http://rdf.ncbi.nlm.nih.gov/pubchem/patent/HU-E034919-T2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_5df91b83742bcb8697bc96f405f4b8e8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5375 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-505 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-506 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K45-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-20 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-12 |
| filingDate | 2013-08-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3b0bf13a045c69a3e9c7faa39478ca15 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8d0122060d119d5049e5a3951b0c0254 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4fe9358aeb6f828e3958ed66d665cda9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_252eb98d7ac07a90b7eeb13edffe914a |
| publicationDate | 2018-03-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | HU-E034919-T2 |
| titleOfInvention | 2,4,5,6-substituted 3,6-dihydropyrimidine derivatives such as hepatitis B virus (HBV) polymerase inhibitors, for example, for the treatment of chronic hepatitis |
| abstract | FIELD: chemistry. n SUBSTANCE: invention relates to new isomeric forms of the dihydropyrimidin derivative represented by formula (I) or (Ia), or a pharmaceutically acceptable salt thereof. In the formula (I) or (Ia) n n each A is -O-; each R is -X-Z; X is - (CR 7 R 7a ) m -; Z has the formula (II) or (IIa) n n where each B is - (CR 7 R 7a ) m -; each W is N; each Y is - (CR 7 R 7a ) m - or -O-, where m has the value 0 or 1; each R 1 is phenyl or phenyl substituted with one or more substituents, which are the same or different, representing H, F, Cl, Br, nitro or trifluoromethyl, for example 3,5-bis(trifluoromethyl)phenyl; each R 2 is H or C 1-4 alkyl; R 3 has one of the following formulas: n n n or n each R 10 is independently H, F, Cl, methyl, ethyl, cyano, hydroxy, nitro, amino, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy, -(CR 7 R 7a ) m -C(=O)O-R 8a , -(CR 7 R 7a ) m -C(=O)N(R 8a ) 2 or trifluoromethylsulfonyl; each R 11 is independently H, methyl, ethyl, propyl, isopropyl, butyl, trifluoromethyl or -(CR 7 R 7a ) m -C(=O)O-R 8a ; each p is independently 0, 1, 2 or 3; each R 4 is H; each R 7a and R 7 is independently H, methyl, ethyl, -(CH 2 ) m -OH -(CH 2 ) m -C(=O)O-R 8 or propyl; each R 8 and R 8a is independently H, methyl, ethyl, propyl, isopropyl, butyl, 2-methylpropyl, 1-methylpropyl, aminomethyl, 1-amino-2-methylpropyl, 1-aminoethyl, 2-aminoethyl, 1-aminobutyl, 1-aminopropyl, 2-aminopropyl, Boc-NH-methyl, 1-Boc-NH-2-methylpropyl, 1-Boc-NH-ethyl, 2-Boc-NH- ethyl, 1-Boc-NH-butyl, 1-Boc-NH-propyl, 2-Boc-NH-propyl, methoxy, ethoxy, -(CH 2 ) m -OH, -(CH 2 ) m -C(=O)O-(CH 2 ) m -H, -(CH 2 ) m -OC(=O)-(CH 2 ) m -H or tert-butyl; Boc is tert-butyloxycarbonyl; each R 9 is independently -(CR 7 R 7a ) t -OH, -(CR 7 R 7a ) m -C(=O)O-R 8 , -(CR 7 R 7a ) m -C(=O)O-(CR 7 R 7a ) m -OC(=O)O-R 8 , -(CR 7 R 7a ) m -C(=O)O-(CR 7 R 7a ) m -OC(=O)-R 8 , -(CR 7 R 7a ) m -C(=O)O-(CR 7 R 7a ) m -C(=O)O-R 8 , -(CR 7 R 7a ) t -OC(=O)-R 8 , triazolyl, tetrazolyl or -(CR 7 R 7a ) m -C(=O)N(R 8 ) 2 , provided that R 9 is -(CR 7 R 7a ) t -OH, R 3 is furyl, imidazolyl, isoxazolyl, oxazolyl, pyrrolyl, pyrimidinyl, pyridazinyl, thiazolyl, triazolyl, tetrazolyl, thienyl, pyrazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyranyl or triazinyl; each n is independently 1 or 2; each t is independently 1, 2, 3 or 4; each m is independently 0, 1, 2, 3 or 4; and arbitrarily each C 1-4 alkyl, C 1-4 haloalkyl, amino-C 1-4- alkyl, C 1-4 alkoxy, furanil, imidazolyl, isoxazolyl, oxazolyl, pyrrolyl, pyrimidinyl, pyridazinyl, thiazolyl, triazolyl, tetrazolyl, thienyl, pyrazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyranyl and triazinyl as described above, is independently substituted by one or more substituents that are the same or different, wherein the substituent is H, F, Cl, Br, I, C 1-4 alkyl, C 1-4 alkoxy, cyano, hydroxy, nitro, alkylamino, amino, trifluoromethyl, trifluoromethoxy, -(CR 7 R 7a ) m -C(=O)O-R 8a or -(CR 7 R 7a ) m -C(=O)N(R 8a ) 2 . n EFFECT: compounds possess the properties of an inhibitor of hepatitis B virus activity and can be used in the treatment of diseases caused by hepatitis B infection, which is cirrhosis or hepatocellular carcinoma. n 12 cl, 3 tbl, 159 ex |
| priorityDate | 2012-08-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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