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Compound for treating bone marrow injury caused by radiotherapy and chemotherapy

A compound and composition technology, applied in the field of medicine, can solve problems such as short validity period, lack of hematopoietic reconstruction drugs, inconvenient storage, etc., and achieve the effect of convenient administration

Inactive Publication Date: 2016-02-17
JILIN HAIGELISI MEDICAL BIOTECH DEVCO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 2. Clinical lack of drugs to promote hematopoietic reconstruction after hematopoietic stem cell transplantation
[0006] 3. At present, there is a lack of effective drugs for the prevention and treatment of nuclear radiation bone marrow injury
[0007] Although nuclear radiation damage is not common in peaceful times, radiation accidents related to nuclear accidents internationally and domestically are not uncommon, and once they occur, the consequences are serious, especially the infection caused by severe anemia, hemorrhage and abnormal decrease in white blood cells caused by radiation-related bone marrow damage
[0008] 4. Lack of effective drugs for the treatment of bone marrow failure diseases
These protein or polypeptide drugs are prone to produce antibodies, and are inconvenient to store. They need to be stored at low temperature and have a short validity period.

Method used

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  • Compound for treating bone marrow injury caused by radiotherapy and chemotherapy
  • Compound for treating bone marrow injury caused by radiotherapy and chemotherapy
  • Compound for treating bone marrow injury caused by radiotherapy and chemotherapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] 1. Synthesis of metformin free base:

[0049] Get 12 grams of metformin hydrochloride, place it in a 250ml round bottom flask, add 1MNaOH80ml, stir at room temperature for 3 hours, detect through TLC (thin layer chromatography), when DCM:MeOH=5:1, the rf value is about 0.4, after Place a 250ml round bottom flask in a rotary evaporator, distill under reduced pressure at 60°C, the pressure is 0.09MPa, distill off the water, then add 100ml of methanol, evaporate to dryness, then add 50ml of methanol, filter through a Buchner funnel, and NaCl generated in the reaction solution was filtered off, and the filtrate was evaporated to dryness to obtain metformin free base.

[0050] 2, the synthesis of metformin mesylate

[0051] Put 9.3 grams of metformin free base in a 250ml round-bottomed flask, add 100ml of ethanol and 8ml of methanesulfonic acid, stir for 3 hours at 80°C, condense, then place in a rotary evaporator, and distill under reduced pressure at 60°C. Ethanol was di...

Embodiment 2

[0058] 1. Synthesis of metformin free base:

[0059] Get 11 grams of metformin hydrochloride, place it in a 250ml round-bottomed flask, add 1M potassium hydroxide 80ml, stir at room temperature for 2 hours, detect through TLC (thin layer chromatography), when DCM:MeOH=5:1, rf value is in After about 0.4, put the 250ml round-bottomed flask in a rotary evaporator, distill under reduced pressure at 55°C, the pressure is 0.09MPa, evaporate the water, add 100ml of ethanol, evaporate to dryness, add 50ml of ethanol, and pass through the Buchner funnel Suction filtration, the potassium chloride generated in the reaction solution was filtered off, and the filtrate was evaporated to dryness to obtain metformin free base.

[0060] 2, the synthesis of metformin mesylate

[0061] Put 8.3 grams of metformin free base in a 250ml round-bottomed flask, add 100ml of ethanol and 8ml of methanesulfonic acid, stir for 4 hours at 75°C, condense, then place in a rotary evaporator, and distill unde...

Embodiment 3

[0068] 1. Synthesis of metformin free base:

[0069] Get 11 grams of metformin hydrochloride, place it in a 250ml round bottom flask, add 1M barium hydroxide 80ml, stir at room temperature for 4 hours, detect through TLC (thin layer chromatography), when DCM:MeOH=5:1, rf value is in After about 0.4, put the 250ml round-bottomed flask in a rotary evaporator, distill under reduced pressure at 65°C, the pressure is 0.09MPa, evaporate the water, then add 100ml of ethanol, evaporate to dryness, then add 50ml of ethanol, and pass through the Buchner funnel Suction filtration, the barium chloride generated in the reaction solution was filtered off, and the filtrate was evaporated to dryness to obtain metformin free base.

[0070] 2, the synthesis of metformin mesylate

[0071] Put 8.3 grams of metformin free base in a 250ml round-bottomed flask, add 100ml of ethanol and 8ml of methanesulfonic acid, stir for 2 hours at 85°C, condense, then place in a rotary evaporator, and distill un...

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Abstract

The present invention provides a compound represented by a formula I, a preparation method of the compound, a pharmaceutical composition containing the compound, and uses of the drug in treatment of bone marrow injury caused by radiotherapy and chemotherapy, and assisted treatment of aplastic anemia. The formula I is defined in the specification.

Description

technical field [0001] The invention belongs to the field of medicine. Specifically, the present invention relates to a novel compound for preventing and treating bone marrow injury caused by radiotherapy and chemotherapy, a preparation method of the compound, a pharmaceutical composition containing the compound, and the compound And the use of the pharmaceutical composition in the preparation of drugs for preventing and treating bone marrow damage caused by radiotherapy and chemotherapy. Background technique [0002] 1. There is a lack of prevention and treatment drugs for myelosuppression related to malignant tumors after radiotherapy and chemotherapy [0003] According to incomplete statistics, the number of new malignant tumor patients is about 3 million every year, and radiotherapy and chemotherapy are still the most common methods for treating tumors. However, it is well known that radiotherapy and chemotherapy lead to myelosuppression, which leads to severe anemia, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C309/04C07C279/26C07C277/08C07C303/32A61P7/00A61P7/06
CPCC07C309/04C07C277/08C07C279/26C07C303/32
Inventor 卢学春
Owner JILIN HAIGELISI MEDICAL BIOTECH DEVCO LTD
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