Pharmaceutically active compounds
    93.
    发明公开
    Pharmaceutically active compounds 失效
    Pharmazeutisch wirksame Verbindungen。

    公开(公告)号:EP0407217A1

    公开(公告)日:1991-01-09

    申请号:EP90307425.0

    申请日:1990-07-06

    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.

    摘要翻译: 所公开的发明是由式表示的化合物及其药学上可接受的酸加成,碱加成和季胺盐及其药学上可接受的溶剂化物,其中每个Z独立地为丁基,苯基,萘基或金刚烷基; 取代的苯基,其中取代基是卤素,低级烷氧基,苯氧基,腈,硝基,苯基磺酰基,低级烷基磺酰基,恶唑-2-基,低级烷酰基,苯甲酰基,低级烷氧基羰基,低级烷基,低级烷硫基,苯基,苯基氨基硫代羰基, 或低级烷基氨基硫代羰基,羟基亚氨基低级烷基羟基低级烷基或羰基; 或含有至少一个氮的4或6元未取代或取代的杂环,其中剩余的成员为至少一个碳,以及任选的硫或氧,其中取代基是羧基,羟甲基,低级烷基,低级烷基羰基 或芳基低级烷基; X和Y各自独立地是键,-O-,各Q独立地是二价取代或未取代的直链或支链低级烷二基,低级烷二基 - 环烷二基 - 低级烷二基,低级烯二基,低级炔二基,亚苯基,二氢呋喃二基 低级烷二基 - 二氢呋喃二基 - 低级烷二基,四氢呋喃二基,四氢吡喃基,低级烷二基 - 四氢吡喃基 - 低级烷二基或低级烷二基 - 四氢呋喃基 - 低级烷二基,其中取代基是羟基,缩酮化的相邻羟基,环氧基,氟,氯,叠氮化物或氨基中的一个或多个。 W是单价取代或未取代的芳基或含有4至10个环原子的杂环单或稠环,其至少一个杂原子是氮原子,剩余的环原子是至少一个碳和任选的硫或氧 其中取代基是羟基,氧代氨基,氨基甲酰基,羧基,腈,硝基,低级烷氧基羰基,卤素,氨基磺酰基,低级烷基,低级烷硫基,低级烷氧基,羟基低级烷基,低级烷氧羰基低级烷基,氨基低级烷基,羧基低级烷基,胍基 ,硫脲基,低级烷基磺酰基氨基,氨基羰基低级烷基,烯丙氧基羰基甲基或氨基甲酰氧基低级烷基; 条件是W不能是取代或未取代的异恶唑基,另外条件是当Z是2-氯-4-甲氧基苯基时,X是-O-,Q是C5-C7链烷二基,Y是一个键,W不是咪唑基 在第2,4和5位被1-3个独立地选自氢,羟基低级烷基,硝基,低级烷氧基羰基,低级烷基和氨基亚甲基的取代基取代。 W min是二价W.该化合物具有抗病毒活性,抗炎活性,是PAF抑制剂。

    Novel imidazole derivatives
    98.
    发明公开
    Novel imidazole derivatives 失效
    Imidazolderivate,

    公开(公告)号:EP0354788A1

    公开(公告)日:1990-02-14

    申请号:EP89308119.0

    申请日:1989-08-10

    IPC分类号: C07D233/84 C07D235/28

    CPC分类号: C07D235/28 C07D233/84

    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。

    Silver halide photographic light-sensitive materials
    100.
    发明公开
    Silver halide photographic light-sensitive materials 失效
    卤化银照相感光材料

    公开(公告)号:EP0175148A3

    公开(公告)日:1988-10-05

    申请号:EP85110265

    申请日:1985-08-16

    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.

    摘要翻译: 一种卤化银照相感光材料,它包括一个载有至少一个卤化银乳剂层和表面保护层的载体,所述卤化银照相感光材料包括光敏卤化银颗粒和内部雾化的卤化银颗粒,所述内部雾化 其上吸附有至少一种由式(I)表示的化合物的卤化银颗粒:其中X表示-O - , - NH-或-S-,R1,R2,R3和R4表示氢原子或取代基,并且至少 R 1,R 2,R 3和R 4中的一个是取代或未取代的具有至多13个碳原子的直接或通过二价连接基团键合的烷基或芳基。