http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-039187-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_bb66d9373d09efad73c142762f6dfb00 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 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/A61P27-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 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/A61P11-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-5377 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P37-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-553 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P27-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-505 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/A61K31-517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-00 |
| filingDate | 2003-03-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a4692c7e45905609ef31c2fdc388fbe9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c77d6bb4c5634c4a27e1f1187c67c23a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_56a02bcf43919d8d5d23c381844bbe97 |
| publicationDate | 2005-02-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-039187-A1 |
| titleOfInvention | BICYCLE HETEROCICLES, MEDICATIONS CONTAINING THESE COMPOUNDS, ITS USE AND PROCEDURES FOR THEIR PREPARATION |
| abstract | Bicyclic heterocycles of general formula (1), in particular their physiologically safe salts with inorganic or organic acids, which possess valuable pharmacological properties, in particular an inhibitory effect on signal transduction provided by tyrosine kinases, their use for the treatment of diseases , in particular of tumor diseases, as well as benign prostatic hyperplasia (BPH), diseases of the lungs and respiratory tract and their preparation. Claim 1: Bicyclic heterocycles of general formula (1) in which Ra means an atom of H or a C1-4 alkyl group; Rb a phenyl or 1-phenylethyl group, in which the phenyl core is substituted in each case with residues R1 to R3, representing R1 and R2, which may be the same or different, in each case an atom of H, F, Cl , Br or Y, a C1-4 alkyl, hydroxy, C1-4 alkoxy, C2-3 alkenyl or C2-3 alkynyl group, an aryl, aryloxy, arylmethyl or arylmethoxy group, a heteroaryl, heteroaryloxy, heteroarylmethyl or heteroarylmethoxy group, a methyl or methoxy group substituted with 1 to 3 atoms of F or a cyano, nitro or amino group, and R3 an atom of H, F, Cl, or Br, a methyl or trifluoromethyl group, Rc a cyclobutyl, cyclopentyl or cyclohexyl group, which is substituted in each case with an R4-N-R5 group, R4 representing an H atom or a C1-3 alkyl group and R5 an H atom or a C1-3 alkyl group; a aminocarbonyl-C1-3 alkyl, C1-3 alkyl-aminocarbonyl-C1-3 alkyl, di- (C1-3 alkyl) aminocarbonyl-C1-3 alkyl, pyrrolidin-1-ylcarbonyl-C1-3 alkyl, piperidin-1 -ylcarbonyl-C1-3 alkyl, homopiperidin-1-ylcarbonyl-C1-3 alkyl, morpholin-4-ylcarbonyl-C1-3 alkyl, homomorpholin-4-ylcarbonyl-C1-3 alkyl, piperazin-1-ylcarbonyl-C1- alkyl 3, 4-C1-3 alkyl-piperazin-1-ylcarbonyl-C1-3 alkyl, homopiperazin-1-ylcarbonyl-C1-3 alkyl or 4-C1-3 alkyl-homopiperazin-1-ylcarbonyl-C1-3 alkyl, a hydroxy-C2-4 alkyl, C1-3 alkyloxy-C2-4 alkyl, C1-4 alkyloxy-C2-4 alkyl, amino C2-4 alkyl, C1-3 alkyl-C2-4 amino alkyl, di - (C1-3 alkyl) amino C2-4 alkyl, C1-3 alkylcarbonylaminoC2-4 alkyl, aminocarbonylaminoC2-4 alkyl, C1-3 alkylcarbonylaminoC2-4 alkyl, di- (C1 alkyl -3) amino-carbonylamino-C2-4 alkyl, pyrrolidin-1-ylcarbonylamino-C2-4 alkyl, piperidin-1-ylcarbonylamino-C2-4 alkyl, morpholin-4-ylcarbonylamino-C2-4 alkyl, C1-3 alkyl sulfo nyl-C2-4 alkyl or C1-3 alkyl-sulfonylamino-C2-4 alkyl, a (2-oxo-pyrrolidin-1-yl) -C2-4 alkyl, (2-oxopiperidin-1-yl) -C2 alkyl -4, (3-oxo-morpholin-4-yl) -C2-4alkyl, (2-oxo-imidazolidin-1-yl) -C2-4alkyl, (2-oxo-3-C1-3alkyl-imidazolidin -1-yl) -C2-4alkyl, (2-oxo-hexahydropyrimidin-1-yl) -C2-4alkyl or (2-oxo-3-C1-3alkyl-hexahydropyrimidin-1-yl) -C2 -alkyl 4, a C1-4 alkyl sulfonyl, chloroC 1-4 alkyl sulfonyl, bromo alkyl C1-4 sulfonyl, amino C1-4 alkyl sulfonyl, C1-3 alkyl amino C1-4 alkyl group sulfonyl, di- (C1-3 alkyl) -amino-C1-4 alkyl sulfonyl, (pyrrolidin-1-yl) -C 1-4 alkyl-sulfonyl, (piperidin-1-yl) -C 1-4 alkyl-sulfonyl, (homopiperidin-1-yl) -C 1-4 alkyl-sulfonyl, (morpholin-4-yl) -C 1-4 alkyl-sulfonyl, (homomorpholin-4-yl) -C 1-4 alkyl-sulfonyl, (piperazin-1- il) -C 1-4 alkyl-sulfonyl, (4-C 1-3 alkyl-piperazin-1-yl) -C 1-4 alkyl-sulfonyl, (homopiperazin-1-yl) -C 1-4 alkyl-sulfonyl or (4- C1-3alkyl-homopiperazin-1-yl) -C1-4alkyl sulfonyl, an al-group C1-4-carbonyl chloxy, a formyl group, C1-4alkylcarbonyl, C1-3alkyloxyC1-4alkylcarbonyl, tetrahydrofuranylcarbonyl, tetrahydropyranylcarbonyl, aminoC1-4alkylcarbonyl, C1-3alkyl C 1-4 alkylcarbonyl, di- (C 1-3 alkyl) aminoC 1-4 alkylcarbonyl, pyrrolidin-1-yl-C 1-4 alkylcarbonyl, piperidin-1-yl-C 1-4 alkylcarbonyl, (homopiperidin-1-yl) -C 1-4 alkyl-carbonyl, morpholin-4-yl-C 1-4 alkyl-carbonyl, (homomorpholin-4-yl) -C 1-4 alkyl-carbonyl, (piperazin-1-yl) -C 1-4 alkyl-carbonyl, (4-C 1-3 alkyl-piperazin-1-yl) -C 1-4 alkyl-carbonyl, (homopiperazin-1-yl) -C 1-4 alkyl-carbonyl, (4-C 1 alkyl) -3-homopiperazin-1-yl) -C 1-4 alkyl-carbonyl or C 1-3 alkyl-sulfonyl-C 1-4 alkylcarbonyl, a cyano group, aminocarbonyl, C 1-3 alkylcarbonyl alkyl, di- (C 1-6 alkyl) 3) amino-carbonyl, (C1-3 alkyloxy-C2-4 alkyl) aminocarbonyl, N- (C1-3 alkyl) -N- (C1-3 alkyloxy-C2-4 alkyl) aminocarbonyl, arylaminocarbonyl, pyrrolidin-1-ylcarbonyl , piperidin-1-ylcarbonyl, homopiperidin- 1-ylcarbonyl, morpholin-4-ylcarbonyl, homomorpholin-4-ylcarbonyl, 2-oxa-5-aza-bicyclo [2.2.1] hept-5-ylcarbonyl, 3-oxa-8-aza-bicyclo [3.2.1] oct-8-ylcarbonyl, 8-oxa-3-aza-bicyclo [3.2.1] oct-3-ylcarbonyl, piperazin-1-ylcarbonyl, 4-alkyl C1-3-piperazin-1-ylcarbonyl, homopiperazin-1-ylcarbonyl , 4-C1-3 alkyl-homopiperazin-1-ylcarbonyl, aminosulfonyl, C1-3 alkyl-aminosulfonyl, di- (C1-3 alkyl) amino-sulfonyl, pyrrolidin-1-yl-sulfonyl, piperidin-1-ylsulfonyl, homopiperidin -1-ylsulfonyl, morpholin-4-ylsulfonyl, homomorpholin-4-ylsulfonyl, piperazin-1-ylsulfonyl, 4-alkyl C1-3-piperazin-1-ylsulfonyl, homopiperazin-1-ylsulfonyl or 4-alkyl C1-3-homopiperazin -1-ylsulfonyl, a cyclobutyl, cyclopentyl or cyclohexyl group, which in each case is substituted with an R6 group, R6 representing a 2-oxo-pyrrolidin-1-yl, 2-oxopiperidin-1-yl, 3-oxo- group morpholin-4-yl, 2-oxo-imidazolidin-1-yl, 2-oxo-3-C1-3-alkyl imidazolidin-1-yl, 2-oxo-hexahydropyrimidin-1-yl or 2-oxo-3-alkyl C1-3- hexahydropyrimidin-1-yl, an azetidin-3-yl group, which in position 1 is substituted with the remainder R5, where R5 is defined as mentioned above, a pyrrolidin-3-yl group, which is substituted in the position 1 with the R5 moiety, R5 being defined as mentioned above, a piperidin-3-yl group, which is substituted in the 1 position with the R5 moiety, R5 being defined as mentioned above, a piperidine group 4-yl, which is substituted in position 1 with the remainder R5, where R5 is defined as mentioned above, or a tetrahydrofuran-3-yl, tetrahydropyran-3-yl or tetrahydropyran-4-yl group, Rd an atom of H or an atom of F, Cl, or Br, a hydroxy group, a C1-4 alkyloxy group, a methoxy group substituted with 1 to 3 F atoms, an ethyloxy group substituted with 1 to 5 F atoms, a group C2-4-alkyloxy, which is substituted with an R6 or R7 moiety, R6 being defined as mentioned above and re R7 having a hydroxy, C1-3 alkyloxy, C3-6 cycloalkyloxy, amino, C1-3-alkyl, di- (C1-3 alkyl) amino, bis- (2-methoxyethyl) -amino, pyrrolidin-1-yl group , piperidin-1-yl, homopiperidin-1-yl, morpholin-4-yl, homomorpholin-4-yl, 2-oxa-5-aza-bicyclo [2.2.1] hept-5-yl, 3-oxa-8 -aza-bicyclo [3.2.1] oct-8-yl, 8-oxa-3-aza-bicyclo [3.2.1] oct-3-yl, piperazin-1-yl, 4-alkyl C1-3-piperazin- 1-yl, homopiperazin-1-yl or C1-3 alkyl-homopiperazin-1-yl, or a formylamino group, C1-4 alkylcarbonylamino, C1-3 alkyloxy-C1-3 alkylcarbonylamino, C1-4 alkyloxy carbonylamino, aminocarbonylamino, C1-3 alkylcarbonylamino, di- (C1-3 alkyl) aminocarbonylamino, pyrrolidin-1-ylcarbonylamino, piperidin-1-ylcarbonylamino, piperazin-1-ylcarbonylamino, 4-C1-3 alkyl-piperazin-1- ilcarbonylamino, morpholin-4-ylcarbonylamino or C 1-4 alkyl sulfonylamino, a C 3-7 cycloalkyloxy or C 3-7 cycloalkyl group, a tetrahydrofuran-3-yloxy, tetrahydropyran-3-yloxy or tetrahydropyran-4- group iloxi, u n tetrahydrofuranyl-C1-4 alkyloxy or tetrahydropyranyl-C1-4 alkyloxy group; a C1-4 alkoxy group, which is substituted with a pyrrolidinyl, piperidinyl or homopiperidinyl group, substituted in the 1 position with the R8 moiety, R8 meaning an H atom or a C1-3 alkyl group, or a C1-4 alkoxy group , which is substituted with a morpholinyl group, substituted in position 4 with the R8 moiety, and X a methine group substituted with a cyano group or an N atom, and a phenyl group being understood in each case from the aryl groups mentioned in the definition of the aforementioned moieties, which is mono or disubstituted with R9, the substituents being the same or different and R9 represents an atom of H, F, Cl, Br, or Y or a C1-3 alkyl, hydroxy, C1 alkyloxy group -3, difluoromethyl, trifluoromethyl, difluoromethoxy, trifluoromethoxy or cyano, with a pyridyl, pyridazinyl, pyrimidinyl, or pyrazinyl group being understood as the heteroaryl groups mentioned in the definition of the aforementioned moieties, the heteroaryl groups being mono- or disubstituted the aforementioned in each case with the remainder R9, the substituents being the same or different and R9 is defined as previously mentioned, and the above-mentioned pyrrolidinyl, piperidinyl, piperazinyl and morpholinyl groups can be substituted with one or two alkyl groups C1-3, and as long as nothing else is mentioned, the aforementioned alkyl groups may be linear or branched, with the proviso that compound 4 - [(3-chloro-4-fluoro-phenyl) amino] -6- is excepted ((S) -tetrahydrofuran-3-yloxy) -7-hydroxy-quinazoline, its tautomers, its stereoisomers, its mixtures and its salts. |
| priorityDate | 2002-03-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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