http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-048692-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_12a9e9ce63eb0bbf3658453fb50a6d9b |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-61 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P29-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-61 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-30 |
| filingDate | 2005-04-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_04241c57d772e7827009024da27ea5eb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b195de3260d825dafa115616755dc393 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c4ea760b854cae5feb0c2ebdf3662222 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c92b7f6e9f50c24b55ecf716e6dc51ee http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4ea9b2df9e8790d76137519558b4a7f1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cd98cd55963a3cbcce42692aa3d7e0d1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_03939819982055cf878f5c94a56e92a1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f622b92add7488650d7b26442dd65bee http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a4aeba6e9e0b1ff96caec15a479a8482 |
| publicationDate | 2006-05-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-048692-A1 |
| titleOfInvention | ALKIN COMPOUNDS WITH ANTAGONIST ACTION ON MCH AND MEDICINES CONTAINING THESE COMPOUNDS |
| abstract | This refers to compounds with an alkyne structure of general formula (1), in which: R1, R2 independently mean each other, H, C1-8 alkyl, C3-7 cycloalkyl or an optionally phenyl or pyridinyl radical mono- or polysubstituted with the same or different R20 radicals and / or monosubstituted with nitro, where the alkyl or cycloalkyl group may be mono- or polysubstituted with the same or different R11 radicals, and where a -CH2- group may be replaced at position 3 or 4 of a cycloalkyl group of 5, 6 or 7 members with -O-, -S- or -NR13-; or R1 and R2 form a C3-8 alkylene bridge, where a group -CH2- not adjacent to the N atom of the group R1R2N can be replaced by -CH = N-, -CH = CH-, -O-, -S- , - SO, - (SO2) -, -CO-, -C (= CH2) - or -NR13-, where in the C3-8 alkylene bridge defined above one or more atoms of H can be replaced by radicals R14 equal or different, and where the alkylene bridge defined above may be replaced by one or more cyclic or heterocyclic groups Cy the same or different such that the bond between the alkylene group and the group Cy occurs: through a single or double bond ; through a common C atom, forming a spirocyclic ring system; through two adjacent common C and / or N atoms, forming a system of condensed bicyclic rings; or through three or more atoms of C and / or N, forming a bridge ring system; X means a C1-6 alkylene bridge having one or more substituents independently of one another, selected from fluorine, chlorine, hydroxy, cyano, CF3, C1-4 alkyl, hydroxy C1-4 alkyl, C3-6 cycloalkyl and alkoxy C1-4, where two alkyl substituents can be linked together, forming a C3-7 cycloalkyl group; or a C2-4 alkyleneoxy or C2-4 alkyleneimino group, where the imino group may be substituted with a C1-4 alkyl group, and where the alkylene unit has one or more substituents independently from each other, selected from fluorine, chlorine , CF3, hydroxyC 1-4 alkyl, C 1-4 alkyl and C 3-6 cycloalkyl, where two alkyl groups may be linked together, forming a C 3-7 cycloalkyl or C 4-6 cycloalkylimino group; or a C3-6 alkenylene or C3-6 alkynylene bridge, which is unsubstituted or having one or more substituents selected, independently from each other, from fluorine, CF3, hydroxyC 1-4 alkyl, C 1-4 alkyl and cycloalkyl C3-6, where two alkyl substituents can be linked together, forming a C3-7 cycloalkyl or C5-7 cycloalkenyl group; and W, Z mean, independently of each other, a single bond or a C1-2 alkylene bridge; where two adjacent C atoms with an additional C1-4 alkylene bridge can be linked together; and where one or two C atoms can be substituted, independently of one another, with one or two identical or different C1-3 alkyl radicals, where two alkyl radicals can be linked together forming a carbocyclic ring; and Y, A are selected independently of each other, from the group consisting of the bivalent cyclic groups phenyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, naphthyl, tetrahydronaphthyl, indolyl, dihydroindolyl, quinolinyl, dihydroquinolinyl, tetrahydroquinolinyl, isoquinolinyl, dihydroisoquinolinyl, tetrahydro -isoquinolinyl, benzimidazolyl, benzoxazolyl, chromanyl, chromen-4-onyl, thienyl, furanyl, benzothienyl or benzofuranyl, where the aforementioned cyclic groups may be mono- or polysubstituted in one or more C atoms with the same or different R20 radicals, in the case of a phenyl ring also monosubstituted with nitro, and / or in one or more NH groups with R21; B has one of the meanings indicated for Y, A or C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C3-7 cycloalkyl, C5-7 cycloalkenyl, C3-7 cycloalkyl-C1-3 alkyl, C3- cycloalkenyl 7-C1-3 alkyl, C3-7 cycloalkyl C1-3- or C3-7 cycloalkyl-C1-3 alkynyl, where one or more C atoms independently of one another, mono or polysubstituted with halogen and / or monosubstituted with hydroxy or cyano and / or mono- or polysubstituted cyclic groups with the same or different R20 radicals; Cy is a carbocyclic or heterocyclic group selected from one of the following meanings: a saturated carbocyclic group of 3 to 7 members; an unsaturated carbocyclic group of 4 to 7 members; a phenyl group; a saturated heterocyclic group of 4 to 7 members or unsaturated of 5 to 7 members with an atom of N, O or S as a heteroatom; a saturated or unsaturated 5- to 7-membered heterocyclic group with two or more N atoms or with one or two N atoms and an O or S atom as heteroatoms; a 5- or 6-membered aromatic heterocyclic group with one or more same or different heteroatoms selected from N, O and / or S; where the 6 or 7-member saturated groups described above may also be present as cyclic bridging systems with an imino bridge, (C1-4 alkyl) -imino, methylene, (C1-4 alkyl) -methylene or di- (C1 alkyl -4) -methylene; and where the above-mentioned cyclic groups mono- or polysubstituted in one or more C atoms may be substituted with the same or different R20 radicals, in the case of a phenyl group also additionally monosubstituted with nitro, and / or one or more NH groups substituted with R21; R11 means halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, R15-O, R15-O-CO-, R15-CO-O-, cyano, R16R17N-, R18R19N-CO- or Cy-, where in the above-mentioned groups one or more C atoms may be mono- or polysubstituted, independently from each other, by substituents selected from halogen, OH, CN, CF3, C1-3 alkyl, hydroxy-C1-3 alkyl; R13 has one of the meanings indicated for R17; R14 is halogen, cyano, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, R15-O-, R15-O-CO-, R15-CO-, R15-CO-O-, R16R17N-, R18R19N- CO-, R15-O-C1-3 alkyl, R15-O-CO-C1-3 alkyl, R15-SO2-NH-, R15-O-CO-NH-C1-3 alkyl, R15-SO2-NH-alkyl C1-3, R15-CO-C1-3 alkyl, R15-CO-O-C1-3 alkyl, R16R17N-C1-3 alkyl, R18R19N-CO-C1-3 alkyl or Cy-C1-3 alkyl; R15 is H, C1-4 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3 alkyl, phenyl, phenyl-C1-3 alkyl, pyridinyl or pyridinyl-C1-3 alkyl; R16 is H, C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3 alkyl, C4-7 cycloalkenyl, C4-7 cycloalkenyl-C1-3 alkyl, w-hydroxy-C2-3 alkyl, w- (C1-4 alkoxy) -C2-3 alkyl, amino C2-6 alkyl, C1-4 alkyl-C2-6 alkyl, di- (C1-4 alkyl) -amino-C2-6 alkyl or cyclo-alkyleneimino C3-6-C2-6 alkyl; R17 has one of the meanings indicated for R16 or is phenyl, phenyl-C 1-3 alkyl, pyridinyl, C 1-4 alkylcarbonyl, hydroxycarbonylC 1-3 alkyl, C 1-4 alkoxycarbonyl, C 1-4 alkoxycarbonyl , C1-4 alkylcarbonylamino-C2-3 alkyl, N- (C1-4 alkylcarbonyl) -N- (C1-4 alkyl) -amino-C2-3 alkyl, C1-4 alkylsulfonyl, C1-4 alkylsulfonylamino-C2-3 alkyl or N- (C1-4 alkylsulfonyl) -N- (C1-4 alkyl) -amino-C2-3 alkyl; R18, R19 are, independently of each other, H or C1-6 alkyl; R20 is halogen, hydroxy, cyano, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3 alkyl, hydroxy-C1-3 alkyl, R22-C1-alkyl 3 or one of the meanings indicated for R22; R21 is C1-4 alkyl, w-hydroxyC2-6 alkyl, w-C1-4 alkoxy-C2-6 alkyl, w-C1-4 alkyl-C2-6 alkyl, w-di- (C1- alkyl 4) -amino-C2-6 alkyl, w-cyclo-C3-6 alkyleneimino-C2-6 alkyl, phenyl, phenyl-C1-3 alkyl, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, C1-alkylsulfonyl 4, aminosulfonyl, C 1-4 alkylaminosulfonyl, C 1-4 di-alkylaminosulfonyl or C 3-6 cyclo-alkylene sulfonyl; R22 is pyridinyl, phenyl, C1-3 phenyl-alkoxy, C3-6 cycloalkyliminoC2-4, OHC-, HO-N = HC-, C1-4-N-alkoxy = HC-, C1-4 alkoxy, C1-alkylthio -4, carboxy, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, aminocarbonyl, C1-4 alkylaminocarbonyl, di- (C1-4 alkyl) -aminocarbonyl, C3-6-amino-carbonyl cycloalkyl, C3-6-cycloalkyliminocarbonyl, phenylaminocarbonyl , C3-6 cycloalkylimino-C2-4-alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylsulfinyl, C1-4 alkylsulfonylamino, amino, C1-4 alkylamino, di- (C1-4 alkyl) -amino, C1-4 alkyl -carbonyl-amino, C3-6 cycloalkyleneimino, phenyl-C1-3alkylamino, N- (C1-4alkyl) -phenyl-C1-3alkylamino, acetylamino, propionylamino, phenylcarbonyl, phenylcarbonylamino, phenylcarbonylmethylamino, hydroxy-C2-3 alkylaminocarbonyl, (4-morpholinyl) carbonyl, (1-pyrrolidinyl) carbo-nyl, (1-piperidinyl) carbonyl, (hexahydro-1-azepinyl) carbonyl, (4-methyl-1-piperazinyl) carbonyl, methylenedioxy, aminocarbonylamino or C1-alkylaminocarbonylamino 4; where in the aforementioned groups and radicals, especially in W, Z, R13 to R22, one or more C atoms additionally mono or polysubstituted with F and / or one or two C atoms, independently of each other, additionally monosubstituted with Cl or Br and / or one or several phenyl rings, of mono independent from each other, additionally have one, two or three substituents selected from the group F, Cl, Br, I, cyano, C1-4 alkyl, C1-4 alkoxy , difluoromethyl, trifluoromethyl, hydroxy, amino, C1-3 alkylamino, di- (C1-3 alkyl) -amino, acetylamino, aminocarbonyl, difluoromethoxy, trifluoromethoxy, amino C1-3 alkyl, C1-3 alkylamino-C1-3 alkyl and di- (C1-3 alkyl) -amino-C1-3 alkyl and / or may be monosubstituted with nitro; and the H atom of an existing carboxy group or an H atom attached to an N atom can be replaced by an in vivo cleavable radical, its tautomers, its diasteroisomers, its enantiomers, mixtures and salts thereof; wherein the following compounds are not included: (1- {5- [5- (4-Chloro-phenyl) -pyridin-2-iletinyl] -pyridin-2-yl} -pyrrolidin-3-yl) -dimethyl-amine; 5 '- [5- (4-Chloro-phenyl) -pyridin-2-iletinyl] -3-pyrrolidin-1-yl-3,4,5,6-tetrahydro-2H- [1,2'] bipyridinyl; 1 '- {5- [5- (4-chloro-phenyl) -pyridin-2-yletinyl] -pyridin-2-yl -} - [1,3'] bipyrrolidinyl; {5- [5- (4-Chloro-phenyl) -pyridin-2-iletinyl] -pyrid |
| priorityDate | 2004-04-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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