Substituted 2-pyridones and pyrid-2-thiones compounds
First Claim
1. A ketone of the formula ##STR75## in which A represents aryl having 6 to 10 carbon atoms, which is optionally monosubstituted to pentasubstituted by identical or different substituents from the group consisting of straight-chain or branched alkyl, alkylthio, alkylsulphonyl, alkoxy and alkoxycarbonyl each having up to 10 carbon atoms, which may in turn be substituted by hydroxyl, alkoxy having up to 6 carbon atoms, phenyl or by a group of the formula --NR1 R2, or by aryl, aryloxy, arylthio or arylsulphonyl having 6 to 10 carbon atoms, or by halogen, nitro, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, benzyloxy or a group of the formula --NR1 R2,B represents straight-chain or branched alkyl having up to 12 carbon atoms, which is optionally substituted by halogen, cyano, azido, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, trifluoromethylsulphonyl, alkoxy having up to 10 carbon atoms, aryl, aryloxy or arylthio having 6 to 10 carbon atoms where the aryl radicals are optionally be monosubstituted to trisubstituted by identical or different substituents from the group consisting of halogen, cyano, trifluoromethyl, trifluoromethoxy, straight-chain or branched alkyl, alkoxy, alkylthio and alkylsulphonyl each having up to 8 carbon atoms, or by a group of the formula --NR1 R2 or --COR3,in whichR1 and R2 are identical or different anddenote hydrogen, aryl or arylsulphonyl having 6 to 10 carbon atoms, straight-chain or branched alkyl or alkylsulphonyl having up to 8 carbon atoms, where said straight chain or branched alkyl or alkylsulphonyl radicals are optionally substituted by aryl having 6 to 10 carbon atoms,denote a group of the formula --COR3 in whichR3 denotes straight chain or branched alkyl or alkoxy having up to 8 carbon atoms or phenyl,represents aryl having 6 to 10 carbon atoms ,which is optionally monosubstituted to trisubstituted by identical or different substituents form the group consisting of halogen, cyano, nitro, trifluoromethyl, straight-chain or branched alkyl, alkoxy and alkoxycarbonyl each having up to 8 carbon atoms or amino,represents cycloalkyl having 3 to 8 carbon atoms, orrepresents straight-chain or branched alky or alkenyl each having up to 12 carbon atoms and optionally substituted by aryl having 6 to 12 carbon atoms or by hydroxyl,D and E are identical or different and represent a group of the formula --NR1 R2, --OR4 or --COR5,in whichR4 denotes hydrogen ordenotes straight-chain or branched alkyl having up to 10 carbon atoms, which is optionally substituted by hydroxyl, trialkylsilyl having up to 10 carbon atoms in the entire alkyl moiety, halogen or aryl having 6 to 10 carbon atoms, which may in turn be substituted by halogen, cyano, nitro, hydroxyl, straight-chain or branched alkyl, alkoxy or alkoxycarbonyl each having up to 8 carbon atoms or amino,denotes trialkylsilyl having up to 10 carbon atoms in the entire alkyl moiety,denotes cycloalkyl having 3 to 8 carbon atoms or aryl having 6 to 10 carbon atoms, optionally substituted by halogen, cyano, nitro or amino, ordenotes a group of the formula --COR7, in whichR7 --denotes straight-chain or branched alkyl having up to 8 carbon atoms aryl having 6 to 10 carbon atoms or the --NR1 R2 group,R5 denotes hydrogen or straight-chain or branched alkyl having up to 10 carbon atoms, which is optionally substituted by hydroxyl, phenyl, halogen or cyano,denotes aryl having 6 to 10 carbon atoms optionally substituted by halogen, amino, hydroxyl, nitro or cyano, ordenotes a group of the formula --NR1 R2 or --OR4,G represents an oxygen or sulphus atom, andR10 represents alkyl having one to three carbon atoms.
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Abstract
For inhibiting HMG-CoA reductase and cholesterol synthesis, the novel 2-pyridones and pyrid-2-thiones of the formula ##STR1## in which A is optionally substituted aryl or heterocyclic,
B is optionally substituted alkyl, cycloalkyl or aryl,
D and E independently are optionally substituted aryl or heterocyclic, H, nitro, cyano, optionally substituted alkyl, alkenyl or imino, amino, alkoxy or acyl, or forms a ring with B,
G is O or S,
X is --CH2 --CH2 -- or --CH═CH--, and
R represents a group of the formula ##STR2## and salts thereof.
9 Citations
2 Claims
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1. A ketone of the formula ##STR75## in which A represents aryl having 6 to 10 carbon atoms, which is optionally monosubstituted to pentasubstituted by identical or different substituents from the group consisting of straight-chain or branched alkyl, alkylthio, alkylsulphonyl, alkoxy and alkoxycarbonyl each having up to 10 carbon atoms, which may in turn be substituted by hydroxyl, alkoxy having up to 6 carbon atoms, phenyl or by a group of the formula --NR1 R2, or by aryl, aryloxy, arylthio or arylsulphonyl having 6 to 10 carbon atoms, or by halogen, nitro, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, benzyloxy or a group of the formula --NR1 R2,
B represents straight-chain or branched alkyl having up to 12 carbon atoms, which is optionally substituted by halogen, cyano, azido, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, trifluoromethylsulphonyl, alkoxy having up to 10 carbon atoms, aryl, aryloxy or arylthio having 6 to 10 carbon atoms where the aryl radicals are optionally be monosubstituted to trisubstituted by identical or different substituents from the group consisting of halogen, cyano, trifluoromethyl, trifluoromethoxy, straight-chain or branched alkyl, alkoxy, alkylthio and alkylsulphonyl each having up to 8 carbon atoms, or by a group of the formula --NR1 R2 or --COR3, in which R1 and R2 are identical or different and denote hydrogen, aryl or arylsulphonyl having 6 to 10 carbon atoms, straight-chain or branched alkyl or alkylsulphonyl having up to 8 carbon atoms, where said straight chain or branched alkyl or alkylsulphonyl radicals are optionally substituted by aryl having 6 to 10 carbon atoms, denote a group of the formula --COR3 in which R3 denotes straight chain or branched alkyl or alkoxy having up to 8 carbon atoms or phenyl, represents aryl having 6 to 10 carbon atoms ,which is optionally monosubstituted to trisubstituted by identical or different substituents form the group consisting of halogen, cyano, nitro, trifluoromethyl, straight-chain or branched alkyl, alkoxy and alkoxycarbonyl each having up to 8 carbon atoms or amino, represents cycloalkyl having 3 to 8 carbon atoms, or represents straight-chain or branched alky or alkenyl each having up to 12 carbon atoms and optionally substituted by aryl having 6 to 12 carbon atoms or by hydroxyl, D and E are identical or different and represent a group of the formula --NR1 R2, --OR4 or --COR5, in which R4 denotes hydrogen or denotes straight-chain or branched alkyl having up to 10 carbon atoms, which is optionally substituted by hydroxyl, trialkylsilyl having up to 10 carbon atoms in the entire alkyl moiety, halogen or aryl having 6 to 10 carbon atoms, which may in turn be substituted by halogen, cyano, nitro, hydroxyl, straight-chain or branched alkyl, alkoxy or alkoxycarbonyl each having up to 8 carbon atoms or amino, denotes trialkylsilyl having up to 10 carbon atoms in the entire alkyl moiety, denotes cycloalkyl having 3 to 8 carbon atoms or aryl having 6 to 10 carbon atoms, optionally substituted by halogen, cyano, nitro or amino, or denotes a group of the formula --COR7, in which R7 --denotes straight-chain or branched alkyl having up to 8 carbon atoms aryl having 6 to 10 carbon atoms or the --NR1 R2 group, R5 denotes hydrogen or straight-chain or branched alkyl having up to 10 carbon atoms, which is optionally substituted by hydroxyl, phenyl, halogen or cyano, denotes aryl having 6 to 10 carbon atoms optionally substituted by halogen, amino, hydroxyl, nitro or cyano, or denotes a group of the formula --NR1 R2 or --OR4, G represents an oxygen or sulphus atom, and R10 represents alkyl having one to three carbon atoms.
Specification
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- Resources
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Current AssigneeBayer AG
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Original AssigneeBayer AG
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InventorsBischoff, Hilmar, Schmidt, Delf, Hubsch, Walter, Fey, Peter, Angerbauer, Rolf, Philipps, Thomas, Petzinna, Dieter, Thomas, Gunter
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Primary Examiner(s)Ivy, C. Warren
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Assistant Examiner(s)NORTHINGTON DAVIS, ZINNA
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Application NumberUS07/673,697Time in Patent Office578 DaysField of Search546/14, 546/208, 546/302, 546/296, 546/297, 546/298, 546/299US Class Current546/296CPC Class CodesC07D 211/90 Carbon atoms having three b...C07D 213/64 attached in position 2 or 6C07D 213/70 Sulfur atomsC07F 7/1804 Compounds having Si-O-C lin...
