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Substituted purinyl derivatives with immunomodulator and chemoprotective activity and use alone or with medium-chain length fatty acids or glycerides

A technology of use and medicine, applied in the direction of organic active ingredients, medical preparations containing active ingredients, antidote, etc.

Inactive Publication Date: 2007-11-28
PROMETIC BIOSCIENCES LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, none of the growth factors or compounds mentioned above can "chemoprotect" the patient while simultaneously stimulating the patient's own subset of immune cells that most effectively exhibit anticancer activity: cytotoxic T lymphocytes (CTLs)

Method used

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  • Substituted purinyl derivatives with immunomodulator and chemoprotective activity and use alone or with medium-chain length fatty acids or glycerides
  • Substituted purinyl derivatives with immunomodulator and chemoprotective activity and use alone or with medium-chain length fatty acids or glycerides
  • Substituted purinyl derivatives with immunomodulator and chemoprotective activity and use alone or with medium-chain length fatty acids or glycerides

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Example 1 Study on chemical protection: the protection of compound I on hematopoietic cells in vivo.

[0057] Female C57BL / 6 mice aged 6 to 8 weeks were treated with 200 mg / kg cyclophosphamide (CY), administered intravenously on day 0 to cause immunosuppression. To examine the chemoprotective effect of compound I, mice were previously injected intraperitoneally with 50 mg / kg of the compound on days -3, -2 and -1. Mice were sacrificed on day +5 by cardiac exsanguination and vertebral dissection. Afterwards, cells were obtained from thymus, spleen and bone marrow to prepare cell suspensions as follows.

[0058] Triturate the tissue in PBS buffer, contaminating red blood cells in ACK buffer (155mM NH 4 Cl, 12mM NaHCO 3 , 0.1 mM EDTA, pH 7.3) dissolved for five minutes. Cells were then harvested by centrifugation, washed three times in PBS, and resuspended in tissue culture medium. Count the cells with a counter.

[0059] After prior administration of Compound I to CY...

Embodiment 2

[0061] Example 2 Study on chemical protection: Combined use of sodium caprate and compound I induces proliferation or protection of immune cells in vivo.

[0062] According to the protocol described in Example 1, the effect of sodium caprate, compound I, and the combination of the two compounds in inducing proliferation or protection of hematopoietic cells in vivo was determined. On days -3, -2 and -1, sodium caprate was administered orally (60.5 mM) and / or compound I was administered intraperitoneally (50 mg / kg). Treated animals compared to their respective control groups: CY+sodium caprate versus CY-PO (CY+PBS per well); CY+compound I versus CY-IP (CY+PBS intraperitoneal injection); CY+caprate Sodium + Compound I compared to CY-POIP (CY + PBS per well and PBS ip injection).

[0063] Accompanying drawing 1 shows the influence of sodium caprate, compound I and two kinds of compounds combination on peripheral red blood cell count. CY-treated mice pre-treated with sodium capra...

Embodiment 3

[0065] Example 3 Study on chemical protection: combined use of tricaprin and compound I induces proliferation or protection of immune cells in vivo.

[0066] According to the protocol described in Example 1, the effects of tricaprin, compound I and the combination of the two compounds in inducing proliferation or protection of hematopoietic cells in vivo were determined. Tricaprin (60.5 mM) was administered orally and / or compound I was injected intraperitoneally on days -3, -2 and -1.

[0067] Table 2 shows the effects of tricaprin, compound I and the combination of the two compounds on bone marrow erythrocyte count. A significant increase in bone marrow erythrocytes was obtained when CY-treated mice were previously treated with the combination of tricaprate and compound I. This is a synergistic effect compared with CY alone. Furthermore, the number of CFU-GEMM cells in bone marrow was significantly increased (3-fold) in mice treated with tricaprate and Compound I (Table 3)....

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Abstract

The present invention describes new biological activities of immunomodulating 6-substituted purinyl compounds which make them particularly useful during the treatment of cancer. Collectively, these new biological activities make these purinyl compounds useful chemoprotective agents for the treatment of myelosuppression which is associated with cancer chemotherapy and / or radiotherapy. This chemoprotective activity is in addition to the immunomodulating and subsequent anticancer activity displayed by these compounds, the chemoprotective usefulness of these compounds is further enhanced by the use of medium-chain fatty acids or salts or triglycerides or mono- or diglycerides in combination with the 6-substituted purinyl compounds of this invention.

Description

[0001] Cross-citations to related applications [0002] This application claims to protect the scope of rights of US Provisional Application No. 60 / 606,915 filed on September 3, 2004; the relevant content is hereby incorporated by reference. technical field [0003] The present invention describes novel biological activities of immunomodulatory 6-substituted purinyl compounds which make them particularly useful in the treatment of cancer. Collectively, the novel biological activities make these purine-based compounds useful chemoprotectants for the treatment of myelosuppression associated with cancer chemotherapy and / or radiation therapy. This chemoprotective activity is in addition to the immunomodulatory and consequential anticancer activity exhibited by these compounds. When the 6-substituted purine compound of the present invention is combined with medium chain fatty acid or salt or triglyceride or monoglyceride or diglyceride, its chemical protection effect will be furth...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/52A61P35/00A61P39/00A61K31/20A61K31/23A61K31/417
CPCA61K31/23A61K31/20A61K31/417A61K31/52A61P35/00A61P39/00A61P7/00A61P7/06A61K2300/00
Inventor 克里斯托弗·彭尼布洛斯·扎沙里耶琼·巴拉贝皮埃尔·劳林莱恩·加尼翁
Owner PROMETIC BIOSCIENCES LTD
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