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US 12,741,971 B2Granted
Certain 2,5-diazabicyclo[4.2.0]octanes and octahydrofuro[3,4-b]pyrazines as GLP-1 receptor modulators
AssigneeAstraZeneca AB
InventorsMagnus Polla, Joakim Bergman, Johan Sundell, Jonas Brånalt, Ekaterina Ratkova, Johan Kajanus, Magnus Johansson
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Abstract
There are disclosed certain 2,5-diazabicyclo[4.2.0]octanes of formula (I) and octahydrofuro[3,4-b]pyrazines, and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are GLP-1 receptor modulators and are thereby particularly useful in the treatment or prophylaxis of cardiovascular disease and metabolic conditions, for example Type 2 diabetes.
Claims7
A compound of Formula (I),
- or a compound of Formula (II),
- wherein
- A is phenyl or pyridyl;
- X is independently N or C, provided that no more than two atoms in the aromatic ring B are N;
- Z1 is N or CR3;
- Z2 and Z3 are each independently N or CR4, provided that when Z1 or Z3 is N, Z2 is CR4;
- R1 is independently selected from F, Cl, Br, CN, OCH3, OCFH2, OCF2H, OCF3, CH3, CFH2, CF2H and CF3;
- R2 is selected from F, Cl or CN;
- R3 is selected from H, F, Cl, N(CH3)2, C1-2alkyl and OC1-2alkyl, wherein said C1-2alkyl is substituted by 0, 1, 2 or 3 F;
- R4 is independently selected from H, F, Cl, OH, CH3, CFH2, CF2H, CF3, OCH3, OCFH2, OCF2H and OCF3;
- R5 is selected from (4- to 6-membered)heterocycloalkyl, (5- to 6-membered)heteroaryl, CN, C1-4alkyl, O(C1-4alkyl), S(C1-4alkyl), cyclopropyl, cyclobutyl, O(cyclopropyl) or S(cyclopropyl), wherein said (4- to 6-membered)heterocycloalkyl and (5- to 6-membered)heteroaryl is substituted by 0 or 1 substituent selected from C1-2alkyl and wherein said C1-4alkyl is substituted by 0 or 1 substituent selected from CN or OCH3, and 0, 1, 2 or 3 F and wherein said cyclopropyl and cyclobutyl is substituted by 0 or 1 substituent selected from CN, OCH3, OCFH2, OCF2H, OCF3 and CH2CN and 0, 1, 2 or 3 F;
- R6 is independently selected from F, C1-2alkyl and OC1-2alkyl, wherein said C1-2alkyl is substituted by 0, 1, 2 or 3 F;
- m is 0, 1, 2 or 3;
- n is 0 or 1;
- p is 1, 2 or 3;
- and
- q is 0, 1 or 2;
- or a pharmaceutically acceptable salt thereof.
15 more elements
Dependencies are inferred from the claim text.