311340-92-8Relevant academic research and scientific papers
4-phenyl-pyrimidine derivatives
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, (2008/06/13)
The invention provides compounds of the formula wherein R1is hydrogen or halogen; R2is hydrogen, halogen, lower alkyl or lower alkoxy; R1and R2may together be —CH═CH—CH═CH—, wherein R1 and R2together with the two carbon ring atoms to which they are attached form a fused ring; R3is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R4/R4′are each independently hydrogen or lower alkyl; R5is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, —(CH2)n-piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, —(CH2)n-morpholinyl, —(CH2)n-piperidinyl, —(CH2)n+1-imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH2)n+1N(R4″)2, —(CH2)n+1N(R4″)2, —O—(CH2)n+1-morpholinyl, —O—(CH2)n+1-piperidinyl or —O—(CH2)n+1N(R4″)2, wherein R4″is hydrogen or lower alkyl; and n is 0-2; X is —C(O)N(R4″)— or —N(R4″)C(O)—; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds have a good affinity to the NK-1 receptor and may therefore used for the treatment of diseases related to this receptor.
