N,6-bis(aryl or heteroaryl)-1,3,5-triazine-2,4-diamine compounds as idh2 mutants inhibitors for the treatment of cancer
US-2017348318-A1 · Dec 7, 2017 · US
US9458116B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9458116-B2 |
| Application number | US-201414909632-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 8, 2014 |
| Priority date | Aug 5, 2013 |
| Publication date | Oct 4, 2016 |
| Grant date | Oct 4, 2016 |
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A benzoguanamine compound having an amino methyl group is represented by the following Formula (1), or a salt thereof: wherein R represents a substituent selected from the group consisting of hydrogen, an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an aryloxy group having 6 to 10 carbon atoms, a hydroxyl group, an amide group, and a halogen atom, and n is an integer of 1 to 2.
Opening claim text (preview).
The invention claimed is: 1. A benzoguanamine compound having an amino methyl group, represented by the following Formula (1), or a salt thereof: wherein R represents a substituent selected from the group consisting of hydrogen, an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an aryloxy group having 6 to 10 carbon atoms, a hydroxyl group, an amide group, and a halogen atom, and n is an integer of 1 to 2. 2. The benzoguanamine compound having an amino methyl group, or a salt thereof according to claim 1 , being o-aminomethylbenzoguanamine, m-aminomethylbenzoguanamine, or p-aminomethylbenzoguanamine, or a salt thereof. 3. A method for manufacturing a benzoguanamine compound having an amino methyl group, or a salt thereof comprising: a reduction step for obtaining the benzoguanamine compound represented by the following Formula (1) having an aminomethyl group, or a salt thereof by hydrogen reduction of a cyanobenzoguanamine compound represented by the following Formula (2), or a salt thereof in the presence of a catalyst and a solvent: wherein R represents a substituent selected from the group consisting of hydrogen, an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an aryloxy group having 6 to 10 carbon atoms, a hydroxyl group, an amide group, and a halogen atom; and n is an integer of 1 to 2. 4. The method for manufacturing the benzoguanamine compound having an amino methyl group, or a salt thereof according to claim 3 , wherein the catalyst comprises a sponge metal catalyst. 5. A method for manufacturing a benzoguanamine compound having an amino methyl group, or a salt thereof comprising: a reaction step for obtaining the benzoguanamine compound represented by the following Formula (1) having an aminomethyl group by reacting an aminomethylbenzonitrile compound represented by the following Formula (3), or a salt thereof with a dicyandiamide compound represented by the following Formula (4) or a salt thereof: wherein R represents a substituent selected from the group consisting of hydrogen, an alkyl group having 1 to 10 carbon atoms, an alkoxy group having 1 to 10 carbon atoms, an aryl group having 6 to 10 carbon atoms, an aryloxy group having 6 to 10 carbon atoms, a hydroxyl group, an amide group, and a halogen atom; and n is an integer of 1 to 2.
Two nitrogen atoms · CPC title
with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines · CPC title
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