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

Combination therapy for glycaemic control

A technology for blood sugar control and use, which is applied in the therapeutic field of blood sugar control, and can solve the problems of low efficiency, time efficacy, reduction, etc.

Inactive Publication Date: 2006-10-11
PROSIDION LIMITED
View PDF31 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Many of the existing treatments for type 2 diabetes that have not changed substantially over the years have limitations, for example they may have undesired side effects, be ineffective or decrease in efficacy over time in long-term treatment

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
  • Combination therapy for glycaemic control
  • Combination therapy for glycaemic control
  • Combination therapy for glycaemic control

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 12

[0088] - No activity against non-DP IV and non-DP IV-like enzymes, such as DP I, prolyl oligopeptidase, aminoacyl proline dipeptidase (see Example 12);

[0089] - high stability in vitro in isolated human plasma (see Example 13);

[0090] - a novel and controllable mechanism for the partial inactivation / metabolism of glutamine to the corresponding pyroglutamyl compound in vivo, resulting in a shorter half-life than other DP IV inhibitors (see Example 8); and

[0091] - Predicted in vivo liver-independent half-life.

[0092] Pharmaceutically acceptable salts of compounds of formula (I) include acid addition salts, ie wherein the basic side chain of the amino acid is protonated with an inorganic or organic acid. Representative organic or inorganic acids include hydrochloric, hydrobromic, perchloric, sulfuric, nitric, phosphoric, acetic, propionic, glycolic, lactic, succinic, maleic, fumaric, malic, tartaric, Citric acid, benzoic acid, mandelic acid, methanesulfonic acid, iseth...

Embodiment 1

[0178] Embodiment 1: the synthesis of glutaminyl pyrrolidine free base

[0179] N-Benzyloxycarbonylglutamine (2.02 g, 7.21 mmol) was dissolved in 35 mL THF and cooled to -15°C. CAIBE (isobutyl chloroformate) (0.937 mL, 7.21 mmol) and 4-methylmorpholine (0.795 mL, 7.21 mmol) were added and the solution was stirred for 15 minutes. The formed mixed anhydride was detected by TLC (eluent: chloroform / methanol: 9 / 1). After warming to -10°C, pyrrolidine (0.596 mL, 7.21 mmol) was added. The mixture was brought to room temperature and stirred overnight. The precipitate formed was filtered off and the solvent was evaporated. The resulting oil was taken up in ethyl acetate (20 mL) and washed with saturated sodium bisulfate solution followed by saturated sodium bicarbonate solution, water and brine. The organic layer was separated, dried and evaporated. The purity of the obtained product was checked by TLC (eluent: chloroform / methanol: 9 / 1). Yield: 1.18 g. This product was dissolved...

Embodiment 2

[0180] Embodiment 2: the synthesis of glutamyl thiazolidine hydrochloride

[0181] N-tert-butoxycarbonylglutamine (2.0 g, 8.12 mmol) was dissolved in THF (5 mL), cooled to -15°C. CAIBE (isobutyl chloroformate) (1.06 mL, 8.12 mmol) and 4-methylmorpholine (0.895 mL, 8.12 mmol) were added and the solution was stirred for 15 minutes. The formed mixed anhydride was detected by TLC (eluent: chloroform / methanol: 9 / 1). After warming to -10°C, another equivalent of 4-methylmorpholine (0.895 mL, 8.12 mmol) and thiazolidine hydrochloride (1.02 g, 8.12 mmol) were added. The mixture was brought to room temperature and stirred overnight. The precipitate formed was filtered off and the solvent was evaporated. The resulting oil was taken up in chloroform (20 mL) and washed with saturated sodium bisulfate solution followed by saturated sodium bicarbonate solution, water and brine. The organic layer was separated, dried and evaporated. The purity of the obtained product was checked by TLC ...

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 method of treatment, in particular to a method for the treatment of diabetes mellitus, especiall non-insulin dependent diabetes mellitus (NIDDM) or Type 2 diabetes and conditions associat d with diabetes mellitus the predi,tbetic state and / or obesity and to compositions for use in s ch method.

Description

technical field [0001] The present invention relates to treatment for glycemic control, in particular to methods for the treatment of diabetes, especially non-insulin-dependent diabetes mellitus (NIDDM) or type 2 diabetes and diabetes-related conditions, prediabetic states and / or obesity, and to methods for such methods Compositions. Background technique [0002] Glycemic control is of therapeutic importance in the treatment of conditions such as diabetes and related disorders. Clinical diabetes can be divided into four basic subtypes, including (1) type 1 or insulin-dependent diabetes mellitus (IDDM) (resulting from beta-cell destruction and characterized by absolute insulin deficiency), (2) type 2 or non-insulin-dependent (NIDDM) (characterized by insulin resistance and relative insulin deficiency), (3) other specific types of diabetes (associated with various identifiable clinical conditions or syndromes such as genetic defects in β-cell function and mitochondrial DNA po...

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): A61K31/40A61K31/426A61K45/06A61P3/10
CPCA61K45/06A61K31/401A61K31/426A61K31/40A61P3/04A61P3/06A61P43/00A61P3/10A61K2300/00
Inventor 汉斯-乌尔里希·德穆特康拉德·格隆德马蒂亚斯·霍夫曼
Owner PROSIDION LIMITED
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