发明名称 Quinolin-4-yl derivatives I and their use in treating neurodegenerative disease
摘要 Described are compounds of the formula as shown, wherein: R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, amino, nitro, cyano, lower alkyl-amino, di-lower alkyl-amino or halogen; R2 is phenyl, optionally substituted by lower alkyl, lower alkoxy, halogen, trifluoromethyl, amino, lower alkyl-amino or di-lower alkyl-amino, 2,3-dihydro-benzofuran-5-yl, chroman-6-yl, napthalen-2-yl, indan-5-yl, lower alkenyl-phenyl, 5,6,7,8-tetrahydro-napthalenyl, 2,3-dihydro-isoindol-2-yl,1,2,3,4-tetrahydro-napthalenyl, benzofuran-2-yl, benzo[b]thiophen-2-yl, lower alkyl-phenyl, 3,4-dihydro-1H-isoquinolin-2-yl or thiophen-3-yl; R3 and R4 are independently from each other hydrogen or lower alkyl; R5 is hydrogen, lower alkyl, - CH2OH or CH2NR2R7; R6 and R7 are independently form each other hydrogen, lower alkyl, -(CH2)n-phenyl, cycloalkyl,-(CH2)m-morpholinyl or form together with the N-atom a saturated ring with 4-6 C-atoms; n is 0 - 3; m is 2 or 3; N is -NR8 - or -O-; or X and R5 are together >N(CH2)2-; or X and R3 are together >N(CH2)3-; and R8 is hydrogen or lower alkyl; and to pharmaceutically acceptable acid addition salts thereof, with the exception of the following compounds: (6-chloro-2-phenyl-4-quinolinyl)-(+)-2-aminobutanol; (6-methyl-2-phenyl-4-quinolinyl)-(+)-2-aminobutanol; (6-methoxy-2-phenyl-4-quinolinyl)-(+)-2-aminobutanol; and (8-methoxy-2-phenyl-4-quinolinyl)-(+)-2-aminobutanol. Also described is the use of a compound in the manufacture of a medicament for the treatment of diseases based on therapeutic indications for NMDA receptor subtype specific blockers, which include acute forms of neurodegeneration caused e.g, by stroke and brain trauma. Included are chronic forms of neurodegeneration such as Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (amyotrophic lateral sclerosis) and neurodegeneration associated with bacterial or viral infection, and chronic or acute pain.
申请公布号 NZ507141(A) 申请公布日期 2002.05.31
申请号 NZ20000507141 申请日期 2000.09.26
申请人 F 发明人 JAESCHKE, GEORG;PINARD, EMMANUEL;WYLER, RENE;ALANINE, ALEXANDER;BURNER, SERGE;HEITZ NEIDHART, MARIE-PAULE;BUETELMANN, BERND
分类号 C07D215/22;A61K31/47;A61K31/4709;A61K31/4725;A61P9/10;A61P21/00;A61P25/00;A61P25/14;A61P25/16;A61P25/28;C07D215/233;C07D215/42;C07D215/46;C07D401/04;C07D401/12;C07D405/04;C07D405/12;C07D409/04;C07D413/12;(IPC1-7):C07D215/14 主分类号 C07D215/22
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