Combination of AMPA Receptor Antagonists and Acetylcholinesterase Inhibitors for the Treatment of Neuropathic Pain
    1.
    发明申请
    Combination of AMPA Receptor Antagonists and Acetylcholinesterase Inhibitors for the Treatment of Neuropathic Pain 审中-公开
    AMPA受体拮抗剂和乙酰胆碱酯酶抑制剂联合治疗神经性疼痛

    公开(公告)号:US20100168174A1

    公开(公告)日:2010-07-01

    申请号:US12663550

    申请日:2008-07-11

    申请人: Takahisa Hanada

    发明人: Takahisa Hanada

    IPC分类号: A61K31/444 A61P25/00

    摘要: The invention provides methods for treating and/or preventing neuropathic pain by administering to patients in need thereof therapeutically effective amounts of AMPA receptor antagonists; and cholinesterase inhibitors and/or anti-neuropathic pain agents. The neuropathic pain may be painful diabetic neuropathy. The invention also provides kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists; and cholinesterase inhibitors and/or anti-neuropathic pain agents. The AMPA receptor antagonists may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. The cholinesterase inhibitor may be, for example, 1-benzyl-4-((5,6-dimethoxy-1-indanon)-2-yl)methylpiperidine (donepezil).

    摘要翻译: 本发明提供了治疗和/或预防神经性疼痛的方法,其通过对有需要的患者施用治疗有效量的AMPA受体拮抗剂; 和胆碱酯酶抑制剂和/或抗神经性疼痛剂。 神经性疼痛可能是疼痛的糖尿病性神经病变。 本发明还提供试剂盒和包含治疗有效量的AMPA受体拮抗剂的药物组合物; 和胆碱酯酶抑制剂和/或抗神经性疼痛剂。 AMPA受体拮抗剂可以是例如3-(2-氰基苯基)-5-(2-吡啶基)-1-苯基-1,2-二氢吡啶-2-酮。 胆碱酯酶抑制剂可以是例如1-苄基-4 - ((5,6-二甲氧基-1-茚满酮)-2-基)甲基哌啶(多奈哌齐)。

    AMPA Receptor Antagonists and Zonisamide for Neuropathic Pain
    2.
    发明申请
    AMPA Receptor Antagonists and Zonisamide for Neuropathic Pain 审中-公开
    AMPA受体拮抗剂和唑尼沙胺用于神经性疼痛

    公开(公告)号:US20100179193A1

    公开(公告)日:2010-07-15

    申请号:US12663559

    申请日:2008-07-11

    申请人: Takahisa Hanada

    发明人: Takahisa Hanada

    IPC分类号: A61K31/444 A61P25/02

    摘要: The invention provides methods for treating and/or preventing neuropathic pain by administering to patients therapeutically effective amounts of AMPA receptor antagonists and zonisamide. The neuropathic pain may be diabetic neuropathy. The invention also provides kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists and zonisamide. The AMPA receptor antagonist may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydropyridin-2-one.

    摘要翻译: 本发明提供了通过向患者施用治疗有效量的AMPA受体拮抗剂和唑尼沙胺来治疗和/或预防神经性疼痛的方法。 神经性疼痛可能是糖尿病性神经病变。 本发明还提供试剂盒和包含治疗有效量的AMPA受体拮抗剂和唑尼沙胺的药物组合物。 AMPA受体拮抗剂可以是例如3-(2-氰基苯基)-5-(2-吡啶基)-1-苯基-1,2-二氢吡啶-2-酮。

    AMPA and NMDA Receptor Antagonists for Neurodegenerative Diseases
    4.
    发明申请
    AMPA and NMDA Receptor Antagonists for Neurodegenerative Diseases 审中-公开
    AMPA和NMDA受体拮抗剂用于神经退行性疾病

    公开(公告)号:US20100099714A1

    公开(公告)日:2010-04-22

    申请号:US12528377

    申请日:2008-03-05

    摘要: The invention provides methods for treating, preventing, and delaying the onset of neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis, multiple sclerosis, Pick's disease, and the like), dementia, mild cognitive impairments, glaucoma, ocular hypertension, and pain (e.g., neuropathic pain, headaches, and the like) by administering therapeutically effective amounts of AMPA receptor antagonists and NMDA receptor antagonists to patents in need thereof. The invention also provides combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists and NMDA receptor antagonists. Exemplary AMPA receptor antagonists include 1,2-dihydropyridine compounds, such as 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. Exemplary NMDA receptor antagonists include adamantane compounds, such as memantine.

    摘要翻译: 本发明提供了用于治疗,预防和延迟神经变性疾病(例如阿尔茨海默氏病,帕金森病,亨廷顿病,肌萎缩性侧索硬化,多发性硬化症,皮克病等),痴呆,轻度认知障碍,青光眼 ,通过向有需要的专利施用治疗有效量的AMPA受体拮抗剂和NMDA受体拮抗剂来治疗眼睛高血压和疼痛(例如神经性疼痛,头痛等)。 本发明还提供包含治疗有效量的AMPA受体拮抗剂和NMDA受体拮抗剂的组合,试剂盒和药物组合物。 示例性AMPA受体拮抗剂包括1,2-二氢吡啶化合物,例如3-(2-氰基苯基)-5-(2-吡啶基)-1-苯基-1,2-二氢吡啶-2-酮。 示例性的NMDA受体拮抗剂包括金刚烷化合物,例如美金刚。

    Pyridazinone and triazinone compounds and use thereof as pharmaceutical preparations
    5.
    发明申请
    Pyridazinone and triazinone compounds and use thereof as pharmaceutical preparations 审中-公开
    哒嗪酮和三嗪酮化合物及其作为药物制剂的用途

    公开(公告)号:US20060189622A1

    公开(公告)日:2006-08-24

    申请号:US11408078

    申请日:2006-04-21

    摘要: The present invention provides a novel compound exhibiting an excellent inhibitory action on AMPA receptor and/or kainate receptor. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. In the formula, A1, A2 and A3 are independent of each other and each represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a 5- to 14-membered non-aromatic heterocyclic group, a C6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may be substituted; Q represents O, S or NH; Z represents C or N; X1, X2 and X3 are independent of each other and each represents a single bond, an optionally substituted C1-6 alkylene group, an optionally substituted C2-6 alkenylene group, an optionally substituted C2-6 alkynylene group, —NH—, —O—, —NHCO—, —CONH—, —SO0-2—, etc.; R1 and R2 are independent of each other and each represents a hydrogen atom or an optionally substituted C1-6 alkyl group, or R1 and R2 may be bound together such that CR2-ZR1 forms C═C; and R3 represents a hydrogen atom or an optionally substituted C1-6 alkyl group etc., or may be bound to any atom in A1 or A3 to form, together with the atom, an optionally substituted C5-8 hydrocarbon ring or an optionally substituted 5- to 8-membered heterocyclic ring.

    摘要翻译: 本发明提供了对AMPA受体和/或红藻氨酸受体具有优异抑制作用的新化合物。 也就是说,它提供由下式表示的化合物,其盐或它们的水合物。 在该式中,A 1,A 2和A 3彼此独立,并且各自表示C 3-8, 环烷基,C 3-8环烯基,5至14元非芳族杂环基,C 6-14芳族烃环基 或5〜14元芳族杂环基,其各自可以被取代; Q表示O,S或NH; Z表示C或N; X 1,X 2和X 3 3彼此独立,各自表示单键,任选取代的C 1〜 6个亚烷基,任选取代的C 2-6亚烯基,任选取代的C 2-6亚炔基,-NH-,-O-, -NHCO - , - CONH - , - SO 2 - 等; R 1和R 2彼此独立,各自表示氢原子或任选取代的C 1-6烷基,或R 可以将“1”和“R”2结合在一起,使得CR 2 -ZR 1'形成CC; 和R 3表示氢原子或任选取代的C 1-6烷基等,或者可以与A 1〜O 2中的任何原子结合 >或A <3>,以与原子一起形成任选取代的C 5 -C 8烃环或任选取代的5至8元杂环。

    AMPA RECEPTOR ANTAGONISTS AND ZONISAMIDE FOR EPILEPSY
    8.
    发明申请
    AMPA RECEPTOR ANTAGONISTS AND ZONISAMIDE FOR EPILEPSY 审中-公开
    AMPA受体拮抗剂和紫杉烷

    公开(公告)号:US20100256191A1

    公开(公告)日:2010-10-07

    申请号:US12744444

    申请日:2008-12-26

    摘要: The invention provides methods for treating epilepsy by administering to patients therapeutically effective amounts of AMPA receptor antagonists in combination with zonisamide useful for treating epilepsy. The invention also provides pharmaceutical combinations, kits, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists, and optionally, zonisamide that are useful for treating epilepsy.

    摘要翻译: 本发明提供了通过向患者施用治疗有效量的AMPA受体拮抗剂与用于治疗癫痫的唑尼沙胺组合来治疗癫痫的方法。 本发明还提供药物组合,试剂盒和药物组合物,其包含治疗有效量的AMPA受体拮抗剂和任选的可用于治疗癫痫的唑尼沙胺。