http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CA-2182530-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_94ff2d78578d95d1e8d3a2233c76188d |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J41-0038 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J17-005 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J3-005 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J41-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J41-0011 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07J19-005 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-565 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-704 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-7036 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J19-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07J41-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 |
| filingDate | 1994-09-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_09cfdcfe68a289e6143c46c8551c57a4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4c47e26ef66e4dc25b76c1f5ac9f1ad3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6a2559894c01115863e408e79fda3643 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7fcc1c2737310e25b0b4d629b1538782 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb40b469dbcbdf0d334672f29a5b73ab |
| publicationDate | 1995-03-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CA-2182530-A1 |
| titleOfInvention | Novel oligosaccharide-containing 14-aminosteroid compounds and novel diastereoselective aminosteroid process chemistry |
| abstract | The present invention relates to oligosaccharide-containing 14-aminosteroid compounds and the pharmaceutically-acceptable acid salts or esters thereof of general formula (I), wherein: a) R1 is (i) COOR5, where R5 is hydrogen, a 1-6 carbon lower alkyl; a 1-6 carbon lower alkyl substituted by an amino group; an arylalkyl or heteroarylalkyl or a carbocyclic ring, or (ii) CHR6OH, where R6 is a hydrogen atom or 1-6 carbon lower alkyl group, or (iii) COR''', where R''' is hydrogen; 1-6 carbon lower alkyl; 1-6 carbon lower alkyl substituted amino; amino or dialkylamino; and b) R2 is -NR7R8, where R7 and R8, which may be the same or different, are hydrogen atoms or a 1-6 carbon lower alkyl; and e) R3 is (i) an oligosaccharide sugar residue having structure (II), where R9 is hydrogen; methyl; hydroxy, carboxy, acetoxy, arylalkyloxy; heteroarylalkyloxy or benzoxy; R10 is hydrogen; methyl; carboxy; acetoxy; arylalkyloxy; heteroarylalkyloxy; benzoxy or hydroxy; R11 is oxygen; wherein further when R11 is a substituent on the terminal monosaccharide sugar residue; R11 is OH; methyl; acetoxy; arylalkyloxy; heteroarylalkyloxy; and R12 is a hydrogen; methyl; methylhydroxymethyl; or acetoxymethyl; or (ii) an oligosaccharide sugar residue having structure (III), where R14 and R15, which may be the same or different, are hydrogen; 1-6 carbon lower alkyl; heteroarylalkyl; arylalkyl; heteroaryl or aryl; R17 can be hydrogen; hydroxy; acetoxy or benzoxy; R18 and R19 are hydroxy; acetoxy and benzoxy; or (iii) an oligosaccharide residue having structure (IV), where R14 and R15, which may be the same or different, are hydrogen; 1-6 carbon lower alkyl; heteroarylalkyl; arylalkyl; heteroaryl or aryl; R14a is oxygen; wherein further when R14a is a substituent on the terminal monosaccharide sugar residue; R14a must be hydroxy; methyl; acetoxy; arylalkyloxy or heteroarylalkyloxy; and d) R4 is (i) OH, or (ii) H, or (iii) OR13, where R13 is a monosaccharide sugar residue; acetoxy; benzoxy; arylalkyl or heteroarylalkyl; and e) Z is (i) -CH-, where a and b are single bonds, or (ii) =C, where either a or b is a double bond. The present invention also relates to a process for introducing an amino group at the 14-position on a steroid nucleus wherein said amino group is diasteroselectively introduced onto the 14-position of the steroid nucleus via an iodoisocyanate addition comprising the steps of: a) adding the iodoisocyanate to the 14-15 position double bond on the steroid nucleus; and b) dehalogenation; and c) isocyanate conversion to the amine moiety on the 14-position of the steroid nucleus. |
| priorityDate | 1993-09-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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