Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof
Inventors
Copp, James Densmore • Newman, Ann W. • Luong, Anne
Assignees
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Publication Number
US-11690836-B2
Publication Date
2023-07-04
Expiration Date
Abstract
Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
Core Innovation
The invention relates to solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid (Compound (I)), including crystalline and amorphous materials identified as Forms A, B, and C, and multiple-component forms such as salts, solvates, and hydrates. The crystalline forms are characterized by X-ray powder diffraction (XRPD) peak sets and differential scanning calorimetry (DSC) melting peak information.
The disclosure defines crystalline Compound (I) by specified XRPD peak patterns and describes the solid as substantially free of other crystalline forms and substantially free of amorphous Compound (I). It also characterizes the solids by very low levels of a related impurity or compound of Formula (II), determined by GC/MS, including embodiments of less than 100 ppm and undetectable amount.
The solid forms are linked to pharmaceutical compositions and therapeutic use for treating or preventing anemia. The therapeutic activity is described in terms of modulation, inhibition, or stabilization of HIF pathways, including PHD/HIFα, HIF prolyl hydroxylase, HIF-1α, HIF-2α, and HIF-3α, and includes the effect of endogenous erythropoietin (EPO).
Claims Coverage
The document includes two independent claims directed to crystalline Compound (I) defined by distinct XRPD peak patterns. The claims further address containment of other crystalline and amorphous material, quantitative Formula (II) impurity limits by GC/MS, and therapeutic use in a pharmaceutical composition for treating anemia.
Crystalline Compound (I) defined by an XRPD peak set
A crystalline Compound (I) having an X-ray powder diffraction pattern comprising peaks at 8.6, 15.3, 22.7, and 28.1 ± 0.2° 2θ.
Crystalline Compound (I) defined by an XRPD peak set
A crystalline Compound (I) having an X-ray powder diffraction pattern comprising peaks at 7.2, 17.4, 22.3, 22.4, 22.4, 28.9, 33.7, and 33.8 ± 0.2° 2θ.
Anemia treatment by administering a pharmaceutical composition
A method of treating anemia by administering a pharmaceutical composition comprising an effective amount of crystalline Compound (I).
Overall, the claim coverage focuses on crystalline Compound (I) defined by specified XRPD peak patterns, with additional limitations on other crystalline and amorphous content and Formula (II) impurity levels measured by GC/MS. The material is also claimed for therapeutic use in treating anemia through administration of a pharmaceutical composition containing an effective amount of the crystalline Compound (I).
Stated Advantages
Crystalline Compound (I) is characterized as being substantially free of other crystalline forms.
Crystalline Compound (I) is characterized as being substantially free of amorphous Compound (I).
Crystalline Compound (I) contains very low levels of a compound of Formula (II), including embodiments of less than 100 ppm and undetectable amount as determined by GC/MS.
Treatment or prevention of anemia via modulation, inhibition, or stabilization of HIF pathways, including PHD/HIFα and the effect of endogenous erythropoietin (EPO).
Documented Applications
Pharmaceutical compositions comprising an effective amount of the crystalline Compound (I) for use in treating anemia.
Methods of treating anemia by administering a pharmaceutical composition comprising an effective amount of crystalline Compound (I).
Treating diseases related to HIF prolyl hydroxylase modulation, including anemia.
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