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US 2019/0315765 A1Published application
Meglumine salts of thienopyrimidines
AssigneeCardurion Pharmaceuticals, LLC
InventorsAnuj K. Kumar, Raymond E. Forslund
Life of this patent
Estimating the term…
Abstract
Disclosed herein are thienopyrimidine meglumine salts according to Formula (I) used for treating or preventing heart failure:
Claims20
A salt according to Formula (I) having the structure:
- or stereoisomers, tautomers or hydrates thereof,
- wherein:
- R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)haloalkyl containing 1-6 halogen atoms;
- R2 is hydrogen, (C1-C6)alkyl, [(C1-C6)alkylene]aryl or amino;
- R3 is hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, [(C1-C6)alkylene]N(R4)(R5), [(C1-C6)alkylene]S(R4) or —X—Y, or R2 and R3 together with the atoms to which they are attached form a heterocyclyl;
- R4 and R5 are independently H or (C1-C6)alkyl;
- X is a chemical bond, —CH2—, —CH(OH)—, —CH(C6H5)—, —CO—, —CH2CH2—, CH2CO—, —COCH2—, S, O or NH;
- Y is cycloalkyl, heterocyclyl, aryl or heteroaryl;
- Z is S or O;
- n is 0, 1, 2, 3 or 4;
- M+ is
- and
- wherein any alkyl, alkylene, cycloalkyl, heterocyclyl, heteroaryl or aryl is optionally substituted with 1, 2 or 3 groups selected from OH, CN, halogen, (C1-C6)alkyl, O(C1-C6)alkyl, (C2-C6)alkenyl, haloalkyl, amino, oxo and nitro.
10 more elements
A method of treating or preventing a cardiovascular disease or condition in a mammal in need thereof comprising administering to the mammal a therapeutically effective amount of a salt of a compound according to Formula (I):
- or stereoisomers, tautomers or hydrates thereof,
- wherein:
- R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy or (C1-C6)haloalkyl containing 1-6 halogen atoms;
- R2 is hydrogen, (C1-C6)alkyl, [(C1-C6)alkylene]aryl or amino;
- R3 is hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, [(C1-C6)alkylene]N(R4)(R5), [(C1-C6)alkylene]S(R4) or —X—Y, or R2 and R3 together with the atoms to which they are attached form a heterocyclyl;
- R4 and R5 are independently H or (C1-C6)alkyl;
- X is a chemical bond, —CH2—, —CH(OH)—, —CH(C6H5)—, —CO—, —CH2CH2—, CH2CO—, —COCH2—, S, O or NH;
- Y is cycloalkyl, heterocyclyl, aryl or heteroaryl;
- Z is S or O;
- n is 0, 1, 2, 3 or 4;
- M+ is
- and
- wherein any alkyl, alkylene, cycloalkyl, heterocyclyl, heteroaryl or aryl is optionally substituted with 1, 2 or 3 groups selected from OH, CN, halogen, (C1-C6)alkyl, O(C1-C6)alkyl, (C2-C6)alkenyl, haloalkyl, amino, oxo and nitro.
10 more elements
Dependencies are inferred from the claim text.