IP Library › Granted Patent US 12,678,436
Granted Patent B2
US 12,678,436 · App. 18/288,296 · Granted Jul 14, 2026

Pharmaceutical composition for preventing or treating fibrosis

Inventors: Caroline Hee Lee (Seoul, KR); Min Jae Cho (Seoul, KR); Min Young Park (Seoul, KR); Ju Mi Han (Seoul, KR); Joon Seok Park (Seoul, KR)
Assignee: Daewoong Pharmaceutical Co., Ltd.
A61K31/496A61K31/4418A61K31/454A61P11/00
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 12,678,436
App. No.
18/288,296
Filed
Oct 25, 2023
Granted
Jul 14, 2026
Kind
B2
Examiner
OH, TAYLOR V
Art Unit
1625
USPC
514/254.01
Abstract

The pharmaceutical composition according to the present invention is used at specific therapeutic regimen and dosage, and can be usefully used for the prevention or treatment of fibrosis.

Claims (6)

1 . A method for treating fibrosis in a subject in need thereof, comprising administering to the subject 100 mg to 150 mg of a compound represented by the following Chemical Formula 1 or a pharmaceutically acceptable salt thereof twice a day (BID):

2 . The method according to claim 1 , wherein the fibrosis is Interstitial lung disease (ILD), Scleroderma, Keloid, Hypertrophic scar, Non-alcoholic Fatty Liver Disease, Primary sclerosing cholangitis (PSC), primary biliary cholangitis (PBC), diabetic retinopathy, Age-related Macular Degeneration (AMD), hypertrophic cardiomyopathy, myocardial infarction, Muscular Dystrophy, Diabetic kidney disease, focal segmental glomerulosclerosis (FSGS), or Inflammatory bowel disease (IBD).

3 . The method according to claim 2 , wherein the Interstitial lung disease (ILD) is idiopathic pulmonary fibrosis (IPF), systemic sclerosis associated interstitial lung disease (SSc-ILD), or chronic fibrosing interstitial lung diseases with a progressive phenotype (PF-ILD).

4 . The method according to claim 1 , wherein the pharmaceutically acceptable salt is hydrochloride.

5 . The method according to claim 1 , wherein the pharmaceutical composition further comprises other active component used for the prevention or treatment of fibrosis.

6 . The method according to claim 5 , wherein the other active component used for the prevention or treatment of fibrosis is Pirfenidone or Nintedanib.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 13, 2024
From: LEE, CAROLINE HEE; CHO, MIN JAE; PARK, MIN YOUNG; HAN, JU MI; PARK, JOON SEOK
To: DAEWOONG PHARMACEUTICAL CO., LTD.
Reel/Frame 066453/0681 →
Priority Claims (2)
KR 10-2021-0062252 · May 13, 2021 · national
KR 10-2021-0110520 · Aug 20, 2021 · national
Continuity (1)
Related Publication 20240216363A1 · Jul 4, 2024
References Cited (58)
US 10981917B2 · Lee et al. · 2021 [cited by applicant]
US 20190282565A1 · Liang · 2019 [cited by applicant]
US 20190359617A1 · Lee et al. · 2019 [cited by applicant]
US 20210205253A1 · Song et al. · 2021 [cited by applicant]
US 20240216363A1 · Lee et al. · 2024 [cited by applicant]
US 20240307365A1 · Lee et al. · 2024 [cited by applicant]
CL 2019002019A1 · 2019 [cited by applicant]
CN 112469406A · 2021 [cited by applicant]
JP 2020506197A · 2020 [cited by applicant]
KR 102084772B1 · 2020 [cited by applicant]
RU 2733384C1 · 2020 [cited by applicant]
WO WO2010018134A1 · 2010 [cited by applicant]
WO WO2018147626A1 · 2018 [cited by applicant]
WO WO2019183006A1 · 2019 [cited by applicant]
WO WO2019231281A1 · 2019 [cited by applicant]
Flaherty et al., “Safety of Nintedanib Added to Pirfenidone Treatment for Idiopathic Pulmonary Fibrosis”, Eur Respir J, 2018, V. 52(2):1800230, [online], [found May 27, 2024]. Found in PubMed, PMID: 29946005, doi: 10.11… [cited by applicant]
Lee et al., “Synergistic Anti-Fibrotic Effect of a First-in-Class PRS Inhibitor, DWN12088, and Standard-of-Care Therapeutic Agents for IPF”, Am J Respir Crit Care Med, 2021, V. 203, Online Abstracts Issue, A4645, publ. … [cited by applicant]
Dhooria et al., A Real-world Study of the Dosing and Tolerability of Pirfenidone and its Effect on Survival in Idiopathic Pulmonary Fibrosis. Sarcoidosis Vasc Diffuse Lung Dis, 2020, V. 37(2), pp. 148-157, [online], [fo… [cited by applicant]
Flaherty et al., “Nintedanib in Progressive Fibrosing Interstitial Lung Diseases”, The New England Journal of Medicine, 2019, V. 381, N. 18, pp. 1718-1727, [online], [found May 27, 2024]. Found in PubMed, PMID: 31566307… [cited by applicant]
Office Action in RU Application No. 2023123353/04(051422) dated May 29, 2024, 18 pages. [cited by applicant]
Office Action in RU Application No. 2023122618/04(049669) dated May 13, 2024, 18 pages. [cited by applicant]
Kim et al., “Recent Development of Aminoacyl-tRNA Synthetase Inhibitors for Human Diseases: A Future Perspective”, Biomolecules, vol. 10, 1625, 2020, 24 pages. [cited by applicant]
Lee et al., “A First-in-Class PRS Inhibitor, DWN12088, as a Novel Therapeutic Agent for Idiopathic Pulmonary Fibrosis”, B20 Therapeutics “2020” in Lung Disease, Mini Symposium, Am J Respir Crit Care Med, 2020, 3 pages. [cited by applicant]
Henderson et al., “Fibrosis: From Mechanisms to Medicines”, Nature, vol. 587 (7835), Nov. 25, 2020, pp. 555-566. [cited by applicant]
Lee et al., “Inhibition of Prolyl-tRNA Synthetase as a Novel Therapeutic Target for Systemic Sclerosis”, Meeting: 2018 ACR/ARHP Annual Meeting, Oct. 21, 2018, Abstract No. 128, 3 pages. [cited by applicant]
Park et al., “Inhibition of Prolyl-tRNA Synthetase as a Novel Mediator of Cardiac Fibrosis”, 2017 Late-Breaking Basic Science Oral Abstracts I, Circulation, 2017, vol. 136, 10 pages. [cited by applicant]
Office Action in Saudi Arabian Application No. 523450897 dated Nov. 21, 2024, 8 pages. [cited by applicant]
Office Action in JP Application No. 2023-567149 dated Dec. 24, 2024, 13 pages. [cited by applicant]
Lee et al., “A First-in-Class PRS Inhibitor, DWN12088, as a Novel Therapeutic Agent for Idiopathic Pulmonary Fibrosis”, In: Therapeutics “2020” in Lung Disease, Mini Symposium, American Journal of Respiratory and Critic… [cited by applicant]
Song et al., “Glutamyl-Prolyl-tRNA Synthetase Regulates Epithelial Expression of Mesenchymal Markers and Extracellular Matrix Proteins: Implications for Idiopathic Pulmonary Fibrosis”, Frontiers in Pharmacology, vol. 9,… [cited by applicant]
Zhou et al., “ATP-Directed Capture of Bioactive Herbal-Based Medicine on Human tRNA Synthetase”, Nature, vol. 494, 2013, pp. 121-125. [cited by applicant]
Kim et al., “Aminoacyl-tRNA Synthetases and Tumorigenesis: More Than Housekeeping”, Nat. Rev. Cancer, vol. 11, Oct. 2011, pp. 708-718. [cited by applicant]
Hübner et al., “Standardized Quantification of Pulmonary Fibrosis in Histological Samples”, BioTechniques, vol. 44, No. 4, 2008, 9 pages. [cited by applicant]
Search Report in International Application No. PCT/KR2022/006230 dated Aug. 10, 2022, 8 pages. [cited by applicant]
Lee et al., “Synergistic Anti-Fibrotic Effect of a First-in-Class PRS Inhibitor, DWN12088, and Standard-of-Care Therapeutic Agents for IPF”, 2019 IPF Summit, Sheraton San Diego Hotel & Marina, CA, Aug. 28, 2019 1 page. [cited by applicant]
Lee et al., “A First-in-Class PRS Inhibitor, DWN12088, As a Novel Therapeutic Agent for Idiopathic Pulmonary Fibrosis”, Am J Respir Crit Care Med 2021, 203:A4645, May 2021, 1 page. [cited by applicant]
Abstract Supplement 2018 ACR/ARHP Annual Meeting, Arthritis & Rheumatology, John Wiley & Sons, Inc, US, vol. 70, Oct. 15, 2018 (Oct. 15, 2018), Abstract 128, pp. 136-137, XP072276985. [cited by applicant]
Kreuter et al., “Pharmacological Treatment of Idiopathic Pulmonary Fibrosis: Current Approaches, Unsolved Issues, and Future Perspectives”, BioMed Research International 2015.1, 2015: 329481, 10 pages. [cited by applicant]
Extended European Search Report in EP Application No. 22807683.2 dated Apr. 8, 2025, 8 pages. [cited by applicant]
Office Action in CL Application No. 202303345 dated Feb. 28, 2025, 18 pages. [cited by applicant]
Office Action in Saudi Arabian Application No. 523450746 dated Mar. 26, 2025, 7 pages. [cited by applicant]
Clinical Trials, To Evaluate Drug-drug Interactions Between DWN12088 and Pirfenidone or Nintedanib in Healthy Volunteers, [online], NCT04888 715, May 11, 2021, [Accessed: Sep. 2, 2025], Source <https://clinicaltrials.go… [cited by applicant]
Notice of Allowance in JP Application No. 2023-567150 dated Nov. 3, 2025, 8 pages. [cited by applicant]
Park et al., “Safety, Tolerability and Pharmacokinetics/Pharmacodynamic Assessment of an Oral, Selective Prolyl-tRNA Synthetase Inhibitor, DWN12088, for the Treatment of Idiopathic Pulmonary Fibrosis in Healthy Subjects… [cited by applicant]
Office Action in CN Application No. 202280033307.4 dated Dec. 17, 2025, 8 pages. [cited by applicant]
Office Action in CN Application No. 202280034620.X dated Jan. 5, 2026, 9 pages. [cited by applicant]
Gan et al., “Comparison of in-vitro anti-fibrotic effects of pirfenidone and nintedanib”, Chinese Pharmacological Bulletin, vol. 35(10), 2019, 6 pages. [cited by applicant]
Office Action in TW Application No. 111118048 dated Dec. 8, 2025, 12 pages. [cited by applicant]
Park et al., “Aminoacyl tRNA synthetases and their connections to disease”, Proc. Natl. Acad. Sci., vol. 105 (32), 2008, pp. 11043-11049. [cited by applicant]
Adachi et al., “Biochemical and Biophysical Research Communications”, Biochemical and Biophysical Research Communications, vol. 488, Issue 2, 2017, pp. 393-399. [cited by applicant]
Li et al., “Functional analysis of keratinocyte and fibroblast gene expression in skin and keloid scar tissue based on deviation analysis of dynamic capabilities”, Exp Ther Med, vol. 12 (6), 2016, pp. 3633-3641. [cited by applicant]
Floreani et al., “Treatment of primary sclerosing cholangitis”, Digestive and Liver Disease, vol. 53, 2021, pp. 1531-1538. [cited by applicant]
Andreas Stahl, “The diagnosis and treatment of age-related macular degeneration”, Dtsch Arztebl Int., vol. 117 (29-30), 2020, pp. 513-520. [cited by applicant]
Shibata et al., “Discovery and pharmacological characterization of a new class of prolyl-tRNA synthetase inhibitor for anti-fibrosis therapy”, PloS One, vol. 12 (10), 2017, 17 pages. [cited by applicant]
King et al., “A phase 3 trial of pirfenidone in patients with idiopathic pulmonary fibrosis”, New England Journal of Medicine, vol. 370, No. 22, 2014, pp. 2083-2092. [cited by applicant]
Richeldi et al., “Efficacy and safety of nintedanib in idiopathic pulmonary fibrosis”, New England Journal of Medicine, vol. 370, IS22, 2014, pp. 2071-2082. [cited by applicant]
Flaherty et al., “Safety of nintedanib added to pirfenidone treatment for idiopathic pulmonary fibrosis”, Eur Respir J, vol. 52, 2018, 11 pages. [cited by applicant]
Wang et al., “Mathematical modeling in cancer drug discovery”, Drug Discovery Today, vol. 19, Issue 2, 2014, pp. 145-150. [cited by applicant]