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Combination drug

A technology of pharmaceutical preparation and action, applied in the directions of pharmaceutical combination, pharmaceutical formulation, active ingredient of heterocyclic compounds, etc., can solve the problem of no report describing the concentration of GLP'2, etc.

Inactive Publication Date: 2005-11-23
EISIA R&D MANAGEMENT CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no reports describing an increase in GLP'2 concentrations when metformin is administered or by the combined use of DPPIV inhibitors and metformin to promote the effects of GLP-2.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0883] 4-[1-(2-Butynyl)-6-methyl-7-oxo-6,7-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperazine -1-tert-butyl carboxylate

[0884] (a) tert-butyl 5-methyl-4-oxo-4,5-dihydroimidazo[4,5-d]pyridazine-1-carboxylate

[0885] Will contain 1.0g of 5-methyl-3,5-dihydroimidazo[4,5-d]pyridazin-4-one, 16mg of 4-dimethylaminopyridine, 1.6g of di-tert-butyl dicarbonate A mixture of the ester and 5 ml of tetrahydrofuran was stirred overnight at room temperature. Then, a 0.5-ml tetrahydrofuran solution containing 300 mg of di-tert-butyl dicarbonate was added to the solution, and the resulting mixture was incubated in a room

[0886] Stir at warm temperature for 3 hours. 5 ml of t-butylmethyl ether was added to the reaction mixture, and the mixture was ice-cooled. The resulting crystals were collected by filtration to obtain 1.63 g of the title compound.

[0887] 1 H-NMR (CDCl 3 )δ1.72 (s, 9H) 3.93 (s, 3H) 8.38 (s, 1H) 8.54 (s, 1H)

[0888] (b) 2-Chloro-5-methyl-1,5-dihydroimidazo[4...

preparation Embodiment 2

[0898] tert-butyl 4-[7-(2-butynyl)-2,6-dichloro-7H-purin-8-yl]piperazine-1-carboxylate (a) 7-(2-butynyl)-3-methyl-3,7-dihydropurine-2,6-dione

[0899] Add 55.3ml of 1-bromo-2-butyne and 84.9g of anhydrous potassium carbonate to 100g of 3-methylxanthine [CAS No. 1076-22-8] and 1000ml of N,N-dimethyl in a mixture of formamides. The resulting mixture was stirred at room temperature for 18 hours. 1000 ml of water was added to the reaction solution, and the mixture was stirred at room temperature for 1 hr. The resulting white precipitate was collected by filtration. The white solid was washed with water and then tert-butyl methyl ether. Thus 112 g of the title compound are obtained.

[0900] 1 H-NMR (DMSO-d6) δ1.82 (t, J = 2.2Hz, 3H) 3.34 (s, 3H) 5.06 (q, J = 2.2Hz, 2H) 8.12 (s, 1H) 11.16 (br.s, 1H)

[0901] (b) 7-(2-butynyl)-8-chloro-3-methyl-3,7-dihydropurine-2,6-dione

[0902] 112g of 7-(2-butynyl)-3-methyl-3,7-dihydropurine-2,6-dione was dissolved in 2200ml of N,N...

Embodiment 1

[0912] [7-(2-Chlorophenyl)-1-methyl-6-oxo-8-(piperazin-1-yl)-6,7-dihydro-1H-purin-2-yloxy] Ethyl acetate trifluoroacetate (trifluoroacetate)

[0913] (a) [7-Benzyl-2,6-dioxo-1,2,6,7-tetrahydropurin-3-yl]methyl 2,2-dimethylpropionate

[0914] 8.66 g of 7-benzylxanthine was dissolved in 300 ml of N,N-dimethylformamide, and 1.57 g of sodium hydride and 7.7 ml of chloromethyl pivalate were added thereto. The resulting mixture was stirred overnight at room temperature. The reaction solution was diluted with ethyl acetate, and washed with water and 1N hydrochloric acid. The organic layer was dried over anhydrous magnesium sulfate, and then filtered. The solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography. Thus, 2.66 g of the title compound were obtained from the fraction eluted with hexane-ethyl acetate (1:1).

[0915] 1 H-NMR (CDCl 3 ) δ 1.18 (s, 9H) 5.45 (s, 2H) 6.06 (s, 2H) 7.34-7.39 (m, 5H) 7.58 (s, 1H) 8.18 (s...

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Abstract

The present invention provides pharmaceutical agents comprising a dipeptidyl peptidase IV (DPPIV) inhibitor and a biguanide agent in combination, which enhance the effects of active circulating glucagon-like peptide-1 (GLP-1) and / or active circulating glucagon-like peptide-2 (GLP-2).

Description

technical field [0001] The present invention relates to pharmaceutical formulations comprising dipeptidyl peptidase IV (DPPIV) inhibitors and biguanide agents that enhance active circulating glucagon-like peptide-1 (GLP-1) and / or blood The role of active glucagon-like peptide-2 (GLP-2). Background technique [0002] Glucagon-like peptide-1 (GLP-1) is a hormone known to be secreted by L cells in the lower small intestine in response to food intake. It increases insulin secretion from pancreatic beta cells in a glucose-dependent manner. GLP-1 can be broken down and rapidly inactivated by dipeptidyl peptidase IV (DPPIV). Therefore, DPPIV inhibitors can be used as drugs for the prevention and / or treatment of diseases related to GLP-1 concentration, such as diabetes (especially type II diabetes) and obesity. DPPIV inhibitors have been studied in clinical trials and disclosed in Patent Documents 1, 2 and 3. [0003] Metformin and biguanide agents are usually used as preventive...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/155
Inventor 安田信之山崎一斗
Owner EISIA R&D MANAGEMENT CO LTD
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