http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-062510-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/A61P3-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P15-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D237-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D237-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-69 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P17-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 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/C07D403-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-435 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-63 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 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/A61P25-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D513-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-24 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-52 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D451-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 |
| filingDate | 2007-08-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f663305903cb818592235c53155d64c7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a4aeba6e9e0b1ff96caec15a479a8482 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2208c3960da42c400f5ecf15f5cff747 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0e015dfe022ebba76ef4b62741ebcb53 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cd98cd55963a3cbcce42692aa3d7e0d1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4ea9b2df9e8790d76137519558b4a7f1 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_04241c57d772e7827009024da27ea5eb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f622b92add7488650d7b26442dd65bee http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d063338cbfbc590d5d0ceb2d9c2f5c8d |
| publicationDate | 2008-11-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-062510-A1 |
| titleOfInvention | PIRIDONA DERIVATIVES WITH MCH ANTAGONIST ACTIVITY AND MEDICINES THAT UNDERSTAND THESE COMPOUNDS |
| abstract | In addition, this refers to pharmaceutical compositions containing at least one compound according to it. By virtue of their MCH receptor antagonistic activity, the pharmaceutical compositions according to the present are suitable for the treatment of metabolic disorders and / or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes. Claim 1: Compounds of general formula (1) in which R1, R2 independently of each other represent H, C1-8 alkyl or C3-7 cycloalkyl, wherein the alkyl or cycloalkyl group may be mono or polysubstituted with the same or different R11 groups, and a group -CH2- in position 3 or 4 of a cycloalkyl group of 5, 6 or 7 members can be substituted by -O-, -S- or -NR13-; or R2 represents a C1-3 alkylene bridge that is attached to a group Y, in which the alkylene bridge can be substituted with one or more C1-3 alkyl groups, and R1 is defined as above or represents a selected group of C1-4 alkyl-CO-, C1-4 alkyl-O-CO-, C1-4 alkyl-NH-CO- and (C1-4 alkyl) 2N-CO- in which the alkyl groups may be mono or polyfluorinated ; or R1 and R2 form a C3-8 alkylene bridge, in which 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) -, -C (= N-OH) -, -C (= N (C1-4 alkyl)) - or -NR13 -, where in the case where R1 and R2 form an alkylene bridge, in the alkylene bridge one or more H atoms can be substituted by the same or different R14 groups, and the alkylene bridge defined above may be substituted with one or two same or different Cy carbo or heterocyclic groups, so that the bond between the alkylene bridge and the Cy group is made by a single bond or a double bond, by a common C atom forming a spirocyclic ring system, by two common adjacent C and / or N atoms that form a system of condensed bicyclic rings or by three or more C and / or N atoms that form a bridge ring system; X represents a C1-3 alkylene bridge, which may comprise one, two or three same or different C1-4 alkyl substituents, where two alkyl groups may be linked together forming a 3- to 7-membered cyclic group, and where in a bridge C2-3 alkylene one or two C atoms may be monosubstituted with R10; and R10 is selected from the group consisting of hydroxy, hydroxy-C1-3alkyl, C1-4alkoxy or C1-4alkoxy-C1-3alkyl; and Y represents a 5- to 6-membered aromatic carbocyclic group, which may contain 1, 2 or 3 heteroatoms independently selected from N, O and / or S; wherein said cyclic group may be mono or polysubstituted with the same or different R20 substituents; Z represents -CH2-CH2-, -C (= O) -CH2-, -C (= CH2) -CH2- or C (OH) H-CH2- all of which may be mono- or polysubstituted with independently selected substituents with each other C1-3 alkyl; U, V represent both CH or one of the groups U, V represents N and the other of U, V represents CH, in which CH may be substituted with L; and L independently of each other represents halogen, cyano or C1-3 alkyl; and k represents 0, 1 or 2; W is selected from the group consisting of -CH2-CH2-, -CH2-O, -O-CH2-, -CH = CH-, -CH2-NRN, -NRN-CH2-, -CH2-, -O-, -S- and -NRN-; RN represents H, C1-4 alkyl, formyl, C1-3 alkylcarbonyl or C1-3 alkyl sulfonyl; and in the case where the group W represents -NRN-CH2-, the group RN can represent a bridge -CH2- or -CH2-CH2- that is attached to the cyclic group B; and B is a 5 or 6 membered unsaturated or aromatic carbocyclic group, which may contain 1, 2, 3 or 4 heteroatoms independently selected from N, O and / or S; wherein said cyclic group may be mono or polysubstituted with the same or different R20 substituents; and Cy refers to a carbo- or heterocyclic group selected from one of the following meanings a carbocyclic, saturated, 3 to 7 members, carbocyclic, unsaturated, 4 to 7 members, phenyl, saturated heterocyclic 4 to 7 members group or unsaturated of 5 to 7 members with an atom of N, O or S as heteroatom, heterocyclic, saturated or unsaturated, of 5 to 7 members with two or more atoms of N or with one or two atoms of N and an atom of O or S as heteroatoms, heterocyclic, aromatic, 5 or 6 members with one or more same or different heteroatoms selected from N, O and / or S, where the group; saturated 6 or 7 members mentioned above may also be present as bridged ring systems with an imino bridge, C1-4 alkyl-imino, methylene, ethylene, C1-4 alkyl-methylene or di-C1-4 alkyl-methylene, and while the aforementioned cyclic groups may be mono or polysubstituted into one or more C atoms with the same or different R20 groups, or in the case of a phenyl group it may also be additionally monosubstituted with nitro, and / or one or more groups NH can be substituted with R21, and in which in the carbo or heterocyclic groups, saturated or unsaturated, mentioned above, a group -CH2- can be replaced by a group - C (= O) -; R11 refers to 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 groups mentioned above one or more C atoms may be independently substituted from each other with substituents selected from halogen, OH, CN, CF3, C1-3 alkyl, C1-3 alkoxy, hydroxy C1-3 alkyl; R13 has the meaning given for R17 or represents formyl; R14 represents halogen, cyano, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, R15-O-, R15-O-CO-, R15-CO-, R15-CO-O-, R16R17N-, HCO- NR15-, R18R19N-CO-, R18R19N-CO-NH-, R15-O-C1-3 alkyl, R15-O-CO-C1-3 alkyl, R15-SO2-NH, R15-SO2-N-C1 alkyl -3-, R15-O-CO-NH-C1-3 alkyl-, R15-SO2-NH-C1-3 alkyl-, 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 refers to H, C1-4 alkyl, C3-7 cycloalkyl, C3-7 alkylcycloalkyl C1-3, phenyl, phenyl-C1-3 alkyl, pyridinyl or pyridinyl-C1-3 alkyl, R16 represents H, C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3 alkyl, C4-7 cycloalkenyl , C4-7 cycloalkenyl-C1-3 alkyl, omega-hydroxy-C2-3 alkyl, omega-C1-4 alkoxy-C2-3 alkyl, C2-6 aminoalkyl, C1-4 alkyl-C2-6 alkyl, di -C 1-4 alkyl-C 2-6 alkyl or C 3-6 cycloalkyl-C 2-6 alkyl, R 17 has one of the meanings given for R 16 or represents phenyl, phenyl-C 1-3 alkyl, pyridinyl, C 1-6 alkyl 4 -carbonyl, C3-7 cycloalkylcarbonyl, hydroxycarbonyl-C1-3alkyl, C1-4alkoxycarbonyl, C1-4alkoxy-C1-3alkyl, C1-4alkylcarbonylaminoC2-3alkyl, N - (( C1-4alkyl) -carbonyl) -N-C1-4alkyl-C2-3alkyl, C1-3alkylcarbonyl, C1-4alkyl sulfonyl, C1-4alkyl-sulfonylamino-C2-3alkyl or N- ( (C 1-4 alkylsulfonyl) -N (-C 1-4 alkyl) -amino-C 2-3 alkyl; R18, R19 independently of each other represent H or C1-6 alkyl where R18, R19 can be joined to form a C3-6 alkylene bridge, in which a non-adjacent group -CH2- an N atom can be replaced by -O-, - S-, -SO-, - (SO2) -, -CO-, -C (= CH2) - or -NR13-; R20 represents halogen, hydroxy, cyano, nitro, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-3 alkyl, C1-3 hydroxyalkyl, R22-C1- alkyl 3 o has one of the meanings given for R22; and R21 refers to C1-4 alkyl, omega-hydroxy-C2-6 alkyl, omega-C1-4 alkoxy-C2-6 alkyl, omega-C1-4 alkyl-C2-6 alkyl, omega-di-alkyl C1-4-amino-C2-6 alkyl, omega-cyclo-C3-6 alkyleneimino-C2-6 alkyl, phenyl, phenyl-C1-3 alkyl, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, C1-alkylsulfonyl -4, aminosulfonyl, C1-4 alkylaminosulfonyl, C1-4 di-alkylaminosulfonyl or C3- 6 -imino-sulfonyl cyclo-alkylene, R22 refers to pyridinyl, phenyl, phenyl-C1-3 alkoxy, C3-6-C2 alkoxyimino -4, OHC-, HO-N = HC-, C1-4 alkoxy-N = HC-, C1-4 alkoxy, C1-4 alkylthio, carboxy, C1-4 alkylcarbonyl, C1-4 alkoxycarbonyl, aminocarbonyl , C1-4-alkylaminocarbonyl, di-C1-4alkylcarbonyl, C3-6-aminocarbonyl cycloalkyl, C3-6-cycloalkyliminoimino, C3-6- phenylaminocarbonyl, C3-6- cycloalkyliminocarbonyl, C1-4 alkylsulfonyl, C1-4 alkylsulfinyl, C1-4 alkyl sulfonylamino, C1-4 alkyl sulfonyl-N-C1-4 alkyl, amino, C1-4 alkylamino, di-alq C1-4-amino alkyl, C1-4 alkylcarbonylamino, C1-4 alkylcarbonyl-N-C1-4alkylamino, C3-6 cycloalkyleneimino, phenyl-C1-3 alkylamino, N-C1-4 alkyl-phenyl-alkyl C1-3-amino, acetylamino, propionylamino, phenylcarbonyl, phenylcarbonylamino, phenylcarbonylmethylamino, hydroxy (C22 alkyl) aminocarbonyl, 4-morpholinylcarbonyl, 1-pyrrolidinylcarbonyl, 1-piperidinylcarbonyl, hexahydro-1-azepinylcarbonyl 4-methyl-1-piperazinylcarbonyl, aminocarbonylamino or C1-4alkylcarbonylamino, in which in the aforementioned groups and radicals, in particular in L, W, X, Z, RN, R10, R11, R13 to R22 , in each case one or more C atoms may be additionally mono or polysubstituted with F and / or in each case one or two C atoms independently of each other may be additionally monosubstituted with CI or Br and / or in each case one or more phenyl rings may additionally independently comprise one, two or three substituents selected from the group of F, CI, Br, I, cyano, C 1-4 alkyl, C 1-4 alkoxy, difluoromethyl, trifluoromethyl, hydroxy, amino, C 1-3 alkylamino, di-C 1-3 alkyl, acetylamino, aminocarbonyl, difluoromethoxy, trifluoromethoxy, amino C 1-3 alkyl , C1-3alkyl-C1-3alkyl- and di-C1-3alkyl-C1-3alkyl and / or may be monosubstituted with nitro, and the H atom of any carboxy group present or an atom of H attached to an atom of N can be replaced in each case by a group that can be cleaved in vivo, tautomers, diastereoisomers, e |
| priorityDate | 2006-08-25-04:00^^<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: 75.