# US 10,946,022 B2 · Imipridones for gliomas > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 10,946,022 B2 - Document ID: US10946022B2 - Status: Granted - Kind: B2 - Application number: 16/526,444 - Filed: 2019-07-30 - Published: 2020-01-23 - Granted: 2021-03-16 - Earliest claimed: 2017-01-30 - Assignees: Oncoceutics, Inc. - Applicants: Oncoceutics, Inc. - Inventors: Joshua E. Allen; Martin Stogniew; Varun Vijay Prabhu - Web page: https://patentgrep.com/patent/US10946022B2 ## CPC - A61K 31/519: ortho- or peri-condensed with heterocyclic rings - A61P 35/00: Antineoplastic agents - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Imipridones selectively modulate Class A G protein-coupled receptors (GPCRs), such as the D2-like subfamily of dopamine receptors, and are useful for treating conditions and disorders in need of such modulation, such as cancers. Specifically, the cancer is a midline glioma, a cancer having a histone H3 mutation, or both. In addition, methods of identifying whether a subject having these conditions, is likely to be responsive to a treatment regimen, such as imipridone administration, are provided. Furthermore, methods of assessing the effectiveness of a treatment regimen, such as imipridone administration, monitoring, or providing a prognosis for a subject with these condition are also provided. ## Claims ### Claim 1 A method of treating cancer in a subject in need thereof, comprising: administering to the subject in need of such treatment a pharmaceutical composition comprising a therapeutically effective amount of a compound having the following structure: or a pharmaceutically acceptable salt thereof, wherein the cancer is a glioma having a histone H3 K27M mutation. ### Claim 2 (depends on 1) The method according to claim 1, wherein the glioma is selected from the group consisting of a diffuse intrinsic pontine glioma, a diffuse midline glioma, a spinal cord glioma, a thalamic glioma, a brainstem glioma, and a cerebellar glioma. ### Claim 3 (depends on 1) The method according to claim 1, wherein the glioma is not a spinal cord tumor. ### Claim 4 (depends on 1) The method according to claim 1, wherein the histone H3 K27M mutation in the glioma is H3.3 K27M or H3.1 K27M. ### Claim 5 (depends on 1) The method according to claim 1, wherein the histone H3 K27M mutation in the glioma is in one or more histone genes selected from H3F3A, H3F3B, HIST1H3A, HIST1H3B, HIST1H3C, HIST1H3D, HIST1H3E, HIST1H3F, HIST1H3G, HIST1H3H, HIST1H3I, or HIST1H3J. ### Claim 6 (depends on 1) The method according to claim 1, wherein in cancerous tissue DRD2 is overexpressed, DRD5 is underexpressed, or both. ### Claim 7 (depends on 1) The method according to claim 1, wherein the subject is a human. ### Claim 8 (depends on 1) The method according to claim 1, wherein the subject is a domesticated pet. ### Claim 9 (depends on 1) The method according to claim 1, wherein the subject is a pediatric subject. ### Claim 10 A method of treating cancer in a subject in need thereof, comprising: administering to the subject in need of such treatment a pharmaceutical composition comprising a therapeutically effective amount of a compound having the following structure: or a pharmaceutically acceptable salt thereof, wherein the cancer has a histone H3 mutation. ### Claim 11 (depends on 10) The method according to claim 10, wherein the cancer is selected from the group consisting of a central nervous system tumor, a brain tumor, a peripheral nervous system tumor, a pheochromocytoma, a paraganglioma, an adrenal cortical carcinoma, an adrenal tumor, and a neuroendocrine tumor. ### Claim 12 (depends on 10) The method according to claim 10, wherein the cancer is selected from the group consisting of meningioma, ependymoma, glioma, neuroblastoma, and diffuse intrinsic pontine glioma. ### Claim 13 (depends on 10) The method according to claim 10, wherein the cancer is selected from the group consisting of a diffuse midline glioma, a spinal cord glioma, a thalamic glioma, a brainstem glioma, and a cerebellar glioma. ### Claim 14 (depends on 10) The method according to claim 10, wherein the histone H3 mutation is H3.3 K27M or H3.1 K27M. ### Claim 15 (depends on 10) The method according to claim 10, wherein the cancer has a K27M mutation in one or more histone genes selected from H3F3A, H3F3B, HIST1H3A, HIST1H3B, HIST1H3C, HIST1H3D, HIST1H3E, HIST1H3F, HIST1H3G, HIST1H3H, HIST1H3I, or HIST1H3J. ### Claim 16 (depends on 10) The method according to claim 10, wherein DRD2 is overexpressed in cancerous tissue. ### Claim 17 (depends on 10) The method according to claim 10, wherein the subject is a human. ### Claim 18 (depends on 10) The method according to claim 10, wherein the subject is a domesticated pet. ### Claim 19 (depends on 10) The method according to claim 10, wherein the subject is a pediatric subject. ### Claim 20 A method of treating cancer in a subject in need thereof, comprising: administering to the subject in need of such treatment a pharmaceutical composition comprising a therapeutically effective amount of a compound having the following structure: or a pharmaceutically acceptable salt thereof, wherein the cancer is a midline glioma. ### Claim 21 (depends on 20) The method according to claim 20, wherein the cancer is selected from the group consisting of a diffuse intrinsic pontine glioma, a diffuse midline glioma, a spinal cord glioma, a thalamic glioma, a brainstem glioma, and a cerebellar glioma. ### Claim 22 (depends on 20) The method according to claim 20, wherein the cancer is not a spinal cord tumor. ### Claim 23 (depends on 20) The method according to claim 20, wherein the cancer has a histone H3 mutation, wherein the histone H3 mutation is H3.3 K27M or H3.1 K27M. ### Claim 24 (depends on 20) The method according to claim 20, wherein the cancer has a histone H3 K27M mutation in one or more histone genes selected from H3F3A, H3F3B, HIST1H3A, HIST1H3B, HIST1H3C, HIST1H3D, HIST1H3E, HIST1H3F, HIST1H3G, HIST1H3H, HIST1H3I, or HIST1H3J. ### Claim 25 (depends on 20) The method according to claim 20, wherein DRD2 is overexpressed in cancerous tissue. ### Claim 26 (depends on 20) The method according to claim 20, wherein the subject is a human. ### Claim 27 (depends on 20) The method according to claim 20, wherein the subject is a domesticated pet. ### Claim 28 (depends on 20) The method according to claim 20, wherein the subject is a pediatric subject.