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Application of tocotrienol derivative

A technology of use and medicine, applied in the field of use of tocotrienol derivatives, can solve the problems of increasing the risk of secondary bone marrow disease in the later stage

Inactive Publication Date: 2017-05-17
BEIJING WEILANZHIYUAN MEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, G-CSF and GM-CSF can increase the later risk (>2 years after treatment) of secondary myeloid disorders such as leukemia and myelodysplasia

Method used

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  • Application of tocotrienol derivative
  • Application of tocotrienol derivative
  • Application of tocotrienol derivative

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Example 1: (2,8-Dimethyl-2R-((3E,7E)-4,8,12-trimethyltrideca-3,7,11-triene base) sodium salt of chroman-6-yloxy)phosphate (i.e. sodium salt of delta-tocotrienol phosphate, Preparation and confirmation of δ-T3HP

[0063] Structural formula:

[0064]

[0065] Reaction equation:

[0066]

[0067] Step a:

[0068]Take 15g of δ-tocotrienol in a 250ml round bottom flask, add 45ml of toluene to dissolve, then add 6ml of pyridine, stir and cool to 0-5°C. Slowly add 4.5ml of phosphorus oxychloride dropwise. After the dropwise addition, move to room temperature and stir for 3h.

[0069] Step b:

[0070] Afterwards, the above reaction system was cooled to below 0°C, and 60ml of distilled water was slowly added. After the dropwise addition, heated to reflux for 4h.

[0071] stepc:

[0072] Add 100ml each of toluene and distilled water to the above reaction solution, shake well and let stand to separate layers. The organic layer was transferred to a rotary evapor...

Embodiment 2

[0075] Example 2: 2,2-Dimethyl-(2R-(4R,8R,12-trimethyltridecyl)chroman -6-yloxy) disodium phosphate (sodium salt of δ-tocopheryl phosphate, referred to as δ-THP) preparation and confirmation

[0076] Structural formula:

[0077]

[0078] Reaction equation:

[0079]

[0080] Step a:

[0081] Take 15g of δ-tocopherol in a 250ml round bottom flask, add 45ml of toluene to dissolve, then add 6ml of pyridine, stir and cool to 0-5°C. Slowly add 4.5ml of phosphorus oxychloride dropwise. After the dropwise addition, move to room temperature and stir for 3h.

[0082] Step b:

[0083] Afterwards, the above reaction system was cooled to below 0°C, and 60ml of distilled water was slowly added. After the dropwise addition, heated to reflux for 4h.

[0084] stepc:

[0085] Add 100ml each of toluene and distilled water to the above reaction solution, shake well and let stand to separate layers. The organic layer was transferred to a rotary evaporator, and the solvent was rem...

Embodiment 3

[0088] Example 3: Effects of δ-T3HP and δ-THP on the Number of Peripheral Blood Images in Cyclophosphamide Chemotherapy Mice

[0089] 3.1 Materials and methods

[0090] 3.1.1 Main reagents and instruments

[0091] Cyclophosphamide was purchased from Jiangsu Hengrui Pharmaceutical Co., Ltd. MEK-7222K automatic blood cell analyzer and peripheral blood detection diluent were purchased from Nihon Kohden Kogyo Co., Ltd.

[0092] 3.1.2 Experimental animals and grouping

[0093] The experiment used SPF grade C57BL / 6J male mice aged 6-8 weeks, weighing (22.6±0.89) g, purchased from Beijing Huafukang Biotechnology Co., Ltd.

[0094] 3.1.3 Chemotherapy conditions

[0095] Cyclophosphamide is used as a chemotherapy drug: 11.25 mg / ml solution is prepared with 0.9% normal saline before use, and 100 mg / Kg per mouse is administered intraperitoneally in 200 μl.

[0096] 3.1.4 Grouping and administration method

[0097] The experiment consisted of rhG-CSF control group and treatment gr...

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Abstract

The invention relates to application of a compound as shown in the general formula (I) or pharmaceutically acceptable salt in the preparation of medicines for preventing and / or treating cytopenia of patents who will receive, is receiving or has received chemotherapy and drug therapy. In the general formula, R1, R2 and R3 can be the same or different and respectively and independently represent H or C1-C3 alkyl group. In comparison with common clinical drugs (such as G-CSF) for increasing haemocyte count for those who receive chemotherapy, the compound of the invention can remarkably increase hemocyte in those who receive chemotherapy, especially increase leucocyte, in particular the number of neutrophile granulocyte and monocyte. The compound of the invention has a good clinical prospect.

Description

technical field [0001] The present invention relates to a compound of general formula (I) as described and defined herein or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the prevention and / or treatment of cytopenias in subjects who will, are or have been treated with chemotherapeutic drugs use in . Background technique [0002] For the treatment of neoplastic diseases, a large number of chemotherapeutic drugs have been recommended. However, chemotherapeutic drugs are often nonspecific and toxic to normal cells. Chemotherapy drugs often produce various side effects in patients receiving chemotherapy. [0003] Myelosuppression is one of the main side effects of chemotherapy drugs. Clinically, the bone marrow hematopoietic system of patients receiving chemotherapy is extremely vulnerable to damage, specifically manifested as decreased peripheral blood leukocyte count, neutrophil count decrease and / or thrombocytopenia. At present, some c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/661A61P7/00A61P7/06
CPCA61K31/661
Inventor 从玉文李忠堂王军
Owner BEIJING WEILANZHIYUAN MEDICAL TECH CO LTD
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