# US 2021/0275469 A1 · Toxic aldehyde related diseases and treatment

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- Number: US 2021/0275469 A1
- Document ID: US20210275469A1
- Status: Published application
- Kind: A1
- Application number: 17/227,568
- Filed: 2021-04-12
- Published: 2021-09-09
- Earliest claimed: 2013-01-23
- Assignees: Aldeyra Therapeutics, Inc.
- Applicants: Aldeyra Therapeutics, Inc.
- Inventors: Todd Brady; Scott Young; William A. Kinney; Kenneth J. Mandell
- Web page: https://patentgrep.com/patent/US20210275469A1

## CPC

- A61K 31/137: Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine {or methadone}
- A61K 8/41: Amines
- A61K 8/44: Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives thereof
- A61K 8/49: containing heterocyclic compounds
- A61K 8/4926: {having six membered rings}
- A61K 31/13: Amines {(A61K31/04 takes precedence)}
- A61K 31/197: the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid (carnitine A61K31/205)
- A61K 31/423: condensed with carbocyclic rings
- A61K 31/435: having six-membered rings with one nitrogen as the only ring hetero atom
- A61K 31/438: The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
- A61K 31/47: Quinolines; Isoquinolines
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- 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 11/00: Drugs for disorders of the respiratory system
- A61P 11/06: Antiasthmatics
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/06: Antipsoriatics
- A61P 17/10: Anti-acne agents
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 21/02: Muscle relaxants, e.g. for tetanus or cramps
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 27/00: Drugs for disorders of the senses
- A61P 27/02: Ophthalmic agents
- A61P 27/12: for cataracts
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 31/04: Antibacterial agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 39/02: Antidotes
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61Q 19/00: Preparations for care of the skin
- A61Q 19/08: Anti-ageing preparations
- C08K 5/04: Oxygen-containing compounds {(C08K5/0091 takes precedence)}
- C08K 5/08: Quinones
- C08K 5/18: with aromatically bound amino groups
- 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
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- C08K: Use of inorganic or non-macromolecular organic substances as compounding ingredients (paints, inks, varnishes, dyes, polishes, adhesives C09)

## Abstract

The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.

## Claims

### Claim at position 1

1-42. (canceled)

### Claim 43

A method of treating scleritis, comprising:
administering to a subject in need thereof a therapeutically effective amount of a compound of formula (I):
or a pharmaceutically acceptable salt thereof, wherein,
X is CH; Z is N; and Y is C with the —NH2 attached;
p is 0, 1, 2, or 3;
each RB is independently a halogen, hydroxyl, carbamoyl, amino, or aryl;
RA is
and
each Qa is independently a C1-C6 straight chain alkyl.

### Claim 44 (depends on 43)

The method of claim 43, wherein p is 1.

### Claim 45 (depends on 43)

The method of claim 43, wherein each Qa is methyl.

### Claim 46 (depends on 43)

The method of claim 43, wherein RB is a halogen.

### Claim 47 (depends on 46)

The method of claim 46, wherein the halogen is chlorine or fluorine.

### Claim 48 (depends on 47)

The method of claim 47, wherein the halogen is chlorine.

### Claim 49 (depends on 43)

The method of claim 43, wherein the compound is present at a concentration of about 0.05-10% w/v.

### Claim 50 (depends on 43)

The method of claim 43, wherein the compound is present at a concentration of about 0.1-5% w/v.

### Claim 51 (depends on 43)

The method of claim 43, wherein the compound is present at a concentration of about 0.1-2% w/v.

### Claim 52 (depends on 43)

The method of claim 43, wherein the compound is present at a concentration of about 0.1-1.0% w/v.

### Claim 53 (depends on 43)

The method of claim 43, wherein the compound is present at a concentration of about 0.09-0.5% w/v.

### Claim 54 (depends on 43)

The method of claim 43, wherein the compound is present in an admixture with a cyclodextrin.

### Claim 55 (depends on 54)

The method of claim 54, wherein the cyclodextrin comprises a β-cyclodextrin or a pharmaceutically acceptable salt thereof.

### Claim 56 (depends on 55)

The method of claim 55, wherein the β-cyclodextrin is selected from the group consisting of sulfobutylether-β-cyclodextrin, 2-hydroxypropyl-β-cyclodextrin, and 3-hydroxypropyl-β-cyclodextrin.

### Claim 57 (depends on 56)

The method of claim 56, wherein the β-cyclodextrin is sulfobutylether-β-cyclodextrin or a pharmaceutically acceptable salt thereof.

### Claim 58 (depends on 57)

The method of claim 57, wherein the salt of sulfobutylether-β-cyclodextrin is sulfobutylether-β-cyclodextrin sodium salt.

### Claim 59 (depends on 58)

The method of claim 58, wherein the sulfobutylether-β-cyclodextrin sodium salt is present at a concentration of about 0.01-30% w/v.

### Claim 60 (depends on 43)

The method of claim 43, wherein the sulfobutylether-β-cyclodextrin is present at a concentration of about 2-25% w/v.

### Claim 61 (depends on 52)

The method of claim 52, wherein the sulfobutylether-β-cyclodextrin is present at a concentration of about 6-20% w/v.

### Claim 62 (depends on 43)

The method of claim 43, wherein for the compound of formula (I):
each Qa is methyl;
RB is halogen; and
p is 1.

### Claim 63 (depends on 43)

The method of claim 43, wherein the compound is
or a pharmaceutically acceptable salt thereof.

### Claim 64 (depends on 63)

The method of claim 63, wherein the subject is a human and the compound is administered topically to one or both eyes of the subject.

### Claim 65 (depends on 61)

The method of claim 61, wherein the compound is
or a pharmaceutically acceptable salt thereof.

### Claim 66 (depends on 62)

The method of claim 62, wherein the compound is administered topically to one or both eyes of the subject as an aqueous composition comprising the compound, and a cyclodextrin or a pharmaceutically acceptable salt thereof.

### Claim 67 (depends on 66)

The method of claim 66, wherein the cyclodextrin is a β-cyclodextrin or a pharmaceutically acceptable salt thereof.

### Claim 68 (depends on 67)

The method of claim 67, wherein the β-cyclodextrin is sulfobutylether-β-cyclodextrin, hydroxypropyl-β-cyclodextrin, or a pharmaceutically acceptable salt thereof.

### Claim 69 (depends on 68)

The method of claim 68, wherein the β-cyclodextrin is hydroxypropyl-β-cyclodextrin, or a pharmaceutically acceptable salt thereof.

### Claim 70 (depends on 69)

The method of claim 69, wherein the hydroxypropyl-β-cyclodextrin is 2-hydroxypropyl-β-cyclodextrin, 3-hydroxypropyl-β-cyclodextrin, or a pharmaceutically acceptable salt thereof.

### Claim 71 (depends on 68)

The method of claim 68, wherein the β-cyclodextrin is sulfobutylether-β-cyclodextrin, or a pharmaceutically acceptable salt thereof.

### Claim 72 (depends on 71)

The method of claim 71, wherein the sulfobutylether-β-cyclodextrin is present at a concentration of about 0.01%-30% w/v.

### Claim 73 (depends on 72)

The method of claim 72, wherein the sulfobutylether-β-cyclodextrin is present at a concentration of about 5%-25% w/v.

### Claim 74 (depends on 73)

The method of claim 73, wherein the compound is present at a concentration of about 0.09-0.5% w/v.

### Claim 75 (depends on 73)

The method of claim 73, wherein the compound is present at a concentration of about 0.08-1% w/v.

### Claim 76 (depends on 73)

The method of claim 73, wherein the compound is present at a concentration of about 0.06-5% w/v.

### Claim 77 (depends on 73)

The method of claim 73, wherein the compound is present at a concentration of about 0.1-5% w/v.

### Claim 78 (depends on 73)

The method of claim 73, wherein the compound is present at a concentration of about 0.2-2.0% w/v.

### Claim 79 (depends on 73)

The method of claim 73, wherein the compound is present at a concentration of about 0.1-1.0% w/v.

### Claim 80 (depends on 64)

The method of claim 64, wherein the compound is present at a concentration of 0.08%-1.0% w/v; and the cyclodextrin is sulfobutylether-β-cyclodextrin, wherein the sulfobutylether-β-cyclodextrin is present at 6%-12% w/v.

### Claim 81 (depends on 80)

The method of claim 80, wherein the compound is present at a concentration of about 0.09%-0.5% w/v.

### Claim 82 (depends on 80)

The method of claim 80, wherein the compound is present at a concentration of about 0.1% w/v.

### Claim 83 (depends on 81)

The method of claim 81, wherein the sulfobutylether-β-cyclodextrin is present at a concentration of about 9.5% w/v.