Fumigillol compounds and methods of making and using same

Patent metadata

Field	Value
Publication number	US-9895339-B2
Application number	US-201715399071-A
Country	US
Kind code	B2
Filing date	Jan 5, 2017
Priority date	May 9, 2012
Publication date	Feb 20, 2018
Grant date	Feb 20, 2018

Abstract

The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.

First claim

We claim:

1. A method of treating and/or controlling obesity, comprising administering to a patient in need thereof an effective amount of a compound represented by:

wherein
R 2 is selected from the group consisting of hydroxyl and isopropyl (optionally substituted with a hydroxyl);
R 3 is selected from the group consisting of H and hydroxyl; or pharmaceutically acceptable salts or stereoisomers thereof.

2. A method of treating and/or controlling obesity, comprising administering to a patient in need thereof an effective amount of a compound represented by:

wherein
R 4 and R 5 , together with the nitrogen to which they are attached, form a 4 membered ring optionally substituted by one or two substituents independently selected from the group consisting of methyl and hydroxyl;
or pharmaceutically acceptable salts or stereoisomers thereof.

3. The method of claim 2 , wherein the compound is represented by:

wherein
R 6 is selected from the group consisting of H, hydroxyl and methyl; and
R 7 is selected from the group consisting of H, hydroxyl and methyl.

4. A method of treating and/or controlling obesity, comprising administering to a patient in need thereof an effective amount of a compound represented by:

wherein
n is 1 or 2; or pharmaceutically acceptable salts or stereoisomers thereof.

5. A method of treating and/or controlling obesity, comprising administering to a patient in need thereof an effective amount of a compound selected from the group consisting of:

and pharmaceutically acceptable salts or stereoisomers thereof.

6. A method of treating and/or controlling obesity, comprising administering to a patient in need thereof an effective amount of a compound selected from the group consisting of:

and pharmaceutically acceptable salts or stereoisomers thereof.

7. The method of claim 1 , wherein the patient is a human.

8. The method claim 1 , wherein the compound is administered orally, intravenously, or subcutaneously.

9. The method of claim 1 , wherein the compound is administered orally.

10. The method of claim 2 , wherein the patient is a human.

11. The method claim 2 , wherein the compound is administered orally, intravenously, or subcutaneously.

12. The method of claim 2 , wherein the compound is administered orally.

13. The method of claim 4 , wherein the patient is a human.

14. The method claim 4 , wherein the compound is administered orally, intravenously, or subcutaneously.

15. The method of claim 4 , wherein the compound is administered orally.

16. The method of claim 5 , wherein the patient is a human.

17. The method claim 5 , wherein the compound is administered orally, intravenously, or subcutaneously.

18. The method of claim 5 , wherein the compound is administered orally.

19. The method of claim 6 , wherein the patient is a human.

20. The method claim 6 , wherein the compound is administered orally, intravenously, or subcutaneously.

21. The method of claim 6 , wherein the compound is administered orally.

Assignees

• Zafgen Inc

Inventors

• Zahler Robert
• Vath James E

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• C07D405/14

  containing three or more hetero rings · CPC title

• C07D303/16

  by esterified hydroxyl radicals · CPC title

• C07D303/31 Primary

  in which the oxirane rings are condensed with a carbocyclic ring system having three or more relevant rings · CPC title