2-(substituted amino) adenosines as antihypertensives
    1.
    发明授权
    2-(substituted amino) adenosines as antihypertensives 失效
    2-(取代氨基)腺苷作为抗高血压药

    公开(公告)号:US5034381A

    公开(公告)日:1991-07-23

    申请号:US193968

    申请日:1988-05-13

    CPC分类号: C07H19/16

    摘要: Disclosed are 2-substituted adenosine derivatives of the formula ##STR1## in which R represents a substituted amino grouping of the formula ##STR2## as defined herein; pharmaceutically acceptable ester derivatives thereof in which free hydroxy groups are esterified in the form of a pharmaceutically acceptable prodrug ester; and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for their preparation; and their use in mammals as therapeutically effective adenosine-2 (A-2) agonists.

    摘要翻译: 公开了式(I)的2-取代腺苷衍生物,其中R表示如本文定义的式IMAGE> IMAGE的取代氨基; 游离羟基以药学上可接受的前药酯的形式酯化的药学上可接受的酯衍生物; 及其药学上可接受的盐; 包含所述化合物的药物组合物; 其准备方法; 以及它们在哺乳动物中作为治疗有效的腺苷-2(A-2)激动剂的用途。

    Imidazo[4,5-b]pyridine derivatives as cardiovascular agents
    2.
    发明授权
    Imidazo[4,5-b]pyridine derivatives as cardiovascular agents 失效
    咪唑并[4,5-b]吡啶衍生物作为心血管药

    公开(公告)号:US4977144A

    公开(公告)日:1990-12-11

    申请号:US405926

    申请日:1989-09-12

    IPC分类号: C07H19/052

    CPC分类号: C07H19/052

    摘要: Disclosed are the compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl or aryl-lower alkyl; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -alkenyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, or optionally lower alkyl substituted (C.sub.3 -C.sub.7 -cycloalkyl, bicycloheptyl, bicycloheptenyl, adamantyl, tetrahydropyranyl or tetrahydrothiopyranyl)-lower alkyl, or diaryl-lower alkyl; R.sub.2 represents hydrogen or lower alkyl; R.sub.3 represents hydroxymethyl or --CONHR.sub.4 in which R.sub.4 represents hydrogen, lower alkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl or hydroxy-lower alkyl; pharmaceutically acceptable ester derivatives thereof in which one or more of the hydroxy groups are esterified in form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; methods of preparation; pharmaceutical compositions; and their use as adenosine-2 agonists in mammals.

    摘要翻译: 公开了式(I)的化合物,其中R表示氢,低级烷基,芳基或芳基 - 低级烷基; 碳原子或杂环芳基 - 低级烷基,C 3 -C 7 - 环烷基或任选的低级烷基取代的(C 3 -C 7 - 环烷基,双环庚基,双环庚烯基,金刚烷基, 四氢吡喃基或四氢噻喃基) - 低级烷基或二芳基 - 低级烷基; R2代表氢或低级烷基; R3表示羟甲基或-CONHR4,其中R4表示氢,低级烷基,芳基 - 低级烷基,C3-C7-环烷基,C3-C7-环烷基 - 低级烷基或羟基 - 低级烷基; 其药学上可接受的酯衍生物,其中一个或多个羟基以药学上可接受的酯的形式酯化; 及其药学上可接受的盐; 准备方法; 药物组合物; 以及它们在哺乳动物中作为腺苷-2激动剂的用途。

    2,3-dihydro-2-(4,5-dihydroimidazol-2-yl)-indoles in composition form for
reducing intraocular pressure
    3.
    发明授权
    2,3-dihydro-2-(4,5-dihydroimidazol-2-yl)-indoles in composition form for reducing intraocular pressure 失效
    2,3-二氢-2-(4,5-二氢咪唑-2-基) - 吲哚,用于降低眼内压

    公开(公告)号:US4908376A

    公开(公告)日:1990-03-13

    申请号:US15820

    申请日:1987-02-17

    IPC分类号: A61K31/415

    CPC分类号: A61K31/415

    摘要: Compounds of the formula ##STR1## wherein each R is hydrogen or one R is hydrogen and the other is lower alkyl, R.sub.1 is hydrogen, lower alkyl, aryl, aralkyl or lower carboalkoxy, R.sub.2 is hydrogen or lower alkyl, and the ring A is unsubstituted or substituted by lower alkyl, lower alkoxy, halo or trifluoromethyl, and pharmaceutically acceptable salts thereof, their preparation, pharmaceutical compositions and the uses thereof, such as .alpha..sub.2 -adrenergic blocking agents, e.g. antidepressants, cognition enhancers and appetite suppressants, and as intraocular pressure reducing agents are disclosed.

    摘要翻译: 式(I)的化合物,其中每个R是氢或一个R是氢,另一个是低级烷基,R 1是氢,低级烷基,芳基,芳烷基或低级烷氧羰基,R 2是氢或低级烷基, 环A是未取代的或被低级烷基,低级烷氧基,卤素或三氟甲基取代,及其药学上可接受的盐,它们的制备,药物组合物及其用途,例如α2-肾上腺素能阻断剂,例如 抗抑郁药,认知增强剂和食欲抑制剂以及作为眼压降低剂。

    Triazoloquinazoline compounds, and their methods of preparation,
pharmaceutical compositions, and uses
    4.
    发明授权
    Triazoloquinazoline compounds, and their methods of preparation, pharmaceutical compositions, and uses 失效
    三唑并喹唑啉化合物及其制备方法,药物组合物和用途

    公开(公告)号:US4713383A

    公开(公告)日:1987-12-15

    申请号:US844447

    申请日:1986-03-26

    IPC分类号: C07D487/04 A61K31/505

    CPC分类号: C07D487/04

    摘要: [1,2,4]triazolo[1,5-c]quinazoline compounds of the formula ##STR1## wherein R.sub.1 is optionally substituted phenyl, pyridyl, furyl thienyl, dihydro or tetrahydro furanyl or thienyl, pyranyl, or 0-ribofuranosyl; R.sub.2 is hydrogen or lower alkyl; X is oxygen or NR.sub.3, R.sub.3 is as defined in the claims, and ring A is unsubstituted or substituted as set forth in the claims. The compounds wherein X is N--R.sub.3 are especially useful as adenosine antagonists and for the treatment of asthma. The compounds wherein X is oxygen are useful as benzodiazepine antagonists and as intermediates in the synthesis of the compounds wherein X is N--R.sub.3.

    摘要翻译: 其中R 1是任选取代的苯基,吡啶基,呋喃基噻吩基,二氢或四氢呋喃基或噻吩基,吡喃基或O-呋喃核糖基的[1,2,4]三唑并[1,5-c]喹唑啉化合物。 R2是氢或低级烷基; X是氧或NR 3,R 3如权利要求中所定义,并且环A是未取代的或如权利要求中所述取代的。 其中X是N-R3的化合物特别可用作腺苷拮抗剂和用于治疗哮喘。 其中X是氧的化合物可用作苯并二氮杂拮抗剂,并且作为合成其中X是N-R 3的化合物的中间体是有用的。

    Auto-up switch for simultaneously retracting a pair of stabilizer legs on a backhoe loader machine
    5.
    发明授权
    Auto-up switch for simultaneously retracting a pair of stabilizer legs on a backhoe loader machine 有权
    自动起动开关,用于同时将一对稳定器支腿缩回到挖土机装载机上

    公开(公告)号:US06481749B2

    公开(公告)日:2002-11-19

    申请号:US09314728

    申请日:1999-05-18

    IPC分类号: B60S902

    CPC分类号: E02F9/085 E02F9/2025

    摘要: Automatic and simultaneous retraction of a pair of stabilizer legs for a backhoe loader machine 10 is beneficial for the operator when operation of the backhoe loader is complete. Instead of retracting the stabilizer legs by manually holding a pair of control switches continuously in a control position, the operator may simply push an auto-up switch with a single, “one-touch” contact. Once the auto-up switch has been activated by the “one-touch” contact, a timer relay is enabled. The timer relay acts independently of the auto-up switch to control the simultaneously retraction of the stabilizer legs without any further contact to the auto-up switch. When the timer relay is enabled, it sends a signal to activate the control switches for a preselected time. The activation of the control switches actuates a pair of solenoid valves which control the movement of the stabilizer legs from any one of a plurality of extended positions to a fully retracted position within the preselected time.

    摘要翻译: 用于挖掘装载机10的一对稳定器腿的自动和同时收回对于操作者在挖掘装载机的操作完成时是有益的。 通过在控制位置上连续地手动保持一对控制开关而不是缩回稳定器支腿,操作者可以简单地用单个“单触”触点推动自动起动开关。 一旦通过“一键式”触点激活了自动启动开关,则启用定时继电器​​。 定时继电器​​独立于自动起动开关进行动作,以控制稳定器支腿的同时回缩,而无需与自动起动开关进一步接触。 当定时器继电器使能时,它发送信号以激活控制开关预选的时间。 控制开关的启动致动一对电磁阀,其控制稳定器腿在预选时间内从多个延伸位置中的任何一个移动到完全缩回位置的运动。

    Cable seal
    6.
    发明授权
    Cable seal 失效
    电缆密封

    公开(公告)号:US5360945A

    公开(公告)日:1994-11-01

    申请号:US693903

    申请日:1991-05-01

    摘要: A re-enterable seal (25) for sealing an elongate object (16) passing through a barrier (24) between two environments (53, 54) includes an invertible enclosing member (30) containing a sealant (40). The sealant (40) is adhered to the inside surface (31) of the enclosing member (30). During insertion of the elongate member (16), the enclosing member (30) is inverted inside-out, with the sealant remaining on the inside surface (31) (now positioned outside the enclosing member). The elongate member (16) is then pulled back, causing the enclosing member (30) to re-invert, and bringing the sealant (40) into sealing compression against the elongate member (16).

    摘要翻译: 用于密封在两个环境(53,54)之间穿过隔离物(24)的细长物体(16)的可重新密封(25)包括容纳密封剂(40)的可逆封闭构件(30)。 密封剂(40)粘附到封闭构件(30)的内​​表面(31)。 在插入细长构件(16)期间,封闭构件(30)内向内翻转,密封剂保留在内表面(31)上(现在位于封闭构件外部)。 然后将细长构件(16)拉回,使包围构件(30)重新反转,并使密封剂(40)抵靠细长构件(16)进行密封压缩。

    Quinolyl or isoquinolyl-lower-alkoxy-phenylene-amino derivatives
    7.
    发明授权
    Quinolyl or isoquinolyl-lower-alkoxy-phenylene-amino derivatives 失效
    喹啉基或异喹啉基 - 低级 - 烷氧基 - 亚苯基 - 氨基衍生物

    公开(公告)号:US4091103A

    公开(公告)日:1978-05-23

    申请号:US699017

    申请日:1976-06-23

    申请人: John E. Francis

    发明人: John E. Francis

    CPC分类号: C07D213/30 C07D215/14

    摘要: New 1-(azacyclic aralkoxyphenyl)-2- or 3-(diphenylalkylamino)-alkanes, e.g those of the formula: ##STR1## R = 5- or 6-membered, mono- or bicyclic, nitrogen-containing aromatic radicalM,n,p= 1-4; r = 1 or 2;R.sub.1 = h or OHor therapeutically acceptable salts thereof are hypotensive and cardioactive agents.

    摘要翻译: 新的1-(氮杂环烷氧基苯基)-2-或3-(二苯基烷基氨基) - 烷烃,例如下式的那些:R = 5-或6-元,单环或双环,含氮芳族基团m,n ,p = 1-4,r = 1或2; R1 = H或OH R = 5-或6-元,单环或双环,含氮芳族基M,N,P = 1-4; R = 1或2; R1 = H或OH或其治疗上可接受的盐是低血压和心脏活性剂。

    Method and apparatus for minimizing loader frame stress
    8.
    发明授权
    Method and apparatus for minimizing loader frame stress 失效
    减轻装载机框架应力的方法和装置

    公开(公告)号:US06363832B1

    公开(公告)日:2002-04-02

    申请号:US09598873

    申请日:2000-06-21

    申请人: John E. Francis

    发明人: John E. Francis

    IPC分类号: F01B2504

    CPC分类号: E02F3/431 E02F9/2203 E02F9/24

    摘要: A method and apparatus for minimizing the loader frame stress induced by the twisting action which results from unequal travel in the actuators. The method includes the use of electro-hydraulics in conjunction with feedback from actuators displacement sensors. Each actuator is controlled by an individual control valve. The amount of extension of each actuator's piston is monitored. Control signals are sent to the control valves which control fluid flow to each actuator to maintain the actuators' piston extensions at the same amount.

    摘要翻译: 一种用于最小化由致动器中不相等的行进引起的扭转作用引起的装载机框架应力的方法和装置。 该方法包括使用电动液压与来自致动器位移传感器的反馈。 每个执行机构均由单独的控制阀控制。 监控每个执行机构活塞的延伸量。 控制信号被发送到控制阀,其控制流向每个致动器的流体流动以将致动器的活塞延伸部维持在相同的量。

    Telecommunications network interface assembly
    9.
    发明授权
    Telecommunications network interface assembly 失效
    电信网络接口组装

    公开(公告)号:US5359654A

    公开(公告)日:1994-10-25

    申请号:US881958

    申请日:1992-05-12

    摘要: Modules integral with the body of the assembly include one for drop wire connections, one for subscriber wire connections, one for an electronics interface, and one for a network interface device. Protective sealant material within the assembly protects contacts from corrosion and other deterioration, and from shorting. Sealant plungers and a chamber containing a compressed gas impose compressive forces upon the sealant material. Shunt plugs associated with two of the modules permit signal transmission across the modules at desired times, and when removed eliminate the possibility of a subscriber being shocked or transmitting a spark when accessing subscriber components of the assembly. The main body and the modules of the assembly preferably are integrally connected and form a unitary sealed assembly.

    摘要翻译: 与组件主体集成的模块包括一个用于分接线连接,一个用于用户线连接,一个用于电子接口,一个用于网络接口设备。 组件内的保护密封剂材料保护接触不受腐蚀和其他变质,并且短路。 密封剂柱塞和包含压缩气体的室对密封剂材料施加压缩力。 与两个模块相关联的分流插头允许在期望的时间跨信号传输信号,并且当被去除时消除了在访问组件的订户部件时用户受到震动或发送火花的可能性。 组件的主体和模块优选地一体地连接并形成一体的密封组件。