申请人:Woodhead Steven John
公开号:US20100210617A1
公开(公告)日:2010-08-19
The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y
1
and Y
2
is CH and the other is selected from CH, CR
8
and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y
1
or Y
2
is CR
8
; R
1
aryl or heteroaryl group of 5 to 10 ring members; R
2a
and R
3a
each are hydrogen, C
1-4
hydrocarbyl or C
1-4
acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR
2a
R
3a
forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R
18
is hydrogen or methyl; R
19
is hydrogen or methyl; R
24
is hydrogen or R
24
, R
2a
and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R
25
is hydrogen or a C
1-4
alkyl group wherein the C
1-4
alkyl group is optionally substituted by hydroxy or amino provided that there are at least two carbon atoms between the hydroxy or amino group and the oxygen atom to which R
25
is attached; and R4 and R
5
each are hydrogen or a substituent as defined in the claims
本发明提供了化合物的公式(II)或其盐、溶剂化物、互变异构体或N-氧化物;其中n为0或1;Y1和Y2中的一个是CH,另一个选自CH、CR8和N;q为0、1或2,但当Y1或Y2为CR8时,q为0或1;R1为5到10个环成员的芳基或杂环基团;R2a和R3a各自为氢、C1-4烃基或C1-4酰基,其中烃基和酰基基团可选地被氟、羟基、氨基、甲基氨基、二甲基氨基或甲氧基取代;或NR2aR3a形成咪唑环或饱和的单环4-7成员杂环基团,可选地包含第二个杂原子环成员,所选自O和N;R18为氢或甲基;R19为氢或甲基;R24为氢或R24、R2a和介于其间的氮原子和碳原子共同形成氮杂环,所选自氮杂环、吡咯烷或哌啶环;R25为氢或C1-4烷基基团,其中C1-4烷基基团可选地被羟基或氨基取代,但在R25连接的氧原子和羟基或氨基基团之间至少有两个碳原子;而R4和R5各自为氢或如权利要求中所定义的取代基。