Preparation of tetrahydroisoquinoline and tetrahydrobenzoazepine derivatives for use as GPR120 modulators.

Research output: Patent

  • Jane Brown (Inventor)
  • Stephen Connolly (Inventor)
  • Steffen V. F. Hansen (Inventor)
  • Gavin Milne (Inventor)
  • Bharat Shimpukade (Inventor)
  • Don Smyth (Inventor)
  • Gerard Thomas (Inventor)
  • Ulven, Trond (Inventor)
  • Matjaz Brvar (Inventor)
  • Aaron. Rigby (Inventor)
Title compds. I [A = CO2H, CH2OH, tetrazolyl, etc.; E and L independently = (un)substituted alkyl, alkoxy, cycloalkyl, etc.; G = (un)substituted aryl, heteroaryl, or fused aryl or heteroaryl ring; J = C(R1)2, O, NR1, or S; M = aryl, heteroaryl, or cycloalkyl; X = absent, O, S, or C(R1)2; Y = absent, O, or C(R1)2; Z = absent or C(R1)2; X and Y, Y and Z, or X and Z may be combined to form an (un)substituted cycloalkyl ring; each R1 independently = H, D, halo, or (un)substituted alkyl; n = 1 or 2; with provisions], and their pharmaceutically acceptable salts, are prepd. and disclosed as GPR120 modulators. Thus, e.g., II was prepd. by a multistep procedure (prepn. given). I were evaluated in human GPR120-B arrestin 2 bio-luminescence resonance energy transfer (BRET) agonist assays, e.g., II demonstrated a pEC50 value of 7.4. [on SciFinder(R)]
Original languageEnglish
Patent numberWO2018172727A1
Country/TerritoryDenmark
Publication statusPublished - 27 Sep 2018

    Research areas

  • tetrahydrobenzoazepine prepn GPR120 modulator, tetrahydroisoquinoline prepn GPR120 modulator

ID: 221841113