CRYSTAL STRUCTURE OF CHORISMATE SYNTHASE AND USES THEREOF
    5.
    发明申请
    CRYSTAL STRUCTURE OF CHORISMATE SYNTHASE AND USES THEREOF 审中-公开
    合成酶的晶体结构及其用途

    公开(公告)号:WO2004029239A9

    公开(公告)日:2004-06-24

    申请号:PCT/GB0304104

    申请日:2003-09-26

    CPC classification number: C12N9/88 C07K2299/00 C12Q1/34 G06F19/16

    Abstract: The invention describes the identification of the structure coordinates for the enzyme Chorismate Synthase. There is a computer programmed to produce a three-dimensional representation of a molecule or molecular complex, wherein the molecule or molecular complex comprises a binding domain defined by the structure coordinates of (a) Arg 39, His 110, Ser 132, Thr 136, Lys 254, Gly 297, Lys 311, Thr 315, Arg 337 and Asp 339 ; or (b) Ser 9, His 10, Arg 39, Asp 54, Arg 107, His 110, Ser 132, Ala 133, Arg 134, Thr 136, Arg 337 and Asp 339. 1, or where the molecular complex or binding domain has a root mean square deviation of conserved residue backbone atoms of less than 2A when superimposed on the relevant backbone atoms described by the structure coordinates of said amino acids.

    Abstract translation: 本发明描述了酶Chorismate Synthase的结构坐标的鉴定。 计算机被编程以产生分子或分子复合物的三维表示,其中分子或分子复合物包含由(a)Arg 39,His 110,Ser 132,Thr 136, Lys 254,Gly 297,Lys 311,Thr 315,Arg 337和Asp 339; 或(b)Ser 9,His 10,Arg 39,Asp 54,Arg 107,His 110,Ser 132,Ala 133,Arg 134,Thr 136,Arg 337和Asp 339. 1,或其中分子复合物或结合结构域 当由所述氨基酸的结构座标描述的相关骨架原子上叠加时,保守残基骨架原子的均方根偏差小于2A。

    CRYSTAL STRUCTURE OF CHORISMATE SYNTHASE AND USES THEREOF
    7.
    发明申请
    CRYSTAL STRUCTURE OF CHORISMATE SYNTHASE AND USES THEREOF 审中-公开
    合成酶的晶体结构及其用途

    公开(公告)号:WO2004029239A1

    公开(公告)日:2004-04-08

    申请号:PCT/GB2003/004104

    申请日:2003-09-26

    CPC classification number: C12N9/88 C07K2299/00 C12Q1/34 G06F19/16

    Abstract: The invention describes the identification of the structure coordinates for the enzyme Chorismate Synthase. There is a computer programmed to produce a three-dimensional representation of a molecule or molecular complex, wherein the molecule or molecular complex comprises a binding domain defined by the structure coordinates of (a) Arg 39, His 110, Ser 132, Thr 136, Lys 254, Gly 297, Lys 311, Thr 315, Arg 337 and Asp 339 ; or (b) Ser 9, His 10, Arg 39, Asp 54, Arg 107, His 110, Ser 132, Ala 133, Arg 134, Thr 136, Arg 337 and Asp 339. 1, or where the molecular complex or binding domain has a root mean square deviation of conserved residue backbone atoms of less than 2A when superimposed on the relevant backbone atoms described by the structure coordinates of said amino acids.

    Abstract translation: 本发明描述了酶Chorismate Synthase的结构坐标的鉴定。 计算机被编程以产生分子或分子复合物的三维表示,其中分子或分子复合物包含由(a)Arg 39,His 110,Ser 132,Thr 136, Lys 254,Gly 297,Lys 311,Thr 315,Arg 337和Asp 339,如图1所示。 1; 或(b)Ser 9,His 10,Arg 39,Asp 54,Arg 107,His 110,Ser 132,Ala 133,Arg 134,Thr 136,Arg 337和Asp 339. 1,或其中分子复合物或结合结构域 当由所述氨基酸的结构座标描述的相关骨架原子上叠加时,保守残基骨架原子的均方根偏差小于2A。

    ( PYRROLIDIN-2 -YL) PHENYL DERIVATIVES FOR USE IN THE TREATMENT OF PAIN
    10.
    发明申请
    ( PYRROLIDIN-2 -YL) PHENYL DERIVATIVES FOR USE IN THE TREATMENT OF PAIN 审中-公开
    (吡咯烷-2-基)苯基衍生物用于治疗疼痛

    公开(公告)号:WO2010052198A1

    公开(公告)日:2010-05-14

    申请号:PCT/EP2009/064490

    申请日:2009-11-03

    CPC classification number: C07D401/10

    Abstract: The invention relates to (pyrrolidin-2-yl)phenyl derivatives having the general Formula (I), wherein R 1 is (C 1-4 )alkyl, halo(C 1-4 )alkyl, (C 1-4 )alkyloxy, or halo(C 1-4 )alkyloxy; R 2 is H, (C 1-4 )alkyl, halo(C 1-4 )alkyl, (C 1-4 )alkyloxy, halo(C 1-4 )alkyloxy or halogen; R 3 is H, (C 1-4 )alkyl or halo(C 1-4 )alkyl; R 4 is H, (C 1-4 )alkyl or halo(C 1-4 )alkyl; R 5 is H, (C 1-4 )alkyl or halo(C 1-4 )alkyl; or R4 and R5, when bonded to the same carbon atom, can together with the carbon atom form a spiro(C 3-6 )cycloalkyl group, optionally substituted with halogen; R 6 is H, (C 1-4 )alkyl, halo(C 1-4 )alkyl, (C 1-4 )alkyloxy, halo(C 1-4 )alkyloxy or halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these (pyrrolidin-2-yl)phenyl derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

    Abstract translation: 本发明涉及具有通式(I)的(吡咯烷-2-基)苯基衍生物,其中R 1为(C 1-4)烷基,卤代(C 1-4)烷基,(C 1-4)烷氧基或卤素 -4)烷氧基; R 2是H,(C 1-4)烷基,卤代(C 1-4)烷基,(C 1-4)烷氧基,卤代(C 1-4)烷氧基或卤素; R3是H,(C1-4)烷基或卤代(C1-4)烷基; R4是H,(C1-4)烷基或卤代(C1-4)烷基; R5是H,(C1-4)烷基或卤代(C1-4)烷基; 或R 4和R 5在与相同碳原子键合时可与碳原子一起形成任选被卤素取代的螺(C 3-6)环烷基; R 6为H,(C 1-4)烷基,卤代(C 1-4)烷基,(C 1-4)烷氧基,卤代(C 1-4)烷氧基或卤素; 或其药学上可接受的盐,包含其的药物组合物,以及这些(吡咯烷-2-基)苯基衍生物用于治疗疼痛如神经性疼痛或炎性疼痛的用途。

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