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4-Phenylpyridine derivatives and their use as NK-1 receptor antagonists
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
申请号:
NL300758
公开号:
NL300758I2
申请日:
2015.08.28
申请国别(地区):
NL
年份:
2015
代理人:
摘要:
The present invention relates to compounds of the general formula <;CHEM>; wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R<;1>; is hydrogen or halogen; or R and R<;1>; may be together -CH=CH-CH=CH-; R<;2>; and R<;2'>; are independently from each other hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; or R<;2>; and R<;2'>; may be together -CH=CH-CH=CH-, optionally substituted by one or two substituents selected from lower alkyl or lower alkoxy; R<;3>; is hydrogen, lower alkyl or form a cycloalkyl group; R<;4>; is hydrogen, -N(R<;5>;)2, -N(R<;5>;)(CH2)nOH, -N(R<;5>;)S(O)2-lower alkyl, -N(R<;5>;)S(O)2-phenyl, -N=CH-N(R<;5>;)2, -N(R<;5>;)C(O)R<;5>; or a cyclic tertiary amine of the group <;CHEM>; R<;5>; is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R<;6>; is hydrogen, hydroxy, lower alkyl, -(CH2)nCOO-lower alkyl, -N(R<;5>;)CO-lower alkyl, hydroxy-lower alkyl, cyano, -(CH2)nO(CH2)nOH, -CHO or a 5-or 6 membered heterocyclic group, optionally bonded via an alkylene group, X is -C(O)N(R<;5>;)-, -(CH2)mO-, -(CH2)mN(R<;5>;)-, -N(R<;5>;)C(O)-, or -N(R<;5>;)(CH2)m-; n is 0-4; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I show a high affinity to the NK- 1 receptor. They may be used for the treatment of diseases, which relate to NK- 1 receptor antagonists.
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