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    Benzomorphans useful as NMDA receptor antagonists
    1.
    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

    申请人： John A. Lawson ,  Itsuo Uchida

    发明人： John A. Lawson ,  Itsuo Uchida

    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。

    Treatment of chemical dependency with substantially nonaddicting normorphine and norcodeine derivatives
    2.
    发明授权
    Treatment of chemical dependency with substantially nonaddicting normorphine and norcodeine derivatives 有权
    治疗化学依赖性与基本上不接受的吗啡和norcodeine衍生物

    公开(公告)号：US07629355B2

    公开(公告)日：2009-12-08

    申请号：US10967098

    申请日：2004-10-14

    申请人： John A. Lawson

    发明人： John A. Lawson

    IPC分类号： A61K31/44

    CPC分类号： A61K31/44

    摘要： A method is provided for treating a drug-dependent individual so as to effect withdrawal from a drug of abuse, e.g., an opiate such as heroin or oxycodone, a stimulant such as cocaine, or alcohol. The method involves substitution therapy wherein a substantially nonaddicting normorphine or norcodeine derivative is substituted for the drug of abuse. The active agent has the structure of formula (I) wherein: R is H, alkyl, or acyl; X is CH(OR′) or C═O, wherein R′ is H or acyl; α is an optional double bond, with the proviso that when α is present, then X is necessarily CH(OH), or an acid addition salt thereof, wherein preferred such agents are in a stereoisomerically pure form that corresponds to that of N-[(1R)-1-cyclopropylethyl]-normorphine (1) which melts at approximately 188° C.-189° C.

    摘要翻译： 提供了一种治疗依赖于药物的个体以便实现从滥用药物中撤出的方法，例如鸦片剂，例如海洛因或羟考酮，兴奋剂如可卡因或酒精。 该方法涉及替代疗法，其中基本上不可接受的吗啡或不可可食衍生物代替滥用药物。 活性剂具有式（I）的结构，其中：R为H，烷基或酰基; X是CH（OR'）或C-O，其中R'是H或酰基; α是任选的双键，条件是当存在α时，则X必须是CH（OH）或其酸加成盐，其中优选的这样的试剂是立体异构体纯的形式，其对应于N- [ （1R）-1-环丙基乙基] - 吗啡（1），其在约188℃-189℃熔化

    Wide angle objective
    3.
    发明授权
    Wide angle objective 失效
    广角目标

    公开(公告)号：US4099849A

    公开(公告)日：1978-07-11

    申请号：US492403

    申请日：1974-07-29

    申请人： John A. Lawson ,  Ellis I. Betensky

    发明人： John A. Lawson ,  Ellis I. Betensky

    IPC分类号： G02B9/62 ,  G02B13/06 ,  G02B9/64

    CPC分类号： G02B13/06 ,  G02B9/62

    摘要： This disclosure relates to a Wide Angle Lens of the retrofocus type having a new lens group arrangement which comprises from the object end to the image end a first negative group, a second negative group in the form of a meniscus having a concave image side surface, a third positive group having a convex object side surface, a fourth positive group having a convex image side surface, a fifth negative group, and a sixth positive group having convex image and object side surfaces.

    摘要翻译： 本公开涉及一种具有新的透镜组布置的反向聚焦型广角镜，其包括从目标端到图像端的第一负极组，具有凹面像侧面的弯液面形式的第二负极组， 具有凸面物侧表面的第三正极组，具有凸像侧面的第四正极组，第五负极组和具有凸形图像和物体侧表面的第六正组。

    Orally active nonaddicting analgesics
    4.
    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

    IPC分类号： A61K31/485 ,  A61P25/04 ,  C07D489/02 ,  A61K31/44

    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。

    Multiple image transfer camera system
    5.
    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

    申请人： Jerome W. Lindenfelser ,  John A. Lawson

    发明人： Jerome W. Lindenfelser ,  John A. Lawson

    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。

    Orally active nonaddicting analgesics
    6.
    发明授权
    Orally active nonaddicting analgesics 失效
    口服活性止痛镇痛药

    公开(公告)号：US4749706A

    公开(公告)日：1988-06-07

    申请号：US843150

    申请日：1986-03-24

    申请人： John A. Lawson ,  Joseph I. DeGraw ,  Gilda H. Loew

    发明人： John A. Lawson ,  Joseph I. DeGraw ,  Gilda H. Loew

    IPC分类号： C07D489/00 ,  A61K31/485 ,  A61P25/04 ,  C07D489/02

    CPC分类号： C07D489/02

    摘要： Stereoisomerically pure forms of normorphine analogs which have superior analgesic and nonaddicting qualities are described. In addition, a method of separating diastereomeric forms of N-sec-alkyl-substituted analogs utilizes the hydrocarbyl(1-8C) diesters of the normorphine derivatives. A new method for preparing the N-methylalkylmethyl derivatives of normorphine and norcodeine and their conventional analogs is also disclosed. This method employs the corresponding methyl alkyl ketones and a reducing agent.

    摘要翻译： 描述了具有优异的止痛和不耐受品质的立体异构体纯形式的吗啡类似物。 此外，分离N-仲烷基取代的类似物的非对映异构形式的方法利用了吗啡衍生物的烃基（1-8C）二酯。 还公开了用于制备正诺啡和不可可碱的N-甲基烷基甲基衍生物及其常规类似物的新方法。 该方法采用相应的甲基烷基酮和还原剂。