Methods of synthesis of morphinans
    1.
    发明申请
    Methods of synthesis of morphinans 有权
    吗啡的合成方法

    公开(公告)号:US20090318699A1

    公开(公告)日:2009-12-24

    申请号:US12143608

    申请日:2008-06-20

    申请人: John A. Lawson

    发明人: John A. Lawson

    IPC分类号: C07D489/00

    CPC分类号: C07D489/04

    摘要: The disclosure describes morphinan compounds and methods for their synthesis. Preferred methods according to the disclosure allow for large-scale preparation of diastereomerically enriched morphinans. Preferred methods according to the disclosure may also allow for the preparation of diastereomerically enriched morphinans using less time, and/or using fewer reaction steps, and/or providing better yield than previously used methods for preparing morphinans. The methods disclosed herein find utility in synthetic organic chemistry as well as medicinal chemistry.

    摘要翻译: 本公开描述了吗啡喃化合物及其合成方法。 根据本公开的优选方法允许大规模制备非对映体富集的吗啡喃。 根据本公开的优选方法还可以允许使用更少的时间和/或使用更少的反应步骤和/或提供比以前使用的制备吗啡喃的方法更好的产量来制备非对映体富集的吗啡喃。 本文公开的方法可用于合成有机化学以及药物化学。

    Zoom lens and magnifier utilizing the same
    2.
    发明授权
    Zoom lens and magnifier utilizing the same 失效
    变焦镜头和放大镜利用它

    公开(公告)号:US5703727A

    公开(公告)日:1997-12-30

    申请号:US279059

    申请日:1994-07-22

    CPC分类号: G02B25/008 G02B7/10

    摘要: A zoom lens is described which is quite simple and yet provides a wide (5:1) zoom range. The lens consists of a front focusing negative lens which provides a stationary virtual image for two rear zooming lens groups. These two zooming groups are positive and reimage the object at a camera pickup device. Such zooming groups are of substantially equal focal length and bear equally in the magnification change. The invention includes a magnifier which utilizes the zoom lens and has the mechanical aspects necessary to provide the needed lens motions.

    摘要翻译: 描述了一种变焦镜头,它非常简单,但提供了宽(5:1)的变焦范围。 透镜由前聚焦负透镜组成,为两个后变焦镜头组提供静态虚像。 这两个缩放组是正的,并且在相机拾取装置处重新对对象进行成像。 这种变焦组具有基本相等的焦距并且在放大变化中同样地承受。 本发明包括利用变焦透镜并具有提供所需透镜运动所需的机械方面的放大镜。

    2-piperidinecarboxylic acid derivatives useful as NMDA receptor
antagonists
    3.
    发明授权
    2-piperidinecarboxylic acid derivatives useful as NMDA receptor antagonists 失效
    可用作NMDA受体拮抗剂的2-哌啶羧酸衍生物

    公开(公告)号:US5260286A

    公开(公告)日:1993-11-09

    申请号:US961811

    申请日:1992-10-16

    CPC分类号: C07F9/598 C07F9/592

    摘要: Compounds of formula I ##STR1## wherein X is ##STR2## or .dbd.N--O--, in which R.sub.4 is hydrogen or halogen, R.sub.1, R.sub.2, and R.sub.3 independently represent hydrogen or a C.sub.1-4 alkyl group, and n has a value of zero to four are disclosed. Also disclosed are pharmaceutically acceptable salts of these compounds, pharmaceutical compositions of these compounds or salts with a pharmaceutically acceptable carrier, the use of these materials as N-methyl-D-aspartate receptor antagonists, processes for preparing these compounds and salts, and methods to treat cerebral diseases by administering an effective amount of these compounds, salts or compositions.

    摘要翻译: 式Ⅰ的化合物其中X为X或= NO-,其中R 4为氢或卤素,R 1,R 2和R 3独立地表示氢或C 1-4烷基,并且n的值为零 到四个被公开。 还公开了这些化合物的药学上可接受的盐,这些化合物的药物组合物或与药学上可接受的载体的盐,这些物质用作N-甲基-D-天冬氨酸受体拮抗剂,制备这些化合物和盐的方法和方法 通过施用有效量的这些化合物,盐或组合物来治疗脑疾病。

    Multiple pentaprism scanning device and method
    4.
    发明授权
    Multiple pentaprism scanning device and method 失效
    多重五棱镜扫描装置及方法

    公开(公告)号:US4945287A

    公开(公告)日:1990-07-31

    申请号:US205993

    申请日:1988-06-13

    申请人: John A. Lawson

    发明人: John A. Lawson

    IPC分类号: G02B5/09 G02B26/10

    CPC分类号: G02B5/09 G02B26/108

    摘要: A scanning device for causing a beam of light to be repetitively swept across a surface includes a laser source for providing a beam of laser light and a pentaprism assembly which redirects the beam of light to the surface. The pentaprism assembly includes a support member and a plurality of pentaprism elements positioned around the periphery of the support member. An arrangement is provided for rotating the support member such that successive ones of the plurality of pentaprism elements are brought into the path of the beam of light and redirect the beam of light to the surface. Movement of each pentaprism element while intersecting the beam of light causes the beam of light to sweep across the surface. The scanning device may also be used without a laser source to scan ambient light which is reflected from a surface and direct the light to a detector.

    Optical system for imaging an electrophotographic member
    5.
    发明授权
    Optical system for imaging an electrophotographic member 失效
    用于对电子照相构件成像的光学系统

    公开(公告)号:US4493549A

    公开(公告)日:1985-01-15

    申请号:US538942

    申请日:1983-10-04

    摘要: A digital plate maker system to receive graphics and text data and selectively discharge incremental areas of a charged electrophotographic member to form thereon the latent images represented by the graphics and text data, the imaged member thereafter being toned and output from the system. Thereafter, the toned image may be fused on the member and the member being used in an offset lithographic printing press. The digital platemaker system includes an optical system which may form a maximum of 22 individual rays which are direct deflected twice through a field flattening lens and then onto the charged member. The optical system further includes an optical scale or grating which provides electrical signals indicating the precise location of the individual rays along scan lines on the member. The digital plate maker system further includes an electronic system which generates electrical signals to form the 22 individual rays. The text data is used to modulate signals produced by the graphics data, the result of the modulation being the beam control signals used to form the 22 individual rays. The digital plate maker system further includes a toning system which provides a vertical meniscus which is essentially stationary with the electrophotographic member as the electrophotographic member is rotated past the toning station.

    摘要翻译: 一种用于接收图形和文本数据并选择性地排出充电的电子照相构件的增量区域以在其上形成由图形和文本数据表示的潜像的数字印版制作系统,其后成像的构件被调色并从系统输出。 此后,调色图像可以熔合在构件和用于胶印平版印刷机中的构件上。 数字制版系统包括一个光学系统,其可以形成最多22个单独的光线,其直接偏转两次通过场平坦化透镜,然后到达带电部件。 光学系统还包括光标或光栅,其提供指示单个光线沿着该部件上的扫描线的精确位置的电信号。 数字印版制造系统还包括一个产生电信号以形成22个单独光线的电子系统。 文本数据用于调制由图形数据产生的信号,调制结果是用于形成22个单独光线的光束控制信号。 数字印版制造系统还包括调色系统,其提供垂直弯液面,当电子照相构件旋转经过调色台时,其垂直弯液面基本上与电子照相构件固定。

    N-Sec-alkyl analogs of norcodeine and normorphine and analgesic
compositions and methods employing the normorphine derivatives
    6.
    发明授权
    N-Sec-alkyl analogs of norcodeine and normorphine and analgesic compositions and methods employing the normorphine derivatives 失效
    不可卡因和正诺啡的N-间 - 烷基类似物和止痛组合物和使用正诺啡诺衍生物的方法

    公开(公告)号:US4269843A

    公开(公告)日:1981-05-26

    申请号:US166948

    申请日:1980-07-08

    IPC分类号: C07D489/02 A61K31/485

    CPC分类号: C07D489/02

    摘要: Novel N-sec-alkyl derivatives of norcodeine and normorphine wherein the sec-alkyl group contains either four or five carbon atoms. Specifically included are those derivatives of norcodeine and normorphine wherein the sec-alkyl group is 2-butyl, 3-pentyl, .alpha.-methylallyl and .alpha.-methylcyclopropylmethyl. The normorphine derivatives having strong agonist potency combined with strong antagonist qualities and indicated low addiction potential. The norcodeine analogs are useful as intermediates in preparing the corresponding normorphine compounds.

    摘要翻译: 新奇的诺可可碱和正诺啡的N-仲烷基衍生物,其中仲烷基含有四个或五个碳原子。 具体包括那些不可可碱和正诺啡的衍生物,其中仲烷基是2-丁基,3-戊基,α-甲基烯丙基和α-甲基环丙基甲基。 具有强激动剂效力的强啡肽衍生物与强烈的拮抗剂质量相结合并表明低成瘾潜能。 不可食用类似物可用作制备相应的吗啡化合物的中间体。

    Wide angle objective
    7.
    发明授权
    Wide angle objective 失效
    广角目标

    公开(公告)号:US3975090A

    公开(公告)日:1976-08-17

    申请号:US492413

    申请日:1974-07-29

    申请人: John A. Lawson

    发明人: John A. Lawson

    CPC分类号: G02B13/00 G02B13/04 G02B7/10

    摘要: A wide angle lens of the retrofocus type comprising six lens groups in front and rear groupings. The rear grouping is movable forward while the front grouping is stationary to focus the lens to within ten equivalent focal lengths of the lens.

    摘要翻译: 后焦点类型的广角镜头包括前组和后组中的六个透镜组。 后分组可以向前移动,而前分组是静止的,以将透镜聚焦在透镜的十个等效焦距内。

    Orally active nonaddicting analgesics
    8.
    发明授权
    Orally active nonaddicting analgesics 失效
    口服活性止痛镇痛药

    公开(公告)号:US5366979A

    公开(公告)日:1994-11-22

    申请号:US534702

    申请日:1990-06-07

    申请人: John A. Lawson

    发明人: John A. Lawson

    CPC分类号: A61K31/485 Y10S514/816

    摘要: Analgesic compositions containing stereoisomerically pure normorphine and norcodeine derivatives or pharmaceutically acceptable acid addition salts thereof are described. Methods of administering the novel compositions to achieve analgesia are described as well.

    摘要翻译: 描述了含有立体异构纯的正吗啡和不可可食衍生物或其药学上可接受的酸加成盐的止痛组合物。 还描述了施用该组合物以达到镇痛的方法。

    Benzomorphans useful as NMDA receptor antagonists
    9.
    发明授权
    Benzomorphans useful as NMDA receptor antagonists 失效
    Benzomorphans可用作NMDA受体拮抗剂

    公开(公告)号:US5354758A

    公开(公告)日:1994-10-11

    申请号:US991365

    申请日:1992-12-16

    IPC分类号: C07D221/26 A61K31/445

    CPC分类号: C07D221/26

    摘要: Compounds of the formula I ##STR1## are disclosed. In this formula, R is a member selected from the group consisting of --CR.sub.1 R.sub.2 R.sub.3, hydroxy, an alkoxy group having 1 to 4 carbon atoms and --NR.sub.4 R.sub.5, in which at most one of R.sub.1, R.sub.2 and R.sub.3 is hydrogen and the remainder are each independently selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, a cycloalkylalkyl having 4 to 9 carbon atoms and a 3 to 6 membered cyclic ether; R.sub.4 and R.sub.5 are each independently hydrogen or an alkyl group having 1 to 4 carbon atoms; R.sub.6 and R.sub.7 are each independently hydrogen or an alkyl group having 1 to 4 carbon atoms; and R.sub.8 is hydrogen, an alkyl group having 1 to 4 carbon atoms, hydroxy, an alkoxy group having 1 to 4 carbon atoms or halogen. Salts of these compounds are also disclosed. Also disclosed are pharmaceutical compositions of these compounds with a pharmaceutically acceptable carrier, the use of these materials as N-methyl-D-aspartate receptor antagonists, processes for preparing these compounds and salts, and methods to treat cerebral diseases by administering an effective amount of these compounds, salts or compositions.

    摘要翻译: 公开了式I的化合物。 在该式中,R是选自-CR 1 R 2 R 3,羟基,具有1至4个碳原子的烷氧基和-NR 4 R 5的成员,其中R 1,R 2和R 3中至多一个是氢,其余各自是 独立地选自碳原子数1〜4的烷基,碳原子数2〜4的烯基,碳原子数2〜4的炔基,碳原子数3〜7的环烷基,环烷基烷基, 4至9个碳原子和3至6元环醚; R4和R5各自独立地为氢或具有1至4个碳原子的烷基; R6和R7各自独立地为氢或具有1至4个碳原子的烷基; R8为氢,碳原子数为1〜4的烷基,羟基,碳原子数1〜4的烷氧基或卤素。 还公开了这些化合物的盐。 还公开了具有药学上可接受的载体的这些化合物的药物组合物,这些材料用作N-甲基-D-天冬氨酸受体拮抗剂,制备这些化合物和盐的方法,以及通过施用有效量的 这些化合物,盐或组合物。

    Multiple image transfer camera system
    10.
    发明授权
    Multiple image transfer camera system 失效
    多图像传输摄像系统

    公开(公告)号:US5055863A

    公开(公告)日:1991-10-08

    申请号:US546099

    申请日:1990-06-29

    IPC分类号: G03B17/48 G03B19/12

    CPC分类号: G03B17/48 G03B19/12

    摘要: A camera system for the simultaneous and substantially exact capturing of images of a subject on separate image reproduction mediums wherein an optical member is interposed between a lens group and a pair of separate, discrete image receiving mediums. One of the mediums is a photographic film and the other is a viewing screen for personal viewing or, alternatively, an electronic system for electronic signal generation, electronic viewing and electronic capture of the image. The optical member allows light rays emanating from the object to pass therethrough to impinge upon one of the mediums while simultaneously reflecting light rays to the second medium. This system allows for the simultaneous transfer and reproduction of the object image onto more than one medium without degradation of the image or depth of field. The system accomplishes the multiple image transfer through a stationary device, thereby eliminating the necessity of moving parts. The system also eliminates problems resulting from refractions of light normally accompanying light ray direction control devices.

    摘要翻译: 一种相机系统,用于在单独的图像再现介质上同时且基本上精确地拍摄被摄体的图像,其中光学构件插入在透镜组和一对分离的离散图像接收介质之间。 其中一种媒体是摄影胶片,另一种是用于个人观看的观看屏幕,或者替代地,用于电子信号产生,电子观看和电子捕获图像的电子系统。 光学构件允许从物体发出的光线通过其中以撞击在一种介质上,同时将光线反射到第二介质。 该系统允许将对象图像同时传送和再现到多于一种介质上,而不会降低图像或景深。 该系统通过固定装置实现多次图像传输,从而消除了移动部件的必要性。 该系统还消除了通常伴随光线方向控制装置的光的折射引起的问题。