3-Phenyl analogs of toxoflavine as kinase inhibitors

    公开(公告)号:US20050239784A1

    公开(公告)日:2005-10-27

    申请号:US10520768

    申请日:2003-07-08

    CPC分类号: C07D487/04

    摘要: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereo-chemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R represents C1-4alkyl; R represents C1-4alkyl; R3 represents C1-4alkyl; or R2 and R3 taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het1 wherein said C3-8cycloalkyl or Het1 each independently may optionally be substituted with C1-4alkyloxycarbonyl; R4 represents halo or C1-4alkyloxy; R5 represents C1-4alkyloxycarbonyl, —O-(mono- or di(C1-4alkyl)aminosulfonyl), C1-4alkyl substituted with one or where possible more substituent being selected from Het3 or NR6R7, C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het4 or NR8R9; R6 and R7 are each independently selected from hydrogen, C1-4alkyl, C1-4alkyloxyC1-4alkyl, -Het5 or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het5; R8 and R9 are each independently selected from hydrogen, C1-4alkyl, -Het7 or mono- or di(C1-4alkyl)aminosulphonyl; Het3 represents a heterocycle selected from piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from hydroxy, aminosulfonyl, amino, mono- or di(C1-4alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het4 represents a heterocycle selected from morpholinyl, piperidinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het5 represents a heterocycle selected from pyridinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, or mono- or di(C1-4alkyl)aminosulfonyl; Het7 represents piperidinyl.

    3-Furanyl analogs of toxoflavine as kinase inhibitors

    公开(公告)号:US20060040943A1

    公开(公告)日:2006-02-23

    申请号:US10520641

    申请日:2003-07-08

    IPC分类号: C07D487/04 A61K31/53

    CPC分类号: C07D487/04

    摘要: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer being 0 or 1; n represents an integer being 0, 1 or 2; R1 represents C1-4alkyl, C1-4alkyl substituted with pyridinyl, phenyl, piperidinyl or piperidinyl substituted with C1-4alkyloxycarbonyl; R2 represents hydrogen or C1-4alkyl; R3 represents hydrogen or C1-4alkyl; or R2 and R3 taken together with the carbon atom to which they are attached form cyclopentyl or piperidinyl wherein said cyclopentyl or piperidinyl each independently may optionally be substituted with one, or where possible, two or three substituents each independently selected from C1-4alkyloxycarbonyl, phenylcarbonyl or —C(═NH)—NH2; R4 represents halo or C1-4alkyloxy; R5 represents Het2, C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy, halo, Het3 or NR6R7, or C1-4alkyloxy substituted with one or where possible more substituents being selected from Het4 or —C(═O)-Het4; R6 and R7 are each independently selected from hydrogen, C1-4alkyl, Het5 or C1-4alkyl substituted with one or where possible more substituents being selected from hydroxy or Het5; Het2 represents piperazinyl; Het3 represents a heterocycle selected from morpholinyl, pyrrolidinyl, piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl preferably methyl, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl, hydroxyC1-4alkyloxyC1-4alkyl, C1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het4 represents a heterocycle selected from morpholinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three C1-4alkyl substituents, preferably methyl; Het5 represents a heterocycle selected from pyridinyl, pyrrolidinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl.

    Surgical drill for osteotomy
    10.
    发明申请
    Surgical drill for osteotomy 审中-公开
    用于截骨术的外科手术

    公开(公告)号:US20070088361A1

    公开(公告)日:2007-04-19

    申请号:US11242579

    申请日:2005-10-03

    申请人: Chih Ho

    发明人: Chih Ho

    IPC分类号: A61B17/00

    摘要: The invention relates to a surgical drill for osteotomy. The surgical drill comprises: a shank, a base portion, a cutting blade, a non-cutting section and a groove. The base portion is formed on the shank. The cutting blade is formed on the edge of the base portion. The non-cutting section is formed on the top of the base portion. The groove is formed on a peripheral section of the base portion, and is adjacent to the cutting blade and extends along a longitudinal direction. According to the invention, the surgical drill utilizes one single cutting blade to drill a socket formed by an implant drill. Because the fewer the blades are, the slower the working speed can be, so the bottom of the socket is not easy to penetrate the bony structure. By using the surgical drill of the invention, an intact bony plate between the implant and sinus membrane is more likely to obtain. Another type of the surgical drill of the invention can turn a tapered socket into a straight one at the posterior mandible.

    摘要翻译: 本发明涉及一种用于截骨术的外科手术钻头。 外科钻头包括:柄,基部,切割刀片,非切割部分和凹槽。 基部形成在柄上。 切割刀片形成在基部的边缘上。 非切割部形成在基部的顶部。 所述槽形成在所述基部的周边部分上,并且与所述切割刀片相邻并且沿着纵向方向延伸。 根据本发明,外科手术钻头使用一个单个切割刀片来钻出由植入钻头形成的插座。 因为刀片越少,工作速度越慢,因此插座的底部不容易穿透骨骼结构。 通过使用本发明的外科钻头,更有可能获得植入物和窦膜之间的完整骨板。 本发明的另一种类型的外科手术钻可以将锥形插座在后颌下方变成直线形插座。