Heterocyclic compound

Patent metadata

Field	Value
Publication number	US-10214498-B2
Application number	US-201515517227-A
Country	US
Kind code	B2
Filing date	Oct 22, 2015
Priority date	Oct 24, 2014
Publication date	Feb 26, 2019
Grant date	Feb 26, 2019

Abstract

Provided is a heterocyclic compound having a superior RBP4-lowering action and useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4. A compound represented by the formula (I):

wherein each symbol is as defined in the Description, or a salt thereof has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of a disease or symptom mediated by an increase in RBP4 or retinol supplied by RBP4.

First claim

The invention claimed is:

1. A compound represented by the formula (I):

wherein
ring A is a pyrazole ring, a pyridine ring, or a pyrimidine ring;
X is CH 2 or O; and
R is a hydrogen atom or a C 1-6 alkyl group,
or a salt thereof.

2. The compound according to claim 1 , wherein R is a hydrogen atom, or a salt thereof.

3. ((2-(3,5 bis(Trifluoromethyl)phenyl)pyrimidin-5-yl)oxy)acetic acid or a salt thereof.

4. ((6-(3,5-bis(Trifluoromethyl)phenyl)pyridin-3-yl)oxy)acetic acid or a salt thereof.

5. 3-(3-(3,5-bis(Trifluoromethyl)phenyl)-1H-pyrazol-1-yl)propanoic acid or a salt thereof.

6. ((1-(3,5-bis(Trifluoromethyl)phenyl)-1H-pyrazol-3-yl)oxy)acetic acid or a salt thereof.

7. A medicament comprising the compound according to claim 1 or a salt thereof.

8. A medicament comprising the compound according to claim 2 or a salt thereof.

9. A method of lowering retinol binding protein 4 in a mammal, comprising administering an effective amount of the compound according to claim 1 , or a salt thereof to the mammal.

10. A method for the prophylaxis or treatment of macular degeneration and/or Stargardt's disease in a mammal, comprising administering an effective amount of the compound according to claim 1 , or a salt thereof to the mammal.

11. A method of lowering retinol binding protein 4 in a mammal, comprising administering an effective amount of the compound according to claim 2 , or a salt thereof to the mammal.

12. A method for the prophylaxis or treatment of macular degeneration and/or Stargardt's disease in a mammal, comprising administering an effective amount of the compound according to claim 2 , or a salt thereof to the mammal.

Assignees

• Takeda Pharmaceuticals Co

Inventors

• Banno Yoshihiro
• Kamaura Masahiro
• Takami Kazuaki
• Fukuda Koichiro
• Sasaki Shigekazu

Classifications

• A61K31/421

  1,3-Oxazoles, e.g. pemoline, trimethadione · CPC title

• A61P27/02

  Ophthalmic agents · CPC title

• C07D231/22 Primary

  with aryl radicals attached to ring nitrogen atoms · CPC title

• C07D239/34 Primary

  One oxygen atom · CPC title

• C07D263/38

  attached in position 2 · CPC title