GLP-1 RECEPTOR AGONISTS AND USE THEREOF Russian patent published in 2021 - IPC C07D401/14 C07D405/14 C07D413/14 C07D471/04 C07D487/04 A61K31/4427 A61K31/497 A61P3/00 

Abstract RU 2740135 C1

FIELD: organic chemistry.

SUBSTANCE: present invention refers to a compound of formula I

,

or its pharmaceutically acceptable salt. In formula I, each R1 independently represents halogen, -CN, -C1-3alkyl or -OC1-3alkyl, where alkyl C1-3alkyl and OC1-3alkyl are substituted with 0–3 F atoms; m is 0, 1, 2 or 3; each R2 independently represents F or Cl; p equals 0 or 1; each R3 independently represents F, -OH, -C1-3alkyl or -C3-4cycloalkyl or 2 R3 can be cyclised together to form -C3-4spirocycloalkyl, wherein said -C1-3alkyl and -C3-4cycloalkyl can be substituted with 0–3 valence by F and 0–1 -OH; q equals 0, 1 or 2; Y is CH or N; R4 is -C1-3alkyl, -C0-3alkylene-C3-6cycloalkyl, -C0-3alkylene-R5 or C1-3alkylene R6, where said alkyl can be substituted with 0–3 substitutes, independently selected from 0–3 atoms of F and 0–1 substituents selected from C0-1alkylene ORO, and where said cycloalkyl can be independently substituted with 0–2 substituents depending on valency of 0, independently selected from 0–2 atoms of F and 0–1 substituents selected from C0-1alkylene ORO; R5 is 4–6 membered heterocycloalkyl (where said heterocycloalkyl can contain 1 to 2 heteroatoms selected from O and/or N), wherein said heterocycloalkyl can be substituted with 0–2 substitutions independently selected from: 0–1 oxo (=O) and 0–2 substitutes independently selected from -C1-3alkyl and -OC1-3alkyl, wherein alkyl C1-3alkyl and -OC1-3alkyl can be substituted with 0–3 substitutes independently selected from: 0–1 -ORO; R6 is 5–6 membered heteroaryl (where said heteroaryl can contain from 1 to 3 heteroatoms selected from O and/or N), where said heteroaryl can be substituted with 0–2 substitutions independently selected from: 0–2 halogens and 0–2-C1-3alkyls, where alkyl can be substituted with 0–3 substitutes independently selected from: 0–1 -ORO; each RO independently represents H or -C1-3alkyl; Z1 is CH or N; Z2 and Z3 each independently represent -CRZ or N, with the proviso that when Z1 or Z3 is N, Z2 is -CRZ; and each RZ independently represents H, F, Cl or -CH3. Pharmaceutical composition is also presented.

EFFECT: disclosed are novel organic compounds which can be used as GLP-1R agonists.

23 cl, 9 tbl, 21 ex

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RU 2 740 135 C1

Authors

Aspnes, Gary Erik

Bagley, Scott W.

Curto, John M.

Dowling, Matthew S.

Edmonds, David James

Flanagan, Mark E.

Futatsugi, Kentaro

Griffith, David A.

Huard, Kim

Ingle, Gajendra

Jiao, Wenhua

Limberakis, Chris

Mathiowetz, Alan M.

Piotrowski, David W.

Ruggeri, Roger B.

Dates

2021-01-11Published

2017-12-01Filed