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Fused imidazolium derivatives

A technology of imidazolium and derivatives, applied in the field of synthetic intermediate compounds, can solve the problems of undisclosed compound drug use and the like

Inactive Publication Date: 2003-03-05
ASTELLAS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, all these documents do not disclose the pharmaceutical use of these compounds

Method used

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  • Fused imidazolium derivatives
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  • Fused imidazolium derivatives

Examples

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reference example 1

[0132] Reference example 1: in the ethanol (50 milliliters) solution of 3-cyano-2-(dimethylamino) pyridine (2.45 grams), add saturated ammonia (17 milliliters) and Raney nickel (3.0 grams), in 1 Stir at room temperature under a hydrogen atmosphere of 1 atm for 8 hours. After 760 ml of hydrogen uptake, the catalyst was removed by filtration. The mother liquor was concentrated to give 3-(aminomethyl)-2-(dimethylamino)pyridine (2.61 g) as a yellow oil.

reference example 2

[0133] Reference example 2: in acetic anhydride (100 milliliters) solution of 2-chloro-3-[(2-methoxyethyl) amino]-1,4-naphthoquinone (33 grams), add several drops of concentrated sulfuric acid, Stir at 45°C for 1 hour. Ethanol (100 ml) was added to the reaction solution to esterify excess acetic anhydride. After cooling, ethyl acetate was added, washed with water and saturated brine, and dried over anhydrous sodium sulfate. The solvent was removed by evaporation, and the residue was crystallized from ether to give N-(3-chloro-1,4-dihydro-1,4-dioxo-2-naphthyl)-N-(2-methoxy ethyl)acetamide (29 g).

reference example 3

[0134] Reference Example 3: In N-(3-chloro-1,4-dihydro-1,4-dioxo-2-naphthyl)acetamide (1.0 g) in benzene (20 ml) solution, add 2-form Oxyethylamine (0.8 mL), stirred at room temperature for 1 hour. Water was added to the reaction liquid, followed by extraction with chloroform. The organic layer was washed with water and saturated brine, and dried over anhydrous sodium sulfate. The solvent was removed by evaporation, and the residue was recrystallized from ethyl acetate to give N-[3-(2-methoxyethyl)amino-1,4-dihydro-1,4-dioxo-2-naphthalene as a red powder base] acetamide (0.87 g).

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Abstract

This invention relates to medicaments, particularly novel fused imidazolium derivatives useful for the treatment of cancers and novel synthetic intermediate compounds thereof. The novel imidazolium derivatives fused with an aryl or heteroaryl ring, characterized in that the 1- and / or 3-position is substituted by an alkyl group etc. having a substituent selected from the group consisting of -ORa, -SRa and the like, have excellent anti-tumor activity and low toxicity and are useful as anticancer agents having wide margins of safety. <CHEM>

Description

technical field [0001] The present invention relates to medicines, in particular to new fused imidazolium derivatives useful for treating cancer and their new synthetic intermediate compounds. Background of the invention [0002] As an imidazolium derivative fused with an aromatic ring or a heteroaromatic ring having antitumor activity, only 4 with the following formula has been disclosed in Khim.Pharm.Zh., 32(6), 10-11 (1998) before. , 9-dioxonaphtho[2,3-d]imidazolium compounds (KP-1, KP-3, etc.). [0003] (In the formula, Et and Me represent ethyl and methyl respectively, the same below). [0004] In J.Med.Chem., (7) 3, 362-364 (1964) discloses the compound with antibacterial effect, in this compound, R 1 and R 2 Both are lower alkyl, or one is lower alkylene-(aryl which may have one or more substituents) and the other is -CH 3 ,-(CH 2 ) 3 CH 3 or phenyl, or one is lower alkylene-CO-(aryl which may have one or more substituents) and the other is -(CH 2 ) 2 CH(CH...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/36A61K31/416A61K31/4188A61K31/424A61K31/4245A61K31/427A61K31/429A61K31/437A61K31/4453A61K31/4468A61K31/454A61K31/47A61K31/4709A61K31/497A61K31/4985A61K31/501A61K31/5025A61K31/506A61K31/519A61K31/5375A61K31/551A61P35/00C07C233/41C07C235/14C07C237/04C07C255/24C07C255/25C07C255/58C07C259/06C07C271/28C07C311/37C07C317/28C07C323/25C07D209/16C07D211/58C07D213/38C07D213/64C07D213/74C07D213/89C07D215/12C07D233/54C07D235/02C07D235/10C07D235/14C07D239/26C07D241/12C07D241/20C07D295/13C07D307/14C07D317/58C07D333/68C07D335/06C07D401/04C07D401/06C07D401/12C07D401/14C07D403/06C07D403/14C07D405/06C07D471/04C07D491/048C07D495/04C07D498/04
CPCC07C255/58C07D211/58A61K31/47A61K31/437A61K31/5025C07D401/06C07D241/20C07D335/06C07D307/14C07D213/64C07C255/24C07D209/16A61K31/4245C07D333/68C07C2102/10C07D213/38A61K31/519C07D215/12C07C2103/74C07D213/74A61K31/4453A61K31/427C07C255/25A61K31/429C07C311/37C07C233/41C07D233/64C07C259/06C07C271/28C07D403/06C07D295/13C07D471/04A61K31/551C07D235/02C07D213/89A61K31/501A61K31/4188C07D403/14C07C237/04A61K31/4985C07D405/06C07D401/14C07D495/04C07D235/14C07D239/26C07C2101/14C07C323/25C07D401/04C07C235/14A61K31/5375A61K31/506A61K31/454A61K31/4709C07D317/58C07D241/12C07C2101/02A61K31/36A61K31/497C07C317/28C07D401/12A61K31/4468A61K31/416A61K31/424C07C2601/02C07C2601/14C07C2602/10C07C2603/74A61P35/00C07D333/64C07D239/16
Inventor 松久彰木野山功丰岛启中原崇人竹内雅博冈田稔
Owner ASTELLAS PHARMA INC
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