Preparation of tetrahydroisoquinoline and tetrahydrobenzoazepine derivatives for use as GPR120 modulators.
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Preparation of tetrahydroisoquinoline and tetrahydrobenzoazepine derivatives for use as GPR120 modulators. / Brown, Jane (Inventor); Connolly, Stephen (Inventor); Hansen, Steffen V. F. (Inventor); Milne, Gavin (Inventor); Shimpukade, Bharat (Inventor); Smyth, Don (Inventor); Thomas, Gerard (Inventor); Ulven, Trond (Inventor); Brvar, Matjaz (Inventor); Rigby, Aaron. (Inventor).
Caldan Therapeutics Limited, UK . Patent No.: WO2018172727A1. Sep 27, 2018.Research output: Patent
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TY - PAT
T1 - Preparation of tetrahydroisoquinoline and tetrahydrobenzoazepine derivatives for use as GPR120 modulators.
AU - Brown, Jane
AU - Connolly, Stephen
AU - Hansen, Steffen V. F.
AU - Milne, Gavin
AU - Shimpukade, Bharat
AU - Smyth, Don
AU - Thomas, Gerard
AU - Ulven, Trond
AU - Brvar, Matjaz
AU - Rigby, Aaron.
PY - 2018/9/27
Y1 - 2018/9/27
N2 - 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)]
AB - 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)]
KW - tetrahydrobenzoazepine prepn GPR120 modulator
KW - tetrahydroisoquinoline prepn GPR120 modulator
M3 - Patent
M1 - WO2018172727A1
PB - Caldan Therapeutics Limited, UK .
ER -
ID: 221841113