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    Dihydropyridine compounds and compositions for headaches
    1.
    发明申请
    Dihydropyridine compounds and compositions for headaches 审中-公开
    二氢吡啶化合物和组合物用于头痛

    公开(公告)号：US20060270709A1

    公开(公告)日：2006-11-30

    申请号：US11396555

    申请日：2006-04-04

    申请人： Julian Gray ,  Yoshiharu Yamanishi ,  Nobuyuki Mori ,  Scott Fields

    发明人： Julian Gray ,  Yoshiharu Yamanishi ,  Nobuyuki Mori ,  Scott Fields

    IPC分类号： A61K31/445 ,  A61K31/444

    CPC分类号： A61K31/4412 ,  A61K31/444 ,  A61K31/445 ,  A61K2300/00

    摘要： The invention provides methods for treating and/or preventing cognitive impairments, dementia, or neurodegenerative diseases and disorders (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis) in patients by administering therapeutically effective amounts of an AMPA receptor antagonist (e.g., 1,2-dihydropyridine compounds) and therapeutically effective amounts of nootropics (e.g., cholinesterase inhibitors) to patients. The invention also provides combinations, commercial packages, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists (e.g., 1,2-dihydropyridine compounds) and therapeutically effective amounts nootropics (e.g., cholinesterase inhibitors). The 1,2-dihydropyridine compound may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. The cholinesterase inhibitor may be, for example, donepezil.

    摘要翻译： 本发明提供了通过施用治疗有效量的AMPA受体拮抗剂（例如，治疗和/或预防）的方法来治疗和/或预防患者的认知障碍，痴呆或神经变性疾病和障碍（例如，阿尔茨海默氏病，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化） ，1,2-二氢吡啶化合物）和治疗有效量的益智酸（例如胆碱酯酶抑制剂）给患者。 本发明还提供了包含治疗有效量的AMPA受体拮抗剂（例如1,2-二氢吡啶化合物）和治疗有效量的精神病药（例如胆碱酯酶抑制剂）的组合，商业包装和药物组合物。 1,2-二氢吡啶化合物可以是例如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多奈哌齐。

    Dihydropyridine Compounds for Neurodegenerative Diseases and Dementia
    2.
    发明申请
    Dihydropyridine Compounds for Neurodegenerative Diseases and Dementia 审中-公开
    二氢吡啶化合物用于神经退行性疾病和痴呆

    公开(公告)号：US20090131480A1

    公开(公告)日：2009-05-21

    申请号：US11887729

    申请日：2006-04-04

    申请人： Julian A. Gray ,  Yoshiharu Yamanishi ,  Julian A. Gray ,  Yoshiharu Yamanishi ,  Nobuyuki Mori ,  Scott Fields

    发明人： Julian A. Gray ,  Yoshiharu Yamanishi ,  Julian A. Gray ,  Yoshiharu Yamanishi ,  Nobuyuki Mori ,  Scott Fields

    IPC分类号： A61K31/444 ,  A61P25/28

    CPC分类号： A61K31/4412 ,  A61K31/444 ,  A61K31/445 ,  A61K2300/00

    摘要： The invention provides methods for treating and/or preventing cognitive impairments, dementia, or neurodegenerative diseases and disorders (e.g., Alzheimer's disease, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis) in patients by administering therapeutically effective amounts of an AMPA receptor antagonist (e.g., 1,2-dihydropyridine compounds) and therapeutically effective amounts of nootropics (e.g., cholinesterase inhibitors) to patients. The invention also provides combinations, commercial packages, and pharmaceutical compositions comprising therapeutically effective amounts of AMPA receptor antagonists (e.g., 1,2-dihydropyridine compounds) and therapeutically effective amounts nootropics (e.g., cholinesterase inhibitors). The 1,2-dihydropyridine compound may be, for example, 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one. The cholinesterase inhibitor may be, for example, donepezil.

    摘要翻译： 本发明提供了通过施用治疗有效量的AMPA受体拮抗剂（例如，治疗和/或预防）的方法来治疗和/或预防患者的认知障碍，痴呆或神经变性疾病和障碍（例如，阿尔茨海默氏病，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化） ，1,2-二氢吡啶化合物）和治疗有效量的益智酸（例如胆碱酯酶抑制剂）给患者。 本发明还提供了包含治疗有效量的AMPA受体拮抗剂（例如1,2-二氢吡啶化合物）和治疗有效量的精神病药（例如胆碱酯酶抑制剂）的组合，商业包装和药物组合物。 1,2-二氢吡啶化合物可以是例如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多奈哌齐。

    Dihydropyridine compounds and compositions for headaches
    3.
    发明申请
    Dihydropyridine compounds and compositions for headaches 审中-公开
    二氢吡啶化合物和组合物用于头痛

    公开(公告)号：US20060276510A1

    公开(公告)日：2006-12-07

    申请号：US11396621

    申请日：2006-04-04

    申请人： Susan Abu-Shakra ,  Julian Gray ,  Yoshiharu Yamanishi ,  Nobuyuki Mori

    发明人： Susan Abu-Shakra ,  Julian Gray ,  Yoshiharu Yamanishi ,  Nobuyuki Mori

    IPC分类号： A61K31/444

    CPC分类号： A61K31/4412 ,  A61K31/444 ,  A61K31/445 ,  A61K2300/00

    摘要： The invention provides methods for treating and/or preventing headaches by administering to patients therapeutically effective amounts of 1,2-dihydropyridine compounds, and, optionally, cholinesterase inhibitors and/or anti-migraine agents. The headaches may be primary headaches, such as migraines, or secondary headaches. The invention also provides combinations, commercial packages, and pharmaceutical compositions comprising therapeutically effective amounts of 1,2-dihydropyridine compounds and, optionally, cholinesterase inhibitors and/or anti-migraine agents. The 1,2-dihydropyridine compound 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.

    摘要翻译： 本发明提供了通过向患者施用治疗有效量的1,2-二氢吡啶化合物和任选的胆碱酯酶抑制剂和/或抗偏头痛药物来治疗和/或预防头痛的方法。 头痛可能是原发性头痛，如偏头痛或继发性头痛。 本发明还提供了包含治疗有效量的1,2-二氢吡啶化合物和任选的胆碱酯酶抑制剂和/或抗偏头痛药物的组合，商业包装和药物组合物。 1,2-二氢吡啶化合物可以是例如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。

    Sigma receptor binder containing indanone derivative
    4.
    发明申请
    Sigma receptor binder containing indanone derivative 审中-公开

    公开(公告)号：US20050107432A1

    公开(公告)日：2005-05-19

    申请号：US10500750

    申请日：2003-01-22

    申请人： Yoichi Iimura ,  Takashi Kosasa ,  Yoshiharu Yamanishi

    发明人： Yoichi Iimura ,  Takashi Kosasa ,  Yoshiharu Yamanishi

    IPC分类号： A61K31/445 ,  A61P21/04 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P27/06 ,  A61P43/00 ,  C07D211/32 ,  C07D405/06 ,  A61K31/454

    CPC分类号： C07D405/06 ,  A61K31/445 ,  C07D211/32

    摘要： The present invention provides an indanone derivative and an excellent sigma receptor binding agent comprising an indanone derivative. More specifically, it provides a sigma receptor binding agent comprising an indanone derivative represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate of them. In the formula (I), R1, R2, R3 and R4 are the same as or different from each other and each represents hydrogen atom, a halogen atom, hydroxyl group, nitrile group, a C1-6 alkyl group which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a C1-6 alkoxy group which may be substituted, a cycloalkoxy group having three to eight carbon atoms which may be substituted, an acyl group having one to six carbon atoms which may be substituted, a C1-6 alkoxycarbonyl group which may be substituted, a C1-6 alkylaminocarbonyloxy group which may be substituted, a di(C1-6 alkyl)aminocarbonyloxy group which may be substituted, nitro group, an amino group which may be substituted, an amido group which may be substituted, mercapto group or a thio-C1-6 alkoxy group which may be substituted, and further R1 with R2, R2 with R3, or R3 with R4 may together form an aliphatic ring, an aromatic ring, a heterocyclic ring or an alkylenedioxy ring; the partial structure: represents a group represented by >CH—CH2—, >C═CH— or >C(—R7)—CH2—; m represents an integer of 0 or 1 to 5; and R5 represents hydrogen atom, a C1-6 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C2-6 alkynyl group which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a 2,2-(alkylenedioxy)ethyl group or a group represented by the formula: (wherein the ring C represents benzene ring, an aliphatic ring or a heterocyclic ring; R6s are the same as or different from each other and each represents hydrogen atom, a halogen atom, hydroxyl group, nitrile group, a C1-6 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C2-6 alkynyl group which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a C1-6 alkoxy group which may be substituted, a C1-6 alkoxyalkoxy group which may be substituted, an aryloxy group which may be substituted or an aralkyloxy group which may be substituted, and further two of R6s may together form an aliphatic ring, an aromatic ring, a heterocyclic ring or an alkylenedioxy ring; R7 represents a halogen atom, hydroxyl group, a C1-6 alkyl group which may be substituted, a C1-6 alkoxy group, nitrile group, a halogeno-C1-6 alkyl group, a hydroxyl-C1-6 alkyl group, a cyano-C1-6 alkyl group, an amino-C1-6 alkyl group, nitro group, azide group, an amino group which may be substituted, a carbamoyl group which may be substituted, a carboxyl group which may be substituted, mercapto group or a thio-C1-6 alkoxy group; and n represents an integer of 1 to 5), provided that 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine, a pharmacologically acceptable salt thereof or a hydrate of them are excluded.