http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-031668-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_bb66d9373d09efad73c142762f6dfb00 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-47 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4706 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-4709 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-54 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-517 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4709 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4706 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-47 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-496 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
filingDate | 2000-02-28-04:00^^<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_56a02bcf43919d8d5d23c381844bbe97 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d99d2219ac76e34977431046ae63a3c5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f1c138d1974ed0dc472ef209c312aacc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b1a16155429b81d162af8b8df8c9ec5e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f5c454b5d90297280d6fc088099ff58b |
publicationDate | 2003-10-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-031668-A1 |
titleOfInvention | BICYCLIC HETEROCICLES, ITS PHYSIOLOGICALLY COMPATIBLE SALTS, THE MEDICINES THAT CONTAIN THEM, THE PROCEDURES FOR THEIR PREPARATION AND THE USE OF THESE TO PREPARE AN ADEQUATE MEDICINAL FOR THE TREATMENT OF CERTAIN DISEASES AS THE TUMOR OF THE RIN, THE RIN. |
abstract | Bicyclic heterocycles of general formula (1) are described, in which Ra means a hydrogen atom or a C1-4 alkyl group, Rb means a phenyl, benzyl or 1-phenylethyl group, in which the phenyl nucleus is substituted in each case with the radicals R1 to R3, where R1 and R2, which may be the same or different, in each case represent a hydrogen, fluorine, chlorine, bromine or iodine atom, a C1-4 alkyl group, hydroxy, C1 alkoxy -4, C3-6 cycloalkyl, C4--6 cycloalkoxy, C2-5 alkenyl or C2-5 alkynyl, an aryl, aryloxy, arylmethyl or arylmethoxy group, a C3-5 alkenyloxy or C3-5 alkynyloxy group, which cannot be linked the unsaturated part with the oxygen atom, a C1-4 alkyl sulfenyl group, C1-4 alkyl sulfulyl C1-4 alkyl sulfonyl, trifluoromethylsulfenyl, trifluoromethylsulfinyl or trifluoromethylsulfonyl group, a methyl or methoxy group substituted with 1 to 3 fluorine atoms, a ethyl or ethoxy group substituted with 1 to 5 fluorine atoms, a cyano or nitro group, or a amino group optionally substituted with one or two C1-4 alkyl groups, the substituents being the same or different, R1 together with R2, if these are attached to adjacent carbon atoms, they mean a group -CH = CH-CH = CH, CH = CH-NH or -CH = N-NH and R3 represents a hydrogen, fluorine, chlorine or bromine atom, a C1-4 alkyl, trifluoromethyl or C1-4 alkoxy group, Rc and Rd, which may be the same or different, they mean in each case a hydrogen, fluorine or chlorine atom, a methoxy group or a methyl group optionally substituted with a methoxy, dimethylamino, diethylamino, pyrrolidino, piperidino or morpholino group, X means a methine group substituted with a cyano group, or a nitrogen atom, A means an oxygen atom or an imino group optionally substituted with a C1-4 alkyl group, B means a carbonyl or sulfonyl group, C means a 1,3-alenylene, 1,1- or 1,2 group -vinylene, which in each case can be substituted with one or two methyl groups or with a triflu group oromethyl, an ethynylene group or a 1,3-butadiene-1,4-ylene group optionally substituted with 1 to 4 methyl groups or with a trifluoromethyl group, D means an alkylene group, -CO-alkylene or -SO2-alkylene, in those that the alkylene part contains in each case 1 to 8 carbon atoms and, additionally, 1 to 4 hydrogen atoms in the alkylene part may be replaced by fluorine atoms, the linking of the -CO-alkylene group must be made and -SO2-alkylene with the group C contiguous in each case through the carbonyl or sulfonyl group, a group -CO-O-alkylene, -CO-NR4-alkylene or -SO2-NR4-alkylene, in which the alkylene part it contains in each case 1 to 8 carbon atoms, the link with the adjacent group C having to be made in each case through the carbonyl or sulfonyl group, in which R4 represents a hydrogen atom or a C1-4 alkyl group, or, in the case that D is attached to a carbon atom of radical E, it also means a bond or, in the if D is attached to a nitrogen atom of the radical E, it also means a carbonyl or sulfonyl group, E means an R6O-CO-alkylene-NR5 group, (R7O-PO-OR8) -alkylene-NR5 or (R7O- PO-R9) -alkylene-NR5, in which in each case the alkylene part, which is straight chain and contains 1 to 6 carbon atoms, can be further substituted with one or two C1-2 alkyl groups or with a R6O-CO or R6O-CO-C1-2 alkyl group, wherein R5 represents a hydrogen atom, a C1-4 alkyl group, which may be substituted with an R6O-CO group, (R7O-PO-OR8) or ( R7O-PO-R9), an ethyl or propyl group optionally substituted with one or two methyl or ethyl groups, which in each case in the terminal position is substituted with a C1-6 alkylcarbonylsulfenyl, C3-7-carbonyl-sulfenyl cycloalkyl group , C 3-7 cycloalkyl-C 1-3 alkylcarbonylsulfenyl, arylcarbonyl sulfenyl or arylC 1-3 alkylcarbonylsulfenyl group, an ethyl or propyl group optionally substituted with one or two methyl or ethyl groups , which in each case in the terminal position is substituted with a C1-6-carbonyloxy alkyl, C3-7-carbonyloxy, C3-7-cycloalkyl-C1-3-carbonyloxy, arylcarbonyloxy or aryl-C1-3-carbonyloxy group, a group ethyl or propyl optionally substituted with one or two methyl or ethyl groups, which in each case in terminal position is substituted with a hydroxy group, C1-4 alkoxy, amino, C1-4 alkyl-amino or di- (C1-4 alkyl) - -amino or with an alkyleneimino group of 4 to 7 members, where in the aforementioned 6 to 7 member alkyleneimino groups in each case a methylene group in position 4 may be replaced by an oxygen or sulfur atom, by a group sulfinyl, sulfonyl, imino or N- (C1-4 alkyl) -imino, a C3-7 cycloalkyl or C3-7 cycloalkyl-C1-3 alkyl, R6, R7 and R8 group, which may be the same or different, represent in each case a hydrogen atom, a C1-8 alkyl group that may be substituted with a hydroxy group, C1-4 alkoxy, amino, alkyl C1-4-amino or di- (C1-4 alkyl) -amino, or with a 4 to 7-membered alkyleneimino group, wherein in the aforementioned 6 to 7-member alkyleneimino groups, in each case a methylene group in position 4 may be replaced by an oxygen or sulfur atom, by a sulfinyl, sulfonyl, imino or N- (C1-4 alkyl) -imino group, a hydroxy group, C1-4 alkoxy, amino, C1-4-alkyl or di- (C1-4 alkyl) - -amino or with a 4 to 7 membered alkyleneimino group, wherein in the aforementioned 6 to 7 member alkyleneimino groups in each case a methylene group in position 4 may be replaced by a oxygen or sulfur atom, by a sulfinyl, sulfonyl, imino or N- (C1-4 alkyl) -imino group, a C3-7 cycloalkyl or C3-7 cycloalkyl-C1-3 alkyl, R6, R7 and R8 group, which they can be the same or different, they represent in each case a hydrogen atom, a C1-8 alkyl group that can be substituted with a hydroxy, C1-4 alkoxy, amino, C1-4-amino alkyl or di- (C1-4 alkyl) -amino, or with a 4 to 7-membered alkyleneimino group, wherein in the aforementioned 6 to 7-member alkyleneimino groups, in each case a methylene group in position 4 may be replaced by an atom of oxygen or sulfur, by a sulfinyl, sulfonyl, imino or N- (C1-4 alkyl) -imino group, a C4-7 cycloalkyl group optionally substituted with 1 or 2 methyl groups, a C3-5 alkenyl or C3-5 alkynyl group , the unsaturated part cannot be linked to the oxygen atom, a C3-7 cycloalkyl group C1-4, aryl, arylalkylC 1-4 or RgCO-O (ReCRf), where Re and Rf, which may be the same or different , in each case, represent a hydrogen atom or a C1-4 alkyl group, Rg represents a C1-4 alkyl, C3-7 cycloalkyl, C1-4 alkoxy or C5-7 cycloalkoxy group, and R9 represents a C1-4 alkyl group , aryl or C 1-4 arylalkyl, a 4- to 7-membered alkyleneimino group that is substituted with an R6O-CO group, (R7O-PO-OR8), (R7O-PO-R9), R6O-CO-alkyl C1-4, bis- (R6O-CO) -C1-4 alkyl, (R7O-PO-OR8) -C1-4 alkyl or (R7O-PO-R9) -C1-4 alkyl, where R6 to R9 are defined as mentioned above, a 4 to 7 membered alkyleneimino group is substituted with two R6O-CO or R6O-CO-C1-4 alkyl groups, or with an R6O-CO group and an R6O-CO-C1-alkyl group -4, in which R6 is defined as mentioned above, a piperazino or homopiperazino group, which in position 4 is substituted with the radical R10 and, additionally, is substituted in a ring carbon atom with a group R6O-CO , (R7O-PO-OR8), (R7O-PO-R9), R6O-CO-C1-4 alkyl, bis- (R6O-CO) - -C1-4 alkyl, (R7O-PO-OR8) -C1 alkyl -4 or (R7O-PO-R9) -C1-4 alkyl, in which R6 to R9 are defined as mentioned above, and R10 represents a hydrogen atom, a C1-4 alkyl group, formyl, C1-alkyl 4-carbonyl or C1-4 alkyl sulfonyl, a piperazino or homopiperazino group, which in position 4 is substituted with the radical R10, and added On the ring carbon atoms it is substituted with two R6O-CO or R6O-CO-C1-4 alkyl groups, or with an R6O-CO group and an R6O-CO-C1-4 alkyl group, in which R6 and R10 are defined as mentioned above, a piperazino or homopiperazino group, which in each case in position 4 is substituted as a group R6O-CO-C1-4 alkyl, bis- (R6O-CO) -C1-4 alkyl, ( R7O-PO-OR8) -C1-4alkyl or (R7O-PO-R9) -C1-4alkyl, and additionally in ring carbon atoms it is substituted with one or two R6O-CO or R6O-CO-alkyl groups C1-4, or with an R6O-CO group and an R6O-CO-C1-4 alkyl group, in which R6 to R9 are defined as mentioned above, a morpholino or homomorpholino group, which in each case is substituted with a group R6-O-CO, ((R7O-PO-OR8), (R7O-PO-R9), R6O-CO-C1-4alkyl, bis- (R6O-CO) -C1-4alkyl, (R7O- PO-OR8) - -C1-4 alkyl or (R7O-PO-R9) -C1-4 alkyl, in which R6 to R9 are defined as mentioned above, a morphol group ino u homomorpholino, which is substituted with two R6O-CO or R6O-CO-C1-4 alkyl groups, or with an R6O-CO group and with an R6O-CO-C1-4 alkyl group, in which R6 is defined as mentioned above, a pyrrolidinyl, piperidinyl or hexahydroazepinyl group substituted in position 1 with the radical R10, the aforementioned 5 to 7 member rings being substituted, in each case additionally in a carbon atom, with an R6O-CO group, (R7O-PO-OR8), (R7O-PO-R9), R6O-CO-C1-4alkyl, bis- (R6O-CO) -C1-4alkyl, (R7O-PO-OR8) -C1-4alkyl or (R7O-PO-R9) -C1-4 alkyl, wherein R6 to R10 are defined as mentioned above, a pyrrolidinyl, piperidinyl or hexahydroazepinyl group substituted in position 1 with the radical R10, the rings of 5 being substituted to 7 members mentioned above, in each case additionally in carbon atoms, with two R6O-CO or R6O-CO-C1-4 alkyl groups, or with an R6O-CO group and with an R6O-CO-alq group C1-4 uyl, in which R6 and R10 are defined as mentioned above |
priorityDate | 1999-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 88.