http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1839654-B9
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_44e0905262f429c7590b40df8448c0c5 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-341 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-365 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-635 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-135 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-137 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-415 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-135 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-415 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-341 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 |
| filingDate | 2003-11-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2012-01-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5895d405394f743791276dc5064c0622 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0ee14365128e7f21779025c1be07da21 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_255bb69cb2f54797aa36b75ea6421dd8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bb62fc80fe9079f000df8ce462f70450 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e0976b4af9961668f32006a0da677692 |
| publicationDate | 2012-01-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-1839654-B9 |
| titleOfInvention | Use of (1R, 2R)-3-(3-dimenthyl amino-1-ethyl-2-methyl-propyl) phenol for treating inflammatory pain |
| abstract | Mixture (X) of at least one analgesic (A) and an inhibitor (B) of cyclo-oxygenase II (COXII). Mixture (X) of at least one analgesic (A) and an inhibitor (B) of cyclo-oxygenase II (COXII), where (A) is a phenyl-substituted tertiary amine of formulae (I)-(III), as racemates, pure or mixed stereoisomers (particularly enantiomers or diastereoisomers), optionally in the form of acids, bases, salts or solvates, preferably hydrates. [Image] X : hydroxy, fluoro, chloro, hydrogen or OCOR 7>; R 1>1-4C linear, branched, saturated or unsaturated alkyl, optionally substituted one or more times, in (I), or 1-4C alkyl, benzyl, trifluoromethyl, hydroxy, benzyloxy. 1-3C alkoxy, chloro or fluoro in (II); R 2> and R 3>hydrogen or 1-4C alkyl (as for R 1>) or together form an optionally substituted 4-7C cycloalkyl; R 9>-R 1> 3>hydrogen, fluoro, chloro, bromo, iodo, (di)fluoromethyl, trifluoromethyl, hydroxy, thiol, OR 1> 4>, trifluoromethoxy, SR 1> 4>, NR 1> 7>R 1> 8>, (trifluoro)methyl- sulfinyl or -sulfonyl, cyano, COOR 1> 4>, nitro, CONR 1> 7>R 1> 8>, 1-6C alkyl (as above) or phenyl, optionally substituted one or more times; R 1> 4>1-6C alkyl, pyridyl, thienyl, thiazolyl, phenyl, benzyl, phenethyl (all optionally substituted one or more times), PO(O-1-4C alkyl)-2, COO1-5C alkyl, CONH(1-3C alkylphenyl), CO(1-5C)alkyl, COCHR 1> 7>-NHR 1> 8>, or CO-phenylene-R 1> 5>; R 1> 5>ortho-OCO(1-3C)alkyl, or meta- or para-CH 2N(R 1> 6>) 2; R 1> 6>1-4C alkyl or morpholino, and all alkyl in R 1> 4>-R 1> 6> are optionally substituted one or more times; R 1> 7> and R 1> 8>hydrogen, 1-6C alkyl (as above), phenyl, benzyl or phenethyl, all optionally substituted one or more times; R 1> 0> with either of R 9> or R 1> together : a OCH 2O, OCH 2CH 2O, OCH=CH, CH=CHO, CH=CMeO, OCMe=CH, (CH 2) 4 or OCH=CHO ring; proviso: in (III), when R 9>, R 1> 1> and R 1> 3> are all hydrogen, one of R 1> 0> and R 1> 2> is hydrogen and the other methoxy, then X is nor hydroxy. ACTIVITY : Analgesic. In the mouse writhing test ( J. Pharmacol. Exp. Ther., 228 (1984) 1) animals were treated with (a) (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol (X); (b) rofecoxib (Y) or (c) a mixture of both at ratio 1:2, then after 30 minutes injected with acetic acid. The ED50 for reduction of writhing was 33 mg/kg for (X) alone and 60.1 mg/kg for (Y) alone, but only 23.3 mg/kg (compare 47 mg/kg for an additive effect) for the mixture. MECHANISM OF ACTION : None given. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-3241550-B1 |
| priorityDate | 2002-11-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 188.