Use of aminoindazole derivatives for the inhibition of tau phosphorylation
    2.
    发明授权
    Use of aminoindazole derivatives for the inhibition of tau phosphorylation 失效
    氨基吲唑衍生物用于抑制tau磷酸化

    公开(公告)号:US07629374B2

    公开(公告)日:2009-12-08

    申请号:US12143070

    申请日:2008-06-20

    IPC分类号: A61K31/415

    摘要: The present invention relates to the use of novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5, R6 and R7 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, OR8, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl, to treat a disease selected from the group consisting of: neurodegenerative diseases, strokes, cranial and spinal traumas and peripheral neuropathies, obesity, metabolic diseases, type II diabetes, essential hypertension, atherosclerotic cardiovascular diseases, polycystic ovaries syndrome, syndrome X, immunodeficiency and cancer.

    摘要翻译: 本发明涉及通式(I)的新型衍生物,其中R3是(1-6C)烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳基或 与(1-10C)环烷基,杂环,杂环烷基,环烷基,金刚烷基,多环烷基,烯基,炔基,CONR1R2,COOR1,SO2R1,C(-NH)R1或C(-NH)NR1基团稠合的杂芳基) R 5,R 6和R 7彼此独立地选自以下基团:卤素,CN,NO 2,NH 2,OH,OR 8,COOH,C(O)OR 8,-OC(O)R 8,NR 8 R 9,NHC )R8,C(O)NR8R9,NHC(S)R8,C(S)NR8R9,SR8,S(O)R8,SO2R8,NHSO2R8,SO2NR8R9,-O-SO2R8,-SO2-O-R8,三氟甲基,三氟甲氧基 ,(1-6C)烷基,(1-6C)烷氧基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,杂环,环烷基,烯基,炔基,金刚烷基或多环烷基, 选自以下的疾病:神经变性疾病,中风,颅脑和脊髓创伤和周围神经病变,肥胖症,代谢疾病,II型糖尿病,原发性高血压,动脉粥样硬化性心血管疾病,多囊卵巢综合征,综合征X,免疫缺陷和癌症。

    OFFSHORE HYDROELECTRIC TURBINE ASSEMBLY AND METHOD
    3.
    发明申请
    OFFSHORE HYDROELECTRIC TURBINE ASSEMBLY AND METHOD 失效
    海洋水电涡轮组件及方法

    公开(公告)号:US20120257955A1

    公开(公告)日:2012-10-11

    申请号:US13444113

    申请日:2012-04-11

    申请人: Thomas Rooney

    发明人: Thomas Rooney

    IPC分类号: F01D25/28

    摘要: The invention is directed to a single moored offshore marine turbine assembly having a central control vessel which includes a main vessel tethered to a control buoy. The main vessel having a first cap, a corresponding second cap and a tubular shell positioned between both the first cap and second cap. The tubular shell contains one or more vertical partitions to assist in ballasting. The control buoy includes a compressor and an air conduit which forces air into the main vessel through a manifold. A hollow suction caisson affixes the central control vessel to the ocean floor. A taut line mooring secures the suction caisson to the main vessel. Electricity is generated via a turbine shroud assembly having a conical shroud and a hydro-turbine. By attaching a plurality of turbine shroud assemblies in series via cables, a horizontal turbine array is formed resulting in a simple, economical and safe layout.

    摘要翻译: 本发明涉及一种具有中央控制容器的单个系泊海上涡轮机组件,该中央控制容器包括连接到控制浮标的主船。 主容器具有第一盖,相应的第二盖和位于第一盖和第二盖之间的管状壳。 管状壳体包含一个或多个垂直隔板以辅助压载。 控制浮标包括压缩机和通过歧管迫使空气进入主容器的空气管道。 空心抽吸沉箱将中央控制船舶固定在海底。 拉紧系泊系统将吸力沉箱固定在主船上。 通过具有锥形护罩和水轮机的涡轮机护罩组件产生电力。 通过经由电缆将多个涡轮机护罩组件串联连接,形成水平涡轮机阵列,从而形成简单,经济和安全的布局。

    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them
    4.
    发明授权
    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 有权
    氨基吲唑衍生物作为药物和药物组合物,包括它们

    公开(公告)号:US07582669B2

    公开(公告)日:2009-09-01

    申请号:US11567442

    申请日:2006-12-06

    IPC分类号: A61K31/416

    摘要: The present invention relates to novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.

    摘要翻译: 本发明涉及通式(I)的新型衍生物,其中R3是(1-6C)烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳基或杂芳基 (1-10C)环烷基,杂环,杂环烷基,环烷基,金刚烷基,多环烷基,烯基,炔基,CONR1R2,COOR1,SO2R1,C(-NH)R1或C(-NH)NR1基; R 5和R 6彼此独立地选自以下基团:卤素,CN,NO 2,NH 2,OH,COOH,C(O)OR 8,-OC(O)R 8,NR 8 R 9,NHC(O) (O)NR8R9,NHC(S)R8,C(S)NR8R9,SR8,S(O)R8,SO2R8,NHSO2R8,SO2NR8R9,-O-SO2R8,-SO2-O-R8,三氟甲基,三氟甲氧基,(1- 6C)烷基,(1-6C)烷氧基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,杂环,环烷基,烯基,炔基,金刚烷基或多环烷基。

    NOVEL AMINOINDAZOLE DERIVATIVES AS MEDICAMENTS AND PHARMACEUTICAL COMPOSITIONS INCLUDING THEM
    5.
    发明申请
    NOVEL AMINOINDAZOLE DERIVATIVES AS MEDICAMENTS AND PHARMACEUTICAL COMPOSITIONS INCLUDING THEM 有权
    作为药物和药物组合物的新型氨基咔唑衍生物包括它们

    公开(公告)号:US20070093479A1

    公开(公告)日:2007-04-26

    申请号:US11567442

    申请日:2006-12-06

    摘要: The present invention relates to novel derivatives of general formula (I) in which R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl fused to a (1-10C) cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1-6C)alkyl, (1-6C)alkoxy, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.

    摘要翻译: 本发明涉及通式(I)的新型衍生物,其中R3是(1-6C)烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳基或杂芳基 (1-10C)环烷基,杂环,杂环烷基,环烷基,金刚烷基,多环烷基,烯基,炔基,CONR1R2,COOR1,SO2R1,C(-NH)R1或C(-NH)NR1 激进; R 5和R 6彼此独立地选自以下基团:卤素,CN,NO 2,NH 2,OH,COOH,C(O)OR 8, -OC(O)R8,NR8R9,NHC(O)R8,C(O)NR8R9,NHC(S)R8,C(S)NR8R9,SR8,S(O) R 8,NHSO 2 R 8,SO 2 NR 8 R 9,-O-SO 2 R 8,-SO 2 -O (1-6C)烷氧基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,杂环,环烷基,链烯基,炔基,金刚烷基 或多环烷基。

    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them
    9.
    发明授权
    Aminoindazole derivatives as medicaments and pharmaceutical compositions including them 有权
    氨基吲唑衍生物作为药物和药物组合物,包括它们

    公开(公告)号:US07166629B2

    公开(公告)日:2007-01-23

    申请号:US10654703

    申请日:2003-09-04

    IPC分类号: A61K31/416 C07D231/56

    摘要: The present invention relates to novel derivatives of general formula (I) in which R3 is a (1–6C)alkyl, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, aryl or heteroaryl fused to a (1–10C)cycloalkyl, heterocycle, heterocycloalkyl, cycloalkyl, adamantyl, polycycloalkyl, alkenyl, alkynyl, CONR1R2, COOR1, SO2R1, C(═NH)R1 or C(═NH)NR1 radical; R5 and R6 are, independently of one another, chosen from the following radicals: halogen, CN, NO2, NH2, OH, COOH, C(O)OR8, —O—C(O)R8, NR8R9, NHC(O)R8, C(O)NR8R9, NHC(S)R8, C(S)NR8R9, SR8, S(O)R8, SO2R8, NHSO2R8, SO2NR8R9, —O—SO2R8, —SO2—O—R8, trifluoromethyl, trifluoromethoxy, (1–6C)alkyl, (1–6C)alkoxy, aryl, aryl(1–6C)alkyl, heteroaryl, heteroaryl(1–6C)alkyl, heterocycle, cycloalkyl, alkenyl, alkynyl, adamantyl or polycycloalkyl.

    摘要翻译: 本发明涉及通式(I)的新型衍生物,其中R3是(1-6C)烷基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,芳基或杂芳基 (1-10C)环烷基,杂环,杂环烷基,环烷基,金刚烷基,多环烷基,烯基,炔基,CONR1R2,COOR1,SO2R1,C(-NH)R1或C(-NH)NR1 激进; R 5和R 6彼此独立地选自以下基团:卤素,CN,NO 2,NH 2,OH,COOH,C(O)OR 8, -OC(O)R8,NR8R9,NHC(O)R8,C(O)NR8R9,NHC(S)R8,C(S)NR8R9,SR8,S(O) R 8,NHSO 2 R 8,SO 2 NR 8 R 9,-O-SO 2 R 8,-SO 2 -O (1-6C)烷氧基,芳基,芳基(1-6C)烷基,杂芳基,杂芳基(1-6C)烷基,杂环,环烷基,链烯基,炔基,金刚烷基 或多环烷基。