# US 8,541,435 B2 · Niacin compositions for reduction of amyloid beta peptide 42 (abeta 42) production and for treatment of Alzheimer's disease (AD)

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- Number: US 8,541,435 B2
- Document ID: US8541435B2
- Status: Granted
- Kind: B2
- Application number: 12/737,323
- Filed: 2009-07-09
- Published: 2011-04-28
- Granted: 2013-09-24
- Earliest claimed: 2008-07-11
- Applicants: Uday Saxena; Venkateswarulu Akella
- Inventors: Uday Saxena; Venkateswarulu Akella
- Web page: https://patentgrep.com/patent/US8541435B2

## CPC

- A61K 31/455: Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
- A61K 31/05: Phenols {(cannabinoids A61K31/658)}
- A61K 31/12: Ketones
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
- 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
- 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 invention discloses (1) phenolic ester hybrids of niacin with m-methoxy-p-hydroxy phenyl compounds like eugenol, vanillin, apocynin, ferulic acid, isoferulic acid and eugenol epoxide and (2) cocrystals of hybrids as above, particularly cocrystal of niacin-eugenol hybrid with cocrystal former like eugenol and oxalic acid (3) novel pharmaceutical compositions comprising a combination of niacin and one or more small molecule/potentiating agent like eugenol, curcumin, cinnamic acid, meclofenamic acid, and their use in the treatment of a disorder or a disease caused by excess production of amyloid beta peptide-42 (Aβ42), its deposition, accumulation, and plaque formation including Alzheimer's Disease, dementia and mild cognitive impairment as well as other neurodegenerative diseases such as Parkinson's Disease and ischemic stroke.

## Claims

### Claim 1

A pharmaceutical composition comprising a niacin hybrid resulting from esterification of niacin with apocynin and wherein the said composition is effective in treatment of a disorder or a disease characterized by excess production of amyloid beta peptide-42 (Abeta42), its deposition, accumulation, and plaque formation.

### Claim 2 (depends on 1)

A method of treatment of a human disorder or a disease condition caused by excess production of amyloid beta peptide-42 (Abeta42), its deposition, accumulation, and plaque formation comprising administering a therapeutically effective amount of the pharmaceutical composition as claimed in claim 1.

### Claim 3 (depends on 2)

The method of claim 2 wherein the said human disorder or disease condition is selected from the group consisting of Alzheimer's disease, dementia and mild cognitive impairment and other neurodegenerative disorders selected from Parkinson's disease and ischemic stroke.

### Claim 4 (depends on 2)

The method of claim 2 wherein the said pharmaceutical composition is administered orally or parenterally.

### Claim 5 (depends on 1)

A pharmaceutical composition comprising at least one pharmaceutically acceptable carrier, diluent or an excipient and a compound according to claim 1.

### Claim 6 (depends on 2)

The method of claim 2 wherein the said pharmaceutical composition is administered in combination therapy with other existing small molecule, protein, vaccine or nucleic acid based approved drugs or those in development for treatment of Alzheimer's disease, dementia's or mild cognitive impairment or other neurodegenerative disorders selected from Parkinson's disease and ischemic stroke.