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US 11,230,532 B2Granted
Pyrimidines and variants thereof, and uses therefor
AssigneeAfferent Pharmaceuticals, Inc.
InventorsRonald Charles Hawley, Prabha Ibrahim, Anthony P. Ford, Joel R. Gever
Life of this patent
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Abstract
The present disclosure provides pyrimidine compounds of Formula 1 and uses thereof, for example, for the potential treatment of diseases associated with P2X purinergic receptors: In certain aspects, the present disclosure provides P2X3 and/or P2X2/3 antagonists which are useful, for example, for the potential treatment of visceral organ, cardiovascular and pain-related diseases, conditions and disorders.
Claims12
A compound of Formula 1:
- or a pharmaceutically acceptable salt thereof, wherein:
- W is selected from O, S and NH;
- X1 is N or CR2;
- X2 is CR3;
- X3 is CR4;
- X4 is CR5;
- X5 is N or CR6, provided, however, when X1 is CR2, W is not O;
- Y is —NRdRe, wherein one of Rd and Re is hydrogen, and the other is selected from hydrogen and C1-12-alkyl;
- D is absent;
- R1 is selected from C1-12-alkyl, C2-12-alkenyl, C2-12-alkynyl, C3-12-cycloalkyl, C3-12-cycloalkenyl, C1-12-haloalkyl, and C1-12-hydroxyalkyl;
- R2, R3, and R4 are each independently selected from hydrogen, C1-12-alkyl, C2-12-alkenyl, C2-12-alkynyl, amino, halo, amido, C1-12-haloalkyl, C1-12-alkoxy, hydroxy, C1-12-haloalkoxy, nitro, C1-12-hydroxyalkyl, C2-12-alkoxyalkyl, C1-12-hydroxyalkoxy, C3-12-alkynylalkoxy, C1-12-alkylsulfonyl, C5-12-arylsulfonyl, cyano, C6-12-aryl, C5-12-heteroaryl, C3-12-heterocyclyl, C4-12-heterocyclylalkoxy, C6-12-aryloxy, C5-12-heteroaryloxy, C7-12-arylalkyloxy, C6-12-heteroaralkyloxy, optionally substituted phenoxy, —(CH2)m—(Z)n—(CO)—Rf and —(CH2)m—(Z)n—SO2—(NRg)n′—Rf, where m, n and n′ are each independently 0 or 1;
- R5 is selected from hydrogen, C1-12-alkyl, C2-12-alkenyl, C2-12-alkynyl, amino, amido, C1-12-haloalkyl, C1-12-alkoxy, hydroxy, C1-12-haloalkoxy, nitro, C1-12-hydroxyalkyl, C2-12-alkoxyalkyl, C1-12-hydroxyalkoxy, C3-12-alkynylalkoxy, C1-12-alkylsulfonyl, C5-12-arylsulfonyl, cyano, C6-12-aryl, C5-12-heteroaryl, C3-12-heterocyclyl, C4-12-heterocyclylalkoxy, C6-12-aryloxy, C5-12-heteroaryloxy, C7-12-arylalkyloxy, C6-12-heteroaralkyloxy, optionally substituted phenoxy, —(CH2)m—(Z)n—(CO)—Rf and —(CH2)m—(Z)n—SO2—(NRg)n′—Rf, where m, n and n′ are each independently 0 or 1;
- Z is O or NRg;
- Rf is selected from hydrogen, C1-12-alkyl, hydroxy, C1-12-alkoxy, amino, C1-12-hydroxyalkyl and C2-12-alkoxyalkyl;
- each Rg is independently selected from hydrogen and C1-12-alkyl;
- R6 is hydrogen;
- and
- R7 is hydrogen.
15 more elements
Dependencies are inferred from the claim text.