http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-043056-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/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D495-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 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/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-554 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P1-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-541 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-454 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D495-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-554 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-541 |
| filingDate | 2003-10-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_681d554e44caa631a54c61ec83651f4f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1a006604ae89706b782c9038251bb8ed http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d85fd19be926051ef4a25746b2c2894a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_117276acedb58bcd8c773f3bbc8334d1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_317dd03db68b820a3a8f03423a6b7e60 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7ad928238c42e464cd56f20a556f1602 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d2ed2ed793330685a87b55c380fcbe36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_959e80db78e16f6acbd8b3368d7ad5ea http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_de265c663ea4200a9eaef9c1e74bba64 |
| publicationDate | 2005-07-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-043056-A1 |
| titleOfInvention | CGRP ANTAGONISTS ELECTED, PROCEDURE FOR PREPARATION, AS WELL AS ITS EMPLOYMENT AS MEDICATIONS |
| abstract | They are the subject of the present GCRP antagonists of the general formula (1) in which they mean: To an oxygen or sulfur atom, a phenylsulfonylimino or cyanimino group, X an oxygen or sulfur atom, an imino group, eventually substituted with a C1-6 alkyl group or a methylene group optionally substituted with a C1-6 alkyl group, Y and Z independently of each other, in each case a straight or branched C1-6 alkyl group, in which each methylene group may be substituted with up to 2 fluorine atoms and each methyl group may be substituted with up to 3 fluorine atoms, the aforementioned alkyl groups may be linked together, together with the carbon atoms to which they are attached, forming a ring of 4 to 8 members, R1 a heterocycle aza, diaza, triaza, oxaza, tiaza, tiadiaza or S, S-dioxide-thiadiaza of 5 to 7 members, saturated, unsaturated once or twice, the above-mentioned heterocycles linked to through a carbon or nitrogen atom, containing one or two carbonyl or thiocarbonyl groups adjacent to a nitrogen atom, one of the nitrogen atoms may be substituted with an alkyl group, and may be substituted in one or two carbon atoms with an alkyl group, with a phenyl, phenylmethyl, naphthyl, biphenylyl, pyridinyl, diazinyl, furyl, thienyl, pyrrolyl, 1,3-oxazolyl, 1,3-thiazolyl, isoxazolyl, pyrazolyl, 1-methylpyrazolyl, imidazolyl or 1- group methylimidazolyl, the substituents being able to be the same or different, and an olefinic double bond of one of the above-mentioned unsaturated heterocycles may be condensed with a phenyl, naphthyl, pyridine, diazine, 1,3-oxazole, thienyl, furan, thiazole ring, N-methylpyrrole or quinoline pyrrole, with a 1H-quinolin-2-one ring optionally substituted on the nitrogen atom with an alkyl group or with an imidazole or N-methylimidazole ring or also two double Olefinic bonds of one of the aforementioned unsaturated heterocycles may be condensed in each case with a phenyl ring, wherein the phenyl, pyridinyl, diazinyl, furyl, thienyl, pyrrolyl, 1,3-oxazolyl, 1,3-thiazolyl groups, isoxazolyl, pyrazolyl, 1-methylpyrazolyl, imidazolyl or 1-methylimidazolyl contained in R1, as well as heterocyclics fused with benzo-, thieno-, pyrido- and diazino- may be mono-, di- or trisubstituted further in the carbon skeleton with atoms of fluorine, chlorine, bromine or iodine, with alkyl, alkoxy, nitro, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylsulfonylamino, phenyl, difluoromethyl, trifluoromethyl, alkoxycarbonyl, carboxy, hydroxy, amino, alkylamino, dialkylamino, acetyl, amino, propylaminocarbonyl groups , alkylaminocarbonyl, dialkylaminocarbonyl, (4-morpholinyl) carbonyl, (1-pyrrolidinyl) carbonyl, (1-piperidinyl) carbonyl, (hexahydro-1-azepinyl) carbonyl, (4-methyl-1-pipe razinyl) carbonyl, methylenedioxy, aminocarbonylamino, alkanoyl, cyano, difluoromethoxy, trifluoromethoxy, trifluoromethylthio, trifluoromethylsulfinyl or trifluoromethylsulfonyl, which may be the same or different substituents, R2 means the hydrogen atom, which is a phenylmethyl group7 Omega may be substituted with a cyclohexyl, phenyl, pyridinyl, diazinyl, hydroxy, amino, alkylamino, dialkylamino, carboxy, alkoxycarbonyl, aminocarbonyl, aminocarbonylamino, acetylamino, 1-pyrrolidinyl, 1-piperidinyl, 4- (1-piperidinyl) -1 group -piperidinyl, 4-morpholinyl, hexahydro-1H-1-azepinyl, [bis- (2-hydroxyethyl)] amino, 4-alkyl-1-piperazinyl or 4- (omega-hydroxy-C2-7 alkyl) -1-piperazinyl , a phenyl or pyridinyl group, wherein the above-mentioned heterocyclic radicals and phenyl groups may be mono-, di- or trisubstituted further in the carbon skeleton with fluorine, chlorine, bromine or iodine atoms, with methy groups lo, alkoxy, difluoromethyl, trifluoromethyl, hydroxy, amino, C1-3 alkylamino, di- (C1-3alkyl) -amino, acetylamino, aminocarbonyl, cyano, methylsulfonyloxy, difluoromethoxy, trifluoromethoxy, trifluoromethylthio, trifluoromethylsulfinyl, alkylsulphonylamino-amino -3, C1-3alkyl C1-3alkyl or di- (C1-3alkyl) -amino-C1-3alkyl and the substituents may be the same or different, R3 the hydrogen atom or a C1-3alkyl group optionally substituted with a phenyl or pyridinyl group, the C1-3 alkyl group may be attached with an alkyl group present in R2 or with a phenyl or pyridyl ring present in R2 and the nitrogen atom to which they are attached, forming a ring, or R2 and R3 together with the included nitrogen atom forms a radical of the general formula (2) in which Y1 means the carbon atom or, when R5 represents a free electron pair, also the nitrogen atom, qyr, when Y1 represents the carbon atom, the n mere 0, 1 or 2, oqyr, when Y1 represents the nitrogen atom, the numbers 1 or 2, R4 means the hydrogen atom, an amino group, alkylamino, dialkylamino, alkyl, cycloalkyl, amino-C2-7 alkyl, alkylamino -C2-7 alkyl, dialkylamino-C2-7 alkyl, aminoiminomethyl, aminocarbonylamino, alkylaminocarbonylamino, cycloalkylaminocarbonylamino, phenylaminocarbonylamino, aminocarbonylalkyl, aminocarbonylaminoalkyl, alkoxycarbonyl, alkoxycarbonylalkyl or carboxyalkyl group, or also represents the group of nitrogen, or also the group of nitrogen, or the group of nitrogen, does not mean the group of nitrogen, or does it mean the group of nitrogen, or the group of nitrogen, or the group of nitrogen, does not mean the group of nitrogen, or does it mean the group of nitrogen, or the group of nitrogen, or the group of nitrogen, does not mean the group of nitrogen, or does it mean the group of nitrogen, or the group of nitrogen, or the group of nitrogen, does not mean the group of nitrogen, or the group of nitrogen, does not mean the group of nitrogen, or does it mean the group of nitrogen, or the group of nitrogen, or the group of nitrogen does not mean aminomethyl, alkylaminomethyl or dialkylaminomethyl, a phenyl, pyridinyl, diazinyl, 1-naphthyl, 2-naphthyl, pyridinylcarbonyl or phenylcarbonyl group which in each case may be mono-, di- or trisubstituted in the carbon skeleton with fluorine atoms, chlorine, bromine or iodine, with alkyl, alkoxy, methylsulfonyloxy, difluoromethyl, trifluoromethyl, hydroxy, amino, acetylamino, aminocarbonyl, amino groups arbonylamino, aminocarbonylaminomethyl, cyano, carboxy, alkoxycarbonyl, carboxyalkyl, alkoxycarbonylalkyl, alkanoyl, omega- (dialkylamino) alkanoyl, omega- (dialkylamino) alkyl, omega- (dialkylamino) hydroxyalkyl, omega- (carboxy) alkanoyl, difluoromethyl, triforomethyl, difluoromethyl, difluoromethyl, difluoromethyl, triforomethyl, difluoromethyl, difluoromethyl, triforomethyl trifluoromethylsulfinyl or trifluoromethylsulfonyl, the substituents being the same or different, a 4 to 10 membered cycloalkyl group, a 6 to 10 membered oxaza, thiaza or diaza group, a 6 to 10 membered azabicycloalkyl group, a 1-alkyl-4 group -piperidinylcarbonyl or 4-alkyl-1-piperazinylcarbonyl, the aforementioned monocyclic and bicyclic heterocycles being linked through a nitrogen atom or a carbon atom, in the above-mentioned monocyclic and bicyclic heterocycles a methylene group not directly attached to an atom of nitrogen, oxygen or sulfur can be substituted with one or two fluorine atoms, the hetero Monocyclic and bicyclic cycles mentioned above as well as the 1-alkyl-4-piperidinylcarbonyl and 4-alkyl-1-piperazinylcarbonyl group may be substituted on the ring once or several times with a C1-7 alkyl group, once with a phenyl group C1-3 alkyl, alkanoyl, dialkylamino, phenylcarbonyl, pyridinylcarbonyl, carboxy, carboxyalkanoyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, alkylsulfonyl, cycloalkyl or cycloalkylalkyl, with a cycloalkylcarbonylcarbonylcarbonylcarbonylcarbonylcarbonylcarbonylcarbonyl group , comprising the alicyclic parts contained in these substituents 3 to 10 members of the ring and the heteroalicyclic parts in each case 4 to 10 members of the ring and the phenyl and pyridinyl radicals contained in the aforementioned radicals may in turn be mono-, di- or trisubstituted with atoms of fluorine, chlorine, bromine or iodine, with alkyl, alkoxy, methylsulfonyloxy, difluoromethyl, trifluoromethyl, hydroxy, amino, acetylamino, aminocarbonyl, aminocarbonylamino, aminocarbonylaminomethyl, cyano, carboxy, alkoxycarbonyl, carboxy alkyl, alkoxycarbonylalkyl, alkoxycarbonylalkyl, alkoxycarbonylalkyl , omega- (carboxy) alkanoyl, difluoromethoxy, trifluoromethoxy, trifluoromethylthio, trifluoromethylsulfinyl or trifluoromethylsulfonyl, the substituents being the same or different substituents, R5 a hydrogen atom, a C1-4 alkyl group, an unbranched alkyl radical may be substituted in the omega position with a phenyl, pyridinyl, diazinyl, amino, alkylamino, dialkylamino, 1-pyrrolidinyl, 1-piperidinyl, 4-methyl-1-piperazinyl, 4-morpholinyl or hexahydro-1H-1-azepinyl group, an alkoxycarbonyl group, the cyano group or aminocarbonyl or also, when Y1 represents a nitrogen atom, a free electron pair, or, when Y1 does not represent a nitrogen atom or, also the fluorine atom, or R4 together with R5 and Y1 a 4 to 7 membered cycloaliphatic ring, in which a methylene group can be replaced by a group -NH- or -N (alkyl) -, being able to be replaced a hydrogen atom attached to a nitrogen atom within the group R4 mentioned above by a protective group, R6 and R7, which may be the same or different, in each case a hydrogen atom, a C1-3 alkyl or dialkylamino group or also , when Y1 does not represent a nitrogen atom, the fluorine atom and R8 and R9, which may be the same or different, in each case a hydrogen atom or a C1-3 alkyl group, wherein all the alkyl and alkoxy groups above mentioned as well as the alkyl groups present within the other mentioned radicals, if not indicated otherwise, cover from 1 to 7 carbon atoms and can be straight chain or branched, each methylene group can be substituted with up to two atoms of fluorine and each methyl group with up to 3 fluorine atoms, all the cycloalkyl groups mentioned above, as well as |
| priorityDate | 2002-10-25-04:00^^<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: 118.