http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CA-2035385-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a09fa84c54c24536575f7f12c1f1db43 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-6899 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/B82Y5-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07H15-252 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07H15-244 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K47-67 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07H15-252 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K47-48 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-704 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7034 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7028 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-70 |
| filingDate | 1991-01-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_666d64e4078d0303203f0f39fce26152 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_198c60aec6c44da4b56bd14b2f43cc68 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3089c6a80cc5a1b57379d89a8e60153e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b9d6b06c2984bc30b16621fc7dac3015 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2caaad40a522bbdf515728dd25f66750 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_22ebe8b6541bde02a880afd119034a0d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c12c912b0f7616f11a6cb3399172638c |
| publicationDate | 1991-08-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CA-2035385-A1 |
| titleOfInvention | Glycosyl prodrugs of anthracyclines, a process for the preparation thereof and the use thereof in combination with unctionalized tumor -specific enzyme conjugates |
| abstract | Abstract of the disclosure: Glycosyl prodrugs of anthracyclines, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugates The invention relates to glycosyl prodrugs of anthra-cyclines, a process for the preparation thereof and the use thereof in combination with functionalized tumor-specific enzyme conjugtes for treating cancers, and it specifically relates to 14-O-glycosylanthracyclines as prodrugs which can be cleaved by the action of tumor-specific enzyme conjugates to cytotoxic active substan-ces, where the liberated active substance is suitable because of its cytotoxic activity for the treatment of cancers. The invention relates to 14-O-glycosylanthracyclines of the formula I and the salts thereof with an inorganic or organic acid I in which R1, R2 and R3 are, independently of one another, hydrogen, hydroxyl, methoxy, R4, R5 and R6 are, independently of one another, hydrogen, hydroxyl, halogen, aliphatic acyloxy (C1-C8), benzoyloxy or substituted benzoyloxy such as para-nitrobenzoyloxy, alkyloxy (C1-C8), allyloxy, benzyloxy or substituted benzyloxy, tetrahydro-pyranyloxy, amino, NH-acyl (C1-C8), NH-(9-fluorenyl-methoxycarbonyl), morpholino or substituted morpholino, preferably 3-O-methylmorpholino or 2-cyanomorpholino, R7 is a carbohydrate of the formula II II with R8 being methyl, hydroxymethyl, acyloxymethyl (C1-C8), alkyloxymethyl (C1-C8), benzyloxymethyl, allyloxy-methyl, carboxyl, carboxymethyl or carboxyallyl, R9, R10 and R11 are, independently of one another, hydro-gen, hydroxyl, acyloxy (C1-C8), benzoyloxy or substi-tuted benzoyloxy such as para-nitrobenzoyloxy, alkyloxy (C1-C8), allyloxy, benzyloxy or substituted benzyloxy, amino, NH-acyl (C1-C8) or NH-(9-fluorenylmethoxycarbonyl). Compounds in which R4=R5=R9=R10=O-acetyl and R5-R11=H in the alpha-L-deoxyfucose conformation are excepted. A functionalized tumor-specific enzyme is intended to mean within the scope of the invention an enzyme of the formula III A-Sp-E III in which A is an antibody or one of its fragments which have specificity for a tumor-associatad antigen, or a biomolecule which accumulates in a tumor, such as EGF (epidermal growth factor), TGF-.alpha. (transforming growth factor .alpha.), PDGF (platelet-derived growth factor), IGF I+II (insulin-like growth factor I+II) or a+b FGF (acidic + basic fibroblast growth factor) E is a glycosidase of little or no immunogenicity, preferably a mammalian glycosidase such as .alpha.- or .beta.-glucosidase, .alpha.-galactosidase, .alpha.- or .beta.-mannosidase, .alpha.-fucosidase, N-acetyl-.alpha.-galactosaminidase, .beta.-acetyl-.beta.-/N-acetyl-.alpha.-glucosaminidase or .beta.-glucuroni-dase, and Sp (spacer) is a bifunctional sulfide or disulfide-containing group of the formula IV X(S)nY IV or (S)n in which X or Y is -CO-R12(N-succinimido)- or -C(=R13)-CH2-CH2- with R12 being -CH2-CH2-, 1,4-cyclohexylidene, 1,3- or 1,4-phenylene or methoxycarbonyl- or chloro-1,4-phenyl-ene and R14 is O or NH, Y is -C(=R13)-CH2-CH2- where R13 has the stated meaning, and n is 1 or 2, or a polypeptide spacer. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6146658-A |
| priorityDate | 1990-02-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 173.