heptapeptide of the general formula **(See formula)** with a dipeptide of the general formula H-Q-Gly-NH2 or react an octapeptide of the general formula **(See formula)** with glycine amide and convert, if desired, the resulting nonapeptide into a pharmaceutically usable non-toxic acid addition salt. In formulas VII to XI, R6 represents a hydroxylic group or an activator group of the boxyl group, q means the arginine or lysine radical and all amino acids with an asymmetric carbon atom have an L configuration. (Machine-translation by Google Translate, not legally binding) |
priorityDate | 1972-07-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 21.