# US 10,765,672 B2 · Pharmaceutical formulations of a HIF hydroxylase inhibitor

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 10,765,672 B2
- Document ID: US10765672B2
- Status: Granted
- Kind: B2
- Application number: 16/035,503
- Filed: 2018-07-13
- Published: 2019-01-10
- Granted: 2020-09-08
- Earliest claimed: 2013-06-06
- Assignees: FibroGen, Inc.
- Applicants: FibroGen, Inc.
- Inventors: David Conca; Lee Allen Flippin; Scott David Leigh; Claudia Witschi; Lee Robert Wright
- Web page: https://patentgrep.com/patent/US10765672B2

## CPC

- A61K 31/472: Non-condensed isoquinolines, e.g. papaverine
- A61K 9/2009: {Inorganic compounds}
- A61K 9/2813: {Inorganic compounds}
- A61K 9/282: {Organic compounds, e.g. fats}
- A61K 9/4816: {Wall or shell material}
- A61K 9/485: {Inorganic compounds}
- A61K 9/4858: {Organic compounds}
- A61K 9/4883: {Capsule finishing, e.g. dyeing, aromatising, polishing}
- A61K 9/4891: {Coated capsules; Multilayered drug free capsule shells (with drug coating for immediate release A61K9/4808; osmotic devices A61K9/0004)}
- A61P 7/06: Antianaemics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 9/2018: {Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates}
- A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61K 9/4825: {Proteins, e.g. gelatin (gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816)}
- 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 disclosure relates to pharmaceutical formulations of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid and methods of use thereof.

## Claims

### Claim 1

A tablet comprising a tablet core and a coating, wherein the tablet core comprises [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, and the coating comprises a photostabilizing agent, wherein the photostabilizing agent:
i) consists essentially of from about 0.1 to about 2 mg/cm2 titanium dioxide and from about 0.1 to about 0.4 mg/cm2 Allura Red AC or from about 0.1 to about 0.4 mg/cm2 Allura Red AC in aluminum lake; and
optionally at least one additional dye selected from the group consisting of:
from about 0.004 to about 0.4 mg/cm2 iron oxide red;
from about 0.009 to about 0.2 mg/cm2 iron oxide yellow;
from about 0.01 to about 0.03 mg/cm2 Sunset Yellow FCF; and
from about 0.01 to about 0.03 mg/cm2 Sunset Yellow FCF in aluminum lake;
wherein the amount of photostabilizing agent is based on surface area of the tablet core; and
ii) prevents the transmission of light at a wavelength range of between about 200 nm and 550 nm
and further wherein the tablet contains less than about 0.2% w/w photodegradation product of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid relative to the amount of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid.

### Claim 2 (depends on 1)

The tablet of claim 1, comprising from about 20 mg to about 200 mg of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid.

### Claim 3 (depends on 1)

The tablet of claim 1, comprising about 20 mg, about 50 mg, or about 100 mg of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid.

### Claim 4 (depends on 1)

The tablet of claim 1, wherein the tablet comprises a tablet core and a coating and the tablet core comprises [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, and the coating comprises the photostabilizing agent, and the coating is present in an amount from about 3% to about 8% w/w based on the weight of the tablet core.

### Claim 5 (depends on 4)

The tablet of claim 4, wherein the coating comprises from about 0.1 to about 0.4 mg/cm2 titanium dioxide and from about 0.1 to about 0.4 mg/cm2 Allura Red AC in aluminum lake, and wherein the amount of titanium dioxide and Allura Red AC in aluminum lake is based on surface area of the tablet core.

### Claim 6 (depends on 5)

The tablet of claim 5, wherein the tablet core comprises about 20 mg, about 50 mg or about 100 mg of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, lactose monohydrate, microcrystalline cellulose, povidone, croscarmellose sodium, and magnesium stearate; and wherein the photostabilizing agent comprises 0.1 to about 0.4 mg/cm2 titanium dioxide and from about 0.1 to about 0.4 mg/cm2 Allura Red AC in aluminum lake wherein the amount of titanium dioxide and Allura Red AC in aluminum lake is based on surface area of the tablet core.