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    • 1. 发明申请
    • SUBSTITUTED BENZODIAZEPINONES, BENZOXAZEPINONES AND BENZOTHIAZEPINONES AS SODIUM CHANNEL BLOCKERS
    • 作为钠通道阻断剂的取代苯并恶嗪酮,苯并恶唑酮和苯并噻唑酮
    • WO2008106077A1
    • 2008-09-04
    • PCT/US2008/002441
    • 2008-02-25
    • MERCK & CO., INC.HOYT, Scott, B.OK, DongOK, Hyun, O.LONDON, ClareDUFFY, Joseph, L.
    • HOYT, Scott, B.OK, DongOK, Hyun, O.LONDON, ClareDUFFY, Joseph, L.
    • A01N43/62A61K31/55
    • C07D281/10C07D245/06C07D267/14
    • The present invention is directed to substituted benzodiazepinones, benzoxazepinones and benzothiazepinones compounds that are sodium channel blockers useful for the treatment of chronic and neuropathic pain. The compounds of the present invention are also useful for the treatment of other conditions, including disorders of the CNS such as anxiety, depression, epilepsy, manic depression and bipolar disorder. This invention also provides pharmaceutical compositions comprising a compound of the present invention, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. This invention further comprises methods for the treatment of acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain and disorders of the CNS including, but not limited to, epilepsy, manic depression, depression, anxiety and bipolar disorder comprising administering the compounds and pharmaceutical compositions of the present invention.
    • 本发明涉及用作治疗慢性和神经性疼痛的钠通道阻滞剂的取代苯并二氮杂酮,苯并氧氮杂酮和苯并噻唑酮化合物。 本发明的化合物还可用于治疗其他病症,包括CNS的疾病如焦虑症,抑郁症,癫痫症,躁狂抑郁症和双相性精神障碍。 本发明还提供包含单独的或与一种或多种治疗活性化合物组合的本发明化合物和药学上可接受的载体的药物组合物。 本发明还包括用于治疗急性疼痛,慢性疼痛,内脏痛,炎性疼痛,神经性疼痛和中枢神经系统疾病的方法,包括但不限于癫痫症,躁狂抑郁症,抑郁症,焦虑和双相情感障碍,包括给予化合物 和本发明的药物组合物。
    • 5. 发明申请
    • BENZAZEPINONES AS SODIUM CHANNEL BLOCKERS
    • 苯并噻吩作为钠通道阻断剂
    • WO2007145922A3
    • 2008-08-21
    • PCT/US2007013202
    • 2007-06-05
    • MERCK & CO INCHOYT SCOTT BLONDON CLAREOK DONGPARSONS WILLIAM H
    • HOYT SCOTT BLONDON CLAREOK DONGPARSONS WILLIAM H
    • C07D223/16A61K31/55A61P29/00A61P29/02
    • C07D223/16C07D401/12C07D403/12C07D409/12C07D413/12
    • Benzazepinone 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, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, 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.
    • 由式(I)表示的苯并氮杂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症状的方法,包括例如急性疼痛,慢性疼痛,内脏痛,炎性疼痛,神经性疼痛,癫痫,肠易激综合征,尿失禁,瘙痒,瘙痒,过敏性皮炎 抑郁,焦虑,多发性硬化和双相性精神障碍,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一起施用有效量的本发明化合物。
    • 6. 发明申请
    • BENZAZEPINONES AS SODIUM CHANNEL BLOCKERS
    • 苯并噻吩作为钠通道阻断剂
    • WO2007145922A2
    • 2007-12-21
    • PCT/US2007/013202
    • 2007-06-05
    • MERCK & CO., INC.HOYT, Scott, B.LONDON, ClareOK, DongPARSONS, William, H.
    • HOYT, Scott, B.LONDON, ClareOK, DongPARSONS, William, H.
    • A61K31/55
    • C07D223/16C07D401/12C07D403/12C07D409/12C07D413/12
    • Benzazepinone 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, epilepsy, irritable bowel syndrome, urinary incontinence, pruritis, itchiness, allergic dermatitis, 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.
    • 由式(I)表示的苯并氮杂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症状的方法,包括例如急性疼痛,慢性疼痛,内脏痛,炎性疼痛,神经性疼痛,癫痫,肠易激综合征,尿失禁,瘙痒,瘙痒,过敏性皮炎 抑郁,焦虑,多发性硬化和双相性精神障碍,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一起施用有效量的本发明化合物。