3 PHENYL PYRIDINE DERIVATIVES
    115.
    发明专利

    公开(公告)号:JO2254B1

    公开(公告)日:2004-10-07

    申请号:JOP20000015

    申请日:2000-02-22

    Abstract: The invention relates to compounds of the formulawhereinR is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R1 is hydrogen or halogen; orR and R1 may be together -CH=CH-CH=CH-; R2 is hydrogen, halogen, trifluoromethyl, lower alkoxy or cyano; R3 is hydrogen, lower alkyl or form a cycloalkyl group; R4 is hydrogen, -N(R5)2, -N(R5)S(O)2-lower alkyl, -N(R5)C(O)R5 or a cyclic tertiary amine of the groupR5 is, independently from each other, hydrogen, C3-6-cycloalkyl, benzyl or lower alkyl; R6 is hydrogen, hydroxy, lower alkyl, -N(R5)CO-lower alkyl, hydroxy-lower alkyl, cyano, -CHO or a 5- or 6 membered heterocyclic group, optionally bonded via an alkylene group,X is -C(O)N(R5)-, -(CH2)mO-, -(CH2)mN(R5)-, -N(R5)C(O)-, or -N(R5)(CH2)m-; n is 0-4; andm is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof.It has been shown that the above mentioned compounds have a good affinity to the NK-1 receptor

    Amino-triazolopyridine derivatives.
    120.
    发明专利

    公开(公告)号:ZA200201055B

    公开(公告)日:2003-07-30

    申请号:ZA200201055

    申请日:2002-02-06

    Abstract: The invention relates to compounds of formulawhereinR1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, -(CH2)nOH, halogen or lower alkoxy, and wherein the heteroaryl groups may be optionally linked to the pyrazole ring via an alkylene or alkenyl group, or isphenyl, optionally substituted by one or two substituents being lower alkyl, hydroxy-lower alkyl, halogen, hydroxy or lower alkoxy or is-O(CH2)n,phenyl, benzofuryl, indolyl or benzothiophenyl, or is-S-lower alkyl;R2 and R4 are independently from each other hydrogen, cyano or -S(O)2-phenyl;R3 is hydrogen, halogen or isa 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, -(CH2)n-aryl, hydroxy, halogen, lower alkoxy, morpholinyl, amino, lower alkylamino or -C(O)NR'2, and wherein R' is lower alkyl or hydrogen, or isphenyl, optionally substituted by one or two substituents being halogen, lower alkyl, lower alkoxy, amino, di-lower alkyl amino, CF3, -OCF3, -NHC(O)lower alkyl, cyano, -C(O)-lower alkyl, -C(O)O-lower alkyl, -S-lower alkyl, -S(O)2NH-phenyl, -S(O)2-methylpiperazinyl; or is-NR'R'', wherein R' and R'' are independently from each other hydrogen, -(CH2)nphenyl, which phenyl ring is optionally substituted by halogen or lower alkoxy, -CH(lower alkyl)-phenyl, indan-1-yl, 1,2,3,4-tetrahydro-naphthalen, or cycloalkyl; or is-O-phenyl, which phenyl ring is optionally substituted by halogen, lower alkyl or lower alkoxy, -O-tetrahydronaphthalenyl or -O-CH2-6-methyl-pyridin-2-yl; or is-benzo[1,3]dioxolyl, -1H-indol-5-yl, naphthyl, benzofuran-2-yl, 1,3,4,9-tetrahydro-b-carbolin-2-yl, piperidin-1-yl, pyrrolidin-1-yl, piperazin-4-yl-methyl or morpholinyl;R5 is -NR2, wherein R may be the same or different and is hydrogen, lower alkyl, phenyl, benzyl, -CO-lower alkyl, -CO-lower alkoxy, -lower alkenyl, -CO(CH2)n-phenyl or -COO(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by CF3, lower alkoxy, halogen or lower alkyl, -CO(CH2)3-NHCO-lower alkoxy, -(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by lower alkoxy, CF3 or halogen, or is 4,5-dihydro-1H-imidazol-2-yl-benzoic acid, 1,4,5,6-tetrahydro-pyrimidin-2-yl-benzoic acid or 4,5,6,7-tetrahydro-1H-[1,3]diazepin-2-yl-benzoic acid;n is 0-4and their pharmaceutically acceptable salts

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