http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1291477-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_4acae202b6a15394281949545e70d2f6 |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K14-62 |
classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-00 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-575 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K14-62 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K1-113 |
filingDate | 1969-12-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1972-10-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-1291477-A |
titleOfInvention | Insulin derivatives |
abstract | 1291477 Insulin derivatives ROUSSEL UCLAF 9 Dec 1969 [9 Dec 1968 7 March 1969] 60113/69 Heading C2C Tris - N<SP>A1</SP>,N<SP>B1</SP>,N<SP>#29</SP> - (3 - X - 3 - oxo - 1 - Y- prop - 1 - ene - 1 - yl) [N8 - (4 - Z - 6 - R pyrimidin-2-yl) ornithine B22]-insulins having the basic molecular pattern (in which X and Y are alkyl, aralkyl, or aryl optionally substituted or X+Y is polymethylene optionally substituted; Z and R are alkyl, aralkyl or aryl, optionally substituted) in a dissociated or slightly associated form and their water-soluble salts with bases; and alkali metal salts of highly associated molecular aggregates of tris - N<SP>A1</SP>,N<SP>B1</SP>,N<SP>#29</SP> - (3 - Z - 3 - oxo - 1 - R- prop - 1 - ene - 1 - yl) [N# - (4 - Z - 6 - R - pyrimidin - 2 - yl) ornithine B22] - insulin (III); alkali metal salts of highly associated molecular aggregates of tris-N<SP>A1</SP>,N<SP>B1</SP>,N<SP>#29</SP> - (3 - X - 3 - oxo- 1 - Y - prop - 1 - ene - 1 - yl) [N# - (4 - Z - R - pyrimidin - 2yl) ornithine B22] - insulin (V); [N# - (4 - Z - 6 - R - pyrimidin - 2 - yl) ornithine B22)-insulins in the dissociated or slightly associated state (IV) and their salts with acids and bases; mixtures of tris-N<SP>A1</SP>,N<SP>B1</SP>,N<SP>#B29</SP> - (3-Z-3- oxo - 1 - R - prop - 1 - en - 1 - yl) insulin (VI) and (III) in strongly associated molecular aggregates; and mixtures of (VI) in a dissociated form (VII) with alkali metal salts of tris-N<SP>A1</SP>, N<SP>B1</SP>,N<SP>#29</SP> - (3 - Z - 3 - oxo - 1 - R - prop - 1 - en- 1 - yl) [N# - (4 - Z - 6- R - pyrimidin - 2 - yl) ornithine B22]-insulin (IA) in a dissociated or slightly associated form soluble in water are prepared by reacting insulin (II) with Z-COCH 2 CO-R in an alkaline medium to give (III) treating this with phenol or a substituted phenol at pH 8 in the presence of an alkali metal hydroxide to give (IA) hydrolysing this under controlled conditions optionally with phenol to give (IV), treating this with XCOCH 2 COY to give (V), treating (V) with phenol as before to give (IB) and optionally forming other salts or free proteins; or (III) is hydrolysed with phenol to give an acid addition salt of (IV). The foregoing reactions are effected in a homogeneous phase. The reactors may be effected in a heterogeneous phase when (II) and ZCOCH 2 COR gives a mixture of (III) and (VI)which is dissociated by phenol to give (VII) and (IA) in turn treated with ZCOCH 2 COR and a phenol to give (III) which is finally dissociated to give (IA). Pharmaceutical compositions comprise compounds (IB) together with a carrier in forms suitable for parenteral and topical administration. (IB) are useful as antidiabetic agents, in psychiatric shock treatment and in the treatment of varicose ulcers, and atonic sores. |
priorityDate | 1968-12-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 105.