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    Compounds useful as alkaline phosphatase inhibitors and therapeutic agents
    1.
    发明授权
    Compounds useful as alkaline phosphatase inhibitors and therapeutic agents 失效
    可用作碱性磷酸酶抑制剂和治疗剂的化合物

    公开(公告)号：US5516647A

    公开(公告)日：1996-05-14

    申请号：US148142

    申请日：1993-11-05

    申请人： Mazhar Husain ,  Dominique Bridon ,  Mark Bures ,  James D. Ratajczyk ,  Fortuna Haviv ,  Christopher Bieniarz

    发明人： Mazhar Husain ,  Dominique Bridon ,  Mark Bures ,  James D. Ratajczyk ,  Fortuna Haviv ,  Christopher Bieniarz

    IPC分类号： C07D513/04 ,  C12Q1/42 ,  C07D513/02

    CPC分类号： C07D513/04 ,  C12Q1/42 ,  Y10S435/81

    摘要： The present invention discloses novel compounds useful as alkaline phosphatase inhibitors and therapeutic agents. Preferably, the novel compounds are useful as selective inhibitors of human alkaline phosphatases as opposed to Escherichia coli alkaline phosphatases. The novel compounds can also be used as cancer therapeutic agents, anti-depressive agents, anti-anergic agents, and antihelminthic agents. The novel compounds have the following general formula: ##STR1## wherein R' is an aryl, aryl ether, aryl thioether, aromatic heterocyclic, aromatic heterocyclic thioether, or aromatic heterocyclic ether group. More preferably, R' is a phenyl or a pyridine. Most preferably, R' is of the following formula: ##STR2## 2-thiopyridine, or ##STR3## 2-oxypyridine. R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.1 ', R.sub.2 ', R.sub.3 ', R.sub.4 ', and R.sub.5 ' can be the same or different, and at least one of which is selected from the group consisting of: H, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, nitro, amino, carboxy, and halo groups with the proviso that each novel compound has no more than three substituents. Hydrogen is not considered a substituent.

    摘要翻译： 本发明公开了可用作碱性磷酸酶抑制剂和治疗剂的新化合物。 优选地，新化合物可用作人碱性磷酸酶的选择性抑制剂，与大肠杆菌碱性磷酸酶相反。 新化合物也可以用作癌症治疗剂，抗抑郁剂，抗过敏剂和抗栓剂。 新化合物具有以下通式：其中R'为芳基，芳基醚，芳基硫醚，芳族杂环，芳族杂环硫醚或芳族杂环醚基团。 更优选地，R'是苯基或吡啶。 最优选地，R'具有下列结构式：2-甲基吡啶或2-氧代吡啶。 R1，R2，R3，R4，R1'，R2'，R3'，R4'和R5'可以相同或不同，其中至少一个选自：H，C 1 -C 6烷基 ，卤素C 1 -C 6烷基，苯基，C 1 -C 6烷氧基，苯氧基，三氟甲基，硝基，氨基，羧基和卤素基团，条件是每个新化合物不超过三个取代基。 氢不被认为是取代基。

    Phosphatase activated crosslinking, conjugating and reducing agents; methods of using such agents; and reagents comprising phosphatase activated crosslinking and conjugating agents
    2.
    发明授权
    Phosphatase activated crosslinking, conjugating and reducing agents; methods of using such agents; and reagents comprising phosphatase activated crosslinking and conjugating agents 失效
    磷酸酶活化交联，共轭和还原剂; 使用这种药剂的方法; 和包含磷酸酶活化的交联和缀合剂的试剂

    公开(公告)号：US5736624A

    公开(公告)日：1998-04-07

    申请号：US349167

    申请日：1994-12-02

    申请人： Christopher Bieniarz ,  Douglas F. Young ,  Michael J. Cornwell ,  Mazhar Husain

    发明人： Christopher Bieniarz ,  Douglas F. Young ,  Michael J. Cornwell ,  Mazhar Husain

    IPC分类号： A61K47/48 ,  C07F9/165 ,  C07F9/553 ,  G01N33/543 ,  C07K16/26 ,  C07K17/00 ,  C12N9/96 ,  C12N11/08

    CPC分类号： G01N33/54353 ,  C07F9/1651 ,  C07F9/1652 ,  C07F9/5537 ,  Y10S530/811 ,  Y10S530/816

    摘要： The present invention provides crosslinking, conjugating and reducing agents which are functional with at least one phosphorothioate monoester group (--SPO.sub.3.sup.-2). Crosslinking and conjugation methods as well as solid phase reagents and conjugates which are useful in immunoassays are also provided. Crosslinking and conjugating agents of the invention generally comprise a compound corresponding to the formula (I), shown below, wherein n is at least 1 and Q is a straight or branched monomer, polymer or oligomer having an average molecular weight between about 200 and about 1,000,000. Additionally, when n is 1, Q comprises at least 1 additional reactive functionality. Q--(S--PO.sub.3.sup.-2)n (I) The reducing agents that are provided conform to a compound of the formula (Y), shown below, wherein (A) and (Z) can be independently selected from C.sub.1 -C.sub.5 alkyl and CONH(CH.sub.2).sub.p wherein p is an integer between 1 and 5. ##STR1##

    摘要翻译： 本发明提供了与至少一种硫代磷酸酯单酯基团（-SPO3-2）起作用的交联，缀合和还原剂。 还提供了可用于免疫测定的交联和缀合方法以及固相试剂和缀合物。 本发明的交联和缀合剂通常包含对应于下面所示的式（I）的化合物，其中n至少为1，Q为直链或支链单体，平均分子量为约200至约200的聚合物或低聚物 1,000,000。 另外，当n为1时，Q包含至少1个额外的反应性官能团。Q-（S-PO3-2）n（I）提供的还原剂符合下面所示的式（Y）化合物，其中 （A）和（Z）可以独立地选自C 1 -C 5烷基和CONH（CH 2）p，其中p是1和5之间的整数。

    Site-specific conjugation of immunoglobulins and detectable labels
    3.
    发明授权
    Site-specific conjugation of immunoglobulins and detectable labels 失效
    免疫球蛋白和可检测标签的特异性结合

    公开(公告)号：US5191066A

    公开(公告)日：1993-03-02

    申请号：US624169

    申请日：1990-12-07

    申请人： Christopher Bieniarz ,  Mazhar Husain ,  Howard E. Bond

    发明人： Christopher Bieniarz ,  Mazhar Husain ,  Howard E. Bond

    IPC分类号： C07K16/00 ,  C07K1/00 ,  C07K1/107 ,  C07K1/113 ,  C07K16/06 ,  G01N33/532 ,  G01N33/547

    CPC分类号： C07K16/065 ,  C07K1/1077

    摘要： A process for producing a derivatized immunoglobulin and conjugates prepared therewith are provided. The derivatized immunoglobulin is produced by introducing sulfhydryl groups in the Fc region of an immunoglobulin wherein the Fab portion of the immunoglobulin is not altered. The derivatized immunoglobulin is used to prepare conjugates with various detectable moieties wherein a controlled distance exists between the Fc region of the immunoglobulin and the detectable moiety. The conjugates are particularly useful for performing immunoassays, and exhibit improved longevity, specificity and sensitivity.

    摘要翻译： 提供了制备衍生化免疫球蛋白的方法及其制备的缀合物。 衍生的免疫球蛋白是通过在免疫球蛋白的Fc区中引入巯基而产生的，其中免疫球蛋白的Fab部分没有被改变。 衍生的免疫球蛋白用于制备具有各种可检测部分的缀合物，其中在免疫球蛋白的Fc区和可检测部分之间存在受控的距离。 缀合物特别可用于进行免疫测定，并显示出改善的寿命，特异性和灵敏度。

    HAPTEN CONJUGATES FOR TARGET DETECTION
    7.
    发明申请
    HAPTEN CONJUGATES FOR TARGET DETECTION 审中-公开
    寻找目标检测

    公开(公告)号：US20130109019A1

    公开(公告)日：2013-05-02

    申请号：US13805978

    申请日：2011-07-01

    申请人： Adrian E. Murillo ,  Jerome W. Kosmeder ,  Eric May ,  William Day ,  Mark Lefever ,  Anne M. Pedata ,  Christopher Bieniarz ,  Phillip Miller

    发明人： Adrian E. Murillo ,  Jerome W. Kosmeder ,  Eric May ,  William Day ,  Mark Lefever ,  Anne M. Pedata ,  Christopher Bieniarz ,  Phillip Miller

    IPC分类号： C07D277/54 ,  C07C237/20 ,  C07D271/12 ,  C07D233/90 ,  C07D243/00 ,  C07D241/52

    CPC分类号： C07D277/54 ,  A61K47/51 ,  C07C235/34 ,  C07C237/20 ,  C07C311/37 ,  C07D233/90 ,  C07D241/52 ,  C07D243/00 ,  C07D271/12 ,  G01N33/581 ,  G01N2333/908

    摘要： Embodiments of hapten conjugates including a hapten, an optional linker, and a peroxidase-activatable aryl moiety are disclosed. In some embodiments, the peroxidase-activatable aryl moiety is tyramine or a tyramine derivative. Embodiments of methods for making and using the hapten conjugates also are disclosed. In particular embodiments, the hapten conjugates are used in a signal amplification assay. In certain embodiments, the hapten is an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, or 7-diethylamino-3-carboxycoumarin. The hapten is coupled to the peroxidase-activatable aryl moiety directly or indirectly via a linker. In certain embodiments, the hapten conjugates are used in multiplexed assays.

    摘要翻译： 公开了包含半抗原，任选接头和过氧化物酶活化的芳基部分的半抗原共轭物的实施方案。 在一些实施方案中，过氧化物酶可活化的芳基部分是酪胺或酪胺衍生物。 还公开了制备和使用半抗原共轭物的方法的实施方案。 在具体实施方案中，半抗原共轭物用于信号放大测定。 在某些实施方案中，半抗原是恶唑，吡唑，噻唑，苯并呋咱，三萜，脲，除罗丹明硫脲以外的硫脲，除二硝基苯基或三硝基苯基以外的硝基芳基，旋环体，环链烷基，异二芳基， 偶氮二芳基，苯并二氮杂或7-二乙基氨基-3-羧基香豆素。 半抗原通过接头直接或间接地与过氧化物酶活化的芳基部分偶联。 在某些实施方案中，半抗原共轭物用于多重测定。