GLP-1 RECEPTOR AGONISTS AND APPLICATION THEREOF Russian patent published in 2022 - IPC C07D401/14 C07D405/14 C07D413/14 C07D471/14 A61K31/4427 A61K31/497 A61K31/506 A61P3/10 

Abstract RU 2765721 C1

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound by the formula I or a pharmaceutically acceptable salt thereof, exhibiting agonistic activity against the GLP-1 receptor and applicable in treatment of diseases associated therewith. In the formula I, A represents A1 or A2, each R1 independently represents a halogen or -CN; m equals 0, 1, 2, or 3; X-L represents N-CH2, CHCH2, or cyclopropyl; Y represents CH or N; ZA1 represents CH, CR2, or N; ZA2 represents CH, CR2, or N; ZA3 represents CH, CR2, or N; provided that ZA2 and ZA3 are simultaneously not N, and additionally provided that one of ZA2 and ZA3 represents N when X-L represents N-CH2; each R2 represents F; each R3 independently represents a -C1-3alkyl; q equals 0, 1 or 2; R4 represents a -C1-3alkyl, -C0-3alkylene-R5 or -C1-3alkylene-R6, wherein said alkyl can be substituted, as permitted by the valency, 0 to 3 substituents independently selected from 0 to 3 F atoms and 0 to 1 substituent selected from -C0-1alkylene-ORO; R5 represents a 4-6-membered heterocycloalkyl containing 1 to 2 heteroatoms independently selected from N and O, wherein said heterocycloalkyl can be substituted with 0-1 oxo (=O); R6 represents a 5-6-membered heteroaryl containing 2 to 3 heteroatoms independently selected from N and O, wherein said heteroaryl can be substituted with 0 to 2 substituents, as permitted by the valency, independently selected from 0-2 -C1-3alkyls; each RO independently represents H or a C1-3alkyl; each of Z1, Z2 and Z3 represents -CRZ or one of Z1, Z2 and Z3 represents N and the other two represent -CRZ; and each RZ independently represents H. The invention also relates to specific compounds, a pharmaceutical composition, and a method for treating a cardiometabolic disease and diseases associated therewith.

EFFECT: creation of a compound for treating diseases associated with the GLP-1 receptor.

20 cl, 11 tbl, 80 ex

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RU 2 765 721 C1

Authors

Aspnes, Gary Erik

Bagley, Scott W.

Conn, Edward L.

Curto, John M.

Edmonds, David James

Flanagan, Mark E.

Futatsugi, Kentaro

Griffith, David A.

Huard, Kim

Limberakis, Chris

Mathiowetz, Alan M.

Piotrowski, David W.

Ruggeri, Roger B.

Dates

2022-02-02Published

2019-06-13Filed