C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 413/12 (2006.01) A61K 31/42 (2006.01) A61K 31/425 (2006.01) A61K 31/435 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) C07D 231/42 (2006.01) C07D 413/14 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01) C07D 453/02 (2006.01) C07D 471/04 (2006.01) C07D 491/048 (2006.01) C07D 498/04 (2006.01) C07D 521/00 (2006.01)
Patent
CA 2240043
Compounds of formula (I) inhibit the activity of endothelin. The symbols are defined as follows: R1, R2, 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.
Les composés de la formule (I) inhibent l'activité de l'endothéline. Dans cette formule, chaque groupe R?1¿, R?2¿, R?3¿ et R?4¿ est lié directement à un carbone de cycle et représente, d'une manière indépendante : (a) un hydrogène; (b) un alkyle, alcényle, alcynyle, alcoxy, cycloalkyle, cycloalkyl-alkyle, cycloalcényle, cycloalcényl-alkyle, aryle, aryloxy, aralkyle ou aralcoxy, qui peuvent tous être substitués par Z?1¿, Z?2¿ et Z?3¿: (c) halo; (d) hydroxyle; (e) cyano; (f) nitro; (g) -C(O)H ou -C(O)R?5¿; (h) -CO¿2?H ou -CO¿2?R?5¿; (i) -Z?4¿-NR?6¿R?7¿; (j) -Z?4¿-N(R?10¿)-Z?5¿-NR?8¿R?9¿; ou (k) R?3¿ et R?4¿ peuvent former ensemble un alkylène ou un alcénylène (éventuellement substitués par Z?1¿, Z?2¿ et Z?3¿) formant avec les atomes de carbone auxquels il est fixé, un cycle à 4 - 8 éléments, saturé, insaturé ou aromatique. La signification des autres symboles est donnée dans la description.
Barrish Joel C.
Murugesan Natesan
Spergel Steven H.
Bristol-Myers Squibb Company
Gowling Lafleur Henderson Llp
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