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    • 39. 发明授权
      US06355653B1 Amino-triazolopyridine derivatives 失效
    • Amino-triazolopyridine derivatives
    • US06355653B1
    • 2002-03-12
    • US09645127
    • 2000-08-24
    • Gerda Huber Trottmann , Walter Hunkeler , Roland Jakob-Roetne , Gavin John Kilpatrick , Matthias Heinrich Nettekoven , Claus Riemer
    • Gerda Huber Trottmann , Walter Hunkeler , Roland Jakob-Roetne , Gavin John Kilpatrick , Matthias Heinrich Nettekoven , Claus Riemer
    • A61K314439
    • C07D471/04
    • The invention relates to compounds of formula wherein R1 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 is phenyl, 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 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)n-aryl, hydroxy, halogen, lower alkoxy, morpholinyl, amino, lower alkylamino or —C(O)NR′2, and wherein R′ is lower alkyl or hydrogen, or is phenyl, 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 0-4 and their pharmaceutically acceptable salts
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