Heterocyclic compounds having cholesterol 24-hydroxylase activity

Patent metadata

Field	Value
Publication number	US-9643957-B2
Application number	US-201314650429-A
Country	US
Kind code	B2
Filing date	Dec 10, 2013
Priority date	Dec 11, 2012
Publication date	May 9, 2017
Grant date	May 9, 2017

Abstract

An object of the present invention is to provide a compound having a superior CH24H inhibitory action, which is useful as an agent for the prophylaxis or treatment of epilepsy, neurodegenerative disease and the like. The present invention relates to a compound represented by the formula:

wherein each symbol is as defined in the specification, or a salt thereof.

First claim

The invention claimed is:

1. A compound or a salt thereof, which is selected from the group consisting of:
(2R)-1-((1-(4-(4-methyl-1H-pyrazol-1-yl)pyridin-3-yl)piperidin-4-yl)carbonyl)pyrrolidine-2-carbonitrile or a salt thereof,
(2R)-1-((1-(4-(4-chloro-1H-pyrazol-1-yl)pyridin-3-yl)piperidin-4-yl)carbonyl)pyrrolidine-2-carbonitrile or a salt thereof, and
(2R)-4,4-difluoro-1-((1-(4-(4-methyl-1H-pyrazol-1-yl)pyridin-3-yl)piperidin-4-yl)carbonyl)pyrrolidine-2-carbonitrile or a salt thereof.

2. A compound or a salt thereof, which is (2R)-1-((1-(4-(4-methyl-1H-pyrazol-1-yl)pyridin-3-yl)piperidin-4-yl)carbonyl)pyrrolidine-2-carbonitrile or a salt thereof.

3. A compound or a salt thereof, which is (2R)-1-((1-(4-(4-chloro-1H-pyrazol-1-yl)pyridin-3-yl)piperidin-4-yl)carbonyl)pyrrolidine-2-carbonitrile or a salt thereof.

4. A compound or a salt thereof, which is (2R)-4,4-difluoro-1-((1-(4-(4-methyl-1H-pyrazol-1-yl)pyridin-3-yl)piperidin-4-yl)carbonyl)pyrrolidine-2-carbonitrile or a salt thereof.

5. A pharmaceutical composition comprising the compound or salt of claim 1 , and a pharmacologically acceptable carrier.

6. A method for the treatment of Alzheimer's disease in a mammal, which comprises administering an effective amount of the compound or salt of claim 1 to the mammal.

7. A pharmaceutical composition comprising the compound or salt of claim 2 , and a pharmacologically acceptable carrier.

8. A method for the treatment of Alzheimer's disease in a mammal, which comprises administering an effective amount of the compound or salt of claim 2 to the mammal.

9. A pharmaceutical composition comprising the compound or salt of claim 3 , and a pharmacologically acceptable carrier.

10. A method for the treatment of Alzheimer's disease in a mammal, which comprises administering an effective amount of the compound or salt of claim 3 to the mammal.

11. A pharmaceutical composition comprising the compound or salt of claim 4 , and a pharmacologically acceptable carrier.

12. A method for the treatment of Alzheimer's disease in a mammal, which comprises administering an effective amount of the compound or salt of claim 4 to the mammal.

Assignees

• Takeda Pharmaceuticals Co

Inventors

• Koike Tatsuki
• Kajita Yuichi
• Yoshikawa Masato
• Ikeda Shuhei
• Fukuda Hiromi

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P25/14

  for treating abnormal movements, e.g. chorea, dyskinesia · CPC title

• A61P25/08

  Antiepileptics; Anticonvulsants · CPC title

• A61P25/28

  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 · CPC title

• A61P25/16

  Anti-Parkinson drugs · CPC title