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    TETRAHYDROPYRAZOLO [1,5-A] PYRIMIDINE AS ANTI-TUBERCULOSIS COMPOUNDS
    1.
    发明申请
    TETRAHYDROPYRAZOLO [1,5-A] PYRIMIDINE AS ANTI-TUBERCULOSIS COMPOUNDS 审中-公开
    四氢吡咯并[1,5-A]吡嗪作为抗结核药物

    公开(公告)号：US20140038989A1

    公开(公告)日：2014-02-06

    申请号：US14112564

    申请日：2012-04-20

    申请人： Emilio Alvarez-Ruiz ,  Luis Ballell-Pages ,  Julia Castro Pichel ,  Lourdes Encinas ,  Jorge Esquivias ,  Franscisco Gamo-Benito ,  Maria Cruz Garcia-Palancar ,  Modesto Jesus Remuinan-Blanco

    发明人： Emilio Alvarez-Ruiz ,  Luis Ballell-Pages ,  Julia Castro Pichel ,  Lourdes Encinas ,  Jorge Esquivias ,  Franscisco Gamo-Benito ,  Maria Cruz Garcia-Palancar ,  Modesto Jesus Remuinan-Blanco

    IPC分类号： C07D487/04 ,  A61K45/06 ,  A61K31/519

    CPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

    摘要： A compound of Formula (I) or a pharmaceutically acceptable salt thereof: wherein: R1 represents a group selected from: i) phenyl optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, Cl and NMe2; furanyl, thiophenyl, pyrrolyl, pyridyl, cyclohexyl or naphthyl, each of which is optionally substituted with one or two substituents independently selected from Me, OMe, CF3, F, Cl and NMe2; and iii) benzo[1,3]dioxo5-yl or 2,3-dihydrobenzo[1,4]dioxin-6-yl; R2 represents CF3, C1-4alkyl, or CHF2; when R1 represents optionally substituted furanyl, thiophenyl, pyrrolyl, pyridyl or naphthyl, R3 represents Et; when R1 represents optionally substituted cyclohexyl, R3 represents Et or Me; otherwise R3 represents Et, Me, Br or OMe, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided, together with certain novel compounds.

    摘要翻译： 式（I）化合物或其药学上可接受的盐：其中：R1表示选自以下的基团：i）任选被一个或两个独立地选自Me，OMe，CF 3，F，Cl和NMe 2的取代基取代的苯基; 呋喃基，噻吩基，吡咯基，吡啶基，环己基或萘基，其各自任选被一个或两个独立地选自Me，OMe，CF 3，F，Cl和NMe 2的取代基取代; 和iii）苯并[1,3]二氧代-5-基或2,3-二氢苯并[1,4]二恶英-6-基; R 2表示CF 3，C 1-4烷基或CHF 2; 当R 1表示任选取代的呋喃基，噻吩基，吡咯基，吡啶基或萘基时，R 3表示Et; 当R 1表示任选取代的环己基时，R 3表示Et或Me; 否则R3表示Et，Me，Br或OMe，含有它们的组合物，它们在治疗中的用途，例如治疗结核病以及制备这些化合物的方法，以及某些新型化合物。

    3-amino-pyrazole derivatives useful against tuberculosis
    2.
    发明授权
    3-amino-pyrazole derivatives useful against tuberculosis 有权
    可用于结核病的3-氨基 - 吡唑衍生物

    公开(公告)号：US08779153B2

    公开(公告)日：2014-07-15

    申请号：US13878889

    申请日：2011-10-11

    申请人： Julia Castro Pichel ,  Raquel Fernandez Menendez ,  Esther Pilar Fernandez Velando ,  Silvia Gonzalez Del Valle ,  Araceli Mallo-Rubio

    发明人： Julia Castro Pichel ,  Raquel Fernandez Menendez ,  Esther Pilar Fernandez Velando ,  Silvia Gonzalez Del Valle ,  Araceli Mallo-Rubio

    IPC分类号： C07D285/135 ,  C07D277/10 ,  A61K31/44

    CPC分类号： C07D417/14 ,  C07D471/04

    摘要： A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, —CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicylic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.

    摘要翻译： 式（I）的化合物或其药学上可接受的盐：其中：Het为5至10元杂芳环; X为N，Y为CR5; 或X为C，Y为S; Z选自N和CH; R1选自H和C1-2烷基; R2选自H，C1-2烷基，OH，-CH2OH和C1-2烷氧基; 每个R 3独立地选自OH，C 1-3烷基，F，Cl，Br，NH 2和C 1-3烷氧基; R 4选自C 1-3烷基和卤代C 1-3烷基; R 5选自H，C 1-3烷基和卤代C 1-3烷基; R6和R7各自独立地选自H，C 1-3烷基和C 1-3烷氧基; 或ii）R6和R7与它们所连接的环一起形成9元双环; p为0-3; 并且RA选自H和C 1-3烷基，含有它们的组合物，它们在治疗中的用途，例如用于治疗结核病以及制备这些化合物的方法。

    3 -AMINO- PYRAZOLE DERIVATIVES USEFUL AGAINST TUBERCULOSIS
    6.
    发明申请
    3 -AMINO- PYRAZOLE DERIVATIVES USEFUL AGAINST TUBERCULOSIS 有权
    3-氨基吡唑衍生物应用于结核病

    公开(公告)号：US20130203802A1

    公开(公告)日：2013-08-08

    申请号：US13878889

    申请日：2011-10-11

    申请人： Julia Castro Pichel ,  Raquel Fernandez Menendez ,  Esther Pilar Fernandez Velando ,  Silvia Gonzalez Del Valle ,  Araceli Mallo-Rubio

    发明人： Julia Castro Pichel ,  Raquel Fernandez Menendez ,  Esther Pilar Fernandez Velando ,  Silvia Gonzalez Del Valle ,  Araceli Mallo-Rubio

    IPC分类号： C07D417/14 ,  C07D471/04

    CPC分类号： C07D417/14 ,  C07D471/04

    摘要： A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR5; or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and C1-2alkyl; R2 is selected from H, C1-2alkyl, OH, —CH2OH and C1-2alkoxy; Each R3 is independently selected from OH, C1-3alkyl, F, Cl, Br, NH2, and C1-3alkoxy; R4 is selected from C1-3alkyl and haloC1-3alkyl; R5 is selected from H, C1-3alkyl and haloC1-3alkyl; R6 and R7 are either i) each independently selected from H, C1-3alkyl and C1-3alkoxy; or ii) R6 and R7 together with the ring to which they are attached form a 9-membered bicyclic ring; p is 0-3; and RA is selected from H and C1-3alkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.

    摘要翻译： 式（I）的化合物或其药学上可接受的盐：其中：Het为5至10元杂芳环; X为N，Y为CR5; 或X为C，Y为S; Z选自N和CH; R1选自H和C1-2烷基; R2选自H，C1-2烷基，OH，-CH2OH和C1-2烷氧基; 每个R 3独立地选自OH，C 1-3烷基，F，Cl，Br，NH 2和C 1-3烷氧基; R 4选自C 1-3烷基和卤代C 1-3烷基; R 5选自H，C 1-3烷基和卤代C 1-3烷基; R6和R7各自独立地选自H，C 1-3烷基和C 1-3烷氧基; 或ii）R6和R7与它们所连接的环一起形成9元双环; p为0-3; 并且RA选自H和C 1-3烷基，含有它们的组合物，它们在治疗中的用途，例如用于治疗结核病以及制备这些化合物的方法。