5 (6)-Benzene ring substituted benzimidazole-2-carbamate derivatives
    1.
    发明授权
    5 (6)-Benzene ring substituted benzimidazole-2-carbamate derivatives 失效
    5(6) - 苯环取代的苯并咪唑-2-氨基甲酸酯衍生物

    公开(公告)号:US3929821A

    公开(公告)日:1975-12-30

    申请号:US41796373

    申请日:1973-11-21

    申请人: SYNTEX INC

    CPC分类号: C07C335/38 C07D235/32

    摘要: R7 is lower alkyl having 1 to 4 carbon atoms or aryl, and n is 1-4; R2 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; and R5 is lower alkenyl, lower alkynyl, or aralkyl. The R1 substitution is at the 5(6)-position. The compounds are useful as pesticides, particularly as anthelmintic and antifungal agents.

    WHERE R is a lower alkyl group having 1 to 4 carbon atoms; R1 is -SOR2, -SO2R2, -SCN, -SR5, -OR5 or M'' (CH2)nMR7 where M and M'' are independently

    Benzene ring substituted benzimidazole-2-carbamate derivatives represented by the formula:

    摘要翻译: 由下式表示的苯环取代的苯并咪唑-2-氨基甲酸酯衍生物:

    4 -Fluoro nucleosides, novel intermediates and methods of preparing same
    2.
    发明授权
    4 -Fluoro nucleosides, novel intermediates and methods of preparing same 失效
    4-氟核苷,新型中间体及其制备方法

    公开(公告)号:US3928319A

    公开(公告)日:1975-12-23

    申请号:US25832772

    申请日:1972-05-31

    申请人: SYNTEX INC

    IPC分类号: C07H19/06 C07H19/16 C07H19/20

    CPC分类号: C07H19/06 C07H19/16

    摘要: 4''-fluoro nucleosides, 4''-fluoro nucleoside analogs of Nucleocidin, 2''-deoxy-4''-fluoro pyrimidine nucleosides and novel intermediates produced in the process of preparing such compounds. The process for preparing the 4''-fluoro nucleosides of the present invention comprises treating a 4'',5''-unsaturated nucleoside with iodine monofluoride to form the corresponding 5''deoxy-4''-fluoro-5''-iodo nucleoside. The latter product is transformed to corresponding 5''-azido-5''-deoxy-4''-fluoro nucleosides, 5''-amino-5''-deoxy-4''-fluoro nucleosides,5''-deoxy-4''fluoro nucleosides, 4''-fluoro nucleosides, 5''-O-phosphoryl-4''fluoro nucleosides, and 5''-sulfamoyl-4''-fluoro nucleosides. The 2''-deoxy-4''-fluoro pyrimidine nucleosides are prepared in an analogous manner from the 4'',5''-unsaturated-2''-deoxy nucleosides. The nucleosides of this invention exhibit general antimetabolite activity and/or are intermediates for compounds exhibiting such activity.

    摘要翻译: 4'-氟核苷,Nucleocidin的4'-氟核苷类似物,2'-脱氧-4'-氟嘧啶核苷和在制备这些化合物的过程中产生的新型中间体。 制备本发明的4'-氟核苷的方法包括用碘一氟处理4',5'-不饱和核苷,形成相应的5'-脱氧-4'-氟-5'-碘核苷。 将后一种产物转化为相应的5'-叠氮基-5'-脱氧-4'-氟核苷,5'-氨基-5'-脱氧-4'-氟核苷,5'-脱氧-4'-氟核苷, 4'-氟核苷,5'-O-磷酰基-4'-氟核苷和5'-氨磺酰-4'-氟核苷。 2'-脱氧-4'-氟嘧啶核苷以与4',5'-不饱和-2'-脱氧核苷类似的方式制备。 本发明的核苷显示出一般抗代谢活性和/或表现出这种活性的化合物的中间体。

    Acridone carboxylic acids and derivatives
    4.
    发明授权
    Acridone carboxylic acids and derivatives 失效
    吖啶酮羧酸及其衍生物

    公开(公告)号:US3886162A

    公开(公告)日:1975-05-27

    申请号:US45035274

    申请日:1974-03-12

    申请人: SYNTEX INC

    IPC分类号: C07D219/06 C07D37/20

    CPC分类号: C07D219/06

    摘要: Compositions containing and methods employing, as the essential ingredient, acridone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions are also disclosed. Nmethylacridone-2-carboxylic acid and 7-methoxyacridone-2carboxylic acid are illustrated as representative of the class.

    摘要翻译: 含有可用于治疗过敏症状的吖啶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和组合物的方法。 示出了N-甲基吖啶酮-2-羧酸和7-甲氧基吖啶酮-2-羧酸的代表。

    Method of using substituted xanthone carboxylic acid
    5.
    发明授权
    Method of using substituted xanthone carboxylic acid 失效
    使用取代的呫吨酮羧酸的方法

    公开(公告)号:US3885038A

    公开(公告)日:1975-05-20

    申请号:US42588573

    申请日:1973-12-18

    申请人: SYNTEX INC

    IPC分类号: A61K31/35 A61K27/00

    CPC分类号: A61K31/35

    摘要: Methods employing as the essential ingredient, novel substituted xanthone carboxylic acid compounds in the treatment of the symptons of the asthmatic condition resulting from an antigenantibody reaction. Methods for preparing these compounds and compositions and intermediates therein are also disclosed - 7 (methylthio) - xanthone - 2 - carbonylic acid is illustrated as representative of the class.

    摘要翻译: 采用新型取代的呫吨酮羧酸化合物作为必需成分的方法,用于治疗由抗原 - 抗体反应产生的哮喘状况的症状。 还公开了制备这些化合物及其组合物和中间体的方法 - 7-(甲硫基) - 呫吨酮-2-羰基酸作为该类的代表。

    New photochemical process for producing 9-oxygenated-11{60 -hydroxymethyl-15{60 -hydroxyprosta-5-cis,13-trans-dienoic acids
    6.
    发明授权
    New photochemical process for producing 9-oxygenated-11{60 -hydroxymethyl-15{60 -hydroxyprosta-5-cis,13-trans-dienoic acids 失效
    用于生产9-氧化-11 {60-羟基甲基-15 {60-羟基丙氧基-5-CIS,13-十二碳二烯酸的新型光化学方法

    公开(公告)号:US3871979A

    公开(公告)日:1975-03-18

    申请号:US44732374

    申请日:1974-03-01

    申请人: SYNTEX INC

    IPC分类号: C07C405/00 B01J1/10

    CPC分类号: C07C405/00

    摘要: New process for the production of 8R-antimeric and racemic 9oxygenated-11 Alpha -hydroxymethyl-15 Alpha -hydroxyprosta-5-cis, 13-trans-dienoic acids in which the key step comprises the sensitized irradiation of natural PGA2 methyl ester or its racemate in methanol solution, in the presence of benzophenone or another sensitizing agent, preferably at a wavelength of about 360 m Mu .

    摘要翻译: 用于生产8R-抗内聚和外消旋9-氧化-11α-羟基甲基-15α-羟基孕甾-5-顺式,13-反式二烯酸的新方法,其中关键步骤包括天然PGA2甲酯的致敏照射或 其在甲醇溶液中的外消旋体,在二苯甲酮或另一种敏化剂存在下,优选波长约360μm。

    Disubstituted xanthone carboxylic acid compounds for inhibiting asthma
    10.
    发明授权
    Disubstituted xanthone carboxylic acid compounds for inhibiting asthma 失效
    用于抑制ASTHMA的分离的XANTHONE CARBOXYLIC ACID化合物

    公开(公告)号:US3849565A

    公开(公告)日:1974-11-19

    申请号:US21728772

    申请日:1972-01-12

    申请人: SYNTEX INC

    摘要: 1. A METHOD FOR INHIBITING THE SYMPTOMS OF THE ASTHMATIC CONDITION RESULTING FROM AN ANTIGEN-ANTIBODY REACTION IN A HOST SUSCEPTIBLE TO SAID REACTION WHICH COMPRISES ADMINISTERING TO SAID HOST AN EFFECTIVE AMOUNT OF FROM ABOUT 0.005 TO ABOUT 100 MG. PER KG. OF BODY WEIGHT PER DAY SUFFICIENT TO PRODUCE SAID INHIBITION OF A COMPOUND REPRESENTED BY THE FORMULAS:

    2-(HOOC-),5,7-DI(R1-),9-(O=)-XANTHENE

    2-(HOOC-),5,7-DI(R2-),9-(O=)-XANTHENE

    WHEREIN THE R1 GROUP ARE IDENTICALLY THE GROUP

    -S(=(O)N)-R

    IN WHICH N IS THE INTEGER 1 OR 2, AND R IS LOWER ALKYL; AND ONE R2 GROUP IS SELECTED FROM THE GROUP CONSISTING OF LOWER ALKYL AND LOWER ALKOXY AND THE OTHER R2 GROUP IS THE GROUP

    -S(=(O)N)-R

    IN WHICH EACH OF N AND R IS AS DEFINED ABOVE OR PHARMACEUTICALLY ACCEPTABLE NON-TOXIC ALKYL OR GLYCEROL ESTER, UNSUBSTITUTED, MONOALKYL, DIALKYL, DIALKYLAMINOALKYL, ALKOXYALKYL OR PHENETHYL SUBSTITUTED AMIDE, OR SALT THEREOF, WHEREIN SAID ALKYL AND ALKOXY GROUPS EACH CONTAIN 1 TO 8 CARBON ATOMS.