IP Library Granted Patent US 9,040,717
Granted Patent B2
US 9,040,717 · App. 14/210,746 · Granted May 26, 2015

Pyrazole-amide compounds and pharmaceutical use thereof

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Quick Facts
Patent No.
US 9,040,717
App. No.
14/210,746
Granted
May 26, 2015
Kind
B2
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 (18)

1. A compound represented by the formula [I]:

wherein n is 1 or 2,

or a pharmaceutically acceptable salt thereof.

2. A compound represented by the formula:

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

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

5. A compound represented by the formula [III]:

6. 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.

7. 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.

8. 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.

9. 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.

10. 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.

11. 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.

12. 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.

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

14. 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.

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

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

Assignments (2)
CHANGE OF ADDRESS Recorded Apr 8, 2026
From: JAPAN TOBACCO INC.
To: JAPAN TOBACCO INC.
Reel/Frame 075366/0624 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 18, 2014
From: MOTOMURA, TAKAHISA; SHOMI, GAKUJUN
To: JAPAN TOBACCO INC.
Reel/Frame 033124/0531 →