http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CZ-20031930-A3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_bb66d9373d09efad73c142762f6dfb00 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P17-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P27-16 |
| filingDate | 2001-12-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6d607b8cfa82e79000193712e741b9e4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_250c94ae88399a51a492719d3130db6c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ee05ad94aa3ce747c6a2e911c045f570 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_994087fbb6b982973bc2988f93510c3f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cd0aed395d27fb818f9734bfb4ec9d89 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_14938dd519b9a442c5ee65921f0bf3a1 |
| publicationDate | 2003-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CZ-20031930-A3 |
| titleOfInvention | Quinazoline derivatives |
| abstract | 4-Amino-6-(4-amino-1-oxo-but-2-enylamino)-quinazoline derivatives (I) are new. 4-Amino-6-(4-amino-1-oxo-but-2-enylamino)-quinazoline derivatives of formula (I) and their tautomers, stereoisomers and salts are new. [Image] R abenzyl, 1-phenylethyl or 3-chloro-4-fluorophenyl; R bdimethylamino, N-methyl-N-ethylamino, Diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)-amino, N-ethyl-N-(2-methoxyethyl)-amino, bis-(2-methoxyethyl)-amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)-amino, N-methyl-N-(tetrahydrofuran-2-yl-methyl)-amino, N-methyl-N-(tetrahydrofuran-3-yl-methyl)-amino, N-methyl-N-(tetrahydropyran-4-yl)-amino or N-methyl-N-(tetrahydropyran-4-ylmethyl)-amino; R ccyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-yl-methoxy, tetrahydrofuran-3-yl-methoxy, tetrahydropyran-4-yloxy or tetrahydropyran-4-ylmethoxy; and provided the following compounds are excluded: (1) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N,N-diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (2) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (3) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(dimethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (4) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclobutyloxy-quinazoline; (5) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclopentyloxy-quinazoline; (6) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclobutyloxy-quinazoline; (7) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopentyloxy-quinazoline; (8) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclobutyloxy-quinazoline; (9) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (10) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(morpholin-4-yl)-1-oxo-2-buten-1-yl)-amino)-7-cyclopentyloxy-quinazoline; (11) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclobutyloxy-quinazoline; (12) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopentyloxy-quinazoline; (13) 4-((R)-(1-phenyl-ethyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (14) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(bis-(2-methoxyethyl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (15) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N-ethyl-N-(2-methoxyethyl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (16) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N-methyl-N-(tetrahydropyran-4-yl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; (17) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-(tetrahydrofuran-2-yl)-methoxy)-quinazoline; (18) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-(tetrahydrofuran-3-yl)-oxy)-quinazoline; (19) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(diethylamino)-1-oxo-2-buten-1-yl)-amino)-7-(tetrahydropyran-4-yl)-oxy)-quinazoline; (20) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N-methyl-N-(tetrahydrofuran-2-yl-methyl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline; and (21) 4-((3-chloro-4-fluorophenyl)-amino)-6-((4-(N-methyl-N-(tetrahydrofuran-3-yl)-amino)-1-oxo-2-buten-1-yl)-amino)-7-cyclopropylmethoxy-quinazoline. An independent claim is included for the preparation of (I). ACTIVITY : Cytostatic; Respiratory; Gastrointestinal; Antiinflammatory; Antiasthmatic; Antiallergic; Antitussive; Antiulcer; Immunosuppressive; Antipsoriatic. MECHANISM OF ACTION : Tyrosine kinase-mediated signal transduction inhibitor. In a test, 4-((3-Chloro-4-fluorophenyl)-amino)-6-((4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl)-amino)-7-((S)-(tetrahydrofuran-2-yl)-methoxy)-quinazoline (Ia) had IC 5 0 value 0.3 MicroM for inhibition of human EGF-receptor kinase. |
| priorityDate | 2000-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 318.