http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1239380-A
Outgoing Links
Predicate | Object |
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classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/D06P3-80 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/D06P1-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5513 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/D06P3-854 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-30 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D- |
filingDate | 1969-06-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1971-07-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-1239380-A |
abstract | 1,239,380. Benzodiazepine derivatives. F. HOFFMANN-LA ROCHE & CO. A.G. 10 June, 1969 [12 June, 1968; 28 Feb., 1969], No. 29347/69. Heading C2C. Compounds of the general Formula I: (B=CO, CH 2 , CS; R a,b =H, halogen, NO 2 , NH 2 , C 1-7 alkylamino, di(C 1-7 alkyl) amino, CF 3 , C 1-7 alkylmercapto, C 1-7 alkoxy; R c =H, C 1-7 alkyl, C 1-7 alkanoyl, C 3-6 cycloalkyl, (C 3-6 cycloalkyl)-(C 1-7 alkyl), C 1-7 haloalkyl, C 1-7 aminoalkyl, alkylamino-(C 1-7 alkyl), dialkylamino- (C 1-7 alkyl), C 1-7 hydroxyalkyl, (CH 2 ) n COR 1 ; n=0-5; R 1 = OH, C 1-7 alkoxy, NR 2 R 3 ; R 2 , 3 = H, C 1-7 alkyl or -NR 2 R 3 =5-6-membered saturated ring; R d =H, C 1-7 alkyl, C 2-7 acyloxy, C 2-7 alkoxycarbonyl, OH, C 1-7 alkoxy, (C 1-7 alkoxy)-(C 1-7 alkyl)) and their acid addition salts are prepared by (a)-B=CO-cyclizing a compound of the Formula IV (X=leaving atom or group) in the presence of ammonia, (b)-B=CH 2 , R c,d =H-reacting a compound of the Formula V: with ethylene diamine, (c)-B=CO, R c , d = alkyl, substituted alkyl-1,3-dialkylating or di- (substituted alkylating) a corresponding compound in which R c,d =H, (d)-R c not H- 1-substituting a compound of Formula I in which R c =H, (e)-B=CS-treating a compound of Formula I in which B = CO with a thiating agent, (f)-amino-substituted compounds-reducing a corresponding nitro-substituted compound, (g)-R a and/or R b =halogensubjecting a corresponding compound in which R a and/or R b =NH 2 to a Sandmeyer reaction, (h)-alkylamino- or dialkylamino-substituted compounds-alkylating a corresponding aminosubstituted compound, (i)-B=CO, R a,b not NH 2 or alkylmercapto, R c not hydroxyalkyl, Rd not OH-oxidizing a compound of the formula (B = CO, CH 2 ; A represents provided that when B=CO the 4,5-bond is single; R a-d as defined under (i)) or (j) introducing an H 2 N#C=NH group in the 5-position of a suitably substituted 1,4-benzodiazepine and building up a pyrimidyl ring thereon, optionally followed in each case by salt formation. The above compounds are anticonvulsants, sedatives and muscle relaxants, and may be administered in the form of pharmaceutical preparations containing them, with or without other (unspecified) active ingredients, in association with a carrier. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/DE-3621551-C1 |
priorityDate | 1968-06-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 24.