# US 8,772,327 B2 · Phenylpropionic acid derivative and use thereof

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

- Number: US 8,772,327 B2
- Document ID: US8772327B2
- Status: Granted
- Kind: B2
- Application number: 13/654,164
- Filed: 2012-10-17
- Published: 2013-05-23
- Granted: 2014-07-08
- Earliest claimed: 2008-04-28
- Assignees: Asahi Kasei Pharma Corporation
- Applicants: Kohei Morita; Hiroshi Kuriyama; Kosuke Tanaka
- Inventors: Kohei Morita; Hiroshi Kuriyama; Kosuke Tanaka
- Web page: https://patentgrep.com/patent/US8772327B2

## CPC

- C07D 231/56: Benzopyrazoles; Hydrogenated benzopyrazoles
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 1/18: for pancreatic disorders, e.g. pancreatic enzymes
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 5/14: of the thyroid hormones, e.g. T3, T4
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 7/06: Antianaemics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/06: Antiarrhythmics
- 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 11/02: Nasal agents, e.g. decongestants
- A61P 11/06: Antiasthmatics
- A61P 13/12: of the kidneys
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 17/00: Drugs for dermatological disorders
- A61P 17/02: for treating wounds, ulcers, burns, scars, keloids, or the like
- A61P 17/04: Antipruritics
- A61P 17/06: Antipsoriatics
- A61P 19/00: Drugs for skeletal disorders
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 19/06: Antigout agents, e.g. antihyperuricemic or uricosuric agents
- A61P 19/08: for bone diseases, e.g. rachitism, Paget's disease
- A61P 19/10: for osteoporosis
- A61P 21/00: Drugs for disorders of the muscular or neuromuscular system
- A61P 21/04: for myasthenia gravis
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 25/06: Antimigraine agents
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/24: Antidepressants
- 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 27/02: Ophthalmic agents
- A61P 27/06: Antiglaucoma agents or miotics
- 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 33/00: Antiparasitic agents
- A61P 35/00: Antineoplastic agents
- A61P 35/02: specific for leukemia
- A61P 35/04: specific for metastasis
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 401/12: linked by a chain containing hetero atoms as chain links
- C07D 403/12: linked by a chain containing hetero atoms as chain links
- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D 411/12: linked by a chain containing hetero atoms as chain links
- C07D 413/12: linked by a chain containing hetero atoms as chain links
- C07D 417/12: linked by a chain containing hetero atoms as chain links
- C07D 417/14: containing three or more hetero rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

A compound represented by the following general formula (1) or a salt thereof, which has superior inhibitory activity against type 4 PLA2, and thus has prostaglandin and/or leucotriene production suppressing action [X represents a halogen atom, an alkyl group which may be substituted, or the like, Y represents hydrogen atom or an alkyl group which may be substituted, and Z represents hydrogen atom or an alkyl group which may be substituted].

## Claims

### Claim 1

The compound defined below or a salt thereof;

### Claim 2

The compound defined below or a salt thereof;

### Claim 3 (depends on 1, 2)

A medicament comprising the compound according to any one of claims 1 to 2 or a pharmaceutically acceptable salt thereof as an active ingredient.

### Claim 4 (depends on 1, 2)

A prostaglandin and/or leucotriene production suppressing agent comprising the compound according to any on of claims 1 to 2 or a pharmaceutically acceptable salt thereof as an active ingredient.

### Claim 5 (depends on 3)

The medicament according to claim 3, which is for prophylactic and/or therapeutic treatment of a disease for which suppression of leucotriene production is effective.

### Claim 6 (depends on 1, 2)

A type 4 phospholipase A2 enzyme activity inhibitor comprising the compound according to any one of claims 1 to 2 or a pharmaceutically acceptable salt thereof as an active ingredient.

### Claim 7 (depends on 3)

The medicament according to claims 3, which is for therapeutic treatment of a disease induced by expression of type 4 phospholipase A2 enzyme activity.

### Claim 8 (depends on 3)

The medicament according to claim 3, which is for therapeutic treatment of an inflammatory disease of a mammal.

### Claim 9 (depends on 3)

The medicament according to claim 3, which is for therapeutic treatment of an autoimmune disease of a mammal.

### Claim 10 (depends on 3)

The medicament according to claim 3, which is for prophylactic and/or therapeutic treatment of an allergic disease of a mammal.

### Claim 11 (depends on 3)

The medicament according to claim 3, which is for defervescence and/or analgesia of a mammal wherein the defervescence and/or analgesia is through suppression of prostaglandins and/or leucotriene production.

### Claim 12 (depends on 1, 2)

A pharmaceutical composition for therapeutic treatment of a condition in living body of a mammal in which an acute or chronic inflammatory reaction is observed, which comprises the compound according to any one of claims 1 to 2 or a pharmaceutically acceptable salt thereof in an amount effective for the prophylactic and/or therapeutic treatment, and a pharmaceutically acceptable carrier.

### Claim 13 (depends on 1, 2)

A method for therapeutic treatment of acute or chronic inflammatory disease or disorder, which comprises the step of administering the compound according to any one of claims 1 to 2 or a pharmaceutically acceptable salt thereof to a mammal in need thereof in an amount effective for the therapeutic treatment.