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    Snake bite therapy
    112.
    发明授权
    Snake bite therapy 失效
    蛇咬伤治疗

    公开(公告)号：US4439443A

    公开(公告)日：1984-03-27

    申请号：US394967

    申请日：1982-07-02

    Applicant: Eugene L. Giroux

    Inventor： Eugene L. Giroux

    IPC: C07D207/32 ,  C07D207/337 ,  C07D307/54 ,  C07D333/24 ,  A61K31/34 ,  A61K31/38 ,  A61K31/40

    CPC classification number: C07D207/337 ,  C07D307/54 ,  C07D333/24 ,  Y10S514/829 ,  Y10S514/83

    Abstract: A method of reducing local hemorrhage and tissue necrosis resulting from the bite or sting of a venomous animal whereby an envenomated mammal is treated with a compound of the formula ##STR1## or a corresponding disulfide wherein n is 1, 2 or 3; Z is O, S or NH; R is H, a straight or branched chain lower alkyl group of from 1 to 4 carbon atoms, hydroxy, a straight or branched chain lower alkoxy group of from 1 to 4 carbon atoms, fluoro, chloro, bromo, iodo or trifluoromethyl; or a pharmaceutically acceptable salt thereof.

    Abstract translation: 一种减少局部出血和由有毒动物的咬伤或刺痛引起的组织坏死的方法，由此使用下式化合物或其相应的二硫化物（其中n为1,2或3）处理被引导的哺乳动物; Z是O，S或NH; R为H，1至4个碳原子的直链或支链低级烷基，羟基，1至4个碳原子的直链或支链低级烷氧基，氟，氯，溴，碘或三氟甲基; 或其药学上可接受的盐。

    Cyclic compounds and their use
    114.
    发明授权
    Cyclic compounds and their use 失效
    环状化合物及其用途

    公开(公告)号：US4396626A

    公开(公告)日：1983-08-02

    申请号：US306534

    申请日：1981-09-28

    Applicant: Robert W. Ward ,  Alexander C. Goudie

    Inventor： Robert W. Ward ,  Alexander C. Goudie

    IPC: A61K31/40 ,  A61P29/00 ,  C07D207/32 ,  C07D207/333 ,  C07D207/337 ,  C07D207/34

    CPC classification number: C07D207/333 ,  C07D207/337 ,  C07D207/34 ,  Y10S514/825

    Abstract: Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts and pro-drugs thereof, wherein: Ar is a phenyl group optionally substituted by one or two moieties selected from halogen, C.sub.1-4 alkyl, methoxy, methylthio or trifluoromethyl, or a 2-thienyl group or N-methyl-2-pyrryl group optionally substituted by one or two C.sub.1-4 alkyl groups;R is hydrogen or methyl; andn is 0 or 1having useful anti-inflammatory and/or analgesic activity, pharmaceutical compositions containing them, and processes for their preparation.

    Abstract translation: 式（I）的化合物：其中I和其药学上可接受的盐和前药，其中：Ar是任选被一个或两个选自卤素，C 1-4烷基，甲氧基，甲硫基的部分取代的苯基 或三氟甲基，或任选被一个或两个C 1-4烷基取代的2-噻吩基或N-甲基-2-吡咯基; R是氢或甲基; 并且n为0或1具有有用的抗炎和/或止痛活性，含有它们的药物组合物及其制备方法。

    Process for the preparation of pyrryl-2-acetonitrile
    117.
    发明授权
    Process for the preparation of pyrryl-2-acetonitrile 失效
    制备吡咯-2-乙腈的方法

    公开(公告)号：US4374256A

    公开(公告)日：1983-02-15

    申请号：US8943

    申请日：1979-02-02

    Applicant: James T. F. Kao ,  Karl E. Wiegand

    Inventor： James T. F. Kao ,  Karl E. Wiegand

    IPC: C07D207/32 ,  C07D207/337

    CPC classification number: C07D207/337

    Abstract: Pyrryl-2-acetonitriles corresponding to the formula ##STR1## in which R.sub.1 stands for hydrogen or an alkyl group having 1-4 carbon atoms prepared from dialkyl-(pyrryl-2-methyl)-amine corresponding to the formula ##STR2## in which R.sub.1 is defined as above and R.sub.2 and R.sub.3 stand for alkyl groups having 1-4 carbon atoms, are alkylated with alkyl halides such as methyl chloride or methyl bromide to form the corresponding trialkyl-(pyrryl-2-methyl)-ammonium chloride quaternary salts and then reacted with an aqueous solution of alkali cyanide in the presence of a water-immiscible solvent under conditions which provide more economical utilization of reactants and process equipment.

    Abstract translation: 对应于式“IMAGE”的吡咯-2-乙腈，其中R1代表对应于式“IMAGE”的二烷基 - （吡咯-2-甲基） - 胺制备的氢或具有1-4个碳原子的烷基，其中 R1如上定义，R2和R3代表具有1-4个碳原子的烷基，用烷基卤如氯甲烷或甲基溴烷基化，形成相应的三烷基 - （吡咯-2-甲基） - 氯化铵季盐 然后在水混溶性溶剂的存在下，在提供更经济地利用反应物和工艺设备的条件下，与碱金属氰化物水溶液反应。

    Benzyl pyrrolyl methyl carboxylate insecticides and acaricides
    118.
    发明授权
    Benzyl pyrrolyl methyl carboxylate insecticides and acaricides 失效
    苄基吡咯甲酸甲酯杀虫剂和杀螨剂

    公开(公告)号：US4336194A

    公开(公告)日：1982-06-22

    申请号：US57282

    申请日：1979-07-13

    Applicant: Tadashi Ohsumi ,  Nobushige Itaya ,  Masachika Hirano

    Inventor： Tadashi Ohsumi ,  Nobushige Itaya ,  Masachika Hirano

    IPC: A01N43/36 ,  A01N53/04 ,  C07D207/00 ,  C07D207/32 ,  C07D207/323 ,  C07D207/325 ,  C07D207/452

    CPC classification number: C07D207/323 ,  C07D207/325

    Abstract: Carboxylic acid esters of the formula (I), ##STR1## wherein X is a hydrogen atom, or a C.sub.1 -C.sub.3 alkyl or a C.sub.1 -C.sub.3 alkoxyl group or a halogen atom linked to the meta or para position and R.sub.1 is a group of the formula (II) or (III), ##STR2## wherein R.sub.2 is a hydrogen atom or a methyl group, and when R.sub.2 is a methyl group R.sub.3 is also a methyl group, and when R.sub.2 is a hydrogen atom R.sub.3 is a group of the formula, ##STR3## (wherein R.sub.5 is a halogen atom or a C.sub.1 -C.sub.3 alkyl, vinyl or a C.sub.1 -C.sub.3 alkoxymethyl group, R.sub.6 is a hydrogen or halogen atom or a methyl group, or, taken together, R.sub.5 and R.sub.6 may form a tetramethylene group by connecting together at ends thereof), R.sub.4 is a halogen atom or a C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxyl or 3,4-methylenedioxy group, n is 1 or 2 and Y is a isopropyl or cyclopropyl group. These carboxylic acid esters are produced by reacting the reactive derivatives of a carboxylic acid represented by the formula, ##STR4## wherein R.sub.1 is a group of the formula (II) or (III), ##STR5## wherein R.sub.2, R.sub.3, R.sub.4, n and Y are as defined above, and Z is a halogen atom, with an alcohol of the formula (IV), ##STR6## wherein X is as defined above, in the presence of an acid-binding agent. These carboxylic acid esters are useful as insecticides and acaricides.

    Abstract translation: 式（I）的羧酸酯，其中X为氢原子，或C1-C3烷基或C1-C3烷氧基或与间位或对位连接的卤素原子，R1为 式（II）或（III）的基团，其中R2是氢原子或甲基，当R2是甲基时，R3也是甲基，当R2是氢原子时R3是 式中的一组基团（其中R 5为卤素原子或C 1 -C 3烷基，乙烯基或C 1 -C 3烷氧基甲基，R 6为氢或卤素原子或甲基，或一起为R 5 R 6是卤原子或C 1 -C 3烷基，C 1 -C 3烷氧基或3,4-亚甲二氧基，n是1或2，Y是异丙基或 环丙基。 这些羧酸酯通过使下式表示的羧酸的反应性衍生物，其中R 1是式（II）或（III）的基团，其中R 2，R 3，R 4，n 和Y如上定义，并且Z是卤素原子，与式（IV）的醇，其中X如上定义，在酸结合剂存在下，其中X如上定义。 这些羧酸酯可用作杀虫剂和杀螨剂。

    Spiro[dihydrobenzofuran-piperidines and -pyrrolidines]
    120.
    发明授权
    Spiro[dihydrobenzofuran-piperidines and -pyrrolidines] 失效
    螺[二氢苯并呋喃 - 哌啶和吡咯烷]

    公开(公告)号：US4329464A

    公开(公告)日：1982-05-11

    申请号：US265520

    申请日：1981-05-20

    Applicant: Richard C. Effland ,  Larry Davis ,  Joseph T. Klein

    Inventor： Richard C. Effland ,  Larry Davis ,  Joseph T. Klein

    IPC: C07D207/32 ,  C07D207/325 ,  C07D491/10 ,  C07D491/107 ,  C07D521/00

    CPC classification number: C07D207/325 ,  C07D491/10

    Abstract: The invention relates to spiro[dihydrobenzofuran-piperidines and -pyrrolidines] of the formula ##STR1## wherein R is the hydrogen atom, alkyl, alkoxycarbonyl, phenoxycarbonyl, cyano, and alkyl, alkanoyl, aralkanoyl, hydroxyalkyl, benzoylalkyl, ##STR2## where p is an integer of 2 or 3 and R.sub.1 and R.sub.2 are the same or different and are hydrogen and alkyl; X is hydrogen and alkyl; Hal is a halogen and q is an integer of 0 or 1; m is an integer of 1 or 2, n is an integer of 1, 2 or 3, where the sum of m and n is 3 or 4; and the pharmaceutically acceptable acid addition salts thereof.

    Abstract translation: 本发明涉及式[IMAGE]的螺[二氢苯并呋喃 - 哌啶和吡咯烷]，其中R是氢原子，烷基，烷氧基羰基，苯氧基羰基，氰基和烷基，烷酰基，芳烷酰基，羟基烷基，苯甲酰基烷基，其中p 是2或3的整数，R 1和R 2相同或不同，为氢和烷基; X是氢和烷基; Hal是卤素，q是0或1的整数; m为1或2的整数，n为1,2或3的整数，m和n之和为3或4; 及其药学上可接受的酸加成盐。

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