4-(2-(pyrrolidine/piperidine-1-yl)benzyl)-piperazine urea TRPV1 antagonist and preparation method and application thereof
The invention discloses a novel 4-(2-(pyrrolidine/piperidine-1-yl)benzyl)-piperazine urea type TRPV1 antagonist and a preparation method and application thereof. The invention relates to a compound ina general formula (I) and a pharmaceutically acceptable salt thereof, in the formula, n is equal to...
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Main Authors | , , , , , |
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Format | Patent |
Language | Chinese English |
Published |
28.07.2020
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Subjects | |
Online Access | Get full text |
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Summary: | The invention discloses a novel 4-(2-(pyrrolidine/piperidine-1-yl)benzyl)-piperazine urea type TRPV1 antagonist and a preparation method and application thereof. The invention relates to a compound ina general formula (I) and a pharmaceutically acceptable salt thereof, in the formula, n is equal to 1 or 2, R is H, F, Cl, Br, I, CF3, CH3 or OH, and Ar is phenyl or aromatic heterocyclic group. Thecompounds have a strong analgesic effect, the activity of part of the compounds is far higher than that of a TRPV1 receptor antagonist BCTC, almost no body temperature rise side effect exists, and theinvention further relates to the preparation method of the compounds and pharmaceutical preparations containing the compounds.
本发明公开了一种4-(2-(吡咯烷/哌啶-1-基)苄基)-哌嗪脲类新型TRPV1拮抗剂及其制备方法和应用。尤其涉及通式(Ⅰ)中化合物及其药学上可接受的盐,式中,n=1或2,R为H、F、Cl、Br、I、CF、CH或OH;Ar为苯基或芳香杂环基。这类化合物具有较强的镇痛作用,部分化合物活性远高于TRPV1受体拮抗剂BCTC,并且几乎无体温升高副作用,本发明还涉及该类化合物的制备方法及含有它们的药物制剂。 |
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Bibliography: | Application Number: CN202010381837 |