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Diamino heterocyclic carboxamide compound

A compound and heterocyclic technology, applied in the directions of active ingredients of heterocyclic compounds, organic chemistry, pharmaceutical combinations, etc., can solve the problems of not specifically disclosing diaminoheterocyclic carboxamide compounds and the like

Active Publication Date: 2012-04-18
ASTELLAS PHARMA INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0093] However, there is no specific disclosure of the diaminoheterocyclic carboxamide compound involved in the present invention

Method used

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  • Diamino heterocyclic carboxamide compound

Examples

Experimental program
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Embodiment

[0387] The preparation method of the compound represented by formula (I) will be described in more detail below based on the examples. Furthermore, the present invention is not limited only to the compounds described in the following examples. In addition, the production methods of the raw material compounds are shown in the production examples, respectively. In addition, the preparation method of the compound shown in (I) is not limited to the preparation method shown in the specific examples below, the compound shown in formula (I) can also be obtained by the combination of these preparation methods, or those skilled in the art method to prepare.

[0388] In addition, the following abbreviations are sometimes used in Examples, Preparation Examples, and Tables described below.

[0389] Rex: Preparation number

[0390] Ex: Example number

[0391] Structure: Chemical structural formula

[0392] Data: Physicochemical data (FAB+: FAB-MS[M+H] + ,ESI+:ESI-MS[M+H] + , APCI / ES...

preparation example 4

[0395] A mixture of 4-methyl-3-nitrobenzoic acid (1.97 g) and thionyl chloride (6 mL) was heated at reflux for 18 hours. After concentrating the reaction solution under reduced pressure, it was azeotroped with toluene to obtain a reddish-brown oil. To a mixture of the reddish-brown oil and THF (25 mL) was added diethylamine (2.6 mL) under ice-cooling, followed by stirring at room temperature for 5 hours. The reaction solution was poured into water, and extracted with ethyl acetate. The organic layer was washed with saturated brine, then dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure to obtain N,N-diethyl-4-methyl-3-nitrobenzamide (2.61g) as a brown oil .

preparation example 41

[0397] To a mixture of 2-methoxy-4-nitrobenzenesulfonyl chloride (600 mg) and THF (5 mL) was added a mixture of piperidine (406 mg) and THF (1 mL), and stirred at room temperature for 12 hours. 10% hydrochloric acid was added to the reaction liquid, followed by extraction with ethyl acetate. The organic layer was washed with saturated brine, dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure to obtain 1-[(2-methoxy-4-nitrophenyl)sulfonyl]piperidine (714 mg) as a yellow solid .

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PUM

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Abstract

Disclosed are a compound represented by formula (I) or a salt thereof; a kinase inhibitor for EML4-ALK fusion protein containing the compound; and use of the compound for the treatment of cancers. (In formula (I), -X- represents a group represented by formula (II) or formula (III); A represents -H, a halogen atom, a lower alkyl group, a cycloalkyl group or a lower alkenyl group; R1 represents a substituted phenyl group, a (substituted) heterocyclic group or a (substituted) bicyclic fused ring; R2 represents a (substituted) cycloalkyl group, a (substituted) non-aromatic heterocyclic group, a (substituted) phenyl group, a (substituted) pyridyl group or a (substituted) lower alkyl group; and R3 represents -H or a lower alkyl group; or alternatively R2 and R3 may combine together to form a cyclic amino group.)

Description

technical field [0001] The present invention relates to a diaminoheterocyclic carboxamide compound useful as an active ingredient of a pharmaceutical composition (especially, a pharmaceutical composition for cancer therapy). Background technique [0002] Lung cancer is caused by the loss of normal function of trachea, bronchi, and alveolar cells, resulting in disordered proliferation. The number of deaths caused by lung cancer accounts for 17% of all cancer deaths, accounting for the largest proportion. About 1.3 million people die every year in the world in lung cancer. [0003] Treatment for lung cancer is broadly classified into surgery (surgical therapy), anticancer agents (chemotherapy), and radiation exposure (radiotherapy), but whether the treatment is effective or not varies depending on the tissue type of lung cancer. For example, the diagnosis of lung cancer is made through cytopathological diagnosis of microscope specimens by medical personnel, but small cell lun...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/48A61K31/4965A61K31/497A61K31/505A61K31/506A61K31/5377A61K31/541A61K31/55A61P35/00A61P43/00C07D241/26C07D401/12C07D401/14C07D403/12C07D405/12C07D405/14C07D409/12C07D413/12C07D417/12C07D471/08C07D491/113
CPCC07D401/14C07D401/12C07D241/28C07D405/14C07D403/12C07D471/08C07D405/12C07D409/12C07D417/12C07D241/26C07D491/113C07D413/12C07D239/48A61P35/00A61P35/02A61P43/00
Inventor 岛田逸郎黑泽一雄松矢高广饭久保一彦近藤裕神川晃雄富山泰岩井辰宪
Owner ASTELLAS PHARMA INC
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