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Publication Number
US-11939306-B2
Publication Date
2024-03-26
Expiration Date
Abstract
The invention relates to crystalline forms of a 3-substituted 1,2,4-oxadiazole compound, including an anhydrous crystalline form, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for pharmaceutical, veterinary, and agriculturally-relevant uses.
Core Innovation
The invention is directed to crystalline anhydrous forms of a 3-substituted 1,2,4-oxadiazole immunomodulator (compound of formula (I)). The crystalline material is defined as anhydrous and non-solvated, and is described as a polymorphable solid characterized by powder X-ray diffraction (XRPD). The disclosure includes crystalline forms identified by XRPD and associated 2θ peak values, including a Form A.
The anhydrous crystalline compound is characterized by XRPD, including specified 2θ peak values, with reference to Table 1 and examples confirming XRPD. Thermal properties are described using DSC/TGA, including onset characteristics, and the solid is further described in relation to humidity stability. The document also describes additional characterization such as dynamic vapor sorption (DVS) and solubility.
The anhydrous crystalline compound of formula (I) is linked to pharmaceutical use in medicament manufacture and treatment of immune-modulated conditions. The therapeutic use is described for treatment and/or prevention of cancer and immune disorders, including immune/inflammatory and infectious diseases, and for transplant rejection. The document provides example support including XRPD confirmation and analytical measurements such as HPLC-based purity/impurities and degradation-related profiling.
Claims Coverage
The document provides one independent claim directed to a therapeutic method, with dependent claims refining the scope either by narrowing the selected cancer types and/or by characterizing the anhydrous crystalline compound using specified XRPD 2θ peak constraints. The independent claim centers on administering an anhydrous crystalline compound of formula (I) to treat cancer in a subject in need thereof, for a broad enumerated list of cancer types.
Administering an anhydrous crystalline compound of formula (I) to treat cancer
A method of therapeutically treating cancer in a subject in need thereof comprising administering to the subject an anhydrous crystalline compound having the structure of formula (I).
Cancer type selection from an extensive enumerated list
The method wherein the cancer is selected from the enumerated list including breast cancer, triple-negative breast cancer, glioblastoma, prostate cancer, colon cancer, melanoma, epithelial cancer, skin cancer, renal cancer, cancer of the head or neck, uterine cancer, ovarian cancer, colorectal cancer, gastric carcinoma, leukemia, lymphomas, myeloma, and other listed cancers.
Characterizing the anhydrous crystalline compound by specified XRPD 2θ peak values
The method wherein the anhydrous crystalline compound has specified X-ray diffraction 2θ peak values, including the enumerated peak set with ±0.2 tolerance.
Further constraining the anhydrous crystalline compound using additional XRPD 2θ peak values
The method wherein the anhydrous crystalline compound is defined by specified 2θ X-ray diffraction values, each with a ±0.2 tolerance.
Restricting the method to a subset of solid tumor cancers
The method applicable to cancer types selected from prostate adenocarcinoma, lung adenocarcinoma, lung squamous cell carcinoma, pancreatic adenocarcinoma, breast cancer, and colorectal adenocarcinoma.
Restricting the method to a detailed set of hematologic cancers and lymphomas
The method applied to a cancer selected from the listed hematologic cancers and lymphomas including leukemia subtypes and lymphoma subtypes.
Restricting the method using an additional enumerated cancer list
The method performed for cancer selected from the listed cancer types including small cell lung cancer, multiple myeloma, bladder carcinoma, primary ductal carcinoma, ovarian carcinoma, Hodgkin's lymphoma, gastric carcinoma, acute myeloid leukemia, and pancreatic cancer.
Overall claim coverage is centered on therapeutic treatment of an enumerated set of cancer types by administering an anhydrous crystalline compound of formula (I). Dependent claims narrow the eligible cancer categories and/or specify the identity of the administered anhydrous crystalline compound using defined XRPD 2θ peak constraints with ±0.2 tolerances.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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