IP Library › Granted Patent US 12,485,108
Granted Patent B2
US 12,485,108 · App. 17/435,061 · Granted Dec 2, 2025

Method for treating fatty liver disease and/or steatohepatitis

Inventors: Yuanyuan Jiang (Beijing, CN); Weiting Zhong (Beijing, CN); Yanping Zhao (Beijing, CN); Hongjun Wang (Beijing, CN); Jing Zhao (Beijing, CN); Jing Li (Beijing, CN); Weina Liu (Beijing, CN); Liying Zhou (Beijing, CN); Yanan Liu (Beijing, CN)
Assignee: BEIJING TIDE PHARMACEUTICAL CO., LTD.
A61K31/416A61P3/04
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 12,485,108
App. No.
17/435,061
Granted
Dec 2, 2025
Kind
B2
Abstract

The present invention falls within the field of biological medicine, and specifically relates to a method for preventing, alleviating and/or treating fatty liver disease and/or steatohepatitis. The method comprises administering, to an individual in need thereof, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt, an ester, a stereoisomer, a polymorph, a solvate, an N-oxide, an isotopically labeled compound, a metabolite or a prodrug thereof.

Claims (17)

1 . A method for preventing, alleviating and/or treating a fatty liver disease and/or steatohepatitis, comprising administering to a subject in need thereof an effective amount of a compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof, wherein the compound has the following structure:

2 . The method according to claim 1 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered in an amount of 0.005 mg/day to 5000 mg/day.

3 . The method according to claim 1 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered in an amount of 1 ng/kg to 200 mg/kg, 1 μg/kg to 100 mg/kg or 1 mg/kg to 50 mg/kg body weight per day.

4 . The method according to claim 1 , wherein the daily dose of the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered at one time or is administered in two, three or four doses.

5 . The method according to claim 1 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered continuously for at least 3 days, at least 4 days, at least 5 days, at least 6 days, at least 7 days, at least 8 days, at least 9 days, at least 10 days, at least 11 days, at least 12 days, at least 13 days, at least 14 days, at least 15 days, at least 16 days, at least 17 days, at least 18 days, at least 19 days, at least 20 days, at least 21 days, at least 22 days, at least 23 days, at least 24 days, at least 25 days, at least 30 days, at least 35 days, at least 40 days, at least 45 days or at least 50 days.

6 . The method according to claim 1 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered for one or more courses of treatment, wherein each course of treatment lasts for at least 3 days, at least 4 days, at least 5 days, at least 6 days, at least 7 days, at least 8 days, at least 9 days, at least 10 days, at least 11 days, at least 12 days, at least 13 days, at least 14 days, at least 15 days, at least 16 days, at least 17 days, at least 18 days, at least 19 days, at least 20 days, at least 21 days, at least 22 days, at least 23 days, at least 24 days, at least 25 days, at least 30 days, at least 35 days, at least 40 days, at least 45 days or at least 50 days; and the interval between every two courses of treatment is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 days, two weeks, three weeks, or four weeks.

7 . The method according to claim 1 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered through injection, or transdermal administration, or is administered via oral, buccal, nasal, transmucosal, topical, as an ophthalmic formulation, or via inhalation.

8 . The method according to claim 1 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered in a dosage form selected from the group consisting of tablet, capsule, lozenge, hard candy, powder, spray, cream, salve, suppository, gel, paste, lotion, ointment, aqueous suspensions, injectable solution, elixir, and syrup.

9 . The method according to claim 1 , wherein the prevention or treatment comprises reduction in fatty degeneration, reduction in collagen accumulation and/or reduction in ballooning degeneration.

10 . The method according to claim 1 , further comprising administering one or more additional therapeutic agents which are suitable for preventing, alleviating and/or treating a fatty liver disease and/or steatohepatitis.

11 . The method according to claim 1 , wherein the fatty liver disease is an alcoholic fatty liver disease (AFLD) or a non-alcoholic fatty liver disease (NAFLD).

12 . The method according to claim 1 , wherein the steatohepatitis is an alcoholic steatohepatitis (ASH) or a non-alcoholic steatohepatitis (NASH).

13 . The method according to claim 2 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered in an amount of 0.005, 0.05, 0.5, 5, 10, 20, 30, 40, 50, 100, 150, 200, 250, 300, 350, 400, 450, 500, 550, 600, 650, 700, 750, 800, 850, 900, 950, 1000, 1500, 2000, 2500, 3000, 3500, 4000, 4500 or 5000 mg/day.

14 . The method according to claim 3 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered in an amount of 1 μg/kg, 10 μg/kg, 25 μg/kg, 50 μg/kg, 75 μg/kg, 100 μg/kg, 125 μg/kg, 150 μg/kg, 175 μg/kg, 200 μg/kg, 225 μg/kg, 250 μg/kg, 275 μg/kg, 300 μg/kg, 325 μg/kg, 350 μg/kg, 375 μg/kg, 400 μg/kg, 425 μg/kg, 450 μg/kg, 475 μg/kg, 500 μg/kg, 525 μg/kg, 550 μg/kg, 575 μg/kg, 600 μg/kg, 625 μg/kg, 650 μg/kg, 675 μg/kg, 700 μg/kg, 725 μg/kg, 750 μg/kg, 775 μg/kg, 800 μg/kg, 825 μg/kg, 850 μg/kg, 875 μg/kg, 900 μg/kg, 925 μg/kg, 950 μg/kg, 975 μg/kg, 1 mg/kg, 5 mg/kg, 10 mg/kg, 15 mg/kg, 20 mg/kg, 25 mg/kg, 30 mg/kg, 35 mg/kg, 40 mg/kg, 45 mg/kg, 50 mg/kg, 60 mg/kg, 70 mg/kg, 80 mg/kg, 90 mg/kg, 100 mg/kg, 125 mg/kg, 150 mg/kg, 175 mg/kg, 200 mg/kg or 300 mg/kg body weight per unit dose.

15 . The method according to claim 6 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered for 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10 courses of treatment.

16 . The method according to claim 7 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered through intravenous, intraarterial, subcutaneous, intraperitoneal, intramuscular injection.

17 . The method according to claim 16 , wherein the compound or a pharmaceutically acceptable salt, ester, stereoisomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof is administered through dripping injection.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 31, 2021
From: JIANG, YUANYUAN; ZHONG, WEITING; ZHAO, YANPING; WANG, HONGJUN; ZHAO, JING; LI, JING; LIU, WEINA; ZHOU, LIYING; LIU, YANAN
To: BEIJING TIDE PHARMACEUTICAL CO., LTD.
Reel/Frame 057335/0992 →
Priority Claims (1)
WO PCT/CN2019/076688 · Mar 1, 2019 · international
Continuity (1)
Related Publication 20220378743A1 · Dec 1, 2022
References Cited (21)
US 10323023B2 · Zhao · 2019 [cited by examiner]
US 10329282B2 · Zhao · 2019 [cited by examiner]
US 11390609B2 · Zhao · 2022 [cited by examiner]
US 20170137385A1 · Chimenti et al. · 2017 [cited by applicant]
US 20190010143A1 · Zhao et al. · 2019 [cited by applicant]
CN 105980361 · 2016 [cited by applicant]
WO 2012040499 · 2011 [cited by applicant]
WO 2016004254 · 2016 [cited by applicant]
WO 2018039539 · 2018 [cited by applicant]
WO 2019000682 · 2019 [cited by applicant]
WO 2019001572 · 2019 [cited by applicant]
WO 2019145729 · 2019 [cited by applicant]
Klein et al. “Rho-kinase inhibitor coupled to peptide-modified albumin carrier reduces portal pressure and increases renal perfusion in cirrhotic rats.” Scientific reports. Feb. 19, 2019;9(1):1-1. [cited by applicant]
Xie et al. “Fasudil alleviates hepatic fibrosis in type 1 diabetic rats: involvement of the inflammation and RhoA/ROCK pathway.” Eur. Rev. Med. Pharmacol. Sci. Sep. 1, 2018;22:5665-77. [cited by applicant]
Tada et al. “A selective ROCK inhibitor, Y27632, prevents dimethylnitrosamine-induced hepatic fibrosis in rats.” Journal of hepatology. Apr. 1, 2001;34(4):529-36. [cited by applicant]
Fernández-Simón et al. “RhoA/ROCK2 signalling is enhanced by PDGF-AA in fibro-adipogenic progenitor cells in DMD.” bioRxiv. Apr. 14, 2021. [cited by applicant]
Zhu X, Xiong T, Liu P, Guo X, Xiao L, Zhou F, Tang Y, Yao P. Quercetin ameliorates HFD-induced NAFLD by promoting hepatic VLDL assembly and lipophagy via the IRE1a/XBP1s pathway. Food and chemical toxicology. Apr. 1, 20… [cited by applicant]
Huang et al. “Rho-kinase/AMPK axis regulates hepatic lipogenesis during overnutrition.” The Journal of clinical 1 investigation. Dec. 3, 2018;128(12):5335-50. [cited by applicant]
Sunamura et al. “Different roles of myocardial ROCK1 and ROCK2 in cardiac dysfunction and postcapillary pulmonary hypertension in mice.” Proceedings of the National Academy of Sciences. Jul. 24, 2018;115(30):E7129-38. [cited by applicant]
Lock et al. “Distinct roles for ROCK1 and ROCK2 in the regulation of keratinocyte differentiation.” PloS one. Dec. 4, 2009;4(12):e8190. [cited by applicant]
Chen et al. “ROCK2, but not ROCK1 interacts with phosphorylated STAT3 and co-occupies TH17/TFH gene promoters in TH17-activated human T cells.” Scientific reports. Nov. 9, 2018;8(1):1-0. [cited by applicant]