http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1277870-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_56ee5285e8e8edccb061046ff20da7a6 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-08 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-08 |
| filingDate | 1970-12-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5d02ec230f4110ae5c81a9df8e938507 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cc156690f3c1786d17ab02bde7b28231 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c4263504355ac1638e5282ae19157979 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f5151a890d2efeeed6b388b52fba6c29 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f67d927d30bb6880e6f47faa6c349388 |
| publicationDate | 1972-06-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1277870-A |
| titleOfInvention | 5,10-METHANO-5H-DIBENZO[a,d]CYCLOHEPTENE DERIVATIVES |
| abstract | 1277870 5,10-Methano-5H-dibenzo[a,d]cycloheptene derivatives BOEHRINGER MANNHEIM GmbH 29 Dec 1970 61576/70 Heading C2C Novel compounds of the Formula (I) wherein R 1 is H or OH, R 2 is H or alkyl, X is and R 3 and R 4 , which may be the same or different, are H, alkyl, hydroxyalkyl, amidine or imidazolyl radicals or R 3 and R 4 can together form a saturated or unsaturated aliphatic hydrocarbon radical containing 3-7 carbon atoms, which may be interrupted by O, S or N atoms, or when X is X, N together with R 3 or R 4 can represent a saturated or unsaturated heterocyclic ring containing 3 or 4 carbons; and the pharmacologically compatible acid-addition salts thereof, may be obtained by (a) hydrogenation of a nitrile of Formula (II) and if desired, subsequent reaction with one equivalent of a compound YR 3 and/or one equivalent of a compound YR 4 , where Y is a reactive ester group; or (b) reaction of a compound of Formula (IV) wherein Z is a halogen atom or an alkoxy group, with an amine HNR 3 R 4 , and, if desired, reduction of the acid amide to the corresponding aminomethyl compound; or (c) reaction of nitrile (II) in an anhydrous medium with an excess of an alkali metal amide and, if desired, alkylation or saponification of the amidine formed; or (d) reaction of nitrile with a diamine H 2 N-W-NH 2 , where W is a C 2-3 saturated or unsaturated aliphatic hydrocarbon radical, to form compounds wherein XNR 3 (or R 4 ) denotes a heterocyclic ring; or (e) alkylation of an amidine of Formula (VII) The preparation of intermediates is described as follows: Nitriles (II) in which R 1 is OH are obtained by reaction of 5H-dibenzo[a,d]cyclohepten-5-one with nitriles R 2 CH 2 CN in liquid NH 3 in the presence of NaNH 2 ; the nitriles can be saponified with NaOH to yield on acidification the 12-carboxylic acid which can be reacted with SOCl 2 to form the acid chloride. Nitriles (II) in which R 1 is H are obtained by cyclization of a 5-CN-CH(R 2 )- substituted 5-H-dibenzo[a,d]- cycloheptene with NaNH 2 in liquid NH 3 . Pharmaceutical compositions having diuretic and saluretic properties comprise compounds of Formula (I) and salts thereof in admixture with a solid or liquid pharmaceutical diluent or carrier in forms suitable for enteral or parenteral administration. |
| priorityDate | 1970-12-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 28.