http://rdf.ncbi.nlm.nih.gov/pubchem/patent/SU-731900-A3
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2ca2e4410855da087e11bf3eea8933fa |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D519-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A23K1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D519-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-475 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-02 |
filingDate | 1974-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 1980-04-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4f8756c7ed674c9580f547ecc7c16b99 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_19a48e0e9916c95d200be60550a7a0c0 |
publicationDate | 1980-04-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | SU-731900-A3 |
titleOfInvention | Method of prepaping vinblastin derivatives |
abstract | 1463575 Novel amides, azides and hydrazides of vinca alkaloids ELI LILLY & CO 25 March 1974 [2 April 1973] 13101/74 Heading C2C Novel compounds of the Formula I wherein R is NH 2 , NH.NH 2 , N(CH 3 ) 3 , NHalk-X, NH(C 3-8 )cycloalkyl, NHalkAm, NHalk(OH) 1-3 or N 3 ; wherein alk is C 1-6 alkylene, Am is NH 2 , NHCH 3 or N(CH 3 ) 2 , X is hydrogen, CN, optionally substituted phenyl, carboxy, carbo- (C 1-3 )-alkoxy, or carboxamido; R<SP>1</SP> is H, alkanoyl or chloroalkanoyl; R<SP>11</SP> is hydrogen, C 1-3 alkyl, formyl or alkanoyl; and one of R<SP>111</SP> and R<SP>1111</SP> is hydroxy and the other is ethyl, in which alkanoyl groups have 1-3 carbon atoms in the alkane moiety, and salts thereof, may be prepared by reacting a compound of the Formula I wherein R is OCH 3 , R<SP>1</SP> is hydrogen or acetyl and R<SP>11</SP>, R<SP>111</SP> and R<SP>1111</SP> are as defined above with ammonia, methylamine or hydrazine to obtain a compound of Formula I wherein R is NH 2 , NHCH 3 or NH.NH 2 , and R<SP>1</SP> is hydrogen and, if desired, when R is NHNH 2 (a) reacting said compound with a nitrosating agent to form an azide in where R 3 N 3 and then reacting said azide with ammonia, an amine of the formula HN(CH 3 ) 2 , NH 2 alk-X, NH 2 -(C 3-8 )cycloalkyl, NH 2 alkAm or NH 2 alk(OH) 1-3 to obtain the corresponding compound of Formula I or (b) hydrogenolysing said compound with Raney nickel in an inert solvent to yield a compound of the Formula I wherein R is NH 2 , and/or, if desired, acylating a product in which R<SP>1</SP> is hydrogen to introduce an alkanoyl or chloroalkanoyl group at R<SP>1</SP>, and, if in the starting material R<SP>11</SP> is hydrogen, to introduce an alkanoyl or chloroalkanoyl at R<SP>11</SP>. Various by-products having the same ring systems as I are formed during some of the above reactions. Pharmaceutical compositions of the compounds I or salts thereof with the usual excipients may be administered orally or parenterally for treating neoplastic disease. The compounds also show antivral activity in vitro against herpes virus. |
priorityDate | 1973-04-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 59.