Renin inhibitors containing phenylalanyl-histidine replacements
    2.
    发明授权
    Renin inhibitors containing phenylalanyl-histidine replacements 失效
    含有苯丙氨酰基 - 组氨酸取代基的肾素抑制剂

    公开(公告)号:US5037807A

    公开(公告)日:1991-08-06

    申请号:US320681

    申请日:1989-03-08

    IPC分类号: C07K5/02

    CPC分类号: C07K5/0207

    摘要: Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving action of renin and have improved bioavailability; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension or congestive heart failure or of establishing renin as a causative factor in these problems which employ the novel peptides.

    摘要翻译: 其包含新型元件的肽,其包含基于底物类比替代肾素抑制肽中的Phe(8)-His(9)序列的新元件,其抑制肾素的底物切割作用并具有改善的生物利用度; 含有这些肾素抑制肽的组合物,任选与其它抗高血压药物组合; 以及在使用新型肽的这些问题中治疗高血压或充血性心力衰竭或建立肾素作为致病因素的方法。

    Renin inhibitors containing phenylalanyl-histidine replacements
    3.
    发明授权
    Renin inhibitors containing phenylalanyl-histidine replacements 失效
    含有苯丙氨酰基 - 组氨酸取代基的肾素抑制剂

    公开(公告)号:US4839357A

    公开(公告)日:1989-06-13

    申请号:US102203

    申请日:1987-10-02

    IPC分类号: C07K5/02

    CPC分类号: C07K5/0207 Y10S530/86

    摘要: Peptides of the formula: ##STR1## which comprise novel elements replacing the Phe(8)-His(9) sequence in renin-inhibitory peptides based on substrate analogy, which inhibit the substrate-cleaving action of renin and have improved bioavailability; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension or congestive heart failure or of establishing renin as a causative factor in these problems which employ the novel peptides.

    摘要翻译: 其包含新型元件的肽,其包含基于底物类比替代肾素抑制肽中的Phe(8)-His(9)序列的新元件,其抑制肾素的底物切割作用并具有改善的生物利用度; 含有这些肾素抑制肽的组合物,任选与其它抗高血压药物组合; 以及在使用新型肽的这些问题中治疗高血压或充血性心力衰竭或建立肾素作为致病因素的方法。

    Substituted Triazoles as Sodium Channel Blockers
    5.
    发明申请
    Substituted Triazoles as Sodium Channel Blockers 审中-公开
    取代三唑作为钠通道阻断剂

    公开(公告)号:US20090074890A1

    公开(公告)日:2009-03-19

    申请号:US10578950

    申请日:2004-11-05

    CPC分类号: C07D249/10 C07D403/10

    摘要: Substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, migraine, headache pain, migraine headache, epilepsy, irritable bowel syndrome, diabetic neuropathy, multiple sclerosis, manic depression and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier (I), (II), (III).

    摘要翻译: 由式I,II或III表示的取代的三唑化合物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的疾病的方法,包括例如急性疼痛,慢性疼痛,内脏痛,炎性疼痛,神经性疼痛,偏头痛,头痛,偏头痛,癫痫,肠易激综合征,糖尿病 神经病,多发性硬化症,躁狂抑郁症和双相性精神障碍,包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体(I),(II),(III) 。

    Biaryl Substituted Pyrazinones as Sodium Channel Blockers
    8.
    发明申请
    Biaryl Substituted Pyrazinones as Sodium Channel Blockers 审中-公开
    二芳基取代的吡嗪酮作为钠通道阻断剂

    公开(公告)号:US20080280873A1

    公开(公告)日:2008-11-13

    申请号:US10594367

    申请日:2005-03-25

    IPC分类号: A61K31/4965 C07D241/24

    摘要: Biaryl substituted pyrazinone compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds. A method of administering local anesthesia comprises administering an effective amount of a compound of the instant invention, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier.

    摘要翻译: 由式I表示的二芳基取代的吡嗪酮化合物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的疾病的方法,包括例如急性疼痛,慢性疼痛,内脏痛,炎性疼痛,神经性疼痛,尿失禁,瘙痒,过敏性皮炎,癫痫,肠易激综合征,抑郁症 ,焦虑,多发性硬化和双相性精神障碍,包括单独或与一种或多种其它治疗活性化合物组合施用有效量的本发明化合物。 施用局部麻醉的方法包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物和药学上可接受的载体组合施用。