ANTIBACTERIAL BENZOTHIAZOLE DERIVATIVES
    5.
    发明申请
    ANTIBACTERIAL BENZOTHIAZOLE DERIVATIVES 审中-公开
    抗真菌苯并噻唑衍生物

    公开(公告)号:WO2016079688A1

    公开(公告)日:2016-05-26

    申请号:PCT/IB2015/058919

    申请日:2015-11-18

    CPC classification number: C07D277/64 C07D277/62

    Abstract: The invention relates to antibacterial compounds formula (I) wherein R 1 is the group M, whereby M is one of the groups M A and M B represented below wherein A is a bond or C≡C; R 1A is H or halogen; R 2A is H or halogen; R 3A is H, alkoxy, hydroxyalkoxy, hydroxyalkyl, dihydroxyalkyl, 2-hydroxyacetamido, substituted cycloprop-1-yl or substituted oxetan-3-yl; and R 1B is hydroxyalkyl, dihydroxyalkyl, aminoalkyl, dialkylaminoalkyl, substituted cycloprop-1-yl, substituted cyclobutan-1-yl, substituted oxetan-3-yl, 3-hydroxythietan-3-yl, substituted azetidin-3-yl, trans -( cis -3,4-dihydroxy)-cyclopent-1-yl, 3-hydroxymethylbicyclo[1,1,1]pentan-1-yl, 4-hydroxytetrahydro-2 H -pyran-4-yl, (3R,6S)-3-aminotetrahydro-2 H -pyran-6-yl, piperidin-4-yl or 1-(2-hydroxyacetyl)piperidin-4-yl; and salts thereof.

    Abstract translation: 本发明涉及式(I)的抗菌化合物,其中R 1是基团M,其中M是下列基团之一,其中A是一个键或C≡C; R1A是H或卤素; R2A是H或卤素; R3A是H,烷氧基,羟基烷氧基,羟基烷基,二羟基烷基,2-羟基乙酰氨基,取代的环丙-1-基或取代的氧杂环丁烷-3-基; 并且R 1B是羟基烷基,二羟基烷基,氨基烷基,二烷基氨基烷基,取代的环丙-1-基,取代的环丁烷-1-基,取代的氧杂环丁烷-3-基,3-羟基硫杂环丁烷-3-基,取代的氮杂环丁烷-3-基,反 - ( 顺式-3,4-二羟基) - 环戊-1-基,3-羟基甲基双环[1,1,1]戊-1-基,4-羟基四氢-2H-吡喃-4-基,(3R,6S)-3 - 氨基四氢-2H-吡喃-6-基,哌啶-4-基或1-(2-羟基乙酰基)哌啶-4-基; 及其盐。

    KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF
    8.
    发明申请
    KYNURENINE-3-MONOOXYGENASE INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF 审中-公开
    吉非烯-3-MONOOXYGENASE抑制剂,药物组合物及其使用方法

    公开(公告)号:WO2015047982A2

    公开(公告)日:2015-04-02

    申请号:PCT/US2014/056898

    申请日:2014-09-23

    Abstract: Certain compounds, or pharmaceutically acceptable salts or prodrugs thereof, are provided herein. Also provided are pharmaceutical compositions comprising at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein as a single active agent or administering at least one compound, or pharmaceutically acceptable salt or prodrug thereof, described herein in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

    Abstract translation: 本文提供了某些化合物或其药学上可接受的盐或前药。 还提供了包含本文所述的至少一种化合物或其药学上可接受的盐或前药和一种或多种药学上可接受的载体的药物组合物。 描述了治疗患有某些对KMO活性抑制作用的疾病和病症的患者的方法,其包括对此类患者施用至少一种有效减少体征或症状的至少一种化合物或其药学上可接受的盐或前药 的疾病或病症。 这些疾病包括神经变性疾病如亨廷顿氏病。 还描述了治疗方法,包括将本文所述的至少一种化合物或其药学上可接受的盐或前药作为单一活性剂施用或给予本文所述的至少一种化合物或其药学上可接受的盐或前药, 更多其他治疗剂。 还提供了用于筛选能够抑制KMO活性的化合物的方法。

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