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    Antibiotic tan-749, its derivatives, production and use thereof
    1.
    发明授权
    Antibiotic tan-749, its derivatives, production and use thereof 失效
    抗生素tan-749，其衍生物，生产和使用

    公开(公告)号：US4906659A

    公开(公告)日：1990-03-06

    申请号：US129737

    申请日：1987-12-07

    Applicant: Setsuo Harada ,  Hideo Ono ,  Hirotomo Masuya ,  Hideaki Natsugari

    Inventor： Setsuo Harada ,  Hideo Ono ,  Hirotomo Masuya ,  Hideaki Natsugari

    IPC: C07C237/22 ,  C07C255/29 ,  C07C257/14 ,  C07D295/13 ,  C07C123/00 ,  A61K35/00

    CPC classification number: C07D295/13 ,  C07C237/22 ,  C07C255/29 ,  C07C257/14 ,  C07C2101/02 ,  Y02P20/55

    Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.4 are independently amino or an organic residue bonded through nitrogen, R.sup.2 is hydrogen or alkyl which may be substituted, R.sup.3 is hydrogen or a protecting group and R5 is hydroxyl which may be substituted or amino which may be substituted or salts thereof; with the proviso that when R.sup.1 is amino, leucylamino, acetylamino or benzyloxycarbonylamino, R.sup.3 is hydrogen, methyl or 2-tettrahydropyranyl, R.sup.4 is amino, acetylamino or benzyloxycarbonylamino and R.sup.5 is hydroxyl which may be substituted or amino which may be substituted, R.sup.2 is alkyl which may be substituted, has antibacterial activities against drug-resistant bacteria and therefore can be useful as a chemotherapeutic drug for bacterial infections in mammals.

    Abstract translation: 式IMA的化合物，其中R 1和R 4独立地为氨基或通过氮键合的有机残基，R 2为氢或可被取代的烷基，R 3为氢或保护基，R 5为可被取代的羟基或氨基 其可以被取代或其盐; 条件是当R1为氨基，亮氨酰氨基，乙酰氨基或苄氧羰基氨基时，R3为氢，甲基或2-四氢吡喃基，R4为氨基，乙酰氨基或苄氧羰基氨基，R5为可被取代的羟基或可被取代的氨基，R2为烷基 其可以被取代，对耐药细菌具有抗菌活性，因此可用作哺乳动物细菌感染的化学治疗药物。

    Carboxyimidamide derivatives
    4.
    发明授权
    Carboxyimidamide derivatives 失效
    羧甲酰胺衍生物

    公开(公告)号：US4499105A

    公开(公告)日：1985-02-12

    申请号：US452194

    申请日：1982-12-28

    Applicant: Harm J. Panneman

    Inventor： Harm J. Panneman

    IPC: A61K31/155 ,  A61K20060101 ,  A61K31/13 ,  A61K31/16 ,  A61K31/22 ,  A61P7/00 ,  C07C20060101 ,  C07C67/00 ,  C07C239/00 ,  C07C257/16 ,  C07C301/00 ,  C07C303/40 ,  C07C311/00 ,  C07C123/00

    CPC classification number: C07C311/21 ,  C07C257/16 ,  C07C257/22 ,  C07C259/16 ,  C07C2102/10 ,  C07C2102/12 ,  C07C2102/24

    Abstract: The present invention is dealing with compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, in which n and m represent the number 1 or 2, X and Y hydrogen, alkyl (1-4 C), alkoxy (1-4 C), hydroxy, halogen, hydroxymethyl, trifluoromethyl, acyl (1-4 C), acyloxy (1-4 C) or the group NR.sub.x R.sub.y, in which R.sub.x and R.sub.y represent hydrogen, alkyl (1-4 C) or a sulphonyl group and R represents the group ##STR2## in which R.sub.1 and R.sub.2 represent hydrogen, alkyl (1-4 C), hydroxy, alkoxy (1-4 C), phenylalkoxy (7-10 C), acyloxy, amino or mono or dialkyl (1-4 C) amino, having potent platelet aggregation inhibiting properties.

    Abstract translation: 本发明涉及下式的化合物及其药学上可接受的盐，其中n和m代表数字1或2，X和Y氢，烷基（1-4C），烷氧基（1-4 （1-4C），酰氧基（1-4C）或NRxRy，其中Rx和Ry代表氢，烷基（1-4C）或磺酰基（1-4C），羟基，卤素，羟甲基， 基团，R表示其中R1和R2表示氢，烷基（1-4C），羟基，烷氧基（1-4C），苯基烷氧基（7-10C），酰氧基，氨基或单或二烷基 （1-4C）氨基，具有有效的血小板聚集抑制性质。

    Process for preparing perfluorotriazine elastomers and precursors thereof
    6.
    发明授权
    Process for preparing perfluorotriazine elastomers and precursors thereof 失效
    全氟三嗪弹性体及其前体的制备方法

    公开(公告)号：US4434106A

    公开(公告)日：1984-02-28

    申请号：US366025

    申请日：1982-04-06

    Applicant: Robert W. Rosser ,  Timothy S. Chen ,  Chung-Heng Cheng

    Inventor： Robert W. Rosser ,  Timothy S. Chen ,  Chung-Heng Cheng

    IPC: C07D251/24 ,  C07C123/00 ,  C07C120/00 ,  C07C121/43

    CPC classification number: C07D251/24

    Abstract: Perfluoroether triazine elastomers having improved properties and utility in seals, gaskets, sealing components and the like are prepared from oligomeric imidoylamidines that have, in turn, been prepared by the process of (a) reacting a perfluorodinitrile with liquid ammonia to yield a perfluorodiamidine, (b) isolating the perfluorodiamidine, (c) reacting the isolated diamidine with a perfluorodinitrile to yield a perfluoro(imidoylamidine) dinitrile, and then repeating steps (a), (b), and (c) to sequentially grow an oligomer of desired molecular size. The isolated amidine and nitrile intermediates are also disclosed.

    Abstract translation: 具有改进的性能和用途的全氟醚三嗪弹性体由密封剂，垫圈，密封组分等制备，其通过以下方法制备：反应通过以下方法制备：（a）使全氟丁腈与液氨反应得到全氟二氨基吡啶（ b）分离全氟二氨基吡啶，（c）使分离的脒与全氟丁腈反应，得到全氟（亚氨基脒）二腈，然后重复步骤（a），（b）和（c）顺序生长所需分子尺寸的低聚物 。 还公开了分离的脒和腈中间体。

    Compounds and methods of making
    8.
    发明授权
    Compounds and methods of making 失效
    化合物和制备方法

    公开(公告)号：US4347178A

    公开(公告)日：1982-08-31

    申请号：US140160

    申请日：1980-04-14

    Applicant: John W. A. Findlay ,  Robert F. Butz ,  Richard M. Welch

    Inventor： John W. A. Findlay ,  Robert F. Butz ,  Richard M. Welch

    IPC: A61K47/48 ,  A61K51/04 ,  C07C45/00 ,  C07C45/54 ,  C07C45/56 ,  C07D263/04 ,  C07D263/10 ,  C07C123/00 ,  C07C131/00 ,  G01N33/54

    CPC classification number: C07D263/10 ,  A61K47/4833 ,  A61K51/0406 ,  C07C255/00 ,  C07C45/00 ,  C07C45/54 ,  C07C45/56 ,  C07D263/04 ,  Y10S436/804 ,  Y10S436/822 ,  Y10S530/806

    Abstract: A radioimmunoassay procedure has been discovered for bupropion [(.+-.)-2-t-butylamino-3-chloropropiophenone], an antidepressant compound, in biological fluids. Novel compounds of formula ##STR1## wherein either R.sub.2 is oxygen and R.sub.1 is (CH.sub.2).sub.n -O-(CO).sub.m -(CH.sub.2).sub.p -COOH where n is an integer from 0 to 5, m is 0 or 1, and p is an integer from 1 to 4; or R.sub.1 is hydrogen and R.sub.2 is N-O-(CH.sub.2).sub.q -COOH where q is an integer from 1 to 3, and novel methods of making them and novel intermediates useful therein are disclosed. Novel immunogens for raising bupropion specific antisera, and novel methods of making them are disclosed comprising conjugates of the novel compounds and suitable carrier material. The drug is added to the antisera together with novel radiolabeled competitor of formula ##STR2## wherein R' is a suitable radioisotope as described above and R.sub.3 is hydrogen, R.sub.4 is Cl, and R.sub.5 is oxygen, or R' is hydrogen and either(a) R.sub.3 is H and R.sub.4 is Cl and R.sub.5 is NO(CH.sub.2).sub.q CO-X where q is as defined for formula I and X is a group having formula III ##STR3## wherein R.sub.6 is a suitable radioisotope as described above, R.sub.7 is hydroxyl, and s is an integer from 1 to 4;(b) R.sub.4 is Cl, R.sub.5 is oxygen, and R.sub.3 is (CH.sub.2).sub.n -O-(CO).sub.m -(CH.sub.2).sub.p -CO-X where n, m, and p are as defined for formula I and X is as defined above; or(c) R.sub.3 is hydroxy, R.sub.5 is oxygen and R.sub.4 is a suitable radioisotope as defined above.The measure of radioactivity of the antisera bound radiolabeled competitor provides a measure of the amount of drug in the assayed biological fluid sample. A standard curve can be constructed from which the amount of drug in the assay sample can be interpolated. A kit is disclosed for practicing the radioimmunoassay.

    Abstract translation: 已经发现了用于生物液体中的安非他酮[（+/-） - 2-叔丁基氨基-3-氯苯丙酮]（一种抗抑郁药）的放射免疫测定方法。 式（IMA）的新型化合物，其中R2是氧，R1是（CH2）nO-（CO）m-（CH2）p-COOH，其中n是0-5的整数，m是0或1，p是 1到4的整数; 或R 1为氢，R 2为N-O-（CH 2）q-COOH，其中q为1至3的整数，并且公开了制备它们的新方法和可用于其中的新型中间体。 公开了用于提高安非他酮特异性抗血清的新型免疫原及其制备方法，其包括新化合物和合适的载体材料的缀合物。 将药物与新的放射性标记的式（IMAGE）竞争剂一起加入到抗血清中，其中R'是如上所述的合适的放射性同位素，R 3是氢，R 4是Cl，R 5是氧，或者R'是氢， ）R3是H，R4是Cl，R5是NO（CH2）qCO-X，其中q如式I所定义，X是具有式III的基团，其中R6是如上所述的合适的放射性同位素，R7是 羟基，s为1至4的整数; （b）R4是Cl，R5是氧，R3是（CH2）nO-（CO）m-（CH2）p-CO-X，其中n，m和p如式I所定义，X如上定义 以上; 或（c）R3是羟基，R5是氧，R4是如上定义的合适的放射性同位素。 抗血清结合的放射性标记的竞争者的放射性测量值提供测定的生物流体样品中药物的量的量度。 可以构建标准曲线，由此可以插入测定样品中的药物量。 公开了用于实施放射免疫测定的试剂盒。

    1-Methyl-2(alkylimino)pyrrolidines and 1-methyl 2(cycloalkylimino) pyrrolidines
    9.
    发明授权
    1-Methyl-2(alkylimino)pyrrolidines and 1-methyl 2(cycloalkylimino) pyrrolidines 失效
    1-甲基-2（烷基亚氨基）吡咯烷和1-甲基2（环丙基亚氨基）吡咯烷

    公开(公告)号：US4321202A

    公开(公告)日：1982-03-23

    申请号：US106677

    申请日：1979-12-26

    Applicant: Victor Mark

    Inventor： Victor Mark

    IPC: C07D207/22 ,  C07C123/00

    CPC classification number: C07D207/22

    Abstract: Amidines are one of the strongest organic bases and find application where this property is needed, such as in phase transfer catalysis in the form of their substituted derivatives. Their use, however, has been hampered by their expensive nature due to only mediocre yields in their preparation. The present invention provides a process for the preparation of substituted amidines in essentially quantitative yields.

    Abstract translation: 脒类是最强有机基质之一，可以找到需要这种性质的应用，例如以其取代衍生物的形式进行相转移催化。 然而，由于它们的制备中只有平均的产量，它们的使用受到其昂贵的性质的阻碍。 本发明提供以基本上定量的产率制备取代的脒的方法。

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