发明名称 Fluorinated 3,4-dihydroquinoline derivatives used as NOS inhibitors in medicaments for treating neurodegenerative diseases
摘要 Described are compounds of formula (I), a method for producing them and to their use in medicaments as NOS inhibitors. In which R1 and R2 independently of one another, mean: a) hydrogen, b) C1-6 alkyl, c) OR8, d) NR8R9, e) CN, f) acyl, g) CO2R10, h) CONR8R9, i) CSNR8R9, R3 means: a saturated or unsaturated C1-5 alkene radical, which can be substituted in 1 to 4 places with OR8, NR1 R12 or C1-4 alkyl and in which 1 or 2 CH2 groups can be replaced by O, S(O)n, NR11, =N- or carbonyl, and which can be bridged with a methano, ethano or propano group, R4, R5, R6 and R7, independently of one another, mean a) hydrogen, b) halogen, c) S(O)nR8, d) OR8, e) COOR8, f) COR8, g) CONR8Rl3, h) CSNR8R13 i) C(NR8)NR9Rl3, j) NR14Rl5, k) C1 6 alkyl, which is optionally substituted with halogen, OR8, SR8,NR14R15, phenyl, 5- to 6- membered heteroaryl with 1 to 4 N, S or O atoms or C3-7 cycloalkyl, I) C3 7 cycloalkyl, m) C2-6 alkenyl, optionally substituted with phenyl or halogen, n) C2-6 alkinyl, optionally substituted with phenyl or halogen, o) C6 10 aryl, which is optionally substituted with halogen, CN, C1-4 alkyl, SR8 or OR8, p) 5 to 6 membered hetaryl with 1 to 4 N, O or S atoms, which contain a slightly condensed benzene ring and can be substituted with halogen, N02, cyano,-OR8, SR8, C1-4 alkyl, CF3 or NR8R13 q) CN, r) N02, s) CF3, t) OCF3, R4 and R5, R5 and R6 or R6 and R7 together with 2 adjacent carbon atoms form a 5- or 6-membered carbocycle, which can be substituted with NR14R15, R8, R9 and R10, independently of one another, mean: a) hydrogen, b) C1-6 alkyl, c) C6-10 aryl, which optionally is substituted with halogen or C1-4 alkyl. Such compounds are suitable for treating diseases of the cardiovascular system and for treating autoimmune and/or inflammatory diseases and they are well suited for inhibiting the neuronal NOS.
申请公布号 NZ510875(A) 申请公布日期 2003.10.31
申请号 NZ19990510875 申请日期 1999.11.10
申请人 SCHERING AKTIENGESELLSCHAFT 发明人 BURTON, GERARDINE ANNE;HILLMANN, MARGRIT;JAROCH,STEFAN;REHWINKEL, HARTMUT;HOLSCHER, PETER;SULZLE, DETLEV;CDONALD, FIONA MACDOUGALL
分类号 A61K31/435;A61K31/437;A61P1/00;A61P1/08;A61P1/16;A61P3/08;A61P3/10;A61P9/00;A61P9/10;A61P13/12;A61P17/00;A61P17/06;A61P19/02;A61P25/00;A61P25/06;A61P25/08;A61P25/14;A61P25/16;A61P25/18;A61P25/20;A61P25/24;A61P25/28;A61P29/00;A61P37/06;C07D221/16;C07D405/04;(IPC1-7):A61K31/435 主分类号 A61K31/435
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