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Pharmaceutical composition for treating hyperplasia diseases

A technology for proliferative diseases and compositions, applied in the field of pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof combined with an anti-proliferative agent, capable of solving problems such as no tumor growth

Active Publication Date: 2010-03-24
JIANGSU HENGRUI MEDICINE CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are three main mechanisms that play an important role in the activity of anti-tumor angiogenesis inhibitors: 1. Inhibition of the growth of blood vessels, especially capillaries, so that ultimately there is no pure tumor growth due to a balance between cell death and proliferation
2. The lack of blood flow into and out of the tumor prevents the migration of tumor cells

Method used

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  • Pharmaceutical composition for treating hyperplasia diseases
  • Pharmaceutical composition for treating hyperplasia diseases
  • Pharmaceutical composition for treating hyperplasia diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0087] Embodiment 1: preparation compound A (the mesylate of formula I compound)

[0088] In a 5L reaction flask, put 170g (0.428mol) of the compound of formula I, 42.5g (0.442mol) of methanesulfonic acid, 2.55L of 95% isopropanol aqueous solution, stir and heat under nitrogen protection and light-shielding conditions until completely dissolved, to obtain The light yellow transparent solution was filtered while it was hot, cooled and crystallized to room temperature, filtered, washed with isopropanol, and dried in vacuum to obtain 180.2 g (0.365 mol) of white needle-like crystals, with a yield of 85.4%.

[0089]In a 5L reaction flask, put 180.2g of compound A, 2.52L of 95% isopropanol aqueous solution, stir and heat until completely dissolved under nitrogen protection and dark conditions, filter while hot, and cool the filtrate to room temperature for crystallization, filter, isopropanol Wash and dry in vacuo to obtain 161.5 g of white needle-like crystals, with a yield of 89...

Embodiment 2

[0090] Embodiment 2: Compound A is used alone or combined with oxaliplatin for the treatment of human colon cancer Ls174t nude mouse transplanted tumor effect

[0091] Explanation: Compound A is the methanesulfonate of the compound of formula I, the same below.

[0092] 1. Experimental animals:

[0093] BALB / cA-nude nude mice, ♀, 5-6 weeks old, were purchased from Shanghai Slack Experimental Animal Co., Ltd. Certificate number: SCXK (Shanghai) 2004-0005. Breeding environment: SPF grade.

[0094] 2. Experimental steps:

[0095] After 1 week of adaptation, the animals were subcutaneously inoculated with human colon cancer Ls174t tumor tissue until the tumor grew to 150-300mm 3 Afterwards, the animals were randomly divided into groups (d0) for administration. Compound A and PTK787 are both 75mg / kg, administered orally (gavage), d0-d13, once a day, a total of 14 times; oxaliplatin 6mg / kg, intravenous injection, d0, d4, d8, a total of 3 times . When used in combination, ...

Embodiment 3

[0102] Embodiment 3: The curative effect of compound A alone or combined with 5-Fu on human colon cancer Ls174t nude mice xenografts

[0103] 1. Experimental animals:

[0104] BALB / cA-nude nude mice, ♀, 5-6 weeks old, were purchased from Shanghai Slack Experimental Animal Co., Ltd. Certificate number: SCXK (Shanghai) 2004-0005. Breeding environment: SPF grade.

[0105] 2. Experimental steps:

[0106] After 1 week of adaptation, the animals were subcutaneously inoculated with human colon cancer Ls174t tumor tissue until the tumor grew to 150-300mm 3 Afterwards, the animals were randomly divided into groups (d0) for administration. Both compound A and PTK787 were given 75 mg / kg orally (gavage), d0-d13, once a day, 14 times in total; 5-Fu 50 mg / kg, intraperitoneally injected, d0, d4, d8, 3 times in total. When used in combination, compound A and PTK787 were used in combination with 5-Fu respectively, and the dosage and regimen remained unchanged. The tumor volume was meas...

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Abstract

The invention relates to a pharmaceutical composition for treating hyperplasia diseases such as tumors, Which contains a compound of a formula I or its pharmaceutically acceptable salts, and at leastan antiproliferative agent. The pharmaceutical composition has a cooperative synergism.

Description

technical field [0001] The present invention relates to proliferative diseases, especially tumor treatment methods and pharmaceutical compositions thereof, in particular to a pharmaceutical composition containing a compound of formula I or a pharmaceutically acceptable salt thereof and an antiproliferative agent. Background technique [0002] The National Cancer Institute estimates that in the United States alone, one in three people will experience cancer during their lifetime. About 50% to 60% of people who develop cancer will die from the disease. The widespread occurrence of this disease presents an urgent need for improved treatment options for tumors, especially malignant tumors. [0003] A variety of cancers have been discovered so far, and many anticancer agents have been developed correspondingly to eliminate cancers in the body. According to their mechanism of action, they are classified as follows: [0004] One type of chemotherapeutic agent is known as a metal...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/444A61P35/00
CPCA61K31/282C07D213/81A61K31/513A61K31/704A61K31/444A61K31/337A61P35/00
Inventor 袁开红孙飘扬
Owner JIANGSU HENGRUI MEDICINE CO LTD
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