- 专利标题： Aminomethyl-functionalized denatonium derivatives, their preparation and use
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申请号： US16975077申请日： 2019-02-20
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公开(公告)号： US11891352B2公开(公告)日： 2024-02-06
- 发明人: Lorenz Meinel , Tessa Luehmann , Martina Raschig
- 申请人： Julius-Maximilians-Universitaet Wuerzburg
- 申请人地址： DE Wuerzburg
- 专利权人： Julius-Maximilians-Universitaet
- 当前专利权人： Julius-Maximilians-Universitaet
- 当前专利权人地址： DE Wuerzburg
- 代理机构： Smith Patent, LLC
- 代理商 Chalin A. Smith
- 优先权： EP 157816 2018.02.21
- 国际申请： PCT/EP2019/054140 2019.02.20
- 国际公布： WO2019/162289A 2019.08.29
- 进入国家日期： 2020-08-21
- 主分类号： C07C237/04
- IPC分类号： C07C237/04 ; C07C231/12 ; C07K1/10
摘要：
The present invention is directed to compounds of the general formula (I) and salts thereof
wherein X− is halide, pseudohalide, sulphate, benzoate, acetate, trifluoroacetate, hydroxide, saccharinate or capsaicinate; R10 is hydrogen or C1-C10-alkyl; and R1-R9 independently are hydrogen, halogen, C1-C5-alkyl, C1-C4-alkoxy, C1-C20-alkoxycarbonyl. The invention is furthermore directed to a method for the preparation of these compounds. The compounds can be used as bitter substances in medicine, pharmaceutics and/or diagnostics. They can furthermore be used for the coupling to proteins and peptides by means of forming a peptide bond between the amino-group of the compounds of the present invention and a carboxyl-group of the protein or peptide.
wherein X− is halide, pseudohalide, sulphate, benzoate, acetate, trifluoroacetate, hydroxide, saccharinate or capsaicinate; R10 is hydrogen or C1-C10-alkyl; and R1-R9 independently are hydrogen, halogen, C1-C5-alkyl, C1-C4-alkoxy, C1-C20-alkoxycarbonyl. The invention is furthermore directed to a method for the preparation of these compounds. The compounds can be used as bitter substances in medicine, pharmaceutics and/or diagnostics. They can furthermore be used for the coupling to proteins and peptides by means of forming a peptide bond between the amino-group of the compounds of the present invention and a carboxyl-group of the protein or peptide.
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