# US 12,213,961 B2 · Treatment of idiopathic pulmonary fibrosis > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,213,961 B2 - Document ID: US12213961B2 - Status: Granted - Kind: B2 - Application number: 18/513,181 - Filed: 2023-11-17 - Published: 2024-04-04 - Granted: 2025-02-04 - Earliest claimed: 2022-02-10 - Assignees: Vicore Pharma AB - Applicants: Vicore Pharma AB - Inventors: Carl-Johan Dalsgaard; Rohit Batta - Web page: https://patentgrep.com/patent/US12213961B2 ## CPC - A61K 31/4178: not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin - A61K 9/485: {Inorganic compounds} - A61K 9/4858: {Organic compounds} - A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system - A61P 11/00: Drugs for disorders of the respiratory system - 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 According to the invention there is provided a method of improving (e.g. restoring) function in a patient having idiopathic pulmonary fibrosis, which method comprises perorally administering a therapeutically-effective amount of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide (C21), or a pharmaceutically acceptable salt thereof, to said patient. Said treatment is capable of treating said IPF in a therapeutic, including a curative, fashion. ## Claims ### Claim 1 A method of treating idiopathic pulmonary fibrosis in a patient having probable usual interstitial pneumonitis as determined by a pattern on an image of the patient's lungs, wherein said method comprises perorally administering to said patient a therapeutically-effective amount of a sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butyl-thiophene-2-sulfonamide, wherein said perorally administering is carried out after a minimum of two hours of fasting and fasting is continued for at least one hour after said perorally administering. ### Claim 2 (depends on 1) The method as claimed in claim 1, wherein the image is a high-resolution computed tomography image. ### Claim 3 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is as a stand-alone treatment of said patient's idiopathic pulmonary fibrosis. ### Claim 4 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is carried out as a first line treatment of said patient's idiopathic pulmonary fibrosis. ### Claim 5 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is carried out in the absence of co-therapy with antifibrotic drugs. ### Claim 6 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is carried out prior to and/or following receiving a prescribed dose of an antifibrotic drug. ### Claim 7 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment. ### Claim 8 (depends on 7) The method as claimed in claim 7, wherein said stabilizing results in one or more of the group: improved breathing, improved lung ventilation, improved ventilatory lung function, increased vital capacity as measured in a standard lung function test, and reduction in acute exacerbations of idiopathic pulmonary fibrosis, in the patient. ### Claim 9 (depends on 1) The method as claimed in claim 1, wherein said treatment occurs in the absence of serious adverse events related to the sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide. ### Claim 10 (depends on 1) The method as claimed in claim 1, wherein the sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide is provided in a dosage form comprising a tablet or a capsule, wherein: said sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide is provided in the form of a powder mixture in which said salt is homogenously distributed throughout a carrier material; or said dosage form comprises an enteric coating. ### Claim 11 (depends on 10) The method as claimed in claim 10, wherein said dosage form comprises the enteric coating and the enteric coating comprises polyvinyl acetate phthalate or a methacrylic acid copolymer. ### Claim 12 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, and wherein the image is a high-resolution computed tomography image. ### Claim 13 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, and is a stand-alone treatment of said patient's idiopathic pulmonary fibrosis. ### Claim 14 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, and carried out as a first line treatment of said patient's idiopathic pulmonary fibrosis. ### Claim 15 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, and carried out in the absence of co-therapy with antifibrotic drugs. ### Claim 16 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, and carried out prior to and/or following receiving a prescribed dose of an antifibrotic drug. ### Claim 17 (depends on 13) The method as claimed in claim 13, wherein said treatment occurs in the absence of serious adverse events related to the sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide. ### Claim 18 (depends on 13) The method as claimed in claim 13, wherein the sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide is provided in a dosage form comprising a tablet or a capsule, wherein: said sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide is provided in the form of a powder mixture in which said salt is homogenously distributed throughout a carrier material; or said dosage form comprises an enteric coating. ### Claim 19 (depends on 18) The method as claimed in claim 18, wherein said dosage form comprises the enteric coating and the enteric coating comprises polyvinyl acetate phthalate or a methacrylic acid copolymer. ### Claim 20 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, said stabilizing results in one or more of the group: improved breathing, improved lung ventilation, improved ventilatory lung function, increased vital capacity as measured in a standard lung function test, and reduction in acute exacerbations of idiopathic pulmonary fibrosis, in the patient, and wherein the image is a high-resolution computed tomography image. ### Claim 21 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, said stabilizing results in one or more of the group: improved breathing, improved lung ventilation, improved ventilatory lung function, increased vital capacity as measured in a standard lung function test, and reduction in acute exacerbations of idiopathic pulmonary fibrosis, in the patient, and is as a stand-alone treatment of said patient's idiopathic pulmonary fibrosis. ### Claim 22 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, said stabilizing results in one or more of the group: improved breathing, improved lung ventilation, improved ventilatory lung function, increased vital capacity as measured in a standard lung function test, and reduction in acute exacerbations of idiopathic pulmonary fibrosis, in the patient, and wherein said perorally administering is carried out as a first line treatment of said patient's idiopathic pulmonary fibrosis. ### Claim 23 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, said stabilizing results in one or more of the group: improved breathing, improved lung ventilation, improved ventilatory lung function, increased vital capacity as measured in a standard lung function test, and reduction in acute exacerbations of idiopathic pulmonary fibrosis, in the patient, and wherein said perorally administering is carried out in the absence of co-therapy with antifibrotic drugs. ### Claim 24 (depends on 1) The method as claimed in claim 1, wherein said perorally administering is effective to stabilize lung function in the patient compared to baseline lung function levels measured before the start of treatment, said stabilizing results in one or more of the group: improved breathing, improved lung ventilation, improved ventilatory lung function, increased vital capacity as measured in a standard lung function test, and reduction in acute exacerbations of idiopathic pulmonary fibrosis, in the patient, and wherein said perorally administering is carried out prior to and/or following receiving a prescribed dose of an antifibrotic drug. ### Claim 25 (depends on 21) The method as claimed in claim 21, wherein said treatment occurs in the absence of serious adverse events related to the sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide. ### Claim 26 (depends on 21) The method as claimed in claim 21, wherein the sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide is provided in a dosage form comprising a tablet or a capsule, wherein: said sodium salt of N-butyloxycarbonyl-3-(4-imidazol-1-ylmethylphenyl)-5-iso-butylthiophene-2-sulfonamide is provided in the form of a powder mixture in which said salt is homogenously distributed throughout a carrier material; or said dosage form comprises an enteric coating. ### Claim 27 (depends on 26) The method as claimed in claim 26, said dosage form comprises the enteric coating and the enteric coating comprises polyvinyl acetate phthalate or a methacrylic acid copolymer.