Interested in licensing this patent?
MTEC can help explore whether this patent might be available for licensing for your application.
Publication Number
US-12252475-B2
Publication Date
2025-03-18
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 describes crystalline anhydrous 3-substituted 1,2,4-oxadiazole compounds of formula (I) as immunomodulators. A specific polymorph is defined as anhydrous Form A, and the crystalline state is characterized using X-ray powder diffraction (XRPD) with specified 2θ diffraction peak values, together with single crystal X-ray diffraction and hydrogen bonding.
The anhydrous Form A is further characterized by thermal behavior including DSC and TGA, and by humidity/solution/solubility stability and dynamic vapor sorption (DVS) characterization. Dynamic vapor sorption isotherms are described in relation to humidity and solution behavior, together with solubility in different conditions.
Therapeutic use is described for immunomodulation, including treating or preventing cancer, immune disorders, immunodeficiency, inflammatory disorders, infectious diseases, and transplant rejection. Pharmaceutical composition options are broadly outlined, including pharmaceutically acceptable excipients and routes of administration, in connection with the anhydrous crystalline compound of formula (I) having the polymorph identification.
Claims Coverage
Only one independent claim is provided. It comprises administering an anhydrous crystalline compound of formula (I) defined by specific XRPD 2θ values for therapeutically treating cancer, with cancer selection narrowed to a list of specified cancer types.
Anhydrous crystalline formula (I) with specified XRPD 2θ values for cancer therapy
A method of therapeutically treating cancer in a subject in need thereof comprising administering an anhydrous crystalline compound having the structure of formula (I), wherein the crystalline compound has 2θ values of 10.2±0.2, 15.2±0.2, 15.8±0.2, 16.5±0.2, 17.6±0.2, 18.1±0.2, 18.8±0.2, 20.5±0.2, 21.8±0.2, 22.3±0.2, 22.9±0.2, 24.2±0.2, 25.4±0.2, 26.1±0.2, 26.4±0.2, 27.5±0.2, 28.1±0.2, 28.8±0.2, 29.3±0.2, 30.4±0.2, 30.6±0.2, 32.0±0.2, 33.4±0.2, 33.6±0.2, 34.6±0.2, 35.8±0.2, 36.7±0.2, 37.3±0.2, 38.2±0.2, 38.6±0.2, and 39.2±0.2.
Cancer selection limited to specified cancer types
The method of therapeutically treating cancer wherein the cancer is selected from mesothelioma, non-small cell lung cancer (NSCLC), small-cell lung cancer, lung adenocarcinoma, lung squamous cell carcinoma, lung cancer, head and neck squamous cell carcinoma (HNSCC), cancer of the head or neck, Hodgkin's lymphoma, breast cancer, colon cancer, colorectal cancer, ovarian cancer, ovarian carcinoma, triple-negative breast cancer, primary ductal carcinoma, gastric cancer, glioblastoma, renal cancer, kidney cancer, multiple myeloma, leukemia, and lymphoma.
The provided independent claim covers therapeutic cancer treatment by administering an anhydrous crystalline compound of formula (I) identified by a specified set of XRPD 2θ values, with cancer limited to a list of named cancer types. The dependent claims further narrow the cancer types into specific lung/mesothelioma categories, head-and-neck categories, additional listed cancers, and specific leukemia and lymphoma subtypes as provided.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Immunomodulation, including treating or preventing cancer in a subject.
Treating or preventing immune disorders, immunodeficiency, inflammatory disorders, and infectious diseases.
Treating transplant rejection.
Interested in licensing this patent?