Crystalline forms of N[4[4-(4-Morpholinyl)-7H-Pyrrolo[2-3-D]Pyrimidin-6-yl]Phenyl]-4-[[3(R)-[(1-Oxo-2-Protein-1-yl)Amino]-1-Piperidinyl]Methyl]2-Pyridinecarboxamide]
Inventors
Puppali, Satish Goud • Palmer, James T. • Kirschberg, Thorsten A. • WONG, Angelina Sau Man • TAN, Heow Meng • Li, Jay • Lin, Jing • Gao, Ming • Ding, Junlu • Li, Shuang • GU, Yuyao • He, Hongyan • Zheng, Bo • Zhou, Yanjing • You, Mei
Assignees
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Publication Number
US-12215113-B2
Publication Date
2025-02-04
Expiration Date
Abstract
Described herein is N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(R)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide (Compound A) (Formula I),including crystalline forms, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions or pharmaceutical formulations that include the compound, as well as methods of using the compound, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, diabetes, and inflammatory diseases or conditions.
Core Innovation
The document relates to crystalline Form K of N-[4-[4-(4-morpholinyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]phenyl]-4-[[3(R)-[(1-oxo-2-propen-1-yl)amino]-1-piperidinyl]methyl]-2-pyridinecarboxamide (Compound A). Crystalline Form K is characterized by an X-ray powder diffraction pattern comprising at least two characteristic peaks at angles (° 2θ) selected from 10.483°±0.2° 2θ, 12.756°±0.2° 2θ, and 19.071°±0.2° 2θ.
The document further characterizes crystalline Form K using infrared spectrum characteristic peaks and thermal properties including melting temperature, differential scanning calorimetry, and thermogravimetric analysis thermograms. Additional characterization includes thermal behavior, hygroscopicity, and aqueous solubility at a specified pH.
The disclosure also links crystalline Form K to pharmaceutical compositions and dosage forms. Pharmaceutical formulations comprise one or more diluents together with crystalline Form K, with excipient categories such as disintegrating agents, glidants, and lubricants.
Claims Coverage
The independent claims include four main inventive features. The coverage is anchored on crystalline Form K of Compound A defined by XRPD characteristic peaks, together with a pharmaceutical formulation containing crystalline Form K and methods for treating diabetes and cancer in a mammal.
Xrpd-defined crystalline form k of compound a
Crystalline Form K of Compound A is characterized by an X-ray powder diffraction pattern comprising at least two characteristic peaks at angles (° 2θ) selected from 10.483°±0.2° 2θ, 12.756°±0.2° 2θ, and 19.071°±0.2° 2θ.
Pharmaceutical formulation comprising diluents and crystalline form k
A pharmaceutical formulation comprising one or more diluents and crystalline Form K of Compound A, wherein the crystalline Form K is characterized by an X-ray powder diffraction pattern comprising at least two characteristic peaks at angles (° 2θ) selected from 10.483°±0.2° 2θ, 12.756°±0.2° 2θ, and 19.071°±0.2° 2θ.
Treating diabetes with crystalline form k
A method for treating diabetes in a mammal comprising administering to the mammal in need thereof a therapeutically effective amount of crystalline Form K of Compound A, wherein the crystalline Form K is characterized by an X-ray powder diffraction pattern comprising at least two characteristic peaks at angles (° 2θ) selected from 10.483°±0.2° 2θ, 12.756°±0.2° 2θ, and 19.071°±0.2° 2θ.
Treating cancer with crystalline form k
A method for treating cancer in a mammal comprising administering to the mammal in need thereof a therapeutically effective amount of crystalline Form K of Compound A, wherein the crystalline Form K is characterized by an X-ray powder diffraction pattern comprising at least two characteristic peaks at angles (° 2θ) selected from 10.483°±0.2° 2θ, 12.756°±0.2° 2θ, and 19.071°±0.2° 2θ.
The claims are centered on crystalline Form K of Compound A defined by XRPD characterization with at least two specified peak angles. This crystalline solid is claimed in pharmaceutical formulations with diluents and in methods for treating diabetes and cancer by administering therapeutically effective amounts.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treating diabetes in a mammal by administering crystalline Form K of Compound A, including via a pharmaceutical formulation containing one or more diluents.
Treating cancer in a mammal by administering crystalline Form K of Compound A, including via a pharmaceutical formulation containing one or more diluents.
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