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Dipeptidase-IV inhibitor derivates

A technology for drugs and compounds, applied in the field of medicine, can solve the problems of inability to meet clinical needs, limited varieties of DPP-IV inhibitors, etc.

Active Publication Date: 2009-04-01
BEIJING AOHE DRUG RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The variety of DPP-IV inhibitors is limited and cannot meet the clinical needs, and there is an urgent need to develop more DPP-IV inhibitor drugs to meet the clinical needs

Method used

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  • Dipeptidase-IV inhibitor derivates
  • Dipeptidase-IV inhibitor derivates
  • Dipeptidase-IV inhibitor derivates

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0134] Example 1 7-[2-[N-(2,4,5-trifluorobenzyl)-N-((1,1-Metguanidine-3-yl)iminomethyl)aminoacetyl ]-3-(three Preparation of fluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazol[4,3-a]pyrazine

[0135] Step 1 7-(2-Chloro-acetyl)-3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazol[4,3-a]pyridine Preparation of oxazine

[0136] In a dry reaction flask, add 9.6g (50mmol) 3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a] Pyrazine (see J.Med.Chem.2005, 48, 141-151 for its preparation method), 100ml of DMF, after slightly heating and stirring to dissolve, lower to -5~0°C, slowly add 6.8g (60mmol) of chloroacetyl chloride dropwise Dichloromethane solution 100ml, dropwise, keep warm for 5h. Then warmed to room temperature and stirred for 0.5h. 100ml of water was added to the reaction solution, and the pH was slowly adjusted to 9 with 5% sodium bicarbonate solution under an ice-water bath. The organic layer was separated, and the aqueous layer was extracted with 50ml×...

Embodiment 2

[0146] Embodiment 2 The preparation of compound tablet of the present invention

[0147] 1. Prescription:

[0148]

[0149] 2. Preparation process: crush the raw materials through a 100-mesh sieve, pass the rest of the auxiliary materials through a 100-mesh sieve, and set aside; weigh the raw materials and auxiliary materials according to the prescription; mix compound 1, microcrystalline cellulose and hydroxypropyl cellulose evenly, add Add an appropriate amount of water to the mixing granulator, stir and granulate; dry the wet granules at a temperature lower than 60°C; add micropowder silica gel and magnesium stearate to the dried granules; take samples and test semi-finished products; The determined tablet weight is pressed; the finished product is fully inspected, packed and put into storage.

Embodiment 3

[0150] Embodiment 3 Preparation of compound capsules of the present invention

[0151] 1. Prescription:

[0152]

[0153] 2. Preparation process: crush the raw materials through a 100-mesh sieve, pass the rest of the auxiliary materials through a 100-mesh sieve respectively, and set aside; weigh the raw materials and auxiliary materials according to the prescription; mix compound 1, microcrystalline cellulose and starch evenly, and add them to the mixing granulator Add appropriate amount of water, stir and granulate; dry the wet granules at a temperature lower than 60°C; add micro-powder silica gel and magnesium stearate to the dried granules; take samples and test the semi-finished products; determine the loading according to the test; Capsule loading, full inspection of finished products, packaging and storage.

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Abstract

The invention belongs to the medical technology field, more particularly relates to a dipeptidase-IV depressor derivative as shown in the formula (I), salt thereof acceptable in pharmacy, or isomers thereof; wherein, Ar, X, Y, Z, R<1>, R<2> and R<3> are defined in the specification; the invention also relates to the preparation method of the compounds, the medicine combination containing the compounds and the application of the compounds for preparing medicines used for treating and / or preventing diabetes, non-insulin-dependent diabetes, high blood-sugar and insulin resistance.

Description

1. Technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to compounds of dipeptidase-IV (DPP-IV) inhibitors, pharmaceutically acceptable salts and isomers thereof, methods for preparing these compounds, and pharmaceutical compositions containing these compounds , and the application of these compounds in the preparation of medicines for treating and / or preventing diabetes, non-insulin-dependent diabetes, hyperglycemia and insulin resistance. 2. Background technology [0002] Diabetes is a systemic chronic metabolic disease caused by uncontrolled blood sugar levels higher than normal. Basically divided into four categories, including: type I (insulin-dependent), type II (non-insulin-dependent), other types and gestational diabetes. Type 1 and type 2 diabetes belong to primary diabetes, the two most common forms, caused by the interaction of genetic and environmental factors. The etiology of diabetes is very complicated, b...

Claims

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Application Information

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IPC IPC(8): C07D487/04A61K31/4985A61P3/10
Inventor 黄振华赵红宇
Owner BEIJING AOHE DRUG RES INST
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