Melanin Concentrating Hormone Receptor Small Molecule Antagonists for the Treatment of Obesity and Related Metabolic Disorders
- Technology Application
- These compounds are efficacious in reducing food intake in rats and may be useful for the treatment of conditions associated with the MCH receptor in humans such as obesity, diabetes, eating disorders and related conditions.
- Detailed Technology Description
- University of California, Irvine researchers have found a class of small molecule MCHR1 antagonists that specifically inhibits MCH activation of MCHR1. These compounds display no affinity to human MCH2R and other peptide GPCRs. To demonstrate the efficacy in vivo, these compounds were administered in rats and MCH-induced food intake was reduced up to 75% in a dose dependent manner. The effects of these compounds lasted for over four hours. These compounds do not affect locomotion or fine movements, and also do not result in ataxis movements
- Supplementary Information
- Patent Number: US8372848B2
Application Number: US2003593941A
Inventor: Houghten, Richard A. | Dooley, Colette | Nefzi, Adel | Wang, Zhiwei | Civelli, Oliver | Nagasaki, Hiroshi
Priority Date: 23 Mar 2004
Priority Number: US8372848B2
Application Date: 1 Jul 2008
Publication Date: 12 Feb 2013
IPC Current: A61K0031495 | A61K00314015 | A61K00314166 | A61K00314168 | C07D023312 | C07D023342 | C07D023910 | C07D023912
US Class: 514256 | 514392 | 544297 | 544298 | 5483245
Assignee Applicant: Mixture Sciences Inc.n Diego | The Regents of the University of California |Nefzi Adeln Diego
Title: Melanin-concentrating hormone receptor antagonists and methods of use
Usefulness: Melanin-concentrating hormone receptor antagonists and methods of use
Summary: (A) is useful in the manufacture of a preparation for administration to a human/animal subject to block or antagonize melanin-concentrating hormone receptors or to decrease food intake or to treat obesity, a metabolic disorder, an eating disorder, depression or urinary incontinence (claimed). (A) is useful to treat psychiatric disorders such as muscle disorder and is also useful for diagnostic purposes.
Novelty: Composition of matter having melanin-concentrating hormone receptor antagonistic activity, useful to treat e.g. obesity, eating disorders, depression and urinary incontinence, comprises imidazole-2-one compounds
- Industry
- Biomedical
- Sub Category
- Medical Composition
- Application No.
- 8372848
- Others
-
Tech ID/UC Case
18858/2003-546-0
Related Cases
2003-546-0
- *Abstract
-
In mammals, Melanin Concentrating Hormone (MCH), a GPCR, has been shown to regulate food consumption and energy metabolism. Central administration of MCH has been shown to promote feeding while mRNA levels of the MCH Receptor 1 (MCHR1) rise as a result of starvation and leptin deficiency. MCH also stimulates insulin and leptin relase in insulinoma cell lines and adipose cells respectively and regulates pituitary hormones. Mice devoid of MCH are lean and hypophagic, while mice over-expressing MCH are obese and hyperphagic. Genetic disruption of MCHR1 on the other hand results in mice that are hyperphagic, but also hypermetabolic and obesity-resistant.
- *IP Issue Date
- Feb 12, 2013
- *Principal Investigator
-
Name: Olivier Civelli
Department:
Name: Colette Dooley
Department:
Name: Richard Houghten
Department:
Name: Hiroshi Nagasaki
Department:
Name: Adel Nefzi
Department:
Name: Zhiwei Wang
Department:
- Country/Region
- USA
