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    COMPOUNDS AND METHODS FOR LOWERING THE ABUSE POTENTIAL AND EXTENDING THE DURATION OF ACTION OF A DRUG
    2.
    发明申请
    COMPOUNDS AND METHODS FOR LOWERING THE ABUSE POTENTIAL AND EXTENDING THE DURATION OF ACTION OF A DRUG 审中-公开
    降低滥用潜力并延长药物持续时间的化合物和方法

    公开(公告)号：US20070203165A1

    公开(公告)日：2007-08-30

    申请号：US11742566

    申请日：2007-04-30

    申请人： Jules Shafer ,  Vladislav Telyatnikov ,  Zhiwei Guo

    发明人： Jules Shafer ,  Vladislav Telyatnikov ,  Zhiwei Guo

    IPC分类号： A61K31/485 ,  C07D489/02

    CPC分类号： C07D489/08 ,  A61K47/555 ,  A61K47/60

    摘要： The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.

    摘要翻译： 降低生物可利用药物如鸦片止痛剂的滥用潜力，并且通过在制剂前将其转化为不良吸收的酯前药或其它前药衍生物来延长其作用时间。 与活性药物的许多现有持续释放制剂不同，其中通过咀嚼，破碎或以其它方式破坏含有活性药剂的片剂或胶囊珠可以释放活性药剂，这种包含本发明前药的片剂或胶囊珠粒的机械加工 既不释放活性药物也不妥协药物对药物的受控转化。 此外，含有本发明前药或其他药物的片剂和胶囊珠可以用足量的增稠剂如羟丙基甲基纤维素或羧甲基纤维素配制，以阻止对这些给药模式未注明的制剂的不适当的静脉内和鼻内施用。

    Method for treating inflammatory diseases by administering a thrombin inhibitor
    5.
    发明授权
    Method for treating inflammatory diseases by administering a thrombin inhibitor 失效
    通过施用凝血酶抑制剂治疗炎性疾病的方法

    公开(公告)号：US06232315B1

    公开(公告)日：2001-05-15

    申请号：US09407821

    申请日：1999-09-28

    申请人： Jules Shafer ,  Denise M. Visco

    发明人： Jules Shafer ,  Denise M. Visco

    IPC分类号： A61K31341

    CPC分类号： A61K31/497 ,  A61K31/00 ,  A61K31/341 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/444 ,  A61K31/445 ,  A61K31/454 ,  A61K31/495 ,  A61K2300/00

    摘要： The invention is a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor. Such diseases include but are not limited to nephritis, systemic lupus erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. In one class of the method, the thrombin inhibitor is selected from the group consisting of 3-(2-phenylethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyrazinone, N′-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]-N-(3,3-diphenylpropionyl)-L-proline amide, and 3-(2-phenethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyridinone or a pharmaceutically acceptable salt thereof. The invention is also a method for treating an inflammatory disease in a patient which comprises treating the patient with a composition comprising a thrombin inhibitor and an NSAID, e.g., a COX-2 inhibitor. Such diseases include but are not limited to nephritis, systemic lupus, erythematosus, rheumatoid arthritis, glomerulonephritis, and sacoidosis. In one class of the method, the thrombin inhibitor is selected from the group consisting of 3-(2-phenylethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylene-carboxamidomethylpyridinyl)-2-pyrazinone, N′-[[1-(aminoiminomethyl)-4-piperidinyl]methyl]-N-(3,3-diphenylpropionyl)-L-proline amide, and 3-(2-phenethylamino)-6-methyl-1-(2-amino-6-methyl-5-methylenecarboxamidomethylpyridinyl)-2-pyridinone or a pharmaceutically acceptable salt thereof and the COX-2 inhibitor is 3-phenyl-4-(4-(methylsulfonyl)phenyl)-2-(5H)-furanone or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明是治疗患者炎性疾病的方法，其包括用包含凝血酶抑制剂的组合物治疗患者。 这些疾病包括但不限于肾炎，系统性红斑狼疮，类风湿性关节炎，肾小球性肾炎和囊状病。 在一类方法中，凝血酶抑制剂选自3-（2-苯乙基氨基）-6-甲基-1-（2-氨基-6-甲基-5-亚甲基甲酰胺甲基吡啶基）-2-吡嗪酮，N ' - [[1-（氨基亚氨基甲基）-4-哌啶基]甲基] -N-（3,3-二苯基丙酰基）-L-脯氨酸酰胺和3-（2-苯乙基氨基）-6-甲基-1-（2- 氨基-6-甲基-5-亚甲基甲酰胺甲基吡啶基）-2-吡啶酮或其药学上可接受的盐。本发明还是一种治疗患者炎症性疾病的方法，其包括用包含凝血酶抑制剂和NSAID的组合物治疗患者 ，例如COX-2抑制剂。 这些疾病包括但不限于肾炎，系统性红斑狼疮，红斑狼疮，类风湿性关节炎，肾小球性肾炎和囊性疾病。 在一类方法中，凝血酶抑制剂选自3-（2-苯乙基氨基）-6-甲基-1-（2-氨基-6-甲基-5-亚甲基 - 甲酰胺基甲基吡啶基）-2-吡嗪酮 ，N' - [[1-（氨基亚氨基甲基）-4-哌啶基]甲基] -N-（3,3-二苯基丙酰基）-L-脯氨酰胺和3-（2-苯乙基氨基）-6-甲基-1-（ 2-氨基-6-甲基-5-亚甲基甲酰胺甲基吡啶基）-2-吡啶酮或其药学上可接受的盐，COX-2抑制剂是3-苯基-4-（4-（甲基磺酰基）苯基）-2-（5H） - 呋喃酮或其药学上可接受的盐。