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Treatment agent for inflammatory bowel disease

A technology for inflammatory bowel disease and treatment agent, which can be used in anti-inflammatory agents, allergic diseases, non-central analgesics, etc., and can solve problems such as unknown antecedent drugs.

Inactive Publication Date: 2009-07-08
ASKA PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, the currently known drugs as prodrugs are mainly steroid compounds for external use, and the prodrugs as p38MAP kinase inhibitors are completely unknown
There are also no examples of prodrugs being used to manage IBD

Method used

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  • Treatment agent for inflammatory bowel disease
  • Treatment agent for inflammatory bowel disease
  • Treatment agent for inflammatory bowel disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0213] Example 1: Formulation example of tablet

[0214]

[0215] The active ingredient is pulverized to a particle size of 70 μm or less, starch, lactose and carboxymethylcellulose calcium are added thereto, and thoroughly mixed. Add 10% starch slurry into the above mixed powder and stir and mix to prepare granules. After drying, adjust the particle size to about 1000 μm, mix talc powder and magnesium stearate therein, and press into tablets.

preparation example 1

[0217] 3-(4-fluorophenyl)-5-(phenylacetylamino)-4-(4-pyrimidinyl)isoxazole

[0218] a: Synthesis of dimethyl-[(E)-2-(4-pyrimidinyl)vinyl]amine

[0219] A mixture of 10 g of 4-methylpyrimidine and 38 g of N,N-dimethylformamide dimethyl acetal (DMFDMA) and 46.6 g of DMF was stirred at 140° C. for 24 hours in a sealed tube. After cooling the reaction solution, the solvent was distilled off under reduced pressure to obtain 15.08 g of the title compound as brown crystals (95% yield).

[0220] 1 H-NMR (CDCl 3 )δ: 8.73 (bs, 1H), 8.22 (d, J=5.5Hz, 1H), 7.77 (d, J=12.9Hz, 1H), 6.72 (dd, J=5.5Hz, 12.9Hz, 1H), 5.00 (d, J=12.9Hz, 1H), 2.96(s, 6H)

[0221] b: Synthesis of 4-pyrimidinylacetonitrile

[0222] 9.48 g of hydroxylamine-O-sulfonic acids were added to 70 mL of aqueous solutions of 5 g of dimethyl-[(E)-2-(4-pyrimidinyl)vinyl]amine, and it stirred at 50 degreeC for 30 minutes. Under ice-cooling, saturated aqueous sodium bicarbonate solution was added to make the reaction s...

preparation example 2

[0233] 5-[(2-Chlorophenyl)acetylamino]-3-(4-fluorophenyl)-4-(4-pyrimidinyl)isoxazole (Compound number: B-1)

[0234] Using 2-chlorophenylacetyl chloride instead of phenylacetyl chloride, the title compound was synthesized in the same manner as in Preparation 1-d.

[0235] 1 H-NMR (CDCl 3 )δ: 11.45(bs, 1H), 8.54(s, 1H), 8.38(d, J=5.7Hz, 1H), 7.55~7.38(m, 6H), 7.20(t, J=8.7Hz, 2H), 6.75(dd, J=1.3Hz, 5.7Hz, 1H), 4.06(s, 2H)

[0236] Mass spectrum, m / e: 408 (M + ), 240 (base peak)

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PUM

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Abstract

A treatment agent for inflammatory bowel disease containing, as an active ingredient, a p38 MAP kinase inhibitor having a property as an antedrug is disclosed.

Description

technical field [0001] The present invention relates to a treatment agent for inflammatory bowel disease characterized by containing a p38MAP kinase inhibitor having properties as an antedrug as an active ingredient. Background technique [0002] Inflammation is a biological response that can be seen when certain damaging factors are applied to biological tissue. Rather than a direct response to tissue damage, it can be understood as a response to chemical mediators of inflammation caused by tissue damage. Such chemical mediators are known, for example, tumor necrosis factor-α (hereinafter referred to as "TNF-α"), interleukin (hereinafter referred to as "IL"), cyclooxygenase (hereinafter referred to as "COX"), prostate Factors such as thromboxane, leukotrienes, etc. [0003] On the other hand, the role of p38MAP kinase in the inflammatory response has been clarified in recent years. TNF-α, IL-1, IL-6, IL-8, COX-II and other cytokines or proteins share with the DNA encoding...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/4439A61K31/444A61K31/506A61P1/00A61P1/04A61P11/00A61P11/02A61P11/06A61P17/00A61P19/02A61P29/00A61P37/08A61P43/00C07D401/04C07D401/14C07D413/04
CPCC07D401/14C07D413/04A61K31/4439A61K31/506A61K31/444C07D401/04A61P1/00A61P1/04A61P11/00A61P11/02A61P11/06A61P17/00A61P19/02A61P29/00A61P37/08A61P43/00
Inventor 莲见幸市太田修治斋藤教久佐藤秀一郎加藤淳也佐藤润铃木弘幸浅野创冈田真美松本康浩代田和彦
Owner ASKA PHARMACEUTICAL CO LTD