# US 9,040,717 B2 · Pyrazole-amide compounds and pharmaceutical use thereof

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- Number: US 9,040,717 B2
- Document ID: US9040717B2
- Status: Granted
- Kind: B2
- Application number: 14/210,746
- Filed: 2014-03-14
- Published: 2014-10-02
- Granted: 2015-05-26
- Earliest claimed: 2013-03-15
- Assignees: Japan Tobacco Inc.
- Applicants: Japan Tobacco Inc.
- Inventors: Takahisa Motomura; Gakujun Shomi
- Web page: https://patentgrep.com/patent/US9040717B2

## CPC

- C07C 39/23: polycyclic, containing six-membered aromatic rings and other rings, with unsaturation outside the aromatic rings
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
- 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 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 13/00: Drugs for disorders of the urinary system
- A61P 13/12: of the kidneys
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 27/00: Drugs for disorders of the senses
- A61P 27/02: Ophthalmic agents
- A61P 27/12: for cataracts
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 69/78: Benzoic acid esters
- A61K 31/415: 1,2-Diazoles
- C07D 231/12: with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

A compound represented by the following formula: wherein n is 1 or 2, or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof.

## Claims

### Claim 1

A compound represented by the formula [I]:
wherein n is 1 or 2,
or a pharmaceutically acceptable salt thereof.

### Claim 2

A compound represented by the formula:

### Claim 3 (depends on 2)

The compound according to claim 2, which is represented by the formula [II]:

### Claim 4 (depends on 2)

The compound according to claim 2, which is represented by the formula [IIh]:

### Claim 5

A compound represented by the formula [III]:

### Claim 6 (depends on 1, 2, 3, 4, 5)

A pharmaceutical composition comprising the compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

### Claim 7 (depends on 1, 2, 3, 4, 5)

A method for inhibiting PDHK in a mammal comprising administering a pharmaceutically effective amount of the compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, to the mammal.

### Claim 8 (depends on 1, 2, 3, 4, 5)

A method for inhibiting PDHK1 in a mammal comprising administering a pharmaceutically effective amount of the compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, to the mammal.

### Claim 9 (depends on 1, 2, 3, 4, 5)

A method for inhibiting PDHK2 in a mammal comprising administering a pharmaceutically effective amount of the compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, to the mammal.

### Claim 10 (depends on 1, 2, 3, 4, 5)

A method for decreasing the blood glucose level in a mammal comprising administering a pharmaceutically effective amount of the compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, to the mammal.

### Claim 11 (depends on 1, 2, 3, 4, 5)

A method for decreasing lactate level in a mammal comprising administering a pharmaceutically effective amount of the compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, to the mammal.

### Claim 12 (depends on 1, 2, 3, 4, 5)

A method for the treatment of diabetes, insulin resistance syndrome, metabolic syndrome, hyperglycemia, hyperlactacidemia, diabetic complications, cardiac failure, cardiomyopathy, myocardial ischemia, myocardial infarction, angina pectoris, dyslipidemia, atherosclerosis, peripheral arterial disease, intermittent claudication, chronic obstructive pulmonary disease, brain ischemia, cerebral apoplexy, mitochondrial disease, mitochondrial encephalomyopathy, cancer or pulmonary hypertension in a mammal, comprising administering a pharmaceutically effective amount of the compound according to any one of claims 1 to 5, or a pharmaceutically acceptable salt thereof, to the mammal.

### Claim 13 (depends on 12)

The method according to claim 12, wherein the diabetes is type 1 diabetes or type 2 diabetes.

### Claim 14 (depends on 12)

The method according to claim 12, wherein the diabetic complications are selected from the group consisting of diabetic neuropathy, diabetic retinopathy, diabetic nephropathy and cataract.

### Claim 15 (depends on 12)

The method according to claim 12, wherein the cardiac failure is acute cardiac failure or chronic cardiac failure.

### Claim 16 (depends on 13)

The method according to claim 13, wherein the diabetes is type 2 diabetes.