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08/16/07 - USPTO Class 514 |  50 views | #20070191283 | Prev - Next | About this Page  514 rss/xml feed  monitor keywords

Method of stimulating the motility of the gastrointestinal system using growth hormone secretagogues

USPTO Application #: 20070191283
Title: Method of stimulating the motility of the gastrointestinal system using growth hormone secretagogues
Abstract: The present invention relates to a method of stimulating the motility of the gastrointestinal system in a subject in need thereof, wherein the subject suffers from maladies (i.e., disorders or diseases) of the gastrointestinal system. The method comprises administering to a subject in need thereof a therapeutically effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof. The growth hormone secretagogue can be co-administered with a laxative, a H2 receptor antagonist, a serotonin 5-HT4 agonist, an antacid, an opioid antagonist, a proton pump inhibitor, a motilin receptor agonist, dopamine antagonist, a cholinergic agonist, a cholinesterase inhibitor, somatostatin, octreotide, or any combination thereof. (end of abstract)



Agent: Palmer & Dodge, LLP Kathleen M. Williams - Boston, MA, US
Inventor: William J. Polvino
USPTO Applicaton #: 20070191283 - Class: 514019000 (USPTO)

Related Patent Categories: Drug, Bio-affecting And Body Treating Compositions, Designated Organic Active Ingredient Containing (doai), Peptide Containing (e.g., Protein, Peptones, Fibrinogen, Etc.) Doai, Cyclopeptides, 2 Peptide Repeating Units In Known Peptide Chain

Method of stimulating the motility of the gastrointestinal system using growth hormone secretagogues description/claims


The Patent Description & Claims data below is from USPTO Patent Application 20070191283, Method of stimulating the motility of the gastrointestinal system using growth hormone secretagogues.

Brief Patent Description - Full Patent Description - Patent Application Claims
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[0001] This application claims priority to U.S. Provisional Patent Application-Ser. No. 60/600,959 filed Aug. 12, 2004, the disclosure of which is incorporated herein by reference in its entirety.

BACKGROUND OF THE INVENTION

[0002] Gastrointestinal (GI) motility is a coordinated neuromuscular process that transports nutrients through the digestive system. C. Scarpignato, "Pharmacological Stimulation of Gastrointestinal Motility: Where We Are And Where Are We Going?" Dig. Dis., 15: 112 (1997). Impaired (i.e., slowed) motility of the gastrointestinal system, which can be involved in gastroesophageal reflux disease, gastroparesis (e.g., diabetic and postsurgical), irritable bowel syndrome and constipation, is one of the largest health care burdens of industrialized nations. S. D. Feighner et al., "Receptor for Motilin Identified in the Human Gastrointestinal System," Science, 284: 2184-2188 (Jun. 25, 1999).

[0003] In view of the above, an effective, physiological way to stimulate motility of the gastrointestinal system is highly desirable.

SUMMARY OF THE INVENTION

[0004] The present invention relates to a method of stimulating the motility of the gastrointestinal system in a subject in need thereof, wherein the subject suffers from maladies (i.e., disorders or diseases) of the gastrointestinal system. The method comprises administering to a subject in need thereof a therapeutically effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof.

[0005] In one embodiment, stimulation of gastrointestinal motility is used in a method of treating opioid induced constipation in a subject in need thereof comprising administering a therapeutically effective amount of a growth hormone secretagogue compound or a pharmaceutically acceptable salt, hydrate or solvate thereof. In one embodiment, the subject is using opioids for post-surgical pain management. In another embodiment, the subject is using opioids for chronic pain management. Suitable opioids included, but are not limited to, percocet, morphine, vicoden, methadone, oxycodone and fentanyl. In a particular embodiment, the growth hormone secretagogue is represented by Formulas I-V, or a pharmaceutically acceptable salt, hydrate or solvate thereof.

[0006] In another embodiment, stimulation of gastrointestinal motility is used in a method of treating diabetes related gastroparesis in a subject in need thereof comprising administering a therapeutically effective amount of a growth hormone secretagogue compound. In a particular embodiment, the growth hormone secretagogue is represented by Formulas I-V, or a pharmaceutically acceptable salt, hydrate or solvate thereof.

[0007] In a further embodiment, stimulation of gastrointestinal motility is used in a method of treating gastroesophageal reflux disease (GERD) in a subject in need thereof comprising administering a therapeutically effective amount of a growth hormone secretagogue compound. In a particular embodiment, the growth hormone secretagogue is represented by Formulas I-V, or a pharmaceutically acceptable salt, hydrate or solvate thereof. In a particular embodiment, the gastroesophageal reflux disease is nocturnal gastroesophageal reflux disease.

[0008] In yet another embodiment, stimulation of gastrointestinal motility is used in a method of treating irritable bowel syndrome (IBS) in a subject in need thereof comprising administering a therapeutically effective amount of a growth hormone secretagogue compound. In a particular embodiment, the growth hormone secretagogue is represented by Formulas I-V, or a pharmaceutically acceptable salt, hydrate or solvate thereof. In one embodiment, the irritable bowel syndrome is constipation-predominant irritable bowel syndrome. In another embodiment, the irritable bowel syndrome is alternating constipation/diarrhea irritable bowel syndrome.

[0009] In one embodiment, stimulation of gastrointestinal motility is used in a method of treating constipation in a subject in need thereof comprising administering a therapeutically effective amount of a growth hormone secretagogue compound. In a particular embodiment, the growth hormone secretagogue is represented by Formulas I-V, or a pharmaceutically acceptable salt, hydrate or solvate thereof.

[0010] In one embodiment, stimulation of gastrointestinal motility is used in a method of treating post-operative ileus in a subject in need thereof comprising administering a therapeutically effective amount of a growth hormone secretagogue compound. In a particular embodiment, the growth hormone secretagogue is represented by Formulas I-V, or a pharmaceutically acceptable salt, hydrate or solvate thereof.

[0011] In a particular embodiment, the growth hormone secretagogue is represented by the structural Formula I: wherein:

[0012] R.sup.1 is hydrogen, or C.sub.1-6-alkyl optionally substituted with one or more aryl or hetaryl;

[0013] a and d are independently 0, 1, 2 or 3;

[0014] b and c are independently 0, 1, 2, 3, 4 or 5, provided that b+c is 3, 4 or 5;

[0015] D is R.sup.2--NH--(CR.sup.3R.sup.4).sub.e--(CH.sub.2).sub.f-M-(CHR.sup.5).sub.- g--(CH.sub.2).sub.h--

wherein:

[0016] R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-6 alkyl optionally substituted with one or more halogen, amino, hydroxyl, aryl or hetaryl; or

[0017] R.sup.2 and R.sup.3 or R.sup.2 and R.sup.4 or R.sup.3 and R.sup.4 can optionally form --(CH.sub.2).sub.i--U--(CH.sub.2).sub.j--, wherein i and j are independently 1 or 2 and U is --O--, --S-- or a valence bond;

[0018] h and f are independently 0, 1, 2, or 3;

[0019] g and e are independently 0 or 1;

[0020] M is a valence bond, --CR.sup.6.dbd.CR.sup.7--, arylene, hetarylene, --O-- or --S--;

[0021] R.sup.6 and R.sup.7 are independently hydrogen, or C.sub.1-6-alkyl optionally substituted with one or more aryl or hetaryl;

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