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    • 81. 发明授权
    • N-phenylsulfonyl-N'-pyrimidinyl-ureas
    • N-苯基磺酰基-N'-嘧啶基 - 脲
    • US4759793A
    • 1988-07-26
    • US30529
    • 1987-03-27
    • Willy MeyerKonrad Oertle
    • Willy MeyerKonrad Oertle
    • C07D249/16A01N43/70A01N47/36C07C20060101C07C67/00C07C301/00C07C309/86C07C311/15C07C311/16C07C311/17C07C311/29C07C311/39C07C311/53C07C311/65C07C325/00C07C331/16C07C331/32C07D239/42C07D239/46C07D239/47C07D239/48C07D239/52C07D239/56C07D239/69C07D251/16C07D251/18C07D251/22C07D251/46C07D251/52C07D521/00A01N43/54
    • C07C309/86A01N47/36C07C311/65C07D521/00
    • N-Phenylsulfonyl-N'-pyrimidinyl- and -triazinylureas of the formula I ##STR1## wherein A is 3,3,3-trifluoropropyl or 3,3-difluorobutyl,R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl, C.sub.1 -C.sub.4 -alkylsulfonyl, --CO-R.sup.6, --NR.sup.7 R.sup.8, --CO--NR.sup.9 R.sup.10 or --SO.sub.2 --NR.sup.11 R.sup.12,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -alkylsulfinyl or C.sub.1 -C.sub.4 -alkylsulfonyl,R.sup.3 and R.sup.4 independently of one another are each hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.2 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkylthio, C.sub.2 -C.sub.4 -alkoxyalkyl, C.sub.1 -C.sub.4 -alkoxy or --NR.sup.12 R.sup.13,R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxy,R.sup.6 is C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.2 -C.sub.6 -alkoxyalkoxy, hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -haloalkyl,R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11, R.sup.12 and R.sup.13 independently of one another are each hydrogen or C.sub.1 -C.sub.4 -alkyl,E is nitrogen or the methine bridge, andZ is oxygen or sulfur;and also the salts of these compounds.
    • 式I的N-苯基磺酰基-N'-嘧啶基 - 和 - 三嗪基脲其中A是3,3,3-三氟丙基或3,3-二氟丁基,R 1是氢,卤素,硝基,氰基,C 1 C 1-4烷基,C 1 -C 4 - 卤代烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 烷硫基,C 1 -C 4 - 烷基亚磺酰基,C 1 -C 4烷基磺酰基,-CO-R 6,-NR 7 R 8,-CO-NR 9 R 10或-SO 2 -NR 11 R 12,R 2是氢,卤素,C 1 -C 4 - 烷基,C 1 -C 4 - 烷氧基,C 1 -C 4 - 烷硫基,C 1 -C 4烷基亚磺酰基或C 1 -C 4烷基磺酰基,R 3和R 4彼此独立地各自为氢, 卤素,C 1 -C 4烷基,C 1 -C 4卤代烷基,C 2 -C 4卤代烷氧基,C 1 -C 4烷硫基,C 1 -C 4卤代烷硫基,C 2 -C 4烷氧基烷基,C 1 -C 4烷氧基或-NR 12 R 13, ,C 1 -C 4烷基或C 1 -C 4 - 烷氧基,R 6是C 1 -C 4 - 烷氧基,C 1 -C 4卤代烷氧基,C 1 -C 4 - 烷硫基,C 2 -C 6 - 烷氧基烷氧基,氢,C 1 -C 4烷基或C 1 -C 4 卤代烷基,R 7,R 8,R 9,R 10,R 11,R 12和R 13各自独立地为氢或C 1 -C 4烷基,E为氮或次甲基桥,Z为氧或硫; 以及这些化合物的盐。
    • 83. 发明授权
    • Phenothiazine compounds
    • 吩噻嗪化合物
    • US4705854A
    • 1987-11-10
    • US738846
    • 1985-05-28
    • Harry J. Leighton
    • Harry J. Leighton
    • A61K31/54A61K31/5415A61P37/08A61P43/00C07C67/00C07C301/00C07C311/16C07C313/00C07C323/67C07D279/28C07D417/04C07D417/06C07D453/02C07F9/6547
    • C07D417/04C07D279/28C07D417/06C07D453/02C07F9/6547
    • The present invention relates to compounds of the formula (I): ##STR1## or a salt, ester or amide thereof; wherein R.sup.1 is a C.sub.1-7 bivalent aliphatic hydrocarbon group or a single bond;R.sub.2 and R.sub.3 are the same or different and are each hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members;R.sup.4 is hydrogen, halogen, C.sub.1-4 alkoxy, C.sub.1-4 alkyl optionally substituted by one to three halogen atoms; or a group R.sub.1 CO.sub.2 H as hereinbefore defined; andA is C.sub.1-4 alkylene or ANR.sub.2 R.sub.3 forms a group --CH.sub.2 --(CH.sub.2).sub.2 or CH.sub.2 --(CH.sub.2).sub.2B is an acidic group other than a mono-carboxylic acid group of comparable or greater acid strength than a carboxylic acid group in a similar chemical environment, provided that any sulphonamide group contains at least one N-H bond.Also disclosed are processes for the preparation of the compounds of the formula (I), chemical intermediates for use in their preparation, and pharmaceutical formulations containing the said compounds.The compounds have antiallergic activity as defined by blockade of anaphylactoid activity. Certain of the compounds also have good antihistaminic activity.
    • 本发明涉及式(I)的化合物或其盐,酯或酰胺: 其中R1是C1-7二价脂族烃基或单键; R2和R3相同或不同,各自为氢,C1-4烷基或与氮一起包含含有4-6个环成员的含氮杂环; R4是氢,卤素,C1-4烷氧基,任选被一至三个卤素原子取代的C 1-4烷基; 或如上文所定义的基团R 1 CO 2 H; 和A是C 1-4亚烷基或ANR2R 3形成基团-CH 2 - (CH 2)2或CH 2 - (CH 2)2 B是与羧酸基相当或更大的酸强度的单羧酸基团以外的酸性基团 在类似的化学环境中,条件是任何磺酰胺基团含有至少一个NH键。 还公开了制备式(I)化合物,其制备中使用的化学中间体和含有所述化合物的药物制剂的方法。 该化合物具有通过阻断过敏性活性所定义的抗过敏活性。 某些化合物也具有良好的抗组胺活性。
    • 90. 发明授权
    • Derivatives of 4-chloro-5-sulfamoyl-anthranilic acid
    • 4-氯代-5-磺酰氨基苯甲酸的衍生物
    • US3860582A
    • 1975-01-14
    • US27131472
    • 1972-07-12
    • TEVA MIDDLE EAST PHARM
    • SCHOENBERG SHLOMOYELLIN HAIM
    • C07C311/16C07C303/40C07C311/40C07D307/52C07D5/16A61K27/00
    • C07D307/52
    • New derivatives of 4-chloro-5-sulfamoyl-anthranilic acid. In the new derivatives the 5-sulfamoyl group is substituted by R1XCH2, where X is oxygen or sulfur and R1 is a straight or branchedchain lower alkyl radical of up to 10 carbon atoms which may be substituted by a hydroxy or alkoxy group or several such groups, a cycloalkyl radical, an alkenyl or alkinyl radical, an aralkyl or heteroarylalkyl radical. The novel compounds are valuable diuretics and saluretics and they are prepared from corresponding free sulfamoyl compounds by reaction with formaldehyde or paraformaldehyde and a compound R1-XH where R1 and X have the same meaning as above.
    • 4-氯-5-氨磺酰 - 邻氨基苯甲酸的新衍生物。 在新衍生物中,5-氨磺酰基被R1XCH2取代,其中X是氧或硫,R1是至多10个碳原子的直链或支链低级烷基,其可被羟基或烷氧基取代或几个 这些基团,环烷基,烯基或炔基,芳烷基或杂芳基烷基。 新型化合物是有价值的利尿剂和盐溶剂,它们是通过与甲醛或多聚甲醛反应制备的相应的游离氨磺酰化合物和化合物R1-XH,其中R1和X具有与上述相同的含义。