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465 条记录 (耗时 0.039 秒)

    Pyridine substituted furan derivatives as Raf kinase inhibitors
    8.
    发明授权
    Pyridine substituted furan derivatives as Raf kinase inhibitors 失效
    吡啶取代的呋喃衍生物作为Raf激酶抑制剂

    公开(公告)号：US07375105B2

    公开(公告)日：2008-05-20

    申请号：US10488650

    申请日：2002-09-05

    申请人： David Kenneth Dean ,  Andrew Kenneth Takle ,  David Matthew Wilson

    发明人： David Kenneth Dean ,  Andrew Kenneth Takle ,  David Matthew Wilson

    IPC分类号： A61K31/5377 ,  A61K31/4545 ,  A61K31/443 ,  C07D413/14 ,  C07D211/32 ,  C07D405/04

    CPC分类号： C07D405/04 ,  C07D405/14

    摘要： Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. Wherein X is O, CH2 CO, S or NH, or the moiety X—R1 is hydrogen; Y1 and Y2 independently represent CH or N; Ar is a mono- or fused bicyclic aromatic or heteroaromatic group which may be optionally substituted; one of X1 and X2 is selected from O, S or NR11 and the other is CH, wherein R11 is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl.

    摘要翻译： 化合物及其作为药物的用途，特别是用作治疗神经创伤性疾病，癌症，慢性神经变性，疼痛，偏头痛和心脏肥大的Raf激酶抑制剂。 其中X是O，CH 2 CO，S或NH，或者X-R 1部分是氢; Y 1和Y 2独立地表示CH或N; Ar是可以任选取代的单或二稠合双环芳族或杂芳族基团; X 1和X 2之一选自O，S或NR 11，另一个是CH，其中R 11， / SUP>是氢，C 1-6烷基，芳基或芳基C 1-6烷基。

    Thiazolidinedione derivative and its use as antidiabetic
    10.
    发明授权
    Thiazolidinedione derivative and its use as antidiabetic 失效
    噻唑烷二酮衍生物及其用作抗糖尿病药

    公开(公告)号：US07358366B2

    公开(公告)日：2008-04-15

    申请号：US11458471

    申请日：2006-07-19

    申请人： Paul David James Blackler ,  Robert Gordon Giles ,  Stephen Moore ,  Michael John Sasse

    发明人： Paul David James Blackler ,  Robert Gordon Giles ,  Stephen Moore ,  Michael John Sasse

    IPC分类号： C07D417/12

    CPC分类号： C07D417/12

    摘要： A polymorphic form of 5-[4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2,4-dione, maleic acid salt (the “Polymorph”) characterised in that it provides: (i) an infra red spectrum containing peaks at 1752, 1546, 1154, 621, and 602 cm−1; and/or (ii) a Raman spectrum containing peaks at 1751, 1243 and 602 cm−1; and/or (iii) a solid-state nuclear magnetic resonance spectrum containing peaks at 111.9, 114.8, 119.6, 129.2, 134.0, 138.0, 144.7, 153.2, 157.1, 170.7, 172.0, and 175.0 ppm; and/or (iv) an X-ray powder diffraction (XRPD) pattern which gives calculated lattice spacings of 6.46, 5.39, 4.83, 4.68, 3.71, 3.63, 3.58, and 3.48 Angstroms; a process for preparing such a compound, a pharmaceutical composition containing such a compound and the use of such a compound in medicine.

    摘要翻译： 5- [4- [2-（N-甲基-N-（2-吡啶基）氨基）乙氧基]苄基]噻唑烷-2,4-二酮，马来酸盐（“多晶型”）的多晶形式，其特征在于 它提供：（i）在1752,1546,1154,621和602cm -1处含有峰的红外光谱; 和/或（ii）在1751,1243和602cm -1处含有峰的拉曼光谱; 和/或（iii）在111.9,114.8,119.6,129.2,134.0,138.0,144.7,153.2,157.1,170.7,172.0和175.0ppm处含有峰的固态核磁共振光谱; 和/或（iv）X射线粉末衍射（XRPD）图案，其给出计算的晶格间距为6.46,5.39,4.83,4.68,3.73,3.63,3.58和3.48埃; 制备这种化合物的方法，含有这种化合物的药物组合物和这种化合物在医药中的用途。