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Pyrimidopyrimidine type derivative as well as preparation method and application thereof to medicines

A technology of pyrimidine and derivatives, applied in the field of chemical drugs, can solve problems such as fluid retention, weight gain, and decreased β-cell function

Inactive Publication Date: 2019-05-17
江西乐成生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, these drugs have certain side effects, such as: hypoglycemia, weight gain, decreased β-cell function, fluid retention and gastrointestinal side effects, etc.

Method used

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  • Pyrimidopyrimidine type derivative as well as preparation method and application thereof to medicines
  • Pyrimidopyrimidine type derivative as well as preparation method and application thereof to medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] 2,6,8-Trichloro-N-(4-thiamphenyl)phenyl)pyrimido[5,4- d ]pyrimidin-4-amine;

[0030] Add tetrachloropyrimido[5,4- d ]pyrimidine (0.65 g, 2.4 mmol), THF (5 mL) and H 2 O (0.6 mL). 4-Methylthioaniline (0.1 mL, 0.8 mmol) was added at 0 °C and the reaction was stirred at room temperature for 1 h. Join CH 2 Cl 2 (10 mL), mCPBA (0.36 g, 77%, 1.6 mmol) was added at 0°C, and the reaction was stirred overnight at room temperature. CH 2 Cl 2 Diluted, the organic phase was washed with saturated sodium thiosulfate solution, saturated sodium bicarbonate solution and saturated brine, dried over anhydrous sodium sulfate, and the solvent was removed by rotary evaporation, and the crude product was subjected to silica gel column chromatography (petroleum ether: ethyl acetate=5: 1) Purification gave a yellow solid, and the yield of the two-step reaction was 32%. 1 H-NMR (600 MHz, CDCl 3 ) δ (ppm): 9.12 (s, 1H), 8.20-8.00 (m, 4H), 3.10 (s, 3H).

Embodiment 2

[0032] 2,6,8-Trichloro-N-(2-fluoro-4-thiamphenicol)phenyl)pyrimido[5,4- d ]pyrimidin-4-amine;

[0033] Referring to the preparation method of Example 1. 1 H-NMR (600 MHz, CDCl 3 ) δ (ppm): 9.37 (s, 1H), 8.99(t, J = 8.5 Hz, 1H), 7.95-7.80 (m, 2H), 3.13 (s, 3H).

Embodiment 3

[0035] 2,6,8-Trichloro-N-(2-fluoro-4-cyano)phenyl)pyrimido[5,4- d ]pyrimidin-4-amine;

[0036] Referring to the preparation method of Example 1. 1 H-NMR (600 MHz, CDCl 3 ) δ (ppm): 9.37(s, 1H), 8.94(t, J = 8.3, 1H), 7.66(d, J = 8.6, 1H), 7.58(dd, J = 10.4, 1.7, 1H).

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Abstract

The invention provides a pyrimidopyrimidine type derivative as well as a preparation method and application thereof to medicines. The invention relates to a novel pyrimidopyrimidine type derivative shown as a general formula I, a preparation method thereof and application of a pharmaceutical composition containing the derivative and pharmaceutically acceptable salt, which are used as a treatment agent, especially a GPR119 agonist, and to medicines for treating anti-diabetic and metabolic diseases and preventing diseases including metabolism disorder and obesity.

Description

technical field [0001] The present invention relates to the field of chemical medicine, and more to a novel pyrimidopyrimidine derivative, a preparation method thereof, a pharmaceutical composition containing the derivative and its use as a therapeutic agent, especially as a GPR119 agonist and in the preparation and treatment of anti-diabetic and metabolic Use of drugs for diseases such as sexually transmitted diseases. Background technique [0002] Diabetes is a disease that seriously threatens human health. Due to long-term high blood sugar, diabetes can cause chronic damage and dysfunction of various organs and tissues, especially eyes, kidneys, heart, blood vessels, and nerves. Diabetes can be divided into type 1 diabetes, type 2 diabetes and gestational diabetes according to different causes. Among them, type 2 diabetes accounts for 90% of the affected population, and islet β-cell dysfunction is the main cause of type 2 diabetes. [0003] Modern pharmacological treatm...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04C07D519/00A61P3/10A61P3/04A61P3/00A61P3/06A61P5/50A61P9/10
Inventor 杨尊华房元英刘荣华何明珍王琦李志峰
Owner 江西乐成生物科技有限公司
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