摘要:
The disclosed invention is compounds represented by the formula and pharmaceutically acceptable acid addition, basic addition and quarternary amine salts thereof and pharmaceutically acceptable solvates thereof, wherein each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl: substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, loweralkylsulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl. phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl, hydroxyiminoloweralkyl hydroxyloweralkyl or carbonyl; or 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining member of the ring being at least one carbon, and optionally sulfur or oxygen, wherein the substituents are one or more of carboxyl, hydroxymethyl, lower alkyl, loweralkylcarbonyl or aryl lower alkyl; X and Y are each independently a bond, -0-,
each Q is independently a divalent substituted or unsubstituted, straight or branched chain lower alkanediyl. lower alkanediyl-cycloalkanediyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofurandiyl, loweralkanediyl-dihydrofurandiyl-loweralkanediyl, tetrahydrofurandiyl, tetrahydropyrandiyl, loweralkanediyl- tetrahydropyrandlyl-loweralkanediyl or, loweralkanediyl-tetrahydrofurandiyl-loweralkanediyl, wherein the substituents are one or more of hydroxy, ketalized adjacent hydroxys, epoxy, fluorine, chlorine, azide, or amino; W is a monovalent substituted or unsubstituted aryl group or a heterocyclic single or fused ring containing from 4 to 10 ring atoms, at least one hetero atom of which is a nitrogen atom and the remaining ring atoms being at least one carbon and optionally sulfur or oxygen, wherein the substituents are one or more of hydroxy, oxo amino, carbamoyl, carboxyl, nitrile, nitro, lower alkoxy carbonyl, halogen, sulfamyl, lower alkyl, lower alkylthio, lower alkoxy, hydroxyloweralkyl, lower alkoxycarbonylloweralkyl, amino loweralkyl, carboxyloweralkyl, guanidino, thioureido, lower alkylsulfonylamino, aminocarbonylloweralkyl, allyloxycarbonylmethyl or carbamoyloxyloweralkyl; with the proviso that W cannot be substituted or unsubstituted isoxazolyl, andwith the further proviso that when Z is 2-chloro-4-methoxyphenyl, X is -0-, Q is C s -C 1 alkanediyl and Y is a bond, W is not imidazolyl substituted at position 2, 4 and 5 with 1-3 substituents independently selected from the group consisting of hydrogen, hydroxyloweralkyl, nitro, loweralkoxycarbonyl, lower alkyl and amino methylene; W' is divalent W. The compounds have antiviral activity, antiinflammatory activity and are PAF inhibitors.
摘要:
The present invention relates to hydantoin derivatives, represented by the formula (I): and non-toxic salts, solvates and solvates of non-toxic salts thereof; wherein q represents a mono- or a fused heterocyclic group which may be substituted by one or more substituents which are same or different and selected from a group consisting of a halogen atom, an alkyl group, a nitro group, a cyano group, an optionally protected carboxy group, an optionally protected carboxymethyl group, a halogenated alkyl group, an alkylthio group, an alkylcarbonyl group, an alkoxy group, an alkylsulfinyl group, an alkylsulfonyl group, an optionally protected hydroxy group, an optionally protected amino group, a carbamoyl group and a phenyl group, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and intermediate compounds in the synthesis of said hydantoin derivatives.
摘要:
The present invention relates to hydantoin derivatives, represented by the formula (I): and non-toxic salts, solvates and solvates of non-toxic salts thereof; wherein q represents a mono- or a fused heterocyclic group which may be substituted by one or more substituents which are same or different and selected from a group consisting of a halogen atom, an alkyl group, a nitro group, a cyano group, an optionally protected carboxy group, an optionally protected carboxymethyl group, a halogenated alkyl group, an alkylthio group, an alkylcarbonyl group, an alkoxy group, an alkylsulfinyl group, an alkylsulfonyl group, an optionally protected hydroxy group, an optionally protected amino group, a carbamoyl group and a phenyl group, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and intermediate compounds in the synthesis of said hydantoin derivatives.
摘要:
Disclosed are novel imidazole derivatives having the formula: wherein R 1 and R 2 are H, alkyl, cycloalkyl, aryl, aralkyl or halogen-substituted alkyl, or R 1 and R 2 are combined to form a heterocyclic ring; R 3 , R 4 , R 5 and R 6 are H, halogen, alkoxy, aralkyloxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, or fluorine substituted-alkoxy, or R 3 is combined with R 2 to form a heterocyclic ring; R 8 and R 9 are H, halogen, alkoxy, alkyl, alkoxycarbonyl, nitro, amino, acyl, fluorine substituted-alkyl, fluorine substituted-alkoxy, or aryl group which may have a substitutent, or R 8 and R 9 are combined to form an alicyclic ring; R 7 is, where R 8 and R 9 are not combined, H, and, where R 8 and R 9 are combined, H, alkyl which may have a substitutent, aryl which may have a substitutent, arylcarbonyl which may have a substitutent, or a sulfur-containing heterocyclic group; and n is 0 or 1. The new imidazole derivatives are effective particularly as anti-ulcer agents.
摘要翻译:公开了具有下式的新型咪唑衍生物:其中R 1和R 2是H,烷基,环烷基,芳基,芳烷基或卤素取代的烷基,或R 1和R 2相结合的 形成杂环; R 3,R 4,R 5和R 6是H,卤素,烷氧基,芳烷氧基,烷基,烷氧基羰基,硝基,氨基,酰基,氟取代的烷基或氟取代的烷氧基 R 3与R 2结合形成杂环; R 8和R 9是可以具有取代基的H,卤素,烷氧基,烷基,烷氧基羰基,硝基,氨基,酰基,氟取代的烷基,氟取代的烷氧基或芳基,或R 8, 和R 9结合形成脂环族环; R 7是其中R 8和R 9不组合的化合物,其中R 8和R 9结合,H可以具有取代基的烷基,其可以具有 可以具有取代基的取代基芳基羰基或含硫杂环基; 并且n为0或1.新的咪唑衍生物特别用作抗溃疡剂。
摘要:
Compounds represented by general formula (I), [wherein R represents a hydrogen atom, a carboxyl protective group or an anionic charge, Q represents a hydrogen atom, a halogen atom, a hydroxy group, an acetoxy group, a carbamoyloxy group, an azido group, an optionally substituted quaternary ammonio group, or an optionally substituted 5- or 6-membered aromatic heterocyclic thio group containing at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom (additionally, the aromatic hetero ring being optionally bound to a benzene ring or a hetero cyclic ring)], nontoxic salts thereof or nontoxic esters thereof capable of being physiologically hydrolized, process for their preparation, and antibacterial agent containing the compound as an effective ingredient. Further, compounds represented by general formula (III), (wherein R3 represents a hydrogen atom or an amino protective group, and R4 and R5, which may be the same or different, each represents a hydrogen atom or a carboxyl protective group) or their salts and process for their preparation.
摘要:
A silver halide photographic light-sensitive material comprising a support having coated thereon at least one silver halide emulsion layer and a surface protecting layer, said silver halide photographic light-sensitive material comprising photosensitive silver halide grains and internally fogged silver halide grains, said intemally fogged silver halide grains having adsorbed thereon at least one compound represented by the formula (I): wherein X represents -0-, -NH- or -S-, R 1 , R 2 , R 3 and R 4 represent hydrogen atom or a substituent, and at least one of R,, R 2 , R, and R. is substituted or unsubstituted alkyl or aryl group having up to 13 carbon atoms, which is bonded directly or through a divalent linkage group, to the aromatic nucleus.