Substituted biphenyl sulfonamide endothelin antagonists

C - Chemistry – Metallurgy – 07 – D

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C07D 413/12 (2006.01) A61K 31/395 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01) C07D 453/02 (2006.01) C07D 471/04 (2006.01) C07D 491/048 (2006.01)

Patent

CA 2168154

Compounds of the formula Image inhibit the activity of endothelin. The symbols are defined as follows: R1 and R2 are each directly bonded to a ring carbon and are each independently (a) hydrogen; (b) alkyl or alkoxy; (c) hydroxyl; (d) halo; or (e) amino; R3 and R4 are each directly bonded to a ring carbon and are each independently (a) 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)R5; (h) -CO2H or -CO2R5; (i) -Z4-NR6R7; (j) -Z4-N(R10)-Z5-NR8R9; or (k) R3 and R4 together may also be alkylene or alkenylene, either of which may be substituted with Z1, Z2 and Z3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; and the remaining symbols are as defined in the specification.

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