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Condensed pyridine compound

A compound, pyridine technology, applied in the directions of active ingredients of heterocyclic compounds, organic chemistry, pharmaceutical combinations, etc., can solve the problems of no implied compounds, no specific disclosed compounds, etc.

Inactive Publication Date: 2009-11-11
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0024] However, in all of the above-mentioned documents, the compound of the present invention is not specifically disclosed, nor is it suggested that the compound of the present invention

Method used

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  • Condensed pyridine compound
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Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0372] Using the corresponding raw materials, according to the Example 6 In the same way, prepare the following table 3 Preparation Examples 1-1 to 1-14 compound of.

preparation example 2

[0374] Using the corresponding raw materials, according to the Example 7 In the same way, prepare the following table 3 Preparation Examples 2-1 to 2-9 compound of.

preparation example 3

[0376] To a mixture of 4,5-dihydro-1H-pyrazole (350 mg) and 4-nitrophenyl chloroformate (1.10 g) in dioxane (3 mL) was added 4M NaHCO at room temperature 3 aqueous solution (3.7 mL), and stirred for 1 hour. After diluting the reaction solution with chloroform, the organic layer was separated and washed with anhydrous MgSO 4 dry. After the white solid was removed by filtration, it was concentrated under reduced pressure to obtain 4-nitrophenyl 4,5-dihydro-1H-pyrazole 1-carboxylate (1.12 g) as a white solid.

[0377] Using the corresponding raw materials, according to the Preparation example 3 In the same way, prepare the following table 3 Preparation Examples 3-1 to 3-7 compound of.

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PUM

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Abstract

The present invention provides a compound having an excellent JAK3-inhibiting activity and useful as an active ingredient for a therapeutic or prophylactic agent for various immune diseases including autoimmune diseases, inflammatory diseases and allergic diseases. A study is made on a novel condensed heterocyclic derivative, and it is confirmed that the condensed pyridine compound of the invention has an excellent JAK3-inhibiting activity. It is confirmed that the compound is useful as an active ingredient for a therapeutic or prophylactic agent for a disease induced by undesirable cytokine signaling such as rejection upon living donor transplantation, an autoimmune disease, asthma, atopic dermatitis, rheumatism, psoriasis and atherosclerosis or a disease induced by abnormal cytokine signaling such as cancer and leukemia because of its inhibitory activity on JAK3.

Description

technical field [0001] The present invention relates to a pharmaceutical composition, in particular to a fused pyridine compound which can be used as an effective pharmaceutical composition for treating diseases caused by unfavorable and / or abnormal cytokine signal transduction. Components, wherein the disease is, for example, organ transplantation, autoimmune disease, asthma, allergy, tumor, myeloid tumor or leukemia. Background technique [0002] Janus kinase 3 (hereinafter referred to as JAK3) is one of the Janus protein kinase family. Although other kinases in this family besides JAK3 are expressed in many tissues, JAK3 is only expressed in hematopoietic cells. This is different from that when JAK3 conducts signal transduction through various receptors such as interleukin (hereinafter referred to as IL)-2, IL-4, IL-7, IL-9, IL-15, and IL-21, through the occurrence of non-identical events with the common γ chain. It is consistent with covalent bonding to play an importa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/437A61K31/4545A61K31/497A61K31/501A61K31/506A61K31/55A61P29/00A61P37/00A61P37/02A61P43/00C07D471/14
CPCC07D471/04C07D471/14A61P11/06A61P17/00A61P29/00A61P35/00A61P37/00A61P37/02A61P37/06A61P43/00A61K31/437
Inventor 白神升平井上隆幸向吉耕一朗中岛丰臼田裕之滨口寿雄东康之畑中惠子
Owner ASTELLAS PHARMA INC