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Publication Number
US-10822346-B2
Publication Date
2020-11-03
Expiration Date
Abstract
Disclosed herein are thienopyrimidine meglumine salts according to Formula (I) used for treating or preventing heart failure:
Core Innovation
The disclosed invention concerns thienopyrimidine carboxylate salts according to Formula (I), including stereoisomers, tautomers or hydrates of the salt. The salts are defined by substituent options for R1, R2 and R3, and by linkage and substituent definitions for X and Y, together with Z being S or O and n taking values of 0, 1, 2, 3 or 4. An M+ counterion is included to form the salt.
A central aspect of the invention is the selection of crystalline solid forms of the Formula (I) salts. The document describes crystalline solids having an X-ray powder diffraction pattern with characteristic 2θ peak positions within about ±0.2°, and also references an X-ray powder diffraction pattern shown in FIG. 1. Specific salt forms are described as crystalline, including anhydrous and monohydrate form.
The invention also addresses the therapeutic use of these Formula (I) salts in mammals for treating cardiovascular disease or condition, including heart failure and related disorders. The method comprises administering a therapeutically effective amount of a salt of a compound according to Formula (I), including stereoisomers, tautomers or hydrates. The document describes use cases including cardiac hypertrophy, heart failure with preserved ejection fraction, heart failure with reduced ejection fraction, hypertensive heart disease, and aortic stenosis.
Claims Coverage
The partial content includes three independent claims: a salt according to Formula (I), a crystalline solid characterized by X-ray powder diffraction, and a method of treating a cardiovascular disease or condition by administering the salt. The inventive features across these independent claims focus on the defined Formula (I) salt structures, specific crystalline solid characterization by X-ray powder diffraction, and cardiovascular treatment by administering a therapeutically effective amount of the Formula (I) salt.
Defined thienopyrimidine salt according to Formula (I)
A salt according to Formula (I) having the structure including stereoisomers, tautomers or hydrates, wherein the substituents R1, R2 and R3 are defined by the stated ranges and linkages, X and Y are defined by the stated chemical bond options, Z is S or O, n is 0, 1, 2, 3 or 4, and M+ is defined as the counterion, with optional substitution rules on alkyl, alkylene, cycloalkyl, heterocyclyl, heteroaryl or aryl.
Crystalline solid characterized by an X-ray powder diffraction peak set
A crystalline solid of a salt according to Formula (I) (or stereoisomers, tautomers or hydrates thereof) having the stated structure and characterized by an X-ray powder diffraction pattern with characteristic 2θ peak positions as defined in the dependent refinements, including characterization by peak positions within about ±0.2° and by an X-ray powder diffraction pattern shown in FIG. 1.
Cardiovascular treatment by administering a therapeutically effective amount of a Formula (I) salt
A method of treating a cardiovascular disease or condition in a mammal in need thereof comprising administering a therapeutically effective amount of a salt of a compound according to Formula (I) (including stereoisomers, tautomers or hydrates thereof), wherein the compound is defined by the stated substituent options for R1, R2 and R3, together with the definitions for X, Y, Z, n, M+, and optional substitution on selected groups.
Claim coverage centers on salts of thienopyrimidine carboxylates defined by Formula (I) substituent and counterion constraints, crystalline solid salt forms characterized by X-ray powder diffraction peak sets and FIG. 1, and therapeutic methods for cardiovascular disease or conditions in mammals using therapeutically effective administration of the Formula (I) salts.
Stated Advantages
Documented Applications
Treating cardiovascular diseases or conditions in a mammal using a therapeutically effective amount of a salt of a compound according to Formula (I), including stereoisomers, tautomers or hydrates thereof.
Application to heart failure, including heart failure with preserved ejection fraction and heart failure with reduced ejection fraction.
Application to related cardiac disorders including cardiac hypertrophy, hypertensive heart disease, and aortic stenosis.
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