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02/23/06 - USPTO Class 424 |  12 views | #20060039862 | Prev - Next | About this Page  424 rss/xml feed  monitor keywords

Identification and use of growth hormone secretagogue receptor type 1a antagonists

USPTO Application #: 20060039862
Title: Identification and use of growth hormone secretagogue receptor type 1a antagonists
Abstract: Compounds that are ligands for the growth hormone secretagogue receptor type 1A (GHS-R 1A), as well as pharmaceutically acceptable salts of such compounds, are useful for the manufacture of medicaments for the regulation of food intake. (end of abstract)



Agent: Novo Nordisk, Inc. Patent Department - Princeton, NJ, US
Inventors: Maibritt Bansholm Andersen, Birgit Sehested Hansen, Kirsten Raun, Soren Tullin, Lars Thim
USPTO Applicaton #: 20060039862 - Class: 424009200 (USPTO)

Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, In Vivo Diagnosis Or In Vivo Testing, Testing Efficacy Or Toxicity Of A Compound Or Composition (e.g., Drug, Vaccine, Etc.)

Identification and use of growth hormone secretagogue receptor type 1a antagonists description/claims


The Patent Description & Claims data below is from USPTO Patent Application 20060039862, Identification and use of growth hormone secretagogue receptor type 1a antagonists.

Brief Patent Description - Full Patent Description - Patent Application Claims
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CROSS-REFERENCE TO RELATED PATENT APPLICATIONS

[0001] This patent application is a continuation of copending U.S. patent application Ser. No. 10/649,386, filed Aug. 27, 2003, which is a continuation of U.S. patent application Ser. No. 09/771,770, filed Jan. 29, 2001, and claims the benefit of U.S. Provisional Patent Application 60/181,303, filed Feb. 9, 2000, and Danish Patent Applications PA 2000 00161 and PA 2000 01107 filed Feb. 1, 2000 and Jul. 17, 2000, respectively, the entire of content of each of which is hereby incorporated by reference.

FIELD OF THE INVENTION

[0002] This invention relates to the use of a compound that is a ligand for the growth hormone secretagogue receptor type 1A (GHS-R 1A) for the regulation of food intake or food intake. The present invention also embraces pharmaceutical compositions comprising these compounds and methods of using the compounds and their pharmaceutical compositions.

BACKGROUND OF THE INVENTION

[0003] Stimulation of food intake is important in connection with patients suffering from anorexia due to chronic medical conditions, eating disorders, and other conditions in which excessive weight loss has produced a detrimental effect on the patients' health.

[0004] In other situations, suppression of food intake is important. Obesity is a well-known risk factor for the development of many very common diseases such as atherosclerosis, hypertension, Type II diabetes (non-insulin dependent diabetes mellitus (NIDDM)), dyslipidemia, coronary heart disease, and osteoarthritis and various malignancies. It also causes considerable problems through reduced mobility and decreased quality of life. The incidence of obesity and thereby also these diseases is increasing throughout the entire industrialized world. Except for exercise, diet and food restriction, no convincing treatment for reducing body weight effectively and acceptably currently exist. However, due to the important effect of obesity as a risk factor in serious and even fatal and common diseases, it will be important to find pharmaceutical compounds useful in prevention and treatment of obesity.

[0005] Even mild obesity increases the risk of premature death, diabetes, hypertension, atherosclerosis, gallbladder disease and certain types of cancer. In the industrialized western world the prevalence of obesity has increased significantly in the past few decades. Because of the high prevalence of obesity and its health consequences, its prevention and treatment should be a high public health priority.

[0006] When energy intake exceeds energy expenditure, the excess calories are stored in adipose tissue, and if this net positive balance is prolonged, obesity results, i.e., there are two components to weight balance, and an abnormality on either side (intake or expenditure) can lead to obesity.

SUMMARY OF THE INVENTION

[0007] The present invention relates, inter alia, to the use of a compound that is a ligand for the receptor GHS-R 1A, or pharmaceutically acceptable salts thereof, for the manufacture of a medicament for the regulation of food intake.

DESCRIPTION OF THE INVENTION

[0008] Accordingly, the present invention provides the use of a compound that is a ligand for the receptor GHS-R 1A, or pharmaceutically acceptable salts thereof, for the manufacture of a medicament for the regulation of food intake.

[0009] A further aspect of the present invention relates to a method for the regulation of food intake, which method comprises administering an effective amount of a compound that is a ligand for the receptor GHS-R 1A, or pharmaceutically acceptable salts thereof, to a patient in need of such a treatment.

[0010] A still further aspect of the present invention relates to the use of a compound that is a ligand for the receptor GHS-R 1A, or pharmaceutically acceptable salts thereof, for the manufacture of a medicament for the regulation of Body Mass Index (BMI).

[0011] A further aspect of the present invention relates to the use of a compound that is a ligand for the receptor GHS-R 1A, or pharmaceutically acceptable salts thereof, for the manufacture of a medicament for the treatment of anorexia.

[0012] A still further aspect of the present invention relates to the use of a compound that is a ligand for the receptor GHS-R 1A, or pharmaceutically acceptable salts thereof, for the manufacture of a medicament for the treatment of lack of appetite in children with a growth hormone deficiency.

[0013] A further aspect of the present invention relates to the use of a compound that is a ligand for the receptor GHS-R 1A, or pharmaceutically acceptable salts thereof, for the manufacture of a medicament for the treatment of obesity.

[0014] A still further aspect of the present invention relates to the use of a compound that is a ligand for the receptor GHS-R 1A, or pharmaceutically acceptable salts thereof, for the manufacture of a medicament for the treatment of Type II diabetes.

[0015] A further aspect of the present invention relates to the use of a compound that is a ligand for the receptor GHS-R 1A, or pharmaceutically acceptable salts thereof, for the manufacture of a medicament for the treatment of wasting associated with various diseases or conditions, e.g., wasting associated with AIDS, chronic liver disease, chronic obstructive pulmonary disease (COPD) or respiratory insufficiency in general, as well as wasting associated with bone fractures or with ageing. Wasting, which involves a progressive loss of body mass, including muscle mass, is normally attributable to a catabolic state of metabolism, and is frequently difficult to reverse by purely dietary means.

[0016] In one embodiment of the present invention the receptor GHS-R 1A is the human GHS-R 1A receptor. In another embodiment the medicament is for humans.

[0017] In a still further embodiment of the invention the compound does not induce a therapeutically effective growth hormone release at the therapeutic dose of the compound.

[0018] In a further embodiment of the invention the medicament is a non-injectable medicament. In a still further embodiment the medicament is an oral medicament.

[0019] The receptor GHS-R 1A (the growth hormone secretagogue receptor type 1A) is described by Howard, A. D. et al. (1996) in Science 273, 974-977.

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