Heterocyclic compounds possessing affinity at 5ht1-type receptors and use thereof in therapy

    公开(公告)号:US20050085458A1

    公开(公告)日:2005-04-21

    申请号:US10504109

    申请日:2003-02-17

    摘要: Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed: wherein A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; b is 1, 2 or 3 and c is 1, 2 or 3, wherein b+c is 2, 3, 4 or 5; X is carbon, Y is CH, is a double bond and e is 0; or X is carbon, Y is CH2 or oxygen, is a single bond and e is 1; or X is nitrogen, Y is CH2, is a single bond and e is 0; R1 is hydrogen, cyano, halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, NHCOCH3 or OCONR5R6, wherein R5 and R6 are independently hydrogen or C1-6alkyl; R2 is halogen, cyano or C1-6alkoxy; d is 0, 1, 2 or 3; R3 is hydrogen, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl or arylC1-6alkyl; and R4, together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring, provided that when a compound of formula (I) has the following structure: wherein A, b, c, R1, e, X, Y, R2 and d are as defined above and R3 is hydrogen, C1-6alkyl or arylC1-6alkyl, then (i) X is carbon, Y is CH and is a double bond; or (ii) b and c are both 1; or (iii) the carbon atom adjacent to the oxo-substituted carbon atom in the morpholinyl ring, marked “*”, is substituted. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.

    Device for measuring incident light in a body cavity
    2.
    发明授权
    Device for measuring incident light in a body cavity 失效
    用于测量体腔内的入射光的装置

    公开(公告)号:US5575751A

    公开(公告)日:1996-11-19

    申请号:US294892

    申请日:1994-08-22

    CPC分类号: A61B18/24 A61N5/0601

    摘要: A device for measuring incident light in a remote situs such as a body cavity which includes a central tubular member through which light is delivered to the remote situs and one or more auxiliary tubular members through which incident light in the remote situs is transmitted to a light detector. Each auxiliary tubular member receives incident light from a different portion of the remote situs. The apparatus is particularly useful for conducting phototherapy in body cavities and has been demonstrated in the phototherapy treatment of superficial cancer in a bladder.

    摘要翻译: 用于测量诸如体腔的远程位置中的入射光的装置,其包括中心管状构件,光通过该中心管状构件传送到远程位置,以及一个或多个辅助管状构件,远程位置中的入射光通过该辅助管状构件传递到光 探测器。 每个辅助管状构件接收来自远程位置的不同部分的入射光。 该装置对于在体腔中进行光疗特别有用,并且已在膀胱中浅层癌症的光疗治疗中得到证实。

    Method for measuring incident light in a body cavity
    3.
    发明授权
    Method for measuring incident light in a body cavity 失效
    测量体腔入射光的方法

    公开(公告)号:US5730700A

    公开(公告)日:1998-03-24

    申请号:US592440

    申请日:1996-01-26

    IPC分类号: A61B18/24 A61N5/06 A61B1/07

    CPC分类号: A61B18/24 A61N5/0601

    摘要: An obturator for measuring incident light in a remote situs such as a body cavity which includes a treatment tubular member through which light is delivered to the remote situs and one or more auxiliary tubular members through which incident light in the remote situs is transmitted to an external light detector. The treatment and auxiliary tubular members are attached to a connector element which is in turn connected to a cystoscope lens port. The treatment and auxiliary tubular members are aligned off-center with respect to the central axis of the obturator so that a cystoscope lens can be inserted in the lens port and pass through the axial center of the obturator. Each auxiliary tubular member receives incident light from a different portion of the remote situs. The apparatus is particularly useful for conducting phototherapy in body cavities and has been demonstrated in the phototherapy treatment of superficial cancer in the bladder.

    摘要翻译: 用于测量诸如体腔的远程位置中的入射光的闭孔器,其包括处理管状构件,光通过该管状构件传送到远程位置,以及一个或多个辅助管状构件,通过该一个或多个辅助管状构件将远程位置的入射光透射到外部 光检测器 治疗和辅助管状构件附接到连接器元件,该连接器元件又连接到膀胱镜透镜端口。 处理和辅助管状构件相对于闭孔器的中心轴线偏离中心,使得可以将透镜端口中的透镜镜头插入并穿过闭塞器的轴向中心。 每个辅助管状构件接收来自远程位置的不同部分的入射光。 该装置对于在体腔中进行光疗特别有用,并已在膀胱中浅层癌症的光疗治疗中得到证实。

    Irradiance attachment for an optical fiber to provide a uniform level of
illumination across a plane
    4.
    发明授权
    Irradiance attachment for an optical fiber to provide a uniform level of illumination across a plane 失效
    用于光纤的辐射附件,以提供跨平面的均匀的照明水平

    公开(公告)号:US5519534A

    公开(公告)日:1996-05-21

    申请号:US248918

    申请日:1994-05-25

    摘要: A irradiation attachment for an optical fiber which provides an output of light that has a highly uniform intensity. The device includes a hollow spherical shell having a diffusive reflective surface or target supported therein. Light is directed into the hollow spherical shell so that it reflects off the diffusive reflective surface or target. The reflected light is internally reflected off the inner surface of the hollow spherical shell several times before passing through an output aperture. As a result of the internal reflection within the hollow spherical shell, the light leaving the device has a highly uniform intensity. The device is particularly useful for photodynamic therapy.

    摘要翻译: 用于光纤的照射附件,其提供具有高度均匀强度的光的输出。 该装置包括具有支撑在其中的漫射反射表面或靶的中空球壳。 光被引导到中空球壳中,使得其反射离开漫射反射表面或靶。 在通过输出孔之前,反射光在中空球壳的内表面内部被反射几次。 由于在空心球壳内的内部反射,离开设备的光具有高度均匀的强度。 该装置对光动力疗法特别有用。

    Laparoscopic SAC holder assembly
    5.
    发明授权
    Laparoscopic SAC holder assembly 有权
    腹腔镜SAC支架组件

    公开(公告)号:US06419639B2

    公开(公告)日:2002-07-16

    申请号:US09368824

    申请日:1999-08-05

    IPC分类号: B16B1000

    摘要: This invention relates to a surgical device and methods for accessing and retrieving a tissue mass from a body cavity through a minimally invasive laparoscopic procedure. The device consists of a handle comprising an inner rod, which is rotatably engaged within a tubular member, and a loop adapted to hold a surgical bag. The loop comprises first and second bowed leaf elements, wherein the first bowed leaf element is attached to the inner rod and the second bowed leaf element is attached to the tubular member. The device further has a rotatable articulation, such as a hinge, joining the first and second bowed leaf elements, wherein rotation of the inner rod causes the first bowed leaf element to rotate about the articulation, such that the surgical bag may be opened and closed by rotation of the inner rod.

    摘要翻译: 本发明涉及一种通过微创腹腔镜手术从体腔进入和取回组织块的手术装置和方法。 该装置包括手柄,该手柄包括可旋转地接合在管状构件内的内杆和适于保持手术袋的环。 该环包括第一和第二弓形叶元件,其中第一弓形叶元件附接到内杆,并且第二弓形叶元件附接到管状构件。 该装置还具有连接第一和第二弓形叶片元件的可旋转关节,例如铰链,其中内杆的旋转使得第一弓形叶片元件围绕关节运动旋转,使得外科手术袋可以被打开和关闭 通过内杆的旋转。

    Device for measuring incident light in a body cavity
    6.
    发明授权
    Device for measuring incident light in a body cavity 失效
    用于测量体腔内的入射光的装置

    公开(公告)号:US5505687A

    公开(公告)日:1996-04-09

    申请号:US395005

    申请日:1995-02-27

    CPC分类号: A61B18/24 A61N5/0601

    摘要: An obturator for measuring incident light in a remote situs such as a body cavity which includes a treatment tubular member through which light is delivered to the remote situs and one or more auxiliary tubular members through which incident light in the remote situs is transmitted to an external light detector. The treatment and auxiliary tubular members are attached to a connector element which is in turn connected to a cystoscope lens port. The treatment and auxiliary tubular members are aligned off-center with respect to the central axis of the obturator so that a cystoscope lens can be inserted in the lens port and pass through the axial center of the obturator. Each auxiliary tubular member receives incident light from a different portion of the remote situs. The apparatus is particularly useful for conducting phototherapy in body cavities and has been demonstrated in the phototherapy treatment of superficial cancer in the bladder.

    摘要翻译: 用于测量诸如体腔的远程位置中的入射光的闭孔器,其包括处理管状构件,光通过该管状构件传送到远程位置,以及一个或多个辅助管状构件,通过该一个或多个辅助管状构件将远程位置的入射光透射到外部 光检测器 治疗和辅助管状构件附接到连接器元件,该连接器元件又连接到膀胱镜透镜端口。 处理和辅助管状构件相对于闭孔器的中心轴线偏离中心,使得可以将透镜端口中的透镜镜头插入并穿过闭塞器的轴向中心。 每个辅助管状构件接收来自远程位置的不同部分的入射光。 该装置对于在体腔中进行光疗特别有用,并已在膀胱中浅层癌症的光疗治疗中得到证实。