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    Inhibitors for GlyT-1
    41.
    发明授权
    Inhibitors for GlyT-1 失效
    GlyT-1抑制剂

    公开(公告)号：US07589089B2

    公开(公告)日：2009-09-15

    申请号：US11895097

    申请日：2007-08-23

    申请人： Synese Jolidon ,  Robert Narquizian ,  Emmanuel Pinard

    发明人： Synese Jolidon ,  Robert Narquizian ,  Emmanuel Pinard

    IPC分类号： C07D261/06 ,  C07D307/02 ,  C07D333/02 ,  C07D333/50 ,  C07D295/00 ,  C07D213/02 ,  C07D317/44 ,  A61K31/5375 ,  A61K31/164 ,  A61K31/341 ,  A61K31/357 ,  A61K31/381 ,  A61K31/42 ,  A61K31/44 ,  C07C233/00

    CPC分类号： C07C237/12 ,  C07C255/57 ,  C07D213/81 ,  C07D213/82 ,  C07D317/52 ,  C07D333/20 ,  C07D333/70

    摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, R4, and X are as defined herein or to pharmaceutically acceptable acid addition salts thereof, with the exception of 4-methoxy-N-[2-oxo-2-(phenylamino)ethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-[2-[5-chloro-2-methoxyphenyl)amino]-2-oxoethyl]-N-benzamide, 4-methyl-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide, N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-methyl-N-[2-[(4-methylphenyl)amino]-2-oxoethyl]-N-phenyl-benzamide, 4-chloro-N-(2-oxo-2-[(2,4,6-trichlorophenyl)amino]ethyl]-N-benzamide and N-[2-[(2,4-dimethoxyphenyl)amino]-2-oxoethyl]-N-[(2-fluorophenyl)methyl]-benzeneacetamide. The compounds are useful in the treatment of neurological and neuropsychiatric disorders.

    摘要翻译： 本发明涉及式I化合物，其中R 1，R 2，R 3，R 4和X如本文所定义，或其药学上可接受的酸加成盐，除了4-甲氧基-N- [2-氧代-2- （苯基氨基）乙基] -N-苯基 - 苯甲酰胺，4-氯-N- [2 - [（4-甲基苯基）氨基] -2-氧代乙基] -N-苯基 - 苯甲酰胺，4-氯-N- [2- [5-氯-2-甲氧基苯基]氨基] -2-氧代乙基] -N-苯甲酰胺，4-甲基-N-（2-氧代-2 - [（2,4,6-三氯苯基）氨基]乙基] -N - 苯甲酰胺，N- [2 - [（4-甲基苯基）氨基] -2-氧代乙基] -N-苯基 - 苯甲酰胺，4-甲基-N- [2 - [（4-甲基苯基）氨基] -2-氧代乙基] -N-苯基 - 苯甲酰胺，4-氯-N-（2-氧代-2 - [（2,4,6-三氯苯基）氨基]乙基] -N-苯甲酰胺和N- [2 - [（2,4- 二甲氧基苯基）氨基] -2-氧代乙基] -N - [（2-氟苯基）甲基] - 苯乙酰胺。该化合物可用于治疗神经和神经精神障碍。

    Hydroxyalkylarylamide Derivatives
    44.
    发明申请
    Hydroxyalkylarylamide Derivatives 审中-公开
    羟烷基芳基酰胺衍生物

    公开(公告)号：US20090062297A1

    公开(公告)日：2009-03-05

    申请号：US12087623

    申请日：2007-01-08

    申请人： Richard W. Heidebrecht ,  Thomas A. Miller ,  Kevin J. Wilson ,  David J. Witter ,  Jonathan Grimm

    发明人： Richard W. Heidebrecht ,  Thomas A. Miller ,  Kevin J. Wilson ,  David J. Witter ,  Jonathan Grimm

    IPC分类号： A61K31/496 ,  C07D333/24 ,  A61K31/381 ,  A61K31/422 ,  C07D413/12 ,  C07D333/70

    CPC分类号： C07D333/70 ,  C07D333/20 ,  C07D413/12

    摘要： The present invention relates to a novel class of hydroxyalkylarylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

    摘要翻译： 本发明涉及一类新的羟烷基芳基酰胺衍生物。 本发明化合物可用于治疗癌症。 氟化芳基酰胺衍生物还可以抑制组蛋白脱乙酰酶，并且适用于选择性诱导终末分化，并阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。 因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统（CNS）的疾病，例如 神经退行性疾病 本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。

    Fluorinated Arylamide Derivatives
    45.
    发明申请
    Fluorinated Arylamide Derivatives 审中-公开
    氟化芳酰胺衍生物

    公开(公告)号：US20090012075A1

    公开(公告)日：2009-01-08

    申请号：US12087624

    申请日：2007-01-08

    申请人： Thomas A. Miller ,  David L. Sloman ,  Matthew G. Stanton ,  Kevin J. Wilson ,  David J. Witter

    发明人： Thomas A. Miller ,  David L. Sloman ,  Matthew G. Stanton ,  Kevin J. Wilson ,  David J. Witter

    IPC分类号： A61K31/381 ,  C07D409/12 ,  C07D333/50 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  A61K31/4436 ,  A61K31/5377 ,  A61K31/4025 ,  A61K31/4245 ,  A61P35/00 ,  A61K31/415 ,  A61K31/496

    CPC分类号： C07D231/40 ,  C07D333/20 ,  C07D333/70 ,  C07D409/12 ,  C07D409/14 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.

    摘要翻译： 本发明涉及一类新型氟化芳基酰胺衍生物。 本化合物可用于治疗癌症。 氟化芳基酰胺衍生物还可以抑制组蛋白脱乙酰酶，并且适用于选择性诱导终末分化，并阻止肿瘤细胞的细胞生长和/或凋亡，从而抑制这些细胞的增殖。 因此，本发明的化合物可用于治疗具有以肿瘤细胞增殖为特征的肿瘤的患者。 本发明的化合物还可用于预防和治疗TRX介导的疾病，例如自身免疫性，过敏性和炎性疾病，以及预防和/或治疗中枢神经系统疾病（CNS），例如 神经退行性疾病 本发明进一步提供包含异羟肟酸衍生物和这些药物组合物的安全投药方案的药物组合物，它们易于遵循，并且其在体内导致治疗有效量的异羟肟酸衍生物。