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(TRPV1 end Prophet)
专利权人:
INC.;CONCENTRIC ANALGESICS
发明人:
CRAIG HUSFELD
申请号:
ARP150103868
公开号:
AR102799A1
申请日:
2015.11.25
申请国别(地区):
AR
年份:
2017
代理人:
摘要:
It introduces the compounds, pharmaceutical components and drugs containing these components, and the methods of using these compounds to regulate the activity of vanilloide 1 (TRPV1) receptor. 1. Property 1: compound (1) with formula structure property,Among them, it is a promoter of phenol TRPV1, where the hydrogen atom of phenol hydroxyl group is covalently linked to a-c (o) - X - (C (1) (R2)); 8345; - Z; xes-c (R1) (R2) -,- that is...-N (R) - o -S-n is an integer between 1 and 10; Z is -NR³R⁴ or -CO₂H; R⁵ is hydrogen, substituted or unsubstituted alkyl, or substituted or unsubstituted aryl, and each R¹ and R² are each independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted acyl, or two R¹ or R² groups in adjacent carbon atoms, together with the carbon atoms to which they are attached, form a substituted or unsubstituted cycloalkyl group, or R¹ and R⁵ groups in adjacent atoms, together with the atoms to which they are together, they form a substituted or unsubstituted heterocycloalkyl group;R3 and r83088 are independent hydrogen, alternative or unsubstituted asphalt, alternative or unsubstituted arilo, or pharmaceutically acceptable, soluble or hydrochloric acid salts.Se describen compuestos, composiciones farmacéuticas y medicamentos que los incluyen, y métodos de uso de dichos compuestos para modular la actividad del receptor de potencial transitorio del receptor vanilloide 1 (TRPV1). Reivindicación 1: Un compuesto caracterizado porque tiene la estructura de fórmula (1), donde: Y es un agonista de TRPV1 fenólico, donde el átomo de hidrógeno del grupo hidroxilo fenólico se reemplaza por un enlace covalente con -C(O)-X-(C(R¹)(R²))ₙ-Z; X es -C(R¹)(R²)-, -O-, -N(R⁵)- o -S-; n es un entero entre 1 y 10; Z es -NR³R⁴ o -CO₂H; R⁵ es hidrógeno, alquilo sustituido o no sustituido, o arilo sustituido o no sustituido, y cada R¹ y R² es cada uno en forma independiente hidrógeno, alquilo sustituido o no s
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