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    Polyunsaturated prostaglandin derivatives
    1.
    发明授权
    Polyunsaturated prostaglandin derivatives 失效
    多不饱和前列腺素衍生物

    公开(公告)号：US3970684A

    公开(公告)日：1976-07-20

    申请号：US488595

    申请日：1974-07-15

    Applicant: Pierre Crabbe ,  John H. Fried ,  Angel Guzman

    Inventor： Pierre Crabbe ,  John H. Fried ,  Angel Guzman

    IPC: C07C405/00 ,  C07F9/40 ,  C07C61/38 ,  C07C69/74

    CPC classification number: C07C405/00 ,  C07F9/4006

    Abstract: Novel prostaglandin dehydro analogs of the PGA and PGB series and the 9-hydroxy-derivatives thereof, which possess a diethylenic unsaturation in the carboxylic acid chain and may be additionally substituted at C-4, C-6, C-9 and/or C-15 by a methyl, ethyl or propyl group, as well as the C-20-nor, bisnor or C-20 alkyl derivatives thereof, the alkyl group being of a straight chain and containing from 1 to 5 carbon atoms inclusive,, and processes for making same. 9-keto-15.alpha.-hydroxyprosta-4,5,10,13-trans-tetraenoic acid and 9-keto-15.alpha.-hydroxyprosta-4,5,8(12),13-trans-tetraenoic acid are representative of the class. Also included are the pharmaceutically acceptable, non toxic esters and salts of the carboxylic acid function and the pharmaceutically acceptable, non toxic esters and/or ethers of the secondary hydroxyl groups. These compounds possess prostaglandin-like activities and thus are useful in the treatment of mammals, where prostaglandins are indicated.

    Abstract translation: PGA和PGB系列的新型前列腺素脱氢类似物及其9-羟基衍生物，其在羧酸链中具有二烯基不饱和键，并且可以在C-4，C-6，C-9和/或C -15的甲基，乙基或丙基，以及它们的C-20-还原，bisnor或C-20烷基衍生物，该烷基是直链并含有1至5个碳原子的烷基，和 制作相同的过程 9-酮-15-α-羟基孕甾-4,5,10,13-反 - 四烯酸和9-酮-15α-羟基孕甾-4,5,8（12），13-反式 - 四烯酸代表 类。 还包括药学上可接受的，无毒的酯和羧酸官能团的盐和仲羟基的药学上可接受的无毒酯和/或醚。 这些化合物具有前列腺素样活性，因此可用于治疗表达前列腺素的哺乳动物。

    5(6)-Benzene ring substituted benzimidazole-2-carbamate derivatives having anthelmintic activity
    6.
    发明授权
    5(6)-Benzene ring substituted benzimidazole-2-carbamate derivatives having anthelmintic activity 失效
    5（6）具有驱虫活性的苯并环取代的苯并咪唑-2-氨基甲酸酯衍生物

    公开(公告)号：US3993768A

    公开(公告)日：1976-11-23

    申请号：US604502

    申请日：1975-08-13

    Applicant: Colin C. Beard ,  John A. Edwards ,  John H. Fried

    Inventor： Colin C. Beard ,  John A. Edwards ,  John H. Fried

    IPC: C07D235/32

    CPC classification number: C07D235/32

    Abstract: This application describes further species embraced by the following generic formula: ##SPC1##Where R is a lower alkyl group having 1 to 4 carbon atoms; R.sup.1 is --SOR.sup.2, --SO.sub.2 R.sup.2, --SCN, --SR.sup.5, --OR.sup.5 or M'(CH.sub.2).sub.n MR.sup.7 where M and M' are independently ##EQU1## R.sup.7 is lower alkyl having 1 to 4 carbon atoms or aryl, and n is 1-4; R.sup.2 is lower alkyl having from 1 to 6 carbon atoms, cycloalkyl having 3 to 7 carbon atoms, lower alkenyl or lower alkynyl having 3 to 6 carbon atoms, or aralkyl or aryl; R.sup.5 is lower alkenyl, lower alkynyl, or aralkyl; and the R.sup.1 substitution is at the 5(6)-position. The above compounds can also be substituted at the 1-position.

    Abstract translation: 本申请描述了由以下通式表示的其它物质：+ q，10，其中R是具有1至4个碳原子的低级烷基; R 1是-SOR 2，-SO 2 R 2，-SCN，-SR 5，-OR 5或M'（CH 2）nMR 7，其中M和M'独立地为O和R a，O，S，S，S和R d' 4个碳原子或芳基，n为1-4; R2是具有1至6个碳原子的低级烷基，具有3至7个碳原子的环烷基，具有3至6个碳原子的低级链烯基或低级炔基，或芳烷基或芳基; R5是低级烯基，低级炔基或芳烷基; 而R1取代位于5（6）位。 上述化合物也可以在1-位取代。

    Method of use of, and compositions containing, disubstituted xanthone carboxylic acid compounds
    8.
    发明授权
    Method of use of, and compositions containing, disubstituted xanthone carboxylic acid compounds 失效
    使用方法和含有二取代的呫吨酮羧酸化合物的组合物

    公开(公告)号：US3951618A

    公开(公告)日：1976-04-20

    申请号：US542477

    申请日：1975-01-20

    Applicant: Jurg R. Pfister ,  Ian T. Harrison ,  John H. Fried

    Inventor： Jurg R. Pfister ,  Ian T. Harrison ,  John H. Fried

    IPC: C07D311/86 ,  A61K31/35

    CPC classification number: C07D311/86

    Abstract: Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methylthio-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di-(methylthio)xanthone-2-carboxylic acid are illustrated as representative compounds.

    Abstract translation: 含有可用于治疗过敏症状的新型二取代呫吨酮羧酸化合物作为必需成分的组合物和方法。 还公开了制备这些化合物及其组合物和中间体的方法。 5-甲硫基-7-异丙氧基呫吨酮-2-羧酸和5,7-二（甲硫基）呫吨酮-2-羧酸作为代表性化合物。

    .beta.-Adrenergic blocking agents in the 1,2,3-thiadiazole series
    9.
    发明授权
    .beta.-Adrenergic blocking agents in the 1,2,3-thiadiazole series 失效
    {62-在1,2,3-噻二唑系列中的肾上腺素能阻断剂

    公开(公告)号：US3940407A

    公开(公告)日：1976-02-24

    申请号：US506659

    申请日：1974-09-16

    Applicant: Joseph M. Muchowski ,  John H. Fried

    Inventor： Joseph M. Muchowski ,  John H. Fried

    IPC: C07C45/54 ,  C07C45/64 ,  C07D285/06

    CPC classification number: C07D285/06 ,  C07C205/45 ,  C07C45/54 ,  C07C45/64

    Abstract: Novel 4-[2,3 or 4(3-amino-2-hydroxypropoxy) phenyl]- and 5-[2,3 or 4(3-amino-2-hydroxypropoxy) phenyl]-1,2,3-thiadiazole derivatives which may be further substituted at the C-5 or C-4 position of the thiadiazole ring, respectively, by a lower alkyl, phenyl, trifluoromethyl, carboxy, alkoxycarbonyl, cyano or an aminocarbonyl group, and the pharmaceutically acceptable acid addition salts thereof and processes for the production of such compounds; 4-[4(3-t-butylamino-2-hydroxypropoxy)phenyl]-1,2,3-thiadiazole and 5-[4(3-t-butylamino-2-hydroxypropoxy)phenyl]-1,2,3-thiadiazole are representative of the class. These compounds possess cardiovascular activity and are useful for the treatment of abnormal heart conditions in mammals.

    Abstract translation: 4- [2,3或4（3-氨基-2-羟丙氧基）苯基]和5- [2,3或4（3-氨基-2-羟基丙氧基）苯基] -1,2,3-噻二唑衍生物 其可以在噻二唑环的C-5或C-4位被低级烷基，苯基，三氟甲基，羧基，烷氧基羰基，氰基或氨基羰基进一步取代，及其药学上可接受的酸加成盐和 生产这些化合物的方法; 4- [4-（3-叔丁基氨基-2-羟基丙氧基）苯基] -1,2,3-噻二唑和5- [4（3-叔丁基氨基-2-羟基丙氧基）苯基] 噻二唑是该类的代表。 这些化合物具有心血管活性，可用于治疗哺乳动物异常心脏病。

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