# US 2014/0194447 A1 · Caffeinated compounds and compositions for treatment of amyloid diseases and synucleinopathies

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

- Number: US 2014/0194447 A1
- Document ID: US20140194447A1
- Status: Published application
- Kind: A1
- Application number: 14/238,755
- Filed: 2012-10-10
- Published: 2014-07-10
- Earliest claimed: 2011-10-27
- Assignees: Proteo Tech, Inc
- Applicants: Proteo Tech Inc
- Inventors: Luke Esposito; Kelsey Hanson; Marisa C. Yadon; Thomas Lake; Alan D. Snow; Joel Cummings; Anil Kumar
- Web page: https://patentgrep.com/patent/US20140194447A1

## CPC

- C07D 473/04: two oxygen atoms
- 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 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
- C07D 473/06: with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
- C07D 473/08: with methyl radicals in positions 1 and 3, e.g. theophylline
- C07D 473/10: with methyl radicals in positions 3 and 7, e.g. theobromine
- C07D 473/12: with methyl radicals in positions 1, 3, and 7, e.g. caffeine
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Compounds and their pharmaceutically acceptable salts for treatment of β-amyloid diseases, such as observed in Alzheimer's disease and synucleinopathies, such as Parkinson's disease.

## Claims

### Claim 1

A compound selected from the group consisting of compounds of the formula
where:
R1-3 are independently substituted with hydrogen, methyl and benzyl groups,
R4 is substituted with a hydrogen, or phenyl group, and
wherein the phenyl or benzyl groups are independently substituted with up to 2 groups selected from H, OH, F, Cl, Br, glucuronide, sulfate, cyano, methyl, NH2, SH, CH2OH, CN, CF3, NHSO2CH3, N(CH3)2, NHCH3, N(CN)2, NHCN, C(CN)3, NH(C═O)NH2, NH(C═O)CH3, (C═NH)NH2, (C═NOH)NH2, O(C═O)OCH3, and NH(C═O)H, and pharmaceutically acceptable salts thereof.

### Claim 2 (depends on 1)

The compound of claim 1 selected from the group consisting of:

### Claim 3 (depends on 1)

The compound of claim 1 where R1 is substituted with a benzyl group, R2 or R3 are independently substituted with either a methyl or benzyl group and R4 is substituted with a hydrogen and wherein the benzyl groups are each substituted with two hydroxyl groups.

### Claim 4 (depends on 1)

A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable excipient.

### Claim 5 (depends on 1)

A method of treating the formation, deposition, accumulation, or persistence of amyloid or α-synuclein fibrils, comprising treating the fibrils with an effective amount of the compound of claim 1.

### Claim 6 (depends on 1)

A method of treating an amyloid disease or a synucleinopathy in a mammal suffering therefrom, comprising administration of a therapeutically effective amount of the compound of claim 1.

### Claim 7 (depends on 5)

The method of claim 5 where the amyloid disease is selected from the group of diseases consisting of Alzheimer's disease, type II diabetes, systemic AA amyloidosis, Down's syndrome, hereditary cerebral hemorrhage with amyloidosis of the Dutch type, and cerebral β-amyloid angiopathy.

### Claim 8 (depends on 5)

The method of claim 5 where the amyloid disease is Alzheimer's disease.

### Claim 9 (depends on 5)

The method of claim 5 where the synucleinopathy is selected from the group consisting of Parkinson's disease, familial Parkinson's disease, Lewy body disease, the Lewy body variant of Alzheimer's disease, dementia with Lewy bodies, multiple system atrophy, and the Parkinsonism-dementia complex of Guam.

### Claim 10 (depends on 5)

The method of claim 5 where the synucleinopathy is Parkinson's disease.

### Claim 11 (depends on 5)

The method of claim 5, where the compound administered is in an amount between 0.1 mg/Kg/day and 1000 mg/Kg/day.

### Claim 12 (depends on 5)

The method of claim 5, where the compound is administered in an amount between 1 mg/Kg/day and 100 mg/Kg/day.

### Claim 13 (depends on 5)

The method of claim 5, where amount of compound administered is in an amount between 10 mg/Kg/day and 100 mg/Kg/day.

### Claim 14 (depends on 1)

An article of manufacture, comprising packaging material, the compound of claim 1, or a pharmaceutically acceptable salt thereof, contained within packaging material, which is used for treating the formation, deposition, accumulation, or persistence of β-amyloid or α-synuclein fibrils and/or aggregates, and a label that indicates that the compound or pharmaceutically acceptable salt thereof is used for treating the formation, deposition, accumulation, or persistence of β-amyloid or α-synuclein fibrils and/or aggregates.