申请人：——
公开号：US20010014677A1
公开（公告）日：2001-08-16
1
Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R
1
and R
2
are optional substituents and independently represent C
1-6
alkyl, C
2-6
alkenyl, optionally substituted by CO
2
H or CO
2
(C
1-6
alkyl), C
2-6
alkynyl, halogen, C
1-3
perfluoroalkyl, (CH
2
)
m
Ar
1
, (CH
2
)
m
Het
1
, (CH
2
)
m
CONR
7
R
8
, (CH
2
)
m
CO
2
R
8
, O(CH
2
)
q
CO
2
R
8
, (CH
2
)
m
COR
8
, (CH
2
)
m
OR
8
, O(CH
2
)
p
OR
8
, (CH
2
)
m
NR
7
R
8
, CO
2
(CH
2
)
q
NR
7
R
8
, (CH
2
)
m
CN, S(O)
n
NR
8
, SO
2
NR
7
R
8
, CONH(CH
2
)
m
Ar
1
or CONH(CH
2
)
m
Het
1
; R
3
represents H, C
1-6
alkyl, (CH
2
)
p
NR
9
R
10
, SO
2
R
10
, SO
2
NR
9
R
10
, (CH
2
)
m
CO
2
R
10
, C
2-6
alkenyl, C
2-6
alkynyl (CH
2
)
m
CONR
9
R
10
, (CH
2
)
m
CO
2
R
10
, (CH
2
)
p
CN, (CH
2
)
p
R
10
or (CH
2
)
p
OR
10
; R
4
represents H or C
1-6
alkyl; R
5
represents H or OH; R
6
represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R
7-10
are fully defined herein and may independently represent Ar
2
or Het
2
; Z represents CO
2
H, CONH(tetrazol-5-yl), CONHSO
2
O(C
1-4
alkyl), CO
2
Ar
3
, CO
2
(C
1-6
alkyl), tetrazol-5-yl, CONHSO
2
Ar
3
, CONHSO
2
(CH
2
)
q
Ar
3
or CONHSO
2
(C
1-4
alkyl); Ar
1-3
independently represent phenyl, naphthyl, or an aromatic heterocycle, which groups are optionally fused and optionally substituted; and Het
1
and Het
2
independently represent a non-aromatic heterocycle which is optionally substituted; are useful in the treatment of restenosis, renal failure and pulmonary hypertension.
式（I）的化合物及其药学上可接受的衍生物，其中R1和R2是可选的取代基，且独立地表示C1-6烷基，C2-6烯基，可选地被CO2H或CO2（C1-6烷基）取代的C2-6炔基，卤素，C1-3全氟烷基，（CH2）mAr1，（CH2）mHet1，（CH2）mCONR7R8，（CH2）mCO2R8，O（CH2）qCO2R8，（CH2）mCOR8，（CH2）mOR8，O（CH2）pOR8，（CH2）mNR7R8，CO2（CH2）qNR7R8，（CH2）mCN，S（O）nNR8，SO2NR7R8，CONH（CH2）mAr1或CONH（CH2）mHet1；R3表示H，C1-6烷基，（CH2）pNR9R10，SO2R10，SO2NR9R10，（CH2）mCO2R10，C2-6烯基，C2-6炔基，（CH2）mCONR9R10，（CH2）mCO2R10，（CH2）pCN，（CH2）pR10或（CH2）pOR10；R4表示H或C1-6烷基；R5表示H或OH；R6表示苯环，可选地融合到杂环上，整个基团可选地被取代；R7-10在此完全定义，可以独立地表示Ar2或Het2；Z表示CO2H，CONH（四唑-5-基），CONHSO2O（C1-4烷基），CO2Ar3，CO2（C1-6烷基），四唑-5-基，CONHSO2Ar3，CONHSO2（CH2）qAr3或CONHSO2（C1-4烷基）；Ar1-3独立地表示苯环，萘环或芳香杂环，这些基团可以可选地融合和可选地被取代；Het1和Het2独立地表示可选地被取代的非芳香杂环；在治疗再狭窄，肾衰竭和肺动脉高压方面有用。
