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Cold menthol receptor antagonists
专利权人:
Janssen Pharmaceutica; N.V.
发明人:
COLBURN, Raymond,DAX, Scott,FLORES, Christopher,LUDOVICI, Donald,XIA, Mingde,XU, Xiaoging,YOUNGMAN, Mark,ZHU, Bin
申请号:
ES09774997
公开号:
ES2610882T3
申请日:
2009.08.11
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of Formula (I) ** Formula ** Where A is phenyl, thienyl, or C5-7cycloalkyl; whereas when A is phenyl, R2 is different from 2-chloro, 2-C1-4alkoxy, 4-C1-4alkoxy, 2-C1-4alkoxycarbonyl or 4-20 C1-4alkoxycarbonyl; or, when A is phenyl, L is -N (R3) (CH2) n- and R1 and L are attached to adjacent carbon atoms of phenyl, R1 and R3 are optionally taken with the atoms to which they are attached to form dihydro -indole-1-yl or dihydro-quinolin-1il; R1 is one to three substituents selected from the group consisting of hydrogen, C1-4alkyl, C1-4alkoxy, fluoro, chloro and hydroxy; L is -Z - (CH2) n- or -CH2-; n is 0 or 1; Z is O, S, or NR3; whereas when Z is O or S, A is phenyl; R2 is hydrogen, C1-4alkyl, C1-4alkoxy, trifluoromethyl, chlorine, fluoro, bromine, carboxy or C1-4alkoxycarbonyl; R3 is hydrogen or C1-3alkyl; R4 is hydrogen or C1-4alkyl; R5 is naphthyl, indanyl, tetralinyl or a 9 to 10-membered heteroaryl selected from the group consisting of benzimidazolyl, cinnolinyl, 1H-indazolyl, indolyl, isoindolyl, isoquinolinyl, naphthyridinyl, phthalazinyl, quinazolinyl, quinolinyl and quinoxalinyl; wherein R5 is optionally substituted with 1 to 2 substituents independently selected from the group consisting of C1-4alkyl, hydroxy, C1-4alkoxy, trifluoromethyl, chlorine, fluoro, bromine, carboxy, C1-44alkoxycarbonyl and cyano; and enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof; while a compound of Formula (I) is different from a compound where A is phenyl, R1 is 3-chloro, R2 is 4-trifluoromethyl, L is -Z- (CH2) n- n is 1, Z is NR3, R3 is hydrogen, R4 is hydrogen, and R5 is isoquinolin-5-yl; a compound where A is phenyl, R1 is 2-fluoro, R2 is 4-trifluoromethyl, L is -Z- (CH2) n-, n is 0, Z is NR3, R3 is hydrogen, R4 is hydrogen, and R5 is indole -4-il; and a compound where A is phenyl, R1 is 4-methoxy, R2 is 4-chloro, L is -Z- (CH2) n-, n is 0, Z is NR3, R3 is hydrogen, R4 is hydrogen, and R5 is isoquinolin-5-il.Un compuesto de Fórmula
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