US 2019/0161448 A1Published application

Substituted tetrahydroisoquinoline compounds useful as gpr120 agonists

AssigneeMerck Sharp & Dohme Corp.

InventorsGregory L. Adams, Jason M. Cox, John S. Debenham, Scott Edmondson, Eric J. Gilbert, Yan Guo, Yu Jiang, Hubert Josien, Hyunjin M. Kim, Ping Lan, Shouwu Miao, Christopher W. Plummer, Murali Rajagopalan, Unmesh Shah, Zhongxiang Sun, Quang T. Truong, Feroze Ujjainwalla, Francisco Velazquez, Srikanth Venkatraman, Takao Suzuki, Nengxue Wang

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Abstract

The present invention relates to a compound represented by formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.

Claims22

Dependent claims

A compound according to the formula I:

or a pharmaceutically acceptable salt thereof, wherein:
X is
(1) bond,
(2) (C1-2)alkyl, or
(3) halo(C1-2)alkyl;
ring A is
(1) aryl,
(2) 5- or 6-membered heteroaryl containing 1, 2, or 3 heteroatoms independently selected from N, O and S, or
(3) 9- or 10-membered fused heteroaryl containing 1, 2, or 3 heteroatoms independently selected from N, O, and S;
R1 is
(1) bond,
(2) (C1-6)alkyl,
(3) —O—(C1-6)alkyl-, or
(4) (C3-6)cycloalkyl;
R2 is
(1) hydrogen,
(2) hydroxy,
(3) COOH,
(4) tetrazole,
(5) hydroxyisoxazole,
(6) triazole,
(7) C(O)NH2,
(8) C(O)NHC1-6alkyl,
(9) C(O)NHC3-6cycloalkyl,
(10) C(O)NHC2-5cycloheteroalkyl,
(11) C(O)NH-aryl,
(12) C(O)NH-heteroaryl,
(13) SO2C1-6alkyl,
(14) SO2C3-6cycloalkyl,
(15) SO2C2-5cycloheteroalkyl,
(16) SO2-aryl, or
(17) SO2-heteroaryl;
R3 is
(1) hydrogen,
(2) halogen,
(3) cyano, or
(4) (C1-3)alkyl;
R4 is
(1) hydrogen,
(2) (C1-3)alkyl,
(3) halo(C1-3)alkyl, or
(4) halogen;
R5 is
(1) cyano,
(2) (C1-3)alkyl,
(3) halo(C1-3)alkyl,
(4) (C1-3)alkoxy,
(5) halo(C1-3)alkoxy, or
(6) halogen;
R6 is
(1) (C1-3)alkoxy,
(2) halo(C1-3)alkoxy,
(3) halo(C1-3)alkyl,
(4) (C3-6)cycloalkyl,
(5) (C3-6)cycloalkyl-O—,
(6) (C3-6)cycloalkyl-S—,
(7) (C3-6)cycloalkyl-(C1-2)alkyl-,
(8) (C3-6)cycloalkyl-halo(C1-2)alkyl-,
(9) phenyl,
(10) 5- to 6-membered heteroaryl-O— wherein the heteroaryl contains 1, 2, or 3 heteroatoms independently selected from N, O and S, or
(11) 5- to 6-membered heteroaryl- wherein the heteroaryl contains 1, 2, or 3 heteroatoms independently selected from N, O and S,
wherein alkyl, cycloalkyl, phenyl and heteroaryl are unsubstituted or substituted with 1-3 substituents selected from (C1-3)alkyl, halo(C1-3)alkyl, (C1-3)alkoxy, halo(C1-3)alkoxy, and halogen;
n is 0, 1, 2 or 3;
m is 0 or 1;
p is 0, 1, 2 or 3;
and
q is 0, 1, or 2.

64 more elements

Dependencies are inferred from the claim text.

Facts

Application: 16/096,710Filed 19 May 2017
Priority: CN PCT/CN2016/08326525 May 2016
Published: 30 May 2019
Term ends: Not estimatedThe source records don’t support an estimate.

Classification21 codes

C07D 217/04
With only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing…
A61K 9/4858
Filling excipients; Inactive ingredients: organic compounds
A61K 31/472
Quinolines; Isoquinolines: non-condensed isoquinolines, e.g. papaverine
A61K 31/4725
Non-condensed isoquinolines, e.g. papaverine: containing further heterocyclic rings