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    Cyclic hydroxamic acids
    2.
    发明授权
    Cyclic hydroxamic acids 失效
    循环羟基酸

    公开(公告)号：US5234933A

    公开(公告)日：1993-08-10

    申请号：US785927

    申请日：1991-10-31

    申请人： Lawrence J. Marnett ,  Kenneth V. Honn ,  Carl R. Johnson ,  Yung-fa Chen ,  Katsu-ichi Shimoji

    发明人： Lawrence J. Marnett ,  Kenneth V. Honn ,  Carl R. Johnson ,  Yung-fa Chen ,  Katsu-ichi Shimoji

    IPC分类号： C07D211/94

    CPC分类号： C07D211/94

    摘要： Novel cyclic hydroxamic acids of the general formula: ##STR1## wherein ring A is 5- or 6-membered; R.sup.1, R.sup.2 and R.sup.3 each, ipendently, is hydrogen, C1-24 alkyl, C2-24 alkenyl or a group of the formula: ##STR2## wherein R.sup.4, R.sup.5, R.sup.7 and R.sup.8 each, independently is hydrogen,C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, halogen or nitro; l is 1-3; m is 1-3; n is 1-3; k is 1-3;R.sup.6 and R.sup.9 each, independently is C1-24 alkylene or C2-24 alkenylene;With the proviso that, more than one of R.sup.1, R.sup.2 and R.sup.3 are not hydrogen at the same time; and the pharmaceutically acceptable salts thereof possesses an inhibitory activity against 12-lipoxygenase, and therefore, may be useful for treating and/or preventing inflammation, immune diseases, psoriasis, arteriosclerosis and/or ischaemic cardiovascular diseases and also for suppressing metastasis of cancer.

    摘要翻译： 新型环状异羟肟酸，其通式为：其中环A为5-或6-元; R1，R2和R3各自独立地是氢，C1-24烷基，C2-24链烯基或下式的基团：其中R4，R5，R7和R8各自独立地是氢，C1- 4烷基，C 1-4烷氧基，三氟甲基，卤素或硝基; l为1-3; m为1-3; n为1-3; k为1-3; R6和R9各自独立地为C1-24亚烷基或C2-24亚烯基; 条件是，R1，R2和R3中的一个以上不是同时为氢; 其药学上可接受的盐具有对12-脂肪氧合酶的抑制活性，因此可用于治疗和/或预防炎症，免疫疾病，牛皮癣，动脉硬化和/或缺血性心血管疾病，也可用于抑制癌转移。

    Process for the preparation of a R-alpha cyclopentenones and R-alpha and R-omega cyclopentanoids
    5.
    发明授权
    Process for the preparation of a R-alpha cyclopentenones and R-alpha and R-omega cyclopentanoids 失效
    制备R-α环戊烯酮和R-α和R-ω环戊烷的方法

    公开(公告)号：US5359110A

    公开(公告)日：1994-10-25

    申请号：US155589

    申请日：1993-11-16

    申请人： Carl R. Johnson ,  Matthew P. Braun

    发明人： Carl R. Johnson ,  Matthew P. Braun

    IPC分类号： C07F7/18 ,  C07F7/08

    CPC分类号： C07F7/1892 ,  Y02P20/55

    摘要： A process for the preparation of R.alpha.-cyclopentenoids and then R.alpha., R.omega.-cyclopentanoids is described. The process involves the reaction of a compound of the formula ##STR1## where X is halo, particularly Br or I and P is a protecting group with an alkylborane to produce the R.alpha.-cyclopentenone. The R.alpha.-cyclopentenone is reacted with a R.omega. cuprate to produce the R.alpha., R.omega.-cyclopentenoid. The process is used for the preparation of prostaglandins which are known pharmaceutically active compounds.

    摘要翻译： 描述了制备Rα-环戊二烯并且然后制备Rα，Rω-环戊二烯的方法。 该方法涉及下式化合物的反应：其中X是卤素，特别是Br或I，P是具有烷基硼烷的保护基，以产生Rα-环戊烯酮。 Rα-环戊烯酮与R omega cuprate反应产生Rα，Rω-环戊烯。 该方法用于制备已知药物活性化合物的前列腺素。

    A.sub.3 adenosine receptor agonists
    6.
    发明授权
    A.sub.3 adenosine receptor agonists 失效
    A3腺苷受体激动剂

    公开(公告)号：US5688774A

    公开(公告)日：1997-11-18

    申请号：US396111

    申请日：1995-02-28

    申请人： Kenneth A. Jacobson ,  Heaok Kim Jeong ,  Suhaib M. Siddiqi ,  Carl R. Johnson ,  John A. Secrist, III ,  Kamal N. Tiwari

    发明人： Kenneth A. Jacobson ,  Heaok Kim Jeong ,  Suhaib M. Siddiqi ,  Carl R. Johnson ,  John A. Secrist, III ,  Kamal N. Tiwari

    IPC分类号： C07H19/16 ,  A61K31/70 ,  C07H19/167 ,  C07H19/173

    CPC分类号： C07H19/16

    摘要： The present invention provides A.sub.3 selective agonists, particularly, adenine compounds having selected substituents at the 2, 6, and 9 positions, and related substituted compounds, particularly those containing substituents on the benzyl and/or uronamide groups, as well as pharmaceutical compositions containing such compounds. The present invention also provides a method of selectively activating an A.sub.3 adenosine receptor in a mammal, which method comprises acutely or chronically administering to a mammal in need of selective activation of its A.sub.3 adenosine receptor a therapeutically or prophylactically effective amount of a compound which binds with the A.sub.3 receptor so as to stimulate an A.sub.3 receptor-dependent response.

    摘要翻译： 本发明提供A3选择性激动剂，特别是在2,6和9位具有选定取代基的腺嘌呤化合物，以及相关的取代化合物，特别是含有苄基和/或脲醛酰胺基团上的取代基的那些，以及含有这些取代基的药物组合物 化合物。 本发明还提供了选择性激活哺乳动物中的A3腺苷受体的方法，该方法包括急性或慢性施用于需要选择性活化其A3腺苷受体的哺乳动物，治疗或预防有效量的与 A3受体，以刺激A3受体依赖性反应。

    Process for the preparation of cyclopentanoids and novel intermediates produced thereby
    7.
    发明授权
    Process for the preparation of cyclopentanoids and novel intermediates produced thereby 失效
    制备环戊烷类的方法和由此制备的新型中间体

    公开(公告)号：US4873360A

    公开(公告)日：1989-10-10

    申请号：US146716

    申请日：1988-01-21

    申请人： Carl R. Johnson ,  Thomas D. Penning

    发明人： Carl R. Johnson ,  Thomas D. Penning

    IPC分类号： C07D317/44

    CPC分类号： C07D317/44

    摘要： Cyclopentanoids (I) of the formula: ##STR1## including stereoisomers are described along with a process for the preparation of I. In particular the preparation of prostanoids of the formula: ##STR2## wherein R.sub.1 is a alkyl group containing 1 to 8 carbon atoms and R.sub.2 CO.sub.2 R.sub.3 is an alkenyl ester group, R.sub.2 contains 2 to 6 carbon atoms and R.sub.3 is a lower alkyl group containing 1 to 6 carbon atoms is described. A particular prostaglandin prepared by the process is PGE.sub.2. The prostanoids have been demonstrated to have pharmacological activity in animals and humans. Novel intermediates of (I) are also described.

    摘要翻译： 本文描述了包含立体异构体的式（I）的环戊烷类（I）以及制备I的方法。特别是下式的前列腺素的制备：其中R1是含有1至 8个碳原子，R2CO2R3为链烯基酯基，R2为2-6个碳原子，R3为含1〜6个碳原子的低级烷基。 通过该方法制备的特定前列腺素是PGE2。 前列腺素已被证明在动物和人体中具有药理活性。 还描述了（I）的新型中间体。

    Belt tensioning apparatus for belt/pulley drive system
    8.
    发明授权
    Belt tensioning apparatus for belt/pulley drive system 失效
    皮带/皮带轮驱动系统皮带张紧装置

    公开(公告)号：US4568318A

    公开(公告)日：1986-02-04

    申请号：US709336

    申请日：1985-03-07

    申请人： Carl R. Johnson ,  Ramon Pareja

    发明人： Carl R. Johnson ,  Ramon Pareja

    IPC分类号： F16H7/14 ,  F16H7/10

    CPC分类号： F16H7/14

    摘要： A mechanical drive mechanism of the endless belt and pulley type having an improved belt tensioning arrangement. The shaft of the machine being driven (or that of the driving member itself) is eccentrically journaled with respect to its cylindrical bearing hub and a rigid arm having a first bore therethrough is disposed with the hub of the machine centered in that first bore. Located at the opposed end of the rigid arm is a parallel bore in which the other drive or driven shaft is journaled. Because of the eccentricity between the first shaft and its hub, as the arm is rotated about the hub as a center, the distance between the centers of the driving and driven shafts is increased or decreased, depending upon the direction of rotation of the rigid arm. As such, the tension of the endless belt coupling the drive and driven pulleys can be varied. The construction of the belt and pulley combination lends itself to being completely enclosed in a protective shroud which need not be removed to make the tensioning adjustment.

    摘要翻译： 环带和皮带轮的机械驱动机构具有改进的带张紧装置。 被驱动的机器的轴（或驱动构件本身的轴）相对于其圆柱形轴承座偏心地轴颈，并且具有穿过其中的第一孔的刚性臂设置在机器的轮毂以该第一孔为中心。 位于刚性臂的相对端的是平行的孔，其中另一个驱动轴或从动轴是轴颈。 由于第一轴和其轮毂之间的偏心度，当臂以毂为中心旋转时，根据刚性臂的旋转方向，驱动轴和从动轴的中心之间的距离增大或减小 。 因此，可以改变联接驱动轮和从动带轮的环形带的张力。 皮带和皮带轮组合的结构使其完全封闭在保护罩中，不需要将其去除以进行张紧调节。