# US 9,750,743 B2 · Composition comprising phosphodiesterase type 5 inhibitor for inhibiting apoptosis of nerve cells

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- Number: US 9,750,743 B2
- Document ID: US9750743B2
- Status: Granted
- Kind: B2
- Application number: 14/649,467
- Filed: 2013-12-04
- Published: 2015-10-22
- Granted: 2017-09-05
- Earliest claimed: 2012-12-04
- Assignees: Aribio Co., Ltd.; SK Chemicals Co., Ltd.
- Applicants: Aribio Inc.; SK Chemicals Co., Ltd.
- Inventors: Myung Hwa Kim; Jae Jun Choung; Sae Kwang Ku
- Web page: https://patentgrep.com/patent/US9750743B2

## CPC

- A61K 31/519: ortho- or peri-condensed with heterocyclic rings
- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/4985: Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
- A61K 31/53: having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine (melarsoprol A61K31/555 {; with four nitrogen atoms A61K31/495})
- 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 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- 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
- A61K 31/4745: condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48)
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 31/505: Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- 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 relates to a composition and health functional food for inhibiting apoptosis of cranial nerve cells, and to a method for inhibiting apoptosis, wherein the composition and health functional food comprising a phosphodiesterase type 5 active inhibitor. According to the present invention, the PDE5 inhibitor exhibits a protective effect on nerve cells by inhibiting apoptosis of cranial nerve cells. Thus, the present invention can be effectively used to prevent, alleviate, and treat cranial nerve disease.

## Claims

### Claim 1

A method for inhibiting brain neuron apoptosis in a subject in need thereof, comprising administering a composition containing a phosphodiesterase type 5 inhibitor that is mirodenafil or a pharmaceutically acceptable salt, solvate, or hydrate thereof in an effective amount to the subject.

### Claim 2 (depends on 1)

The method of claim 1, wherein the subject is a patient with brain nerve disease.

### Claim 3 (depends on 1)

The method of claim 1, wherein the brain nerve disease is selected from the group consisting of neuronal degenerative disease, ischemic stroke, cognitive dysfunction, and motor dysfunction.

### Claim 4 (depends on 1)

The method of claim 1, wherein the neuronal degenerative disease is selected from the group consisting of dementia, Huntington's disease, Parkinson's disease, and amyotrophic lateral sclerosis.

### Claim 5 (depends on 1)

The method of claim 1, wherein the cognitive dysfunction is memory loss, learning disability, agnosia, amnesia, aphasia, apraxia, or delirium.

### Claim 6 (depends on 1)

The method of claim 1, wherein the motor dysfunction is motor disturbance, paralysis, ataxia, dyskinesia, spasticity, or dystonia.

### Claim 7 (depends on 1)

The method of claim 1, wherein the phosphodiesterase type 5 inhibitor inhibits the formation of degenerative neurons in brain tissues or inhibits the expression of caspase-3 or poly ADP ribose polymerase (PARP) in neurons.

### Claim 8 (depends on 1)

The method of claim 1, wherein the composition is administered to a human orally or parentally through a part other than the head.

### Claim 9 (depends on 1)

The method of claim 1, wherein the composition is a film dosage form when the phosphodiesterase type 5 inhibitor is orally administered.