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    39-Desmethoxy Derivatives of Rapamycin
    1.
    发明申请
    39-Desmethoxy Derivatives of Rapamycin 有权
    雷帕霉素的39-去甲氧基衍生物

    公开(公告)号：US20100081682A1

    公开(公告)日：2010-04-01

    申请号：US12630251

    申请日：2009-12-03

    申请人： Christoph Hendrik Beckmann ,  Steven James Moss ,  Rose Mary Sheridan ,  Mingqiang Zhang ,  Barrie Wilkinson

    发明人： Christoph Hendrik Beckmann ,  Steven James Moss ,  Rose Mary Sheridan ,  Mingqiang Zhang ,  Barrie Wilkinson

    IPC分类号： A61K31/436

    CPC分类号： C07D498/18

    摘要： The present invention relates to 39-desmethoxyrapamycin derivatives and their uses thereof. The present invention provides for the use of these compounds in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.

    摘要翻译： 本发明涉及39-去甲氧基嘧啶霉素衍生物及其用途。 本发明提供了这些化合物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥反应，移植物抗宿主病，自身免疫性疾病，炎症疾病，血管 疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。

    39-Desmethoxy Derivatives of Rapamycin
    2.
    发明申请
    39-Desmethoxy Derivatives of Rapamycin 有权
    雷帕霉素的39-去甲氧基衍生物

    公开(公告)号：US20080188511A1

    公开(公告)日：2008-08-07

    申请号：US11908250

    申请日：2006-03-10

    申请人： Christoph Hendrik Beckmann ,  Steven James Moss ,  Rose Mary Sheridan ,  Mingqiang Zhang ,  Barrie Wilkinson

    发明人： Christoph Hendrik Beckmann ,  Steven James Moss ,  Rose Mary Sheridan ,  Mingqiang Zhang ,  Barrie Wilkinson

    IPC分类号： A61K31/436 ,  C07D498/18 ,  A61P35/04

    CPC分类号： C07D498/18

    摘要： The present invention relates to novel 39-desmethoxyrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxyrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.

    摘要翻译： 本发明涉及新型的39-去甲氧基嘧啶霉素衍生物，其制备方法及其应用。 在另一方面，本发明提供了这些39-去甲氧基丙酰胺衍生物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥反应，移植物抗宿主病，自身免疫的治疗 疾病，炎症疾病，血管疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。

    39-desmethoxy derivatives of rapamycin
    3.
    发明授权
    39-desmethoxy derivatives of rapamycin 有权
    雷帕霉素的39-去甲氧基衍生物

    公开(公告)号：US08008318B2

    公开(公告)日：2011-08-30

    申请号：US12630251

    申请日：2009-12-03

    申请人： Christoph Hendrik Beckmann ,  Steven James Moss ,  Rose Mary Sheridan ,  Mingqiang Zhang ,  Barrie Wilkinson

    发明人： Christoph Hendrik Beckmann ,  Steven James Moss ,  Rose Mary Sheridan ,  Mingqiang Zhang ,  Barrie Wilkinson

    IPC分类号： A61P35/00

    CPC分类号： C07D498/18

    摘要： The present invention relates to 39-desmethoxyrapamycin derivatives and their uses thereof. The present invention provides for the use of these compounds in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.

    摘要翻译： 本发明涉及39-去甲氧基嘧啶霉素衍生物及其用途。 本发明提供了这些化合物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥反应，移植物抗宿主病，自身免疫性疾病，炎症疾病，血管 疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。

    39-desmethoxy derivatives of rapamycin
    4.
    发明授权
    39-desmethoxy derivatives of rapamycin 有权
    雷帕霉素的39-去甲氧基衍生物

    公开(公告)号：US07648996B2

    公开(公告)日：2010-01-19

    申请号：US11908250

    申请日：2006-03-10

    申请人： Christoph Hendrik Beckmann ,  Steven James Moss ,  Rose Mary Sheridan ,  Mingqiang Zhang ,  Barrie Wilkinson

    发明人： Christoph Hendrik Beckmann ,  Steven James Moss ,  Rose Mary Sheridan ,  Mingqiang Zhang ,  Barrie Wilkinson

    IPC分类号： C07D498/18 ,  A61K31/436

    CPC分类号： C07D498/18

    摘要： The present invention relates to novel 39-desmethoxyrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxyrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.

    摘要翻译： 本发明涉及新型的39-去甲氧基嘧啶霉素衍生物，其制备方法及其应用。 在另一方面，本发明提供了这些39-去甲氧基丙酰胺衍生物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥反应，移植物抗宿主病，自身免疫的治疗 疾病，炎症疾病，血管疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。

    39-desmethoxy-39-methyl derivatives of rapamycin
    5.
    发明授权
    39-desmethoxy-39-methyl derivatives of rapamycin 失效
    雷帕霉素的39-去甲氧基-39-甲基衍生物

    公开(公告)号：US07897608B2

    公开(公告)日：2011-03-01

    申请号：US12273917

    申请日：2008-11-19

    申请人： Barrie Wilkinson ,  Mingqiang Zhang ,  Rose Mary Sheridan

    发明人： Barrie Wilkinson ,  Mingqiang Zhang ,  Rose Mary Sheridan

    IPC分类号： C07D498/18 ,  A61K31/436

    CPC分类号： C07D498/18

    摘要： The present invention relates to novel 39-desmethoxy-39-methylrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxy-39 -methylrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.

    摘要翻译： 本发明涉及新的39-脱甲氧基-39-甲基雷帕霉素衍生物，其制备方法及其应用。 在另一方面，本发明提供了这些39-脱甲氧基-39-甲基雷帕霉素衍生物在治疗癌症和/或B细胞恶性肿瘤中的用途，诱导或维持免疫抑制，移植排斥治疗，移植物抗 - 宿主病，自身免疫性疾病，炎症疾病，血管疾病和纤维化疾病，刺激神经元再生或治疗真菌感染。

    (Pyrido/thieno)-[f]-oxazepine-5-one derivatives
    10.
    发明授权
    (Pyrido/thieno)-[f]-oxazepine-5-one derivatives 失效
    （吡啶并噻吩） - [f] - 氧氮杂-5-酮衍生物

    公开(公告)号：US07566778B2

    公开(公告)日：2009-07-28

    申请号：US12024597

    申请日：2008-02-01

    申请人： Simon James Anthony Grove ,  Julia Adam-Worrall ,  Mingqiang Zhang ,  Robert Gilfillan

    发明人： Simon James Anthony Grove ,  Julia Adam-Worrall ,  Mingqiang Zhang ,  Robert Gilfillan

    IPC分类号： C07D498/14

    CPC分类号： C07D498/14

    摘要： The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R1, R2 and R3 are independently H or (C1-4)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkyloxy(C1-4)alkyl, CF3, halogen, nitro, cyano, NR4R5, NR4COR6, and CONR4R5; R4 and R5 are independently H or (C1-4-)alkyl; or R4 and R5 form together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR6; R6 is (C1-4)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.

    摘要翻译： 本发明涉及具有通式I的（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物，其中R 1，R 2和R 3独立地为H或（C 1-4）烷基; Ar表示任选被一个或多个选自（C 1-4）烷基，（C 1-4）烷氧基，（C 1-4）烷氧基（C 1-4）烷基，CF 3，卤素，硝基， 氰基，NR4R5，NR4COR6和CONR4R5; R 4和R 5独立地为H或（C 1-4 - ）烷基; 或R 4和R 5与它们所连接的氮原子一起形成5-或6-元饱和杂环，任选地含有选自O，S或NR 6的另外的杂原子; R6是（C1-4）烷基; A表示任选含有氧原子的4-7元饱和杂环的残基，该环任选被1-3个选自（C 1-4）烷基，（C 1-4）烷氧基，羟基，卤素和 氧代 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物，以及这些（吡啶并噻吩并[f] - 氧氮杂-5-酮衍生物在治疗对增强突触反应有反应的神经疾病和精神疾病的用途中的用途） 由AMPA受体介导的中枢神经系统。