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    • 27. 发明授权
    • Phenyl sulfonamide endothelin antagonists
    • 苯磺酰胺内皮素拮抗剂
    • US06673824B1
    • 2004-01-06
    • US09552543
    • 2000-04-19
    • Natesan MurugesanJohn T. HuntPhilip D. Stein
    • Natesan MurugesanJohn T. HuntPhilip D. Stein
    • A61K3142
    • C07D261/20C07D261/16C07D261/18
    • Compounds of the formula inhibit the activity of endothelin. The symbols are defined as follows: R1, R2 and R3 are each independently (a) hydrogen, except that R1 is other than hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) —C(O)H or —C(O)R6; (h) —CO2H or —CO2R6; (i) —SH, —S(O)nR6, —S(O)m—OH, —S(O)m—OR6, —O—S(O)m—R6, —O—S(O)mOH or —O—S(O)m—OR6; (j) —Z4—NR7R8; or (k) —Z4—N(R11)—Z5—NR9R10; and the remaining symbols are as defined in the specification.
    • 化合物抑制内皮素的活性。 符号定义如下:R 1,R 2和R 3各自独立地为(a)氢,除了R 1不是氢;(b)烷基,烯基,炔基,烷氧基 ,环烷基,环烷基烷基,环烯基,环烯基烷基,芳基,芳氧基,芳烷基或芳烷氧基,其中任何一个可被Z 1,Z 2和Z 3取代;(c)卤素;(d)羟基; e)氰基;(f)硝基;(g)-C(O)H或-C(O)R 6;(h)-CO 2 H或-CO 2 R 6;(ⅰ)-SH,-S O)n R 6,-S(O)m -OH,-S(O)m OR 6,-OS(O)m R 6,-OS(O)mOH或-OS(O) m-OR 6;(j)-Z 4 -NR 7 R 8; 或(k)-Z 4 -N(R 11)-Z 5 -NR 9 R 10;其余符号如说明书中所定义。