(Pyrido/thieno)-[f]-oxazepine-5-one derivatives
    2.
    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

    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。

    Piperidine derivatives
    5.
    发明授权
    Piperidine derivatives 失效
    哌啶衍生物

    公开(公告)号:US5714501A

    公开(公告)日:1998-02-03

    申请号:US634427

    申请日:1996-04-18

    CPC分类号: C07D211/46 C07D211/70

    摘要: A piperidine derivative of formula (1) or salts thereof: ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or together represent O, R.sup.3 represents H, --R.sup.5 --COOR.sup.6, or --COOR.sup.6 (wherein R.sup.5 is a lower alkylene group, --CONH--, or --CONHCH.sub.2, and R.sup.6 is H or a lower alkyl group), R.sup.4 represents H, an aralkyloxy carbonyl group, an aminomethyl carbonyl group, or an aralkyloxy carbonyl aminomethyl carbonyl group, A represents O or a double bond, and the broken line has the meaning that a bonding hand may be present; and preventive and therapeutic agents for allergies, antihistaminic agents, and antileucotriene agents comprising the derivative or salts as their effective component. The compound of formula (1) has excellent antihistaminic activities and antileukotriene activities, which are well balanced, and is useful as a drug for the prevention and treatment of allergies such as asthma, allergic rhinitis, allergic dermatosis and urticaria.

    摘要翻译: 式(1)的哌啶衍生物或其盐:其中R1和R2独立地表示H或一起代表O,R3表示H,-R5-COOR6或-COOR6(其中R5是低级亚烷基 ,-CONH-或-CONHCH 2,R6为H或低级烷基),R4表示H,芳烷氧基羰基,氨基甲基羰基或芳烷氧基羰基氨基甲基羰基,A表示O或双键, 虚线具有粘合手可能存在的意思; 以及包含所述衍生物或盐作为其有效成分的过敏,抗组胺剂和抗孕妇三烯试剂的预防和治疗剂。 式(1)化合物具有优异的抗组胺活性和抗白细胞三烯活性,其平衡良好,可用作预防和治疗哮喘,过敏性鼻炎,过敏性皮肤病和荨麻疹等过敏症的药物。

    39-Desmethoxy Derivatives of Rapamycin
    6.
    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

    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。