Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Novel MCH receptor antagonists

A CH2, enantiomer technology, used in the medical field, can solve problems such as unproven patient efficacy and long-term efficacy

Inactive Publication Date: 2006-01-25
ELI LILLY & CO
View PDF24 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These drugs have not been shown to be effective and effective for long periods of time in all patients

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
  • Novel MCH receptor antagonists
  • Novel MCH receptor antagonists
  • Novel MCH receptor antagonists

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment

[0395] Preparation 1

[0396] tablet

[0397] Ingredient Quantity (mg / tablet)

[0398] Active ingredient 5-500

[0399] Microcrystalline cellulose 200-650

[0400] Fumed silica 10-650

[0401] Stearic acid 5-15

[0402] The ingredients are blended and compressed into tablets.

[0403] Preparation 2

[0404] Suspension

[0405] Component Quantity (mg / 5ml)

[0406] Active ingredient 5-500mg

[0407] Sodium Carboxymethyl Cellulose 50mg

[0408] Syrup 1.25mg

[0409] Benzoic acid solution 0.10mL

[0410] Flavoring q.v.

[0411] pigment q.v.

[0412] Purified water, to 5mL

[0413] The active ingredient is passed through a No. 45 mesh U.S. sieve (approximately 355 micron openings) and mixed with the sodium carboxymethylcellulose and syrup to form a homogeneous paste. The benzoic acid solution, flavor and color are diluted with some of the water and added with stirring. Sufficient water is then added to achieve the desired volume.

[0414] Preparation 3

[04...

Embodiment 1

[0473] Preparation of 4'(2-phenoxy-ethylthiomethyl)-biphenyl-3-carboxylic acid (3-dimethylamino-propyl)-amide oxalate

[0474]

[0475] A solution of 4'-(2-phenoxy-ethylthiomethyl)-biphenyl-3-carboxylic acid (0.91 g, 2.5 mmol, 1 eq.) in anhydrous THF (10 mL) was treated with 1,1'-carbonyl di Imidazole (0.41 g, 2.55 mmol, 1.02 eq.) was treated and the resulting solution was heated to 60° C. for 25 minutes. The solution was then allowed to cool and 3-(dimethylamino)propylamine (0.31 g, 0.38 mL, 3 mmol, 1.2 eq.) was added via syringe. The reaction was stirred at room temperature. After 2 hours, the reaction was diluted with water and extracted 2 x 150 mL with EtOAc. The combined organic layers were washed with MgSO 4 Dry, filter, and remove the solvent in vacuo to leave 4'-(2-phenoxy-ethylthiomethyl)-biphenyl-3-carboxylic acid (3-dimethylamino-propyl)-amide (0.97 g , 87% yield), as a yellow oil. 4'-(2-Phenoxy-ethylthiomethyl)-biphenyl-3-carboxylic acid (3-dimethylamino-pr...

Embodiment 2

[0478] Preparation of 4'-(2-phenoxy-ethylthiomethyl)-biphenyl-3-carboxylic acid (2-dimethylamino-ethyl)-amide oxalate

[0479]

[0480] Prepared in the same manner as described in Example 1. A solution of 4'-(2-phenoxy-ethylthiomethyl)-biphenyl-3-carboxylic acid (0.68 g, 1.87 mmol, 1 eq.) was treated with 1,1'-carbonyldiimidazole (0.31 g , 1.91 mmol, 1.02 eq.) was treated and heated. The reaction was allowed to cool then treated with N',N-dimethylethylenediamine (0.20 g, 2.24 mmol, 1.2 eq.). The reaction was worked up as described in Example 1 to afford 4'-(2-phenoxy-ethylthiomethyl)-biphenyl-3-carboxylic acid (2-dimethylamino-ethyl)-amide (0.76 g, 94% yield) as a yellowish oil. Conversion of the free base to the oxalate salt as described in Example 1 using 0.20 g of oxalic acid afforded 4'-(2-phenoxy-ethylthiomethyl)-biphenyl-3-carboxylic acid (2-dimethylamino- Ethyl)-amide oxalate (0.5584 g) as a white solid.

[0481] 1 H NMR (DMSO-d6) δ8.89 (br, 1H), 8.14 (s, 1H), ...

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

No PUM Login to View More

Abstract

The present invention relates to a melanin concentrating hormone antagonist compound of Formula I: (I) wherein Ar<1>, Ar<2>, Ar<3>, L<1>, L<2> and Q areas defined, or a pharmaceutically acceptable salt, solvate, enantiomer or mixture of diastereomers thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and Related Diseases.

Description

field of invention [0001] The present invention belongs to the field of medicine, specifically treating obesity and diseases caused or exacerbated by obesity. More specifically, the present invention relates to melanin-enriching hormone antagonists useful for the prevention and / or treatment of obesity and related diseases. Background of the invention [0002] Since the 1990s, the impact of exponential growth in food production, especially in Western countries and Asian economies, has resulted in obesity-inducing dietary patterns. Obesity is defined as being overweight. Excess weight is generally characterized by excess body fat because unused energy is stored as fat in adipose tissue. [0003] Obesity is associated with economic and social costs. Obesity, a growing proportion in most Western societies, is seen as out-of-control eating habits and is often associated with low self-esteem. Also, obese people are more likely to face medical problems related to or exacerbated...

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(China)
IPC IPC(8): C07C323/60A61K31/166A61P3/04
CPCC07C323/60A61P1/04A61P11/00A61P11/06A61P13/08A61P13/10A61P25/24A61P27/02A61P27/06A61P3/04A61P43/00A61P9/00A61P3/10
Inventor J·R·吉利格L·J·海因茨M·D·金尼克Y-S·莱J·M·J·莫林N·J·斯奈德
Owner ELI LILLY & CO
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap 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