Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Melanin concentrating hormone antagonist

a technology of concentrating hormone and antagonistic action, which is applied in the field of concentrating hormone antagonists, can solve the problems of arthritis and pain, obesity is now becoming a social problem, and achieve the effect of excellent mch antagonistic action

Inactive Publication Date: 2007-07-26
KATO KANEYOSHI +6
View PDF2 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

A compound of the invention possesses an excellent MCH receptor antagonistic action, therefore, it is useful as an agent for preventing or treating diseases caused by MCH. Also, a compound of the invention is low in toxicity, and is excellent in oral absorbency and intracerebral transitivity.
Therefore, a melanin-concentrating hormone antagonist (hereafter, also abbreviated as “MCH antagonist”) comprising a compound of the invention can be safely administered to mammals (e.g. rats, mice, guinea pigs, rabbits, sheep, horses, swine, cattle, monkeys, humans, etc.) as an agent for preventing or treating diseases caused by MCH.
The pharmaceutical provides excellent effects such as “strengthening of therapeutic effect against obesity”, “reduction of dose of MCH antagonist”, etc. as compared to single use of each drug.

Problems solved by technology

Therefore, if irregularities in feeding behavior occur, disorders, often connected to diseases, will occur in normal life-maintaining activities.
Accompanying recent changes of our dietary environment, obesity is now becoming a social problem.
In addition, not only is obesity a serious risk factor for life-style diseases such as diabetes, hypertension, and arteriosclerosis; it is also widely known that increased body weight places excessive burdens on joints such as knee joints, causing arthritis and pain.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Melanin concentrating hormone antagonist
  • Melanin concentrating hormone antagonist
  • Melanin concentrating hormone antagonist

Examples

Experimental program
Comparison scheme
Effect test

reference example 1

2-(R)-[2-(N,N-Dimethylamino)ethy]-6-(4-[(4-methoxyphenyl)carbonyloxy]benzyloxy)tetralin

Diethyl azodicarboxylate (40% toluene solution, 0.95 g) was added dropwise to THF solution (6 ml) of 2-(R)-[2-(N,N-dimethylamino)ethyl]-6-hydroxytetralin (300 mg), 4-(hydroxymethyl)phenyl 4-methoxybenzoate (530 mg), and triphenylphosphine (430 mg) under ice-cooling. After stirring for 2 hours at room temperature, the reaction mixture was concentrated. The residue was purified using alumina column chromatography (development solvent; hexane˜hexane: ethyl acetate=10:1), and the titled compound (320 mg) was obtained after recrystallization (ethyl acetate-hexane).

Melting point: 111-114° C.

[α]D20=+44.4° (c=0.502, methanol)

reference example 2

N-Phenyl-4-[[2-(2-piperidinoethyl)-6-tetralinyl]oxymethyl]benzamide

Triethylamine (0.11 ml) was added to THF suspension (3 ml) of 4-[[2-(2-piperidinoethyl)-6-tetralinyl]oxymethyl]benzoate (300 mg). Further, THF solution (0.5 ml) of trimethylacetyl chloride (92 mg) was added dropwise under ice-cooling, which was stirred for 30 minutes. The temperature of the reaction mixture was raised to room temperature, which was stirred for 1 hour. THF solution (0.5 ml) of aniline (85 mg) was added dropwise to the reaction mixture under ice-cooling, which was stirred for 1 hour. After the reaction mixture was stirred for 24 hours at room temperature, saturated sodium bicarbonate solution was added, and extraction was conducted using a mixed solution of ethyl acetate and THF. The organic layer was washed with water and saturated aqueous sodium chloride solution, dried, and then concentrated. The residue was recrystallized from THF-methanol-IPE to give the titled compound (150 mg).

Melting point:...

references example 3

4-[[2-(2-Piperidinoethyl)-6-tetralinyl]oxymethyl]-N-(2-pyridinyl)benzamide

Triethylamine (0.11 ml) was added to THF suspension (6 ml) of 4-[[2-(2-piperidinoethyl)-6-tetralinyl]oxymethyl]benzoate (300 mg). Trimethylacetyl chloride (0.095 ml) was added dropwise to the obtained suspension under ice-cooling, which was stirred for 30 minutes. The temperature of the reaction mixture was raised to room temperature, which was stirred for 1 hour. THF solution (1.0 ml) of 2-aminopyridine (110 mg) was added dropwise to the reaction mixture under ice-cooling, which was stirred for 1 hour. Then the reaction mixture was stirred at room temperature for 6 hours, and at 60° C. for 12 hours, which was refluxed with heating for 6 hours. Saturated sodium bicarbonate solution was added to the reaction mixture, and extraction was conducted using ethyl acetate. The organic layer was washed with water and saturated aqueous sodium chloride solution, dried, and then concentrated. The residue was purified us...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
body weightaaaaaaaaaa
stressaaaaaaaaaa
body weightsaaaaaaaaaa
Login to View More

Abstract

A melanin-concentrating hormone antagonist which comprises a compound of the formula: wherein Ar1 is a cyclic group which may have substituents; X is a spacer having a main chain of 1 to 6 atoms; Y is a bond or a spacer having a main chain of 1 to 6 atoms; Ar is a monocyclic aromatic ring which may be condensed with a 4 to 8 membered non-aromatic ring, and may have further substituents; R1 and R2 are independently hydrogen atom or a hydrocarbon group which may have substituents; R1 and R2, together with the adjacent nitrogen atom, may form a nitrogen-containing hetero ring which may have substituents; R2 may form a spiro ring together with Ar; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing hetero ring which may have substituents; or a salt thereof; which is useful as an agent for preventing or treating obesity, etc.

Description

TECHNICAL FIELD The present invention relates to a melanin-concentrating hormone antagonist which is useful as an agent for preventing or treating obesity, etc. BACKGROUND ART Feeding behavior is an essential action for many living beings including humans. Therefore, if irregularities in feeding behavior occur, disorders, often connected to diseases, will occur in normal life-maintaining activities. Accompanying recent changes of our dietary environment, obesity is now becoming a social problem. In addition, not only is obesity a serious risk factor for life-style diseases such as diabetes, hypertension, and arteriosclerosis; it is also widely known that increased body weight places excessive burdens on joints such as knee joints, causing arthritis and pain. The “diet boom,” etc. show that there is a potentially great percentage of the population hoping to reduce body weight; on the other hand, many cases of feeding problems such as overeating, occurring due to causes such as her...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/538A61K31/4706A61K31/40A61K31/165A61K31/353C07C217/74C07C219/28C07C233/29C07C233/44C07C233/80C07C235/42C07C235/50C07C235/56C07C235/64C07C235/84C07C237/40C07C271/28C07C275/42C07C311/21C07D207/26C07D207/277C07D209/18C07D209/22C07D209/42C07D211/16C07D211/18C07D211/22C07D211/26C07D211/32C07D211/52C07D211/62C07D211/70C07D213/56C07D213/81C07D213/82C07D215/14C07D215/38C07D233/24C07D239/28C07D239/30C07D261/18C07D263/14C07D263/34C07D265/28C07D271/06C07D295/096C07D295/13C07D295/185C07D307/68C07D307/81C07D311/58C07D317/60C07D319/20C07D333/24C07D333/28C07D333/38C07D335/16C07D405/04C07D405/12C07D413/04C07D413/12C07D493/04
CPCC07C217/74C07D493/04C07C233/29C07C233/44C07C233/80C07C235/42C07C235/50C07C235/56C07C235/64C07C235/84C07C237/40C07C271/28C07C275/42C07C311/21C07C2102/10C07C2102/12C07D207/277C07D209/18C07D209/22C07D209/42C07D211/16C07D211/18C07D211/22C07D211/26C07D211/32C07D211/52C07D211/62C07D211/70C07D213/56C07D213/81C07D213/82C07D215/14C07D215/38C07D233/24C07D239/28C07D239/30C07D261/18C07D263/14C07D263/34C07D265/28C07D271/06C07D295/096C07D295/13C07D295/185C07D307/68C07D307/81C07D311/58C07D317/60C07D319/20C07D333/24C07D333/28C07D333/38C07D335/16C07D405/04C07D405/12C07D413/04C07D413/12C07C219/28C07C2602/10C07C2602/12
Inventor KATO, KANEYOSHITERAUCHI, JUNMORI, MASAAKISUZUKI, NOBUHIROSHIMOMURA, YUKIOTAKEKAWA, SHIROISHIHARA, YUJI
Owner KATO KANEYOSHI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com