Piperidine and piperazine derivatives possessing affinity at 5ht-1 type receptors

    公开(公告)号:US20050176724A1

    公开(公告)日:2005-08-11

    申请号:US10504114

    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, indolyl, quinolinyl, quinazolinyl, indazolyl or isoquinolinyl; X is carbon, Y is CH and ═ is a double bond; or X is CH, Y is CH2 or oxygen and ═ is a single bond; or X is nitrogen, Y is CH2 and ═ is a single bond; R1 is halogen, cyano, nitro, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy, C3-7heterocyclylC1-6alkyl, C3-7heterocyclyl C1-6alkoxy; a is 0, 1, 2, 3 or 4; R2 is either: halogen, —CN, an optionally substituted C3-7cycloalkyl, an optionally substituted aryl or an optionally substituted C-linked 3-7 membered heterocyclic group; or a group -(Z)b-B wherein: (i) Z is oxygen, CH2, C═O, SO2 or C═N—OR3 wherein R3 is hydrogen or C1-6alkyl; b is 1, 2, or 3; and B is hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or NR4R5 wherein R4 and R5 are independently hydrogen, C1-6alkyl, C3-7cycloalkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl or C1-6alkylcarbamoyl, or R4 and R5, together with the nitrogen atom to which they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group; or (ii) Z is oxygen, CH or CH2, b is 1, and B forms the rest of an aryl or a C3-7heterocyclic group fused to the phenyl ring; excluding 1-[2-[2-(phenylmethyl)phenoxy]ethyl]-4-[(2,3,4-trimethoxyphenyl)methyl]-piperazine and pharmaceutically acceptable salts thereof, and N-[4-[2-[4-[(3,4-dimethoxyphenyl)methyl]-1-piperazinyl]ethoxy]phenyl]-ethanesulfonamide and pharmaceutically acceptable salts thereof. Methods of preparing the compounds and uses of the compounds in therapy, in particular for CNS disorders such as depression and anxiety, are also disclosed.

    Compound possessing affinity at 5ht1-type receptors and use thereof in therapy of cns disorders
    2.
    发明申请
    Compound possessing affinity at 5ht1-type receptors and use thereof in therapy of cns disorders 审中-公开
    在5ht1型受体具有亲和力的化合物及其在治疗cns病症中的用途

    公开(公告)号:US20050107410A1

    公开(公告)日:2005-05-19

    申请号:US10503833

    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; X is carbon, Y is CH and is a double bond; or X is CH, Y is CH2 or oxygen and is a single bond; or X is nitrogen, Y is CH2 and is a single bond; is halogen, hydroxy, cyano, C1-6alkyl, haloC1-6alkyl or C1-6alkoxy; a is 0, 1, 2, 3 or 4; R2 and R3, together with the nitrogen atom to which they are attached, form a nitro group or an optionally substituted 3 to 7 membered heterocyclic group, or R2 and R3 are independently hydrogen, aroyl, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl, arylC1-6alkyl or a group CO(CH2)bNR4R5 wherein b is 1, 2, 3 or 4; and R4 and R5 are independently hydrogen or C1-6alkyl, or R4 and R5, together with the nitrogen atom to they are attached, form part of an optionally substituted 3 to 7 membered heterocyclic group. Methods of preparing the compounds and uses of the compounds in therapy, in particular for CNS disorders such as depression and anxiety, are also disclosed.

    摘要翻译: 公开了式(I)化合物及其药学上可接受的盐:其中:A为任选取代的苯基,萘基,吲哚基,喹啉基,喹唑啉基,吲唑基,异喹啉基或苯并呋喃基; X是碳,Y是CH并且是双键; 或X是CH,Y是CH 2或氧并且是单键; 或X是氮,Y是CH 2,并且是单键; 是卤素,羟基,氰基,C 1-6烷基,卤代C 1-6烷基或C 1-6烷氧基; a是0,1,2,3或4; R2和R3与它们所连接的氮原子一起形成硝基或任选取代的3至7元杂环基,或R 2和R 3独立地是氢,芳酰基,C 1-6 烷基,C 1-6烷酰基,氟代C 1-6烷酰基,C 1-6烷基磺酰基,氟代C 1-6烷基, 烷基磺酰基,氨基甲酰基,C 1-6烷基氨基甲酰基,芳基C 1-6 - 烷基或基团CO(CH 2)2 bRR 4 R 5,其中b 是1,2,3或4; 并且R 4和R 5独立地为氢或C 1-6烷基,或者R 4和R 5与它们连接的氮原子一起形成任选取代的3至7元杂环基的一部分。 还公开了制备化合物的方法和化合物在治疗中的用途,特别是CNS障碍如抑郁和焦虑。

    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.

    STREAMING DIGITAL MEDIA BOOKMARK CREATION AND MANAGEMENT

    公开(公告)号:US20180047429A1

    公开(公告)日:2018-02-15

    申请号:US15673641

    申请日:2017-08-10

    申请人: Paul Smith

    发明人: Paul Smith

    摘要: A user can quickly and efficiently create, edit, search, playback and share bookmarks in one or more videos that are pre-recorded or being recorded or streaming live. The bookmark includes reference to a portion of the video for an amount of time. The bookmark portions may not include a specified end time. The bookmark may include the source of the video, a start time of the bookmarked portion of the video stream or file, a length of the referenced video portion, and content such as text, emoticons, or other content received from a user that creates, edits, or manages the bookmark. The bookmarks may be grouped together into a set of bookmarks, thereby forming an edit of the original streaming or pre-recorded videos when played sequentially, wherein the edit includes a set of bookmarked video portions (bookmarked videos) taken from one or more particular live streaming or pre-recorded videos.

    Low profile mount for flat panel electronic display
    8.
    发明授权
    Low profile mount for flat panel electronic display 有权
    薄型安装用于平板电子显示屏

    公开(公告)号:US09109742B2

    公开(公告)日:2015-08-18

    申请号:US13061910

    申请日:2009-08-31

    申请人: Paul Smith

    发明人: Paul Smith

    IPC分类号: H04N5/64 F16M13/02 F16M11/10

    摘要: A low-profile mount for a flat panel electronic display that is selectively shiftable between a wall-confronting position wherein the back of the flat panel electronic display is disposed parallel and proximate to the wall surface and a tilt position wherein the top of the display is tilted away from the wall surface. The mount is configured so that points spaced apart forwardly from display receiving surfaces of the mount are shifted along a substantially horizontal axis as the mount is shifted between the wall confronting position and the tilt position. Advantageously, the display can be attached to the mount so that the points are horizontally registered with a center of gravity of the display such that the display is self-balancing at any point along the travel between the wall confronting position and the tilt position.

    摘要翻译: 一种用于平板电子显示器的薄型安装件,其可在壁对面位置之间选择性地移动,其中平板电子显示器的背面平行并靠近壁表面,以及倾斜位置,其中显示器的顶部为 倾斜远离墙面。 安装件被构造成使得当安装件在壁面相对位置和倾斜位置之间移动时,使得从安装件的显示器接收表面向前间隔开的点沿着基本上水平的轴线移动。 有利地,显示器可以附接到安装件,使得点与显示器的重心水平地对准,使得显示器在沿着面向对面的位置和倾斜位置之间的行进的任何点处是自平衡的。

    CUTTING TOOL WITH CIRCULATING WIRE
    10.
    发明申请
    CUTTING TOOL WITH CIRCULATING WIRE 有权
    带循环线的切割工具

    公开(公告)号:US20130211403A1

    公开(公告)日:2013-08-15

    申请号:US13763220

    申请日:2013-02-08

    IPC分类号: A61B18/04

    摘要: A medical device and related method of use for cutting tissue is described. The device includes an elongate tubular member having a proximal end, a distal end, and first and second lumens extending between the proximal and distal ends. The device further includes a first elongate arm having a third lumen extending distally from the first lumen and a second elongate arm having a fourth lumen extending distally from the second lumen. A cutting element extends from the third lumen of the first arm to the fourth lumen of the second arm, such that the cutting element is slidably disposed in at least one of the third and fourth lumens.

    摘要翻译: 描述了用于切割组织的医疗装置和相关的使用方法。 该装置包括具有近端,远端以及在近端和远端之间延伸的第一和第二腔的细长管状构件。 该装置还包括具有从第一内腔向远侧延伸的第三腔的第一细长臂和具有从第二腔向远侧延伸的第四腔的第二细长臂。 切割元件从第一臂的第三腔延伸到第二臂的第四腔,使得切割元件可滑动地设置在第三和第四腔中的至少一个腔中。