http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1377650-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3e9445e5e3626f36e932c6451a928250 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D309-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D243-16 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D243-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4985 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D309-12 |
| filingDate | 1971-11-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1974-12-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1377650-A |
| titleOfInvention | Diazepine derivatives and a process for their manufacture |
| abstract | 1377650 5 - Triazolo - benzodiazepine derivatives CIBA-GEIGY AG 22 Nov 1971 [23 Nov 1970] 54047/71 Heading C2C Novel compounds of the general Formula I wherein R 1 is hydrogen or C 1-3 alkyl; R 2 is hydroxy, C 1-6 alkoxy or alkanoyloxy, a mono- or di-aryl methoxy, a 2-oxacycloalkoxy having 5 to 7 ring members or fluorine; and A is a C 1-3 alkylene group and wherein each of the rings B and C may be substituted by one or more fluorine, chlorine bromine, trifluoromethyl or C 1-6 alkyl or alkoxy, and 5-N-oxides and their salts may be prepared by (a) where R 2 is other than C 1-6 alkanoyloxy condensing a compound II wherein X is mercapto, C 1-2 alkoxy or alkylthio optionally activated by a substituent, or an unsubstituted or mono- or di-substituted amino, with a compound R 2 -A-CONHNH 2 where R 2 is other than alkanoyloxy; (b) where R 2 is hydroxy and A is methylene, ethylene, trimethylene or propylene, reduction of a compound IV wherein A<SP>1</SP> has one less methylene group than the required A group and Y is a hydrocarbon radical having up to 8 carbon atoms; (c) cleaving of a compound I in which R 2 is mono- or diarylmethoxy or 2-oxacycloalkoxy to yield a compound I in which R 2 is hydroxy (d) esterification of the R 2 hydroxy group to give a C 1-6 alkanoyloxy group at R 2 ; (e) forming a 5-N-oxide of the compound I and/or (f) salt formation. The intermediate compound 6-phenyl-8-chloro- 4H - s - triazolo[4,3-a][1,4]benzodiazepine - 1- carboxylic acid ethyl ester may be prepared by a similar method to (a) using a corresponding compound II wherein X is methylthio and oxalic acid mono ethyl ester hydrazide in place of R 2 -A-CONHNH 2 . The intermediate hydrazides may be prepared by reaction of an alkyl ester of R 2 -A-COOH with hydrazine hydrate optionally followed where R 2 is hydroxy by debenzylation of the appropriate compound in which R 2 is benzyloxy. 2 - (Tetrahydropyran - 2 - yloxy) - acetic acid n-butyl ester may be prepared by reacting 3,4- dihydro-2H-pyran with glycollic acid n-butyl ester in acid conditions. Pharmaceutical compositions of the compounds I show anticonvulsant and tranquilizing activity and may be used to treat epilepsy by administering orally or rectally with the usual excipients. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0104053-A1 |
| priorityDate | 1970-11-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 53.