http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1507103-A
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_69c91bbf0395db010b4806f50d808c4e |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J53-004 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J53-00 |
filingDate | 1976-02-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1978-04-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-1507103-A |
titleOfInvention | 6-amino-5beta,19-cycloandrostane derivatives and process for the preparation thereof |
abstract | 1507103 6-Amino-5,19-cyclosteroids RICHTER GEDEON VEGYESZETI GYAR RT 13 Feb 1976 05736/76 Heading C2W The invention comprises compounds of Formula I and their pharmaceutically acceptable acid-addition salts wherein X is >C = O, >CH(OR) or >C=N-OR 1 and Y is >C=O, >CH(OR 1 ), >C=N-OR 1 or ethylenedioxymethylene, R being H, C 1-4 alkyl or C 2-5 acyl, and R 1 being H or C 2-5 acyl; R 2 and R 3 are each H, a C 1-5 aliphatic hydrocarbon group (optionally substituted with OH, C 1-4 alkoxy, or with acyloxy), a C 3-8 alicyclic group, or a C 7-10 aralkyl group (optionally arsubstituted with C 1-4 alkoxy), with the provisos that (i) when R 2 is sec- or tert-alkyl or an alicyclic group, then R 3 is H, and (ii) when R 2 is aralkyl then R 3 is H or primary alkyl; alternatively NR 2 R 3 represents 1 - pyrrolidinyl, 1 - piperidinyl, 4 - morpholinyl, 1 - piperazinyl, 4- alkyl - 1 - piperazinyl, 4 - (hydroxyalkyl) - 1- piperazinyl, 4 - (alkoxyalkyl) - 1 - piperazinyl 4 - (acyloxyalkyl) - 1 - piperazinyl or 4- aralkyl-1-piperazinyl. Preparation of the above is from compounds of formula (where Y<SP>1</SP> is carbonyl or ethylene dioxymethylene; R 4 is C 1-4 alkyl or C 2-5 acyl; and R 5 is C 1-4 alkyl, phenyl or tolyl) by reaction with NHR 2 R 3 to yield I (X=>CH(OR 4 ); Y=Y<SP>1</SP>) followed when required by conversion to other compounds I by one or more of: hydrolysis hydrogenolysis, oxidation, oxime formation, ethynylation, acylation, reduction, salification desalification. Diuretic and aldosterone-antagonistic compositions for parenteral administration comprise a compound I or acceptable acid-addition salt thereof, and a carrier. |
priorityDate | 1976-02-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 17.