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1. 发明授权

US5098996A Process for introducing fluorine into biologically active materials 失效
标题翻译：将氟引入生物活性物质的方法
公开(公告)号：US5098996A
公开(公告)日：1992-03-24
申请号：US168494
申请日：1988-03-15
申请人： Kenneth A. Jacobson , Kenneth L. Kirk , David C. Furlano , Yechiel Shai
发明人： Kenneth A. Jacobson , Kenneth L. Kirk , David C. Furlano , Yechiel Shai
IPC分类号： A61K38/00 , C07D473/06 , C07D473/08 , C07D519/00 , C07K5/06 , C07K5/065
CPC分类号： C07D473/06 , C07D473/08 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： Radioactive fluorine can be easily introduced into biologically active molecules containing amino groups. A p-bromomethyl benzoyl group is coupled to the amino group of the biologically active molecule, and bromine is displaced by fluorine. Alternatively, the bromine on the bromomethylbenzoyl group is first displaced by fluorine, and the fluoromethyl benzoyl group is then coupled to the amino group of the biologically active molecule. The compounds so produced are useful in diagnostic nuclear medicine.
摘要翻译：放射性氟可以容易地引入到含有氨基的生物活性分子中。对溴甲基苯甲酰基与生物活性分子的氨基偶联，溴被氟取代。或者，溴甲基苯甲酰基上的溴首先被氟取代，然后将氟甲基苯甲酰基与生物活性分子的氨基偶联。如此制备的化合物可用于诊断性核医学。

2. 发明授权

US5284834A Adenosine functionalized congeners as cardiovascular treating agents for animals and methods for using same 失效
标题翻译：腺苷功能化同系物作为动物的心血管治疗剂和使用它们的方法
公开(公告)号：US5284834A
公开(公告)日：1994-02-08
申请号：US924792
申请日：1992-08-06
申请人： Kenneth A. Jacobson , Kenneth L. Kirk , John W. Daly
发明人： Kenneth A. Jacobson , Kenneth L. Kirk , John W. Daly
IPC分类号： C07H19/16 , A61K31/52 , C07H17/00
CPC分类号： C07H19/16
摘要： This invention comprises a series of N.sup.6 -substituted adenosine analogues bearing functionalized chains for the covalent attachment to probes or solid supports. In these compounds coronary vasodilation in the open thorax dog model, typical of A.sub.2 -adenosine receptor agonists, is shown. The potency is modulated by distal structural changes in the chain, with the highest A.sub.2 -potency observed for two methylamides, a primary amine congener, and a biotin conjugate. These compounds have antihypertensive activity and certain components are charged and are excluded from crossing the blood-brain barrier.
摘要翻译：本发明包括一系列具有用于与探针或固体支持物共价连接的官能化链的N6-取代的腺苷类似物。在这些化合物中，显示了A2-腺苷受体激动剂的典型的开放性胸部狗模型中的冠状动脉血管舒张。效价由链中的远端结构变化调节，对于两种甲基酰胺，伯胺同类物和生物素缀合物观察到最高的A2效能。这些化合物具有抗高血压活性，并且将某些组分带入并排除与血脑屏障交叉。

3. 发明授权

US4696932A Biologically-active xanthine derivatives 失效
标题翻译：生物活性黄嘌呤衍生物
公开(公告)号：US4696932A
公开(公告)日：1987-09-29
申请号：US717616
申请日：1985-03-29
申请人： Kenneth A. Jacobson , John W. Daly , Kenneth L. Kirk
发明人： Kenneth A. Jacobson , John W. Daly , Kenneth L. Kirk
IPC分类号： A61K38/00 , C07D473/06 , C07D473/08 , C07D519/00 , C07K5/06 , C07K5/065 , A61K31/52
CPC分类号： C07D473/06 , C07D473/08 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： Certain functionalized cogeners of 1,3-dialkylxanthine exhibit high potency and selectivity as antagonists for A.sub.1 - and A.sub.2 -adenosine receptors and are suitable for attachment to probes, drug carriers, or solid supports. These derivatives are characterized by the presence of a phenyl at the 8 position para-substituted with a functionalized chain to provide high water solubility and high receptor affinity. Some of these analogs, containing a distal amino- or carboxylic-functionalized chain, are suitable for synthesis of amino acid conjugates. The compounds of this invention are suitable for use as antiallergenic, antiasthmatic, or cardiotonic drugs, central nervous system stimulants, and diuretics.
摘要翻译：某些功能化的1,3-二烷基黄嘌呤的同系物作为A1-和A2-腺苷受体的拮抗剂显示出高的效力和选择性，并且适于附着于探针，药物载体或固体支持物。这些衍生物的特征在于在被官能化链对位取代的8位上存在苯基以提供高水溶性和高受体亲和力。含有远端氨基或羧基官能化链的这些类似物中的一些适用于合成氨基酸缀合物。本发明的化合物适合用作抗过敏，抗哮喘或强心药物，中枢神经系统兴奋剂和利尿剂。

4. 发明授权

US4968672A Adenosine receptor prodrugs 失效
标题翻译：腺苷受体前药
公开(公告)号：US4968672A
公开(公告)日：1990-11-06
申请号：US229
申请日：1987-01-02
申请人： Kenneth A. Jacobson , Kenneth L. Kirk , John W. Daly
发明人： Kenneth A. Jacobson , Kenneth L. Kirk , John W. Daly
IPC分类号： C07D473/06 , C07H19/16
CPC分类号： C07H19/16 , C07D473/06
摘要： A functionalized congener approach to drugs acting at A.sub.1 and A.sub.2 adenosine receptor types is applicable to prodrug design. The prodrugs affect a more efficient delivery of the drug at the particular site of the body affected and take advantage of selective biochemical cleavages and alteration in distribution characteristics. In particular, kidney functions and lipid functions are stressed in the invention.
摘要翻译：在A1和A2腺苷受体类型上作用的药物的功能化同侪方法适用于前药设计。前药影响药物在受影响身体的特定部位的更有效的递送，并利用选择性生化裂解和分布特征的改变。特别地，在本发明中肾功能和脂质功能受到重视。

5. 发明授权

US4612315A Biologically-active 1,3-dipropyl-8-phenylxanthine derivatives 失效
标题翻译：生物活性的1,3-二丙基-8-苯基黄嘌呤衍生物
公开(公告)号：US4612315A
公开(公告)日：1986-09-16
申请号：US664953
申请日：1984-10-26
申请人： Kenneth A. Jacobson , John W. Daly , Kenneth L. Kirk
发明人： Kenneth A. Jacobson , John W. Daly , Kenneth L. Kirk
IPC分类号： A61K38/00 , C07D473/06 , C07D473/08 , C07D519/00 , C07K5/06 , C07K5/065 , A61K31/41
CPC分类号： C07K5/06026 , C07D473/06 , C07D473/08 , C07K5/06078 , A61K38/00
摘要： Certain functionalized congeners of 1,3-dialkylxanthine exhibit high potency and selectivity as antagonists for A.sub.1 - and A.sub.2 -adenosine receptors and are suitable for attachment to probes, drug carriers, or solid supports. These derivatives are characterized by the presence of a phenyl at the 8 position para-substituted with a functionalized chain to provide high water solubility and high receptor affinity to such an extent that these compounds are suitable for use as antiallergenic, antiasthmatic, or cardiotonic drugs, central nervous system stimulants, and diuretics.
摘要翻译：某些1,3-二烷基黄嘌呤的功能化同系物作为A1-和A2-腺苷受体的拮抗剂显示出高效力和选择性，并且适合于附着于探针，药物载体或固体支持物。这些衍生物的特征在于在被官能化链对位取代的8位上存在苯基，以提供高水溶性和高受体亲和力，使得这些化合物适合用作抗过敏，抗哮喘或强心药物，中枢神经系统兴奋剂和利尿剂。

6. 发明授权

US5248770A Molecular probes for adenosine receptors 失效
标题翻译：腺苷受体的分子探针
公开(公告)号：US5248770A
公开(公告)日：1993-09-28
申请号：US287539
申请日：1988-12-19
申请人： Kenneth A. Jacobson , John W. Daly , Kenneth L. Kirk
发明人： Kenneth A. Jacobson , John W. Daly , Kenneth L. Kirk
IPC分类号： A61K38/00 , C07D473/06 , C07D473/08 , C07D519/00 , C07K5/06 , C07K5/065
CPC分类号： C07D473/08 , C07D473/06 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： This application discloses probes for adenosine receptors which are functionalized congeners of the following compound: ##STR1## wherein R is --CH.sub.2 --C(O)--R' or ##STR2## These probes bind to A.sub.2 and A.sub.3 adenosine receptors and aid in quantifying and characterizing the receptors. The compounds may be labeled, for example with fluorescent compounds or radioactive compounds, or unlabeled.
摘要翻译：本申请公开了用于腺苷受体的探针，其是以下化合物的官能化同系物：其中R是-CH 2 -C（O）-R'或这些探针结合A2和A3腺苷受体，并有助于量化和表征受体。化合物可以用例如荧光化合物或放射性化合物标记，或未标记。

7. 发明授权

US4908322A Derivatization of amines for electrochemical detection 失效
标题翻译：用于电化学检测的胺的衍生化
公开(公告)号：US4908322A
公开(公告)日：1990-03-13
申请号：US290279
申请日：1988-12-27
申请人： Kenneth A. Jacobson , Kenneth L. Kirk , Markku I. Linnoila , Thomas Miller , Kazunori Mine
发明人： Kenneth A. Jacobson , Kenneth L. Kirk , Markku I. Linnoila , Thomas Miller , Kazunori Mine
IPC分类号： G01N33/52
CPC分类号： G01N33/52 , Y10S436/816 , Y10S436/901 , Y10T436/17 , Y10T436/173845 , Y10T436/174614
摘要： Primary and secondary amines in biological fluids are selectively derivitized by reaction with esters of N-hydroxysuccinimide or N-hydroxysulfosuccinimide to form an N-acylated derivative. Those N-acylated derivatives may then be extracted into a polar organic phase and extracted. Non-electroactive amines may be made suitable for coulometric analysis by selecting the ester used so as to attach an electroactive group to the amine. For example, histamine may be reacted with the Bolton-Hunter reagent to form a suitable derivative in high yield.
摘要翻译：通过与N-羟基琥珀酰亚胺或N-羟基磺基琥珀酰亚胺的酯反应来选择性地衍生生物流体中的伯胺和仲胺以形成N-酰化衍生物。然后将那些N-酰化衍生物萃取到极性有机相中并萃取。非电活性胺可以通过选择用于将电活性基团连接到胺上的酯而适于库仑分析。例如，组胺可以与Bolton-Hunter试剂反应以高产率形成合适的衍生物。

8. 发明授权

US4597559A Diaphragm valve 失效
标题翻译：隔膜阀
公开(公告)号：US4597559A
公开(公告)日：1986-07-01
申请号：US719065
申请日：1985-04-02
申请人： Kenneth L. Kirk
发明人： Kenneth L. Kirk
IPC分类号： F16K7/16
CPC分类号： F16K7/16
摘要： In combination, a pressurized-gas container having a port and a diaphragm valve having a hollow elongated body. A flexible diaphragm is sealingly positioned in the valve. The diaphragm forms a first chamber and a second chamber in the hollow valve. A valve stem is rotatably positioned in the first chamber. A port located in the side of the valve communicates with the second chamber. A short member, affixed in the port, has a central passageway. One end of the short member is adapted to be connected to a source of pressurized gas. A second elongated member, having a central passageway, is positioned in the second chamber of the valve. One end of the elongated member is sealingly affixed to the inside of the wall of the container around the port of the container. One end of the second elongated member forms a valve seat, which is positioned near but not in contact with the diaphragm. A cup member is positioned in the first chamber of the valve. The valve stem can be rotated into a closed position whereby the flat bottom of the cup member sealingly presses the diaphragm against the valve seat.
摘要翻译：组合地，具有端口的压缩气体容器和具有中空细长体的隔膜阀。密封地安装在阀中的柔性膜片。隔膜在中空阀中形成第一室和第二室。阀杆可旋转地定位在第一腔室中。位于阀侧的端口与第二室连通。一个简短的会员，固定在港口，有一个中央通道。短构件的一端适于连接到加压气体源。具有中心通道的第二细长构件被定位在阀的第二腔室中。细长构件的一端密封地固定在围绕容器端口的容器壁的内部。第二细长构件的一端形成阀座，该阀座位于隔膜附近但不接触隔膜。杯构件定位在阀的第一室中。阀杆可以旋转到关闭位置，由此杯形件的平坦底部将隔膜密封地压靠在阀座上。

9. 发明授权

US4688694A Safety means for pressurized gas containers 失效
标题翻译：加压气体容器的安全装置
公开(公告)号：US4688694A
公开(公告)日：1987-08-25
申请号：US819386
申请日：1986-01-16
申请人： Kenneth L. Kirk , Robert F. O'Connor
发明人： Kenneth L. Kirk , Robert F. O'Connor
IPC分类号： F17C13/04 , F17C13/12 , B65D25/00
CPC分类号： F17C13/04 , F17C13/123 , F17C2201/0109 , F17C2201/0123 , F17C2205/0165 , F17C2205/018 , F17C2205/0329 , F17C2209/234
摘要： A container for pressurized gas, having a valve for filling and emptying the container, a frangible safety relief cup located near the valve and a deflector plate attached to the bottom portion of the valve. The safety relief cup is frangible so that the safety relief cup will rupture if the container is filled to too high of a gas pressure. The problem with such safety feature is that upon rupture the escaping gas often travels in an upwards direction at a very high speed, allowing the discharging contents to spray on the face or upper torso by the person causing injury to the face of refrigerant frost bite or the like. The deflector plate is wide enough and extends far enough over top of the frangible safety relief cup to prevent the upwards flow of the escaping pressurized gas from the ruptured safety relief device. Also, if the safety relief cup itself breaks lose due to gas pressure in the container, the deflector plate protects the person standing above the container from being hit in the face or upper torso by the flying safety relief device.
摘要翻译：一种用于加压气体的容器，其具有用于填充和排空容器的阀，位于阀附近的易碎安全释放杯和附接到阀底部的偏转板。安全释放杯是易碎的，因此如果容器充满太高的气体压力，安全泄压杯就会破裂。这种安全特征的问题是，在破裂时，逸出的气体通常以非常高的速度沿向上的方向行进，允许排出物体在造成对制冷剂霜冻面或面部的伤害的人的脸上或上身上喷洒，类似。导流板足够宽，并且在易碎安全释放杯的顶部延伸得足够远，以防止泄漏的加压气体从破裂的安全释放装置向上流动。此外，如果安全释放杯本身由于容器中的气体压力而损失，则偏转板保护站在容器上方的人员不被飞行安全释放装置撞击在脸部或上身上。

10. 发明授权

US4344645A Tee-type leg bracket 失效
标题翻译：三通型支架
公开(公告)号：US4344645A
公开(公告)日：1982-08-17
申请号：US194280
申请日：1980-10-06
申请人： Kenneth L. Kirk
发明人： Kenneth L. Kirk
IPC分类号： B65D90/12 , F16L3/00
CPC分类号： B65D90/12
摘要： Tee-type leg bracket for supporting a tank, which has a hemispherical-type of bottom surface and a short nipple mounted on the bottom surface at substantially a right angle thereto. The bracket has a central frame, a tee vertically mounted on the central frame, and three support legs detachably attached to the central frame. The bottom surface of the tank rests on the top portion of the support legs. The contour of the top surface of the support legs matches the contour of the bottom surface of the tank. The top arm of the vertically-mounted tee mates with the short nipple mounted on the bottom of the tank. The means of attaching the support legs to the central frame involves vertical grooves in the edge region of the central frame. The mouth of each of the vertical grooves is narrower than the interior portion thereof. The number of vertical grooves is also equal in number to the support legs. There is a vertical rib on one end of each of the support legs. Each of the vertical ribs has the same horizontal cross-section as the horizontal cross-section of each of the vertical grooves in the central frame and slidably fits into one of the vertical grooves. The tee-type leg bracket has the important advantages: that it provides a unit which contains support legs which self-adjust and self-level when supporting a tank; that it allows easy installation in a piping system and is easily accessible.
摘要翻译：用于支撑具有半球形底面的坦克的三通型支架支架和以大致直角安装在底表面上的短接头。支架具有中央框架，垂直安装在中央框架上的三通和可拆卸地连接到中央框架的三个支撑腿。容器的底部表面位于支撑腿的顶部。支撑腿的顶面的轮廓与油箱底面的轮廓相匹配。垂直安装的三通的顶臂与安装在油箱底部的短乳头相配。将支撑腿连接到中央框架的装置涉及中央框架的边缘区域中的垂直凹槽。每个垂直槽的口部比其内部部分窄。垂直槽的数量也与支撑腿数相等。每个支撑腿的一端上有一个垂直肋。每个垂直肋具有与中央框架中的每个垂直槽的水平横截面相同的水平横截面，并且可滑动地装配到一个垂直槽中。三通型支架具有重要的优点：它提供了一个单元，其包含支撑水箱时自调节和自身水平的支撑腿; 它容易安装在管道系统中，并且易于接近。

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