http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1462493-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_5c24684033fba97d1ad845ce453a57e3 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y10S930-29 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-0819 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-1021 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K1-1075 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K1-107 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K7-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-81 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-113 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-093 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-00 |
| filingDate | 1974-09-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1977-01-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1462493-A |
| titleOfInvention | Trypsin inhibitors and process for the production thereof |
| abstract | 1462493 Trypsin-callicrein inhibitor derivatives HOECHST AG 6 Sept 1974 [6 Sept 1973] 39110/74 Heading C3H A derivative of trypsin-callicrein inhibitor (TCI) in which each of the five free carboxyl groups in the inhibitor is bonded via a peptidic linkage to a residue of general formula wherein (i) x is zero; Y is a straight or branched chain alkyl radical having from 1 to 5 carbon atoms and which is substituted by a carboxyl group and W is hydroxyl or (ii) x is 1-10; Y is hydrogen or a straight or branched alkyl radical of 1-5 carbon atoms which may be substituted by carboxyl, hydroxyl or carbonamide groups and/or which together with the carbon atom to which it is bonded and together with the nitrogen atom adjacent to that carbon atom, may form a cycloaliphatic, nitrogen-containing ring, W is hydroxyl or, when two or more radicals Y contain a carboxyl group, W may represent NH 2 , NHCH 3 , NHC 2 H 5 , OCH 3 , OC 2 H 5 , may be prepared by (i) protection of the five primary amino groups of the trypsin-callicrein inhibitor easily removable by an acid, (ii) reaction with an amino acid or peptide of formula wherein Y is present as the t-butyl ester of any carboxyl group, W<SP>1</SP> is a tertiary butoxy group and, when 2 or more radical Y contain tertiary butyl groups, W<SP>1</SP> may be NH 2 , NHCH 3 , NHC 2 H 5 , OCH 3 , OC 2 H 5 , in the presence of 1- hydroxybenzotriazole and dicyclohexylcarbodiimide; (iii) deprotection of all protective groups with at least one acid. In the examples, the following peptides are prepared: penta(Glu-Glu-Glu-Glu-OH) -TCI, penta(Glu-Asp-Glu-Asp-OH)TCI, penta(Glu-Glu-Glu-OH)-TCI, penta(Glu-Glu-Asp-OH)-TCI, penta(Asp-Glu-Asp-OH)-TCI, penta(Asp-Ser-Asp-OH)-TCI, penta(Glu-Glu-D-Glu-OH)-TCI, penta(D-Glu-D-Glu-D-Glu-OH) -TCI, penta(Glu-Glu-OH)-TCI, penta(Glu-Asp-OH)-TCI, penta(Glu-D-Glu-OCH 3 )-TCI, penta(Asp-Glu-NH 2 )-TCI, penta(h-glutamic acid)-TCI, penta(h-aspartic acid)-TCI. The following intermediates are prepared: penta-BOC-TCI. TETRAPEPTIDES: Z and HCl.H - Glu- (Obu<SP>t</SP>) - Gtu(OBu<SP>t</SP>) - Glu(OBut) - Glu(OBu<SP>t</SP>)- OBu<SP>t</SP>; Z and HCl.H - Glu(OBu<SP>t</SP>) - Asp(OBu<SP>t</SP>)- Glu(OBu<SP>t</SP>)-Asp(OBu<SP>t</SP>)-OBu<SP>t</SP>. TRIPEPTIDES: Z and HCl.H-Glu(OBu<SP>t</SP>)- Glu(OBu<SP>t</SP>) - Glu(OBu<SP>t</SP>) - OBu<SP>t</SP>; Z and HCl.HGlu(OBu<SP>t</SP>) - Glu(OBu<SP>t</SP>) - Asp(OBu<SP>t</SP>) - OBu<SP>t</SP>; Z and HCl.HAsp(OBu<SP>t</SP>) -Glu(OBu<SP>t</SP>) -Asp(OBu<SP>t</SP>)- OBu<SP>t</SP>; HCl.H - D - Glu(OBut) - D - Glu(OBu<SP>t</SP>)- D - Glu(OBu<SP>t</SP>) - OBu<SP>t</SP>; Z and HCl.H - Glu- (OBu<SP>t</SP>) - Glu(OBu<SP>t</SP>) - D - Glu(OBu<SP>t</SP>)-OBu<SP>t</SP>. The dipeptide intermediates prepared are Z and HCl.H - Glu(OBu<SP>t</SP>) - Glu(OBu<SP>t</SP>) - OBu<SP>t</SP>; Z and HCl.H - Glu(OBut) - Asp(OBu<SP>t</SP>) - OBu<SP>t</SP>; Z and HCl.H - Glu(OBut) - D - Glu(OBu<SP>t</SP>)- OBu'. Pharmaceutical compositions, suitable for parenthal administration (especially infusion or intravenous injection), comprise the derivatives of callicrein-trypsin inhibitor in admixture with a pharmaceutically acceptable carrier. |
| priorityDate | 1973-09-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 34.