# US 9,433,631 B2 · 4-pregenen-11β-17-21-triol-3,20-dione derivatives

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- Number: US 9,433,631 B2
- Document ID: US9433631B2
- Status: Granted
- Kind: B2
- Application number: 14/533,847
- Filed: 2014-11-05
- Published: 2015-02-26
- Granted: 2016-09-06
- Earliest claimed: 2011-11-11
- Assignees: Allergan, Inc.
- Applicants: Allergan, Inc.
- Inventors: Jeffrey L. Edelman; Alissar Nehme; Thomas C. Malone
- Web page: https://patentgrep.com/patent/US9433631B2

## CPC

- A61K 31/58: containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin (digitoxin {A61K31/7048})
- A61K 9/0048: {Eye, e.g. artificial tears}
- A61K 31/56: Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61P 27/02: Ophthalmic agents
- A61P 27/04: Artificial tears; Irrigation solutions
- A61P 27/06: Antiglaucoma agents or miotics
- A61P 27/14: Decongestants or antiallergics
- A61P 31/04: Antibacterial agents
- A61P 31/22: for herpes viruses
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07J 5/0053: {not substituted in position 16}
- C07J 7/008: {substituted in position 21}
- C07J 17/00: Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton (cardanolide, bufanolide C07J19/00)
- C07J 31/006: {not covered by C07J31/003}
- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- A61K 2121/00: Preparations for use in therapy
- 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
- C07J: STEROIDS (seco-steroids C07C)

## Abstract

The present invention relates to novel 4-pregenen-11β-17-21-triol-3,20-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of glucocorticoid or mineralocorticoid receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with glucocorticoid or mineralocorticoid receptor modulation.

## Claims

### Claim 1

A method of treating a disorder associated with glucocorticoid receptor modulation, which comprises administering to a patient an ophthalmically acceptable pharmaceutical composition comprising a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, wherein the compound is selected from the group consisting of:

### Claim 2 (depends on 1)

The method according to claim 1 wherein the disorder associated with glucocorticoid receptor modulation is selected from the group consisting of elevated intraocular pressure, glaucoma, retinal vein occlusions, diabetic retinopathy, various forms of macular edema, post-surgical inflammation, inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe, retinal detachment, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, selected infective conjunctivitis, corneal injury from chemical, radiation, or thermal burns, penetration of foreign bodies, allergy, or combinations thereof.

### Claim 3 (depends on 1)

The method according to claim 1 wherein the disorder associated with glucocorticoid receptor modulation is selected from dry eye, blepharitis, ocular rosacea, meibomian gland dysfunction, uveitis and macular degeneration.

### Claim 4 (depends on 3)

The method according to claim 3 wherein the disorder associated with glucocorticoid receptor modulation is dry eye.

### Claim 5 (depends on 1)

The method according to claim 1 wherein the ophthalmically acceptable pharmaceutical composition is topically administered.

### Claim 6 (depends on 4)

The method according to claim 4 wherein the ophthalmically acceptable pharmaceutical composition is topically administered.

### Claim 7 (depends on 1)

The method according to claim 1 wherein the ophthalmically acceptable pharmaceutical composition is formulated for intraocular injection.

### Claim 8 (depends on 4)

The method according to claim 4 wherein the ophthalmically acceptable pharmaceutical composition is formulated for intraocular injection.

### Claim 9 (depends on 1)

The method according to claim 1 wherein the ophthalmically acceptable pharmaceutical composition is formulated into sustained release or controlled release intraocular implants comprising biodegradable polymers.

### Claim 10 (depends on 4)

The method according to claim 4 wherein the ophthalmically acceptable pharmaceutical composition is formulated into sustained release or controlled release intraocular implants comprising biodegradable polymers.

### Claim 11 (depends on 9)

The method according to claim 9, wherein the biodegradable polymer is selected from the group consisting of polylactic acid, plyglycolic acid, and combinations thereof.

### Claim 12 (depends on 10)

The method according to claim 10, wherein the biodegradable polymer is selected from the group consisting of polylactic acid, plyglycolic acid, and combinations thereof.