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DERIVADO DE MORFINANO.
专利权人:
UNIVERSITY OF TSUKUBA
发明人:
Hiroshi NAGASE,Hideaki FUJII,Akiyoshi SAITOH,Eriko NAKATA,Masaaki HIROSE,Isao OOI,Kohei HAYASHIDA
申请号:
MX2017011824
公开号:
MX2017011824A
申请日:
2016.03.17
申请国别(地区):
MX
年份:
2018
代理人:
摘要:
The morphinan derivatives represented by general formula (I) (wherein R1 represents hydrogen, a C1-10alkyl, a cycloalkylalkyl in which the cycloalkyl moiety has 3-6 carbon atoms and the alkylene moiety has 1-5 carbon atoms, or the like; R2 represents a heterocycle including at least one carbon atom and 1-4 heteroatoms selected from among N, O and S as constituent annular atoms, with at least one set of adjacent constituent annular atoms having a double bond, said heterocycle also including at least one oxo group as a substituent; Y is bonded to a carbon atom that is a constituent annular atom of R2; R3, R4 and R5 represent hydrogen, hydroxy or the like; R6a and R6b represent hydrogen or the like; R7 and R8 represent hydrogen or the like; R9 and R10 are the same or different, and represent hydrogen or the like; X represents O or CH2; and Y represents C(=O)), variants and stereoisomers of the derivatives, pharmaceutically acceptable salts thereof, and solvates thereof according to the present invention are used as antianxiety drugs, antidepressants and the like.Se describe un derivado de morfinano representado por la siguiente fórmula general (I): (ver Fórmula) en donde R1 representa hidrógeno, alquilo de C1-10, cicloalquilalquilo donde la porción cicloalquilo tiene de 3 a 6 átomos de carbono, y la porción alquileno tiene de 1 a 5 átomos de carbono, etc., R2 representa un anillo heterocíclico que contiene de 1 a 4 heteroátomos seleccionados de N, O y S y al menos un átomo de carbono como los átomos constituyentes del anillo, que contienen al menos un conjunto de átomos constituyentes del anillo adyacentes unidos mediante un doble enlace, y sustituidos adicionalmente con al menos un grupo oxo, Y se une a un átomo de carbono como un átomo constituyente del anillo de R2, R3, R4, y R5 representan hidrógeno; hidroxi, etc., y R6a y R6b representan hidrógeno, etc., R7 y R8 representan hidrógeno, etc., R9 y R10, que son iguales o diferentes, representan hidrógeno, etc., X rep
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