Preparation of N-aryl urea derivatives as IDO inhibitors.

  • Markwalder J
  • Seitz S
  • Balog J
  • et al.
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Abstract

There are disclosed compds. of formula I that modulate or inhibit the enzymic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compns. contg. said compds. and methods of treating proliferative disorders, such as cancer, viral infections and/or autoimmune diseases utilizing the compds. of the invention. Compds. of formula I wherein W is CR4 and N; V is CR5 and N; Y is CR6 and N; A is (un)substituted aryl and (un)substituted 5- to 7-membered heteroaryl; R1 is CO2H, (un)substituted heterocyclyl, sulfonylamino, etc.; R2 and R3 are independently H, halo, (un)substituted C1-6 alkyl, etc.; R4, R5 and R6 are independently H, halo, CN, OH, etc.; R7 and R8 are independently H, (un)substituted C1-6 alkyl, (un)substituted C1-6 alkyl, (un)substituted aryl, etc.; provided that only one of R7 and R8 is H; R9 is (un)substituted aryl, (un)substituted C3-8 cycloalkyl, (un)substituted C1-6 alkyl, etc.; and stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, are claimed. Example compd. II was prepd. by a multistep procedure (procedure given). The invention compds. were evaluated for there IDO inhibitory activity (data given). [on SciFinder(R)]

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Markwalder, J. A., Seitz, S. P., Balog, J. A., Huang, A., Williams, D. K., Chen, L., … Srivastava, Shefali. (2015, March 5). Preparation of N-aryl urea derivatives as IDO inhibitors. PCT Int. Appl. Bristol-Myers Squibb Company, USA .

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