申请人:Allen David George
公开号:US20080132536A1
公开(公告)日:2008-06-05
The invention provides a compound of formula (I) or a salt thereof:
wherein Ar has the sub-formula (x) or (z):
and wherein R
3
is optionally substituted C
3-8
cycloalkyl, optionally substituted C
5-7
cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc), or a bicyclic group (ee);
and wherein R
4
is H, C
1-3
alkyl, C
1-2
fluoroalkyl, cyclopropyl, —CH
2
OR
4a
, —CH(Me)OR
4a
, or —CH
2
CH
2
OR
4a
; and R
5
is inter alia H, C
1-8
alkyl, C
1-3
fluoroalkyl, C
3-8
cycloalkyl, certain substituted alkyl groups, —(CH
2
)
n
13
-Het, or optionally substituted phenyl or —CH
2
-Ph;
or R
4
and R
5
taken together are —(CH
2
)
p
1
— or —(CH
2
)
p
3
—X
5
—(CH
2
)
p
4
—;
provided that at least one of R
4
and R
5
is not a hydrogen atom (H).
The invention also provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, allergic rhinitis or atopic dermatitis.
该发明提供了式(I)的化合物或其盐:
其中Ar具有亚式(x)或(z):
其中,R3是可选的取代C3-8环烷基,可选的取代C5-7环烯基,可选的取代的杂环基(aa),(bb)或(cc),或者是双环基(ee);
其中,R4是氢,C1-3烷基,C1-2氟代烷基,环丙基,—CH2OR4a,—CH(Me)OR4a或—CH2CH2OR4a;
而R5则是包括氢、C1-8烷基、C1-3氟代烷基、C3-8环烷基、某些取代烷基、—(CH2)n13-Het,或可选取代的苯基或—CH2-Ph等的基团;
或者,R4和R5在一起是—(CH2)p1—或—(CH2)p3—X5—(CH2)p4—;
但是至少其中一个R4和R5不是氢原子(H)。
该发明还提供了将这些化合物用作磷酸二酯酶IV(PDE4)的抑制剂和/或用于治疗和/或预防炎症和/或过敏性疾病,如慢性阻塞性肺疾病(COPD)、哮喘、类风湿性关节炎、过敏性鼻炎或特应性皮炎的用途。