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    Novel use of 5-phenyl-2-furan esters, amides and ketones as neuroprotective agents
    2.
    发明公开
    Novel use of 5-phenyl-2-furan esters, amides and ketones as neuroprotective agents 失效
    作为神经保护剂的5-苯基-2-呋喃酯，氨基酸和酮类的新用途

    公开(公告)号：EP0404233A3

    公开(公告)日：1992-01-08

    申请号：EP90201540.3

    申请日：1990-06-14

    申请人： Norwich Eaton Pharmaceuticals, Inc.

    发明人： Drust, Eugene George

    IPC分类号： A61K31/34 ,  A61K31/495

    CPC分类号： A61K31/495 ,  A61K31/34

    摘要： The present invention encompasses methods of using 5-phenyl-­2-furan esters, amides and ketones and compositions thereof to prevent or limit neuronal death or degeneration in a human or lower animal. These methods comprise systemically administering to such human or other animal a safe and effective amount of a compound of the formula:
    wherein
    (1) X is halo or nil; and Y is a substituent selected from the group consisting of unsubstituted or halogen-substituted methyl, halo, nitro, amino, and methoxy; and (2) R is R¹C(O)OH, R¹C(O)N(R³)₂, N(R³)₂, OR¹N(R³)₂, R¹N(R³)₂, N(R²)R¹N(R³)₂, or N(R²)N(R³)₂; where
    R¹ is C₁-C₃ alkyl which is unsubstituted or substituted with C₁-C₂ alkyl;
    R² is hydrogen or lower alkyl; and
    each R³ is, independently, hydrogen or lower alkyl; or both R³ groups are connected to form a saturated 5- or 6-membered heterocycle containing 1 or 2 heteroatoms selected from oxygen and nitrogen, and said heterocycle is unsubstituted or substituted with lower alkyl or hydroxy-substituted lower alkyl; or a pharmaceutically acceptable salt thereof.

    Dual-action tablet
    5.
    发明公开
    Dual-action tablet 失效
    双作用片

    公开(公告)号：EP0384514A3

    公开(公告)日：1991-04-03

    申请号：EP90200313.6

    申请日：1990-02-12

    申请人： Norwich Eaton Pharmaceuticals, Inc.

    发明人： Dansereau, Richard John ,  Kane, Michael John

    IPC分类号： A61K9/24

    CPC分类号： A61K9/209

    摘要： The present invention provides a dual-action tablet composi­tion comprising:
    (a) an outer tablet comprising a first dose of active ingredient dispersed in a pH independent hydrophilic polymer matrix; and (b) an inner tablet comprising a second dose of active ingredient in a rapidly disintegrating excipient base. This dual-action tablet is especially efficacious for those active ingredients which half lives of less than two hours and which experience decreased absorption efficiency in the lower gastrointestinal tract. Among the preferred dual-action tablet composition is one wherein the active ingredient in both the inner and outer tablets is guaifenesin. Upon administration, the outer tablet provides a controlled release of the active ingredient while the inner tablet gives a second dose of active ingredient after the outer tablet has partially dissolved.

    Liquid suspensions of nitrofurantoin
    6.
    发明公开
    Liquid suspensions of nitrofurantoin 失效
    Flüssige呋喃丹因子悬浮液。

    公开(公告)号：EP0410517A1

    公开(公告)日：1991-01-30

    申请号：EP90201966.0

    申请日：1990-07-18

    申请人： Norwich Eaton Pharmaceuticals, Inc.

    发明人： McGowan, Margaret Anne ,  Shahi, Vijay ,  Kane, Michael John

    IPC分类号： A61K31/415

    CPC分类号： A61K9/0095 ,  A61K31/4178

    摘要： Compositions, for the administration of nitrofurantoin to a human or other animal, comprising:
    (a) a safe and effective amount of nitrofurantoin particulates having a surface consisting of nitrofurantoin monohydrate, wherein said particulates have a mean particle size greater than about 200 mesh size;
    (b) nitrofurantoin monohydrate;
    (c) an effective amount of suspending agent; and
    (d) water;
    wherein the pH of said composition is from about 1 to about 6; and said nitrofurantoin monohydrate is dissolved in said water at saturation level. The nitrofurantoin of this invention are highly efficacious for the oral delivery of nitrofurantoin.

    摘要翻译： 用于向人或其他动物施用呋喃妥因的组合物，其包含：（a）安全有效量的具有由呋喃妥因一水合物组成的表面的呋喃妥因颗粒，其中所述颗粒具有大于约200目尺寸的平均粒度; （b）呋喃妥因一水合物; （c）有效量的悬浮剂; 和（d）水; 其中所述组合物的pH为约1至约6; 并且所述呋喃妥因一水合物在饱和水平下溶解在所述水中。 本发明的呋喃妥因对于口服输送呋喃妥因是非常有效的。

    Compositions for the transdermal delivery of buprenorphine salts
    7.
    发明公开
    Compositions for the transdermal delivery of buprenorphine salts 失效
    用于快速递送布地尼泮盐的组合物

    公开(公告)号：EP0368409A3

    公开(公告)日：1990-12-19

    申请号：EP89202799.6

    申请日：1989-11-07

    申请人： Norwich Eaton Pharmaceuticals, Inc.

    发明人： Szuktak, Joan Bolduc ,  Manring, Gary Lee ,  Smith, Ronald Lee ,  Drust, Eugene George

    IPC分类号： A61K31/485 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

    CPC分类号： A61K9/7084 ,  A61K9/0014 ,  A61K31/485 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

    摘要： Compositions for the transdermal delivery of buprenorphine salts comprising a safe and effective amount of a pharmaceutically-acceptable buprenorphine salt in a carrier comprising:
    (a) a polar solvent material selected from the group consist­ing of C₃-C₄ diols, C₃-C₆ triols, and mixtures thereof; and (b) a polar lipid material selected from the group consisting of fatty acids, fatty alcohols, fatty alcohol esters, fatty acid esters, and mixtures thereof; wherein said polar solvent material and said polar lipid material are present in a weight ratio of solvent material:lipid material of from about 60:40 to about 99:1. Preferably, the polar solvent material is propylene glycol, and the polar lipid material is a C₁₂- C₁₈ fatty alcohol, a C₁₂-C₁₈ fatty acid, or an ester of a C₈-C₁₂ fatty alcohol or fatty acid. Particularly preferred polar lipid materials include oleic acid, lauryl alcohol, methyl laurate and methyl caprylate. The ratio of polar solvent material to polar lipld material is preferably from about 90:10 to about 98:2.