Methods of Treating an Overweight or Obese Subject

Patent metadata

Field	Value
Publication number	US-2018016249-A1
Application number	US-201715617595-A
Country	US
Kind code	A1
Filing date	Jun 8, 2017
Priority date	Dec 4, 2008
Publication date	Jan 18, 2018
Grant date	—

Abstract

The disclosure herein generally relates to methods of treating an overweight or obese condition, and overweight- or obesity-related conditions. In one embodiment, the disclosure provides a method of treating an overweight or obese condition involving administering to the subject in need thereof, an amount of a pharmaceutical composition including a MetAP-2 inhibitory compound, or a salt, ester, or prodrug thereof, effective to result in weight loss in the subject.

First claim

What is claimed is:

1 . A method of treating a subject having an overweight or obese condition, the method comprising: administering to the subject in need thereof, a therapeutically effective amount of a pharmaceutical composition comprising a compound of Formula III:

wherein:
W is O or NR;
each R is, independently hydrogen or a C 1 -C 4 -alkyl;
Q is hydrogen, a linear, branched or cyclic C 1 -C 6 -alkyl; or aryl;
R 1 is hydroxy, C 1 -C 4 -alkoxy or halogen; and
Z is —C(O)— or C 1 -C 4 -alkylene-C(O)—; and P is NHR, OR, or a peptide consisting of 1 to about 100 amino acid residues attached to Z at the N-terminus;
or Z is alkylene-O or alkylene-NR; and P is hydrogen or peptide comprising 1 to 100 amino acid residues attached to Z at the C-terminus;

or a pharmaceutically acceptable salt, ester, or prodrug thereof.

2 . A method of treating a subject having an overweight or obese condition, the method comprising: administering to the subject a therapeutically effective amount of a pharmaceutical composition comprises a compound selected from the group consisting of:

3 . The method of claim 1 , wherein the subject has a Body Mass Index measurement selected from the group consisting of: at least about 25 kg/m 2 , at least about 30 kg/m 2 , and at least about 40 kg/m 2 .

4 .- 12 . (canceled)

13 . A method of improving exercise capacity in a subject in need thereof comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising a compound of Formula III:

wherein:
W is O or NR;
each R is, independently hydrogen or a C 1 -C 4 -alkyl;
Q is hydrogen, a linear, branched or cyclic C 1 -C 6 -alkyl; or aryl;
R 1 is hydroxy, C 1 -C 4 -alkoxy or halogen; and
Z is —C(O)— or C 1 -C 4 -alkylene-C(O)—; and P is NHR, OR, or a peptide consisting of 1 to about 100 amino acid residues attached to Z at the N-terminus;
or Z is alkylene-O or alkylene-NR; and P is hydrogen or peptide comprising 1 to 100 amino acid residues attached to Z at the C-terminus;

or a pharmaceutically acceptable salt, ester, or prodrug thereof.

14 . (canceled)

15 . A method of restoring normal metabolic action in an obese subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising a compound of Formula III:

wherein:
W is O or NR;
each R is, independently hydrogen or a C 1 -C 4 -alkyl;
Q is hydrogen, a linear, branched or cyclic C 1 -C 6 -alkyl; or aryl;
R 1 is hydroxy, C 1 -C 4 -alkoxy or halogen; and
Z is —C(O)— or C 1 -C 4 -alkylene-C(O)—; and P is NHR, OR, or a peptide consisting of 1 to about 100 amino acid residues attached to Z at the N-terminus;
or Z is alkylene-O or alkylene-NR; and P is hydrogen or peptide comprising 1 to 100 amino acid residues attached to Z at the C-terminus;

or a pharmaceutically acceptable salt, ester, or prodrug thereof.

Assignees

• Zafgen Inc

Inventors

• Vath James E

Classifications

• A61K31/439

  the ring forming part of a bridged ring system, e.g. quinuclidine (8-azabicyclo [3.2.1] octanes A61K31/46) · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• C07D303/22 Primary

  with monohydroxy compounds · CPC title

• A61K31/4025

  not condensed and containing further heterocyclic rings, e.g. cromakalim · CPC title

• C07D303/10

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