# US 11,896,578 B2 · Methods of treating conditions related to the S1P1 receptor

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- Number: US 11,896,578 B2
- Document ID: US11896578B2
- Status: Granted
- Kind: B2
- Application number: 17/235,468
- Filed: 2021-04-20
- Published: 2021-11-04
- Granted: 2024-02-13
- Earliest claimed: 2015-01-06
- Assignees: Arena Pharmaceuticals, Inc.
- Applicants: Arena Pharmaceuticals, Inc.
- Inventors: Alan Glicklich; Maria Matilde Sanchez Kam; William R. Shanahan
- Web page: https://patentgrep.com/patent/US11896578B2

## CPC

- A61K 31/403: condensed with carbocyclic rings, e.g. carbazole
- A61K 9/4825: {Proteins, e.g. gelatin (gelatin capsule shells with substantial amounts of other macromolecular substances A61K9/4816)}
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/00: Drugs for disorders of the endocrine system
- A61P 17/06: Antipsoriatics
- A61P 17/10: Anti-acne agents
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/02: Immunomodulators
- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- 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

Provided are methods of treatment of a sphingosine 1-phosphate subtype 1 (S1P1) receptor-associated disorder comprising prescribing and/or administering to an individual in need thereof a standard dose of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, in an amount equivalent to about 1.5 to about 2.5 mg of Compound 1, for example, a disease or disorder mediated by lymphocytes, an autoimmune disease or disorder, an inflammatory disease or disorder, ankylosing spondylitis, biliary cirrhosis, cancer, psoriasis, psoriatic arthritis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, inflammatory bowel disease, ulcerative colitis, type I diabetes, hypertensive nephropathy, glomerulosclerosis, myocardial ischemia-reperfusion injury, and acne.

## Claims

### Claim 1

A method of treatment of atopic dermatitis in an individual, comprising
administering to the individual (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, once daily
in an amount equivalent to about 2.0 mg of Compound 1.

### Claim 2 (depends on 1)

The method of claim 1, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is administered in an amount equivalent to 2.0 mg of Compound 1.

### Claim 3 (depends on 1)

The method of claim 1, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is administered orally.

### Claim 4 (depends on 1)

The method of claim 1, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is formulated as a capsule or tablet suitable for oral administration.

### Claim 5 (depends on 1)

The method of claim 1, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is selected from:
Compound 1;
a calcium salt of Compound 1;
and
an L-arginine salt of Compound 1.

### Claim 6 (depends on 1)

The method of claim 1, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is an L-arginine salt of Compound 1.

### Claim 7 (depends on 1)

The method of claim 1, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is an anhydrous, non-solvated, crystalline form of an L-arginine salt of Compound 1.

### Claim 8 (depends on 1)

The method of claim 1, wherein the Compound 1, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, is an anhydrous, non-solvated, crystalline form of Compound 1.

### Claim 9

A method of treatment of atopic dermatitis in an individual, comprising administering to the individual (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid (Compound 1), or a pharmaceutically acceptable salt thereof, once daily in an amount equivalent to 2.0 mg of Compound 1.

### Claim 10 (depends on 9)

The method of claim 9, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is administered orally.

### Claim 11 (depends on 9)

The method of claim 9, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is formulated as a capsule or tablet suitable for oral administration.

### Claim 12 (depends on 9)

The method of claim 9, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is selected from:
Compound 1;
a calcium salt of Compound 1;
and
an L-arginine salt of Compound 1.

### Claim 13 (depends on 9)

The method of claim 9, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is an L-arginine salt of Compound 1.

### Claim 14 (depends on 9)

The method of claim 9, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is an anhydrous, non-solvated, crystalline form of an L-arginine salt of Compound 1.

### Claim 15 (depends on 9)

The method of claim 9, wherein the Compound 1, or a pharmaceutically acceptable salt thereof, is an anhydrous, non-solvated, crystalline form of Compound 1.