# US 2014/0194517 A1 · Treatment of Graft-Versus-Host Disease Disorders using RAR Antagonists > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2014/0194517 A1 - Document ID: US20140194517A1 - Status: Published application - Kind: A1 - Application number: 14/150,574 - Filed: 2014-01-08 - Published: 2014-07-10 - Earliest claimed: 2013-01-08 - Assignees: Io Therapeutics, Inc.; Regents of the University of Minnesota - Applicants: Io Therapeutics, Inc.; The Regents of the University of Minnesota - Inventors: Bruce Blazer; Kazutoshi Aoyama; Roshantha Chandraratna - Web page: https://patentgrep.com/patent/US20140194517A1 ## CPC - A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil - A61K 31/195: having an amino group - A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] - 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 The present specification provides RAR antagonist compounds, compositions comprising such RAR antagonists, and methods using such compounds and compositions to treat an autoimmune disorder, inflammation associated with an autoimmune disorder and/or a transplant rejection as well as use of such RAR antagonists to manufacture a medicament and use of such compounds and compositions to treat an autoimmune disorder, inflammation associated with an autoimmune disorder and/or a transplant rejection. ## Claims ### Claim 1 A method of treating a transplant rejection, the method comprising administering to an individual in need thereof a therapeutically effective amount of a RAR antagonist, thereby treating the transplant rejection in the individual. ### Claim 2 (depends on 1) The method according to claim 1, wherein the RAR antagonist is a RARα antagonist and/or a RARγ antagonist. ### Claim 3 (depends on 2) The method according to claim 2, wherein the RARα antagonist is ### Claim 4 (depends on 2) The method or use according to claim 2, wherein the RARγ antagonist is ### Claim 5 (depends on 1) The method according to claim 1, wherein the transplant rejection is a graft-versus-host-disease (GVHD) disorder. ### Claim 6 (depends on 5) The method according to claim 5, wherein the GVHD disorder is an acute GVHD disorder or a chronic GVHD disorder. ### Claim 7 (depends on 1) The method according to claim 1, wherein the transplant rejection is a hyperacute rejection, an acute rejection, or a chronic rejection. ### Claim 8 (depends on 1) The method according to claim 1, wherein the therapeutically effective amount is about 0.01 mg/kg/day to about 100 mg/kg/day. ### Claim 9 (depends on 1) The method according to claim 1, wherein the therapeutically effective amount is about 0.1 mg/m2/day to about 100 mg/m2/day. ### Claim 10 (depends on 1) The method according to claim 1, wherein administration causes reduction of at least one symptom of transplant rejection selected from inflammation, fatigue, dizziness, malaise, elevated fever and high body temperature, extreme sensitivity to cold in the hands and feet, weakness and stiffness in muscles and joints, weight changes, digestive or gastrointestinal problems, low or high blood pressure, irritability, anxiety, or depression, infertility or reduced sex drive (low libido), blood sugar changes, and the destruction of an organ or tissue. ### Claim 11 (depends on 10) The method or use according to claim 10, wherein the administration causes a reduction in at least one symptom of inflammation selected from edema, hyperemia, erythema, bruising, tenderness, stiffness, swollenness, fever, a chill, congestion of the respiratory tract including nose and bronchi, congestion of a sinus, a breathing problem, fluid retention, a blood clot, a loss of appetite, an increased heart rate, a formation of granulomas, fibrinous, pus, or non-viscous serous fluid, a formation of an ulcer, or pain. ### Claim 12 A method of treating graft-versus-host disease, the method comprising administering to an individual in need thereof a therapeutically effective amount of a RAR antagonist, thereby treating the graft-versus-host disease in the individual. ### Claim 13 (depends on 12) The method according to claim 12, wherein the RAR antagonist is a RARα antagonist and/or a RARγ antagonist. ### Claim 14 (depends on 13) The method according to claim 13, wherein the RARα antagonist is ### Claim 15 (depends on 13) The method or use according to claim 13, wherein the RARγ antagonist is ### Claim 16 (depends on 12) The method according to claim 12, wherein the GVHD disorder is an acute GVHD disorder or a chronic GVHD disorder. ### Claim 17 (depends on 12) The method according to claim 12, wherein the therapeutically effective amount is about 0.01 mg/kg/day to about 100 mg/kg/day. ### Claim 18 (depends on 12) The method according to claim 12, wherein the therapeutically effective amount is about 0.1 mg/m2/day to about 100 mg/m2/day. ### Claim 19 (depends on 12) The method according to claim 12, wherein administration causes reduction of at least one symptom of transplant rejection selected from inflammation, fatigue, dizziness, malaise, elevated fever and high body temperature, extreme sensitivity to cold in the hands and feet, weakness and stiffness in muscles and joints, weight changes, digestive or gastrointestinal problems, low or high blood pressure, irritability, anxiety, or depression, infertility or reduced sex drive (low libido), blood sugar changes, and the destruction of an organ or tissue. ### Claim 20 (depends on 19) The method or use according to claim 19, wherein the administration causes a reduction in at least one symptom of inflammation selected from edema, hyperemia, erythema, bruising, tenderness, stiffness, swollenness, fever, a chill, congestion of the respiratory tract including nose and bronchi, congestion of a sinus, a breathing problem, fluid retention, a blood clot, a loss of appetite, an increased heart rate, a formation of granulomas, fibrinous, pus, or non-viscous serous fluid, a formation of an ulcer, or pain.