# US 9,040,589 B2 · Continuous administration of dopa decarboxylase inhibitors and compositions for same

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- Number: US 9,040,589 B2
- Document ID: US9040589B2
- Status: Granted
- Kind: B2
- Application number: 14/276,211
- Filed: 2014-05-13
- Published: 2014-09-04
- Granted: 2015-05-26
- Earliest claimed: 2009-05-19
- Assignees: NeuroDerm, Ltd.
- Applicants: Neuroderm, Ltd.
- Inventors: Oron Yacoby-Zeevi; Mara Nemas
- Web page: https://patentgrep.com/patent/US9040589B2

## CPC

- A61K 31/198: Alpha-amino acids, e.g. alanine or edetic acid [EDTA] (betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00)
- A61K 9/0014: {Skin, i.e. galenical aspects of topical compositions (non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00)}
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 31/12: Ketones
- A61K 31/277: having a ring, e.g. verapamil
- A61K 47/183: {Amino acids, e.g. glycine, EDTA or aspartame}
- A61K 47/22: Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/14: for treating abnormal movements, e.g. chorea, dyskinesia
- 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 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 243/18: containing rings
- C07C 279/14: being further substituted by carboxyl groups
- A61K 31/15: Oximes (>C=N—O—); Hydrazines (>N—N<); Hydrazones (>N—N=) {; Imines (C—N=C)}
- 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
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS

## Abstract

Disclosed herein are compositions that include for example the arginine salt of carbidopa, and methods for treating neurological or movement diseases or disorders such as restless leg syndrome, Parkinson's disease, secondary parkinsonism, Huntington's disease, Parkinson's like syndrome, PSP, MSA, ALS, Shy-Drager syndrome and conditions resulting from brain injury including carbon monoxide or manganese intoxication, using substantially continuous administration of carbidopa or salt thereof together with administration of levodopa.

## Claims

### Claim 1

A pharmaceutically acceptable liquid composition comprising levodopa, arginine, and about 0.5% to about 3% by weight carbidopa, wherein the pH of the liquid composition is 8 to 10 at 25° C.

### Claim 2 (depends on 1)

The pharmaceutically acceptable liquid composition of claim 1, wherein the pH is about 9.5 at 25° C.

### Claim 3 (depends on 2)

The composition of claim 2, comprising up to about 2% by weight carbidopa.

### Claim 4 (depends on 2)

The pharmaceutically acceptable liquid composition of claim 2, comprising about 6% by weight levodopa.

### Claim 5 (depends on 4)

The pharmaceutically acceptable liquid composition of claim 4, comprising about 1 to about 20% by weight arginine.

### Claim 6 (depends on 5)

The pharmaceutically acceptable liquid composition of claim 5, further comprising N-acetyl cysteine.

### Claim 7 (depends on 5)

The pharmaceutically acceptable liquid composition of claim 5, further comprising ascorbic acid.

### Claim 8 (depends on 1)

The pharmaceutically acceptable liquid composition of claim 1, wherein the liquid composition has no precipitation when held for 48 hours at room temperature.

### Claim 9

A pharmaceutically acceptable liquid composition with a pH of 9.5 at 25° C., comprising about 6% by weight levodopa, about 1 to about 20% by weight arginine, and ascorbic acid.

### Claim 10 (depends on 9)

The pharmaceutically acceptable liquid composition of claim 9, further comprising about 0.5% to about 3% by weight carbidopa.

### Claim 11 (depends on 10)

The pharmaceutically acceptable liquid composition of claim 10 comprising up to 2% by weight carbidopa.

### Claim 12

A pharmaceutically acceptable liquid composition with a pH of 9.5 at 25° C., comprising about 6% by weight levodopa, about 1 to about 20% by weight arginine, about 0.5% to about 3% by weight carbidopa, and ascorbic acid.

### Claim 13 (depends on 12)

The pharmaceutically acceptable liquid composition of claim 12, further comprising N-acetyl cysteine.

### Claim 14 (depends on 1)

A method of treating a disease or disorder characterized by reduced levels of dopamine in a patient's brain, comprising administering to said patient an amount of a composition of claim 1 in an amount effective to treat said disease or disorder.

### Claim 15 (depends on 14)

The method of claim 14, wherein said administering is subcutaneous, transdermal, intradermal, intravenous, oral, intraduodenal, intramuscular, and/or direct absorption through mucous membrane tissues.

### Claim 16 (depends on 14)

The method of claim 14, wherein said administration is continuous.

### Claim 17 (depends on 14)

The method of claim 14, wherein said disease or disorder is Parkinson's disease or secondary parkinsonism.

### Claim 18 (depends on 17)

The method of claim 17, wherein said disease is Parkinson's disease.

### Claim 19 (depends on 18)

The method of claim 18, wherein said administering is continuous.

### Claim 20 (depends on 19)

The method of claim 19, wherein said administering is subcutaneous.

### Claim 21 (depends on 1)

An infusion pump comprising the composition of claim 1.