Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing
Reexamination Certificate
2001-04-24
2004-03-02
Kemmerer, Elizabeth (Department: 1647)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
C514S002600
Reexamination Certificate
active
06699832
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to methods of treating obesity, diabetes, sexual dysfunction (including erectile dysfunction), atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia, or hypertrigylceridemia using a compound that is a neurotensin receptor ligand. The present invention also relates to compositions and kits that comprise a neurotensin receptor ligand.
BACKGROUND OF THE INVENTION
Obesity is a devastating disease. In addition to harming physical health, obesity can wreak havoc on mental health because obesity affects self-esteem, which ultimately can affect a person's ability to interact socially with others. Unfortunately, obesity is not well understood, and societal stereotypes and presumptions regarding obesity only tend to exacerbate the psychological effects of the disease. Because of the impact of obesity on individuals and society, much effort has been expended to find ways to treat obesity, but little success has been achieved in the long-term treatment and/or prevention of obesity.
Neurotensin is a thirteen amino acid peptide that appears to have functions as a neurotransmitter and neuromodulator in the nervous system and as a local hormone in the periphery. Specifically, neurotensin is a neuromodulator of dopamine transmission and of anterior pituitary hormone secretion, and exerts potent hypothermic and analgesic effects in the brain. In the periphery, neurotensin is a paracrine and endocrine modulator of the digestive tract and acts as a growth factor on a variety of cells.
So far, three types of neurotensin receptors have been identified: neurotensin-1 receptors, neurotensin-2 receptors, and neurotensisn-3 receptors. (The neurotensin-3 receptor is also called sortlin or gp95.) The neurotensin-1 and neurotensin-2 receptors are G protein coupled receptors; the neurotensin-3 receptor is not a G protein coupled receptor.
SUMMARY OF THE INVENTION
The present invention provides methods of treating obesity, the methods comprising the step of administering to an obese patient or a patient at risk of becoming obese a therapeutically effective amount of a compound that is a neurotensin receptor ligand.
In a preferred embodiment of the methods, the neurotensin receptor ligand is a neurotensin-1 receptor ligand.
In another preferred embodiment of the methods, the neurotensin receptor ligand is a neurotensin-2 receptor ligand.
In another preferred embodiment of the methods, the neurotensin receptor ligand is a neurotensin-3 receptor ligand.
In another preferred embodiment of the methods, the ligand is an agonist.
In another preferred embodiment of the methods, the ligand is an antagonist.
In another preferred embodiment of the methods, the neurotensin receptor ligand is a neurotensin-1 receptor agonist.
Also provided are methods of treating obesity, the methods comprising the step of administering to an obese patient or a patient at risk of becoming obese a therapeutically effective amount of a compound that is a selective neurotensin-1 receptor agonist.
Also provided are pharmaceutical compositions comprising:
a) a compound that is a neurotensin receptor ligand; and
b) a second compound useful for the treatment of obesity, diabetes, sexual dysfunction, atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia or hypertrigylceridemia.
In a preferred embodiment of the compositions, the neurotensin receptor ligand is a neurotensin-1 receptor agonist.
In another preferred embodiment of the method, the second compound is a &bgr;
3
-adrenergic receptor agonist, a cholecystokinin-A agonist, a monoamine reuptake inhibitor, a sympathomimetic agent, a serotoninergic agent, a dopamine agonist, a melanocyte-stimulating hormone receptor agonist or mimetic, a melanocyte-stimulating hormone receptor analog, a cannabinoid receptor antagonist, a melanin concentrating hormone antagonist, leptin, a leptin analog, a leptin receptor agonist, a galanin antagonist, a bombesin agonist, a neuropeptide-Y antagonist, a thyromimetic agent, dehydroeplandrosterone or an analog thereof, a glucocorticoid receptor agonist or antagonist, an orexin receptor antagonist, a urocortin binding protein antagonist, a glucagon-like peptide-1 receptor agonist, or a ciliary neurotrophic factor.
Also provided are kits that comprises:
a) a first pharmaceutical composition comprising a compound that is a neurotensin receptor ligand;
b) a second pharmaceutical composition comprising a compound that is useful for the treatment of obesity, diabetes, sexual dysfunction, atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia or hypertrigylceridemia; and
c) a container for the first and second compositions.
In a preferred embodiment of the kits, the neurotensin receptor ligand is a neurotensin-1 receptor agonist.
In another preferred embodiment of the kits, the second pharmaceutical composition comprises a compound that is a &bgr;
3
-adrenergic receptor agonist, a cholecystokinin-A agonist, a monoamine reuptake inhibitor, a sympathomimetic agent, a serotoninergic agent, a dopamine agonist, a melanocyte-stimulating hormone receptor agonist or mimetic, a melanocyte-stimulating hormone receptor analog, a cannabinoid receptor antagonist, a melanin concentrating hormone antagonist, leptin, a leptin analog, a leptin receptor agonist, a galanin antagonist, a bombesin agonist, a neuropeptide-Y antagonist, a thyromimetic agent, dehydroepiandrosterone or an analog thereof, a glucocorticoid receptor agonist or antagonist, an orexin receptor antagonist, a urocortin binding protein antagonist, a glucagon-like peptide-1 receptor agonist, or a ciliary neurotrophic factor.
Also provided are methods of treating diabetes, sexual dysfunction, atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia or hypertrigylceridemia, the methods comprising the step of administering to a patient having or at risk of having, diabetes, sexual dysfunction, atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia or hypertrigylceridemia a therapeutically effective amount of a neurotensin receptor ligand.
In a preferred embodiment of the method, the neurotensin receptor ligand is a neurotension-1 receptor ligand.
DETAILED DESCRIPTION OF THE INVENTION
The present invention relates to methods of treating obesity, diabetes, sexual dysfunction (including erectile dysfunction), atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia or hypertrigylceridemia using a compound that is a neurotensin receptor ligand. In addition, the present invention provides pharmaceutical compositions and kits comprising a neurotensin receptor ligand.
In accordance with the present invention, obesity, diabetes, sexual dysfunction (including erectile dysfunction), atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia or hypertrigylceridemia can be treated by administering to an obese patient or a patent at risk of becoming obese or a patent having or at risk of having, diabetes, sexual dysfunction (including erectile dysfunction), atherosclerosis, insulin resistance, impaired glucose tolerance, hypercholesterolemia, or hypertrigylceridemia a therapeutically effective amount of a neurotensin receptor ligand. In a preferred embodiment of the invention, the neurotensin receptor ligand is a neurotensin-1 receptor ligand. In a more preferred embodiment of the invention, the neurotensin receptor ligand is a selective neurotensin-1 receptor agonist.
The term “therapeutically effective amount” means an amount of a compound or combination of compounds that treats a disease; ameliorates, attenuates, or eliminates one or more symptoms of a particular disease; or prevents or delays the onset of one of more symptoms of a disease.
The term “patient” means animals, such as dogs, cats, cows, horses, sheep, geese, and humans. Particularly preferred patients are mammals, including humans of both sexes.
The term “pharmaceutically acceptable” means that the substan
Benson Gregg C.
Kemmerer Elizabeth
Kennedy Robert M.
Nichols Christopher James
Pfizer Inc.
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