发明公开
EP0230110A1 Pharmacologically active pyrrole and pyrazole derivatives
失效
Pharmakologisch aktive Pyrrol- und Pyrazolderivate。
- 专利标题： Pharmacologically active pyrrole and pyrazole derivatives
- 专利标题（中）： Pharmakologisch aktive Pyrrol- und Pyrazolderivate。
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申请号： EP86309235.9申请日： 1986-11-26
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公开(公告)号： EP0230110A1公开(公告)日： 1987-07-29
- 发明人: Baxter, Andrew John Gilby , Dixon, John , Ince, Francis , Springthorpe, Brian , Tinker, Alan Charles
- 申请人： FISONS plc
- 申请人地址： Fison House Princes Street Ipswich Suffolk IP1 1QH GB
- 专利权人： FISONS plc
- 当前专利权人： FISONS plc
- 当前专利权人地址： Fison House Princes Street Ipswich Suffolk IP1 1QH GB
- 代理机构： Craig, Christopher Bradberry
- 优先权： GB8529557 19851130; GB8529558 19851130; GB8529563 19851130; GB8529564 19851130; GB8610218 19860425; GB8616096 19860702; GB8616097 19860702; GB8616100 19860702; GB8616101 19860702; GB8616102 19860702; GB8616103 19860702; GB8621942 19860911
- 主分类号： C07D207/337
- IPC分类号： C07D207/337 ; C07D231/14 ; C07D401/06 ; C07D413/06 ; A61K31/395
摘要：
There are described compounds of formula I,
wherein
either one of Y and Z (which may be the same or different) represents CH, CR 2 or C-COOR 21 , in which R 2 represents alkyl C 1 to C6 optionally substituted by halogen, hydroxy, amino, isothioureido or a group R 5 COO- in which R 5 represents alkyl C 1 to C6, R 2 being optionally interrupted by O or S, and R 21 represents alkyl C 1 to C6, and the other one of Y and Z represents CR 2 or C-COOR 21 ,
or one of Y and Z represents N and the other CH, CR 2 or C-COOR 21 ,
R 4 represents Ar 1 -B-(W) x , in which
W represents C=O, S, SO, SO 2 or C=N-OH,
x represents 0 or 1,
B represents a single bond or (CH 2 )p in which p represents 1 or 2, the group (CH 2 )p being optionally substituted by alkyl C1 to
Ar 1 represents phenyl, naphthyl or benzofurazanyl, Ar 1 being optionally substituted by one or more of X, CX 3 , OCH n X 3-n , hydroxy, alkyl C 1 to C6, Oalkyl C 1 to C6, nitro, amino, carboxy, -SCH 2 Ar 2 , -OCH 2 Ar 2 or -OCOAr 2 in which
X represents halogen,
n represents 0,1, 2 or 3, and
Ar 2 represents phenyl or phenyl substituted by hydroxy, halogen, alkyl C 1 to C6 or Oalkyl C 1 to C6, and
R 3 and R 1 are as defined in the specification.
There are also described processes for the preparation of compounds of formula I and pharmaceutical, eg cardiovascular, compositions containing them.
wherein
either one of Y and Z (which may be the same or different) represents CH, CR 2 or C-COOR 21 , in which R 2 represents alkyl C 1 to C6 optionally substituted by halogen, hydroxy, amino, isothioureido or a group R 5 COO- in which R 5 represents alkyl C 1 to C6, R 2 being optionally interrupted by O or S, and R 21 represents alkyl C 1 to C6, and the other one of Y and Z represents CR 2 or C-COOR 21 ,
or one of Y and Z represents N and the other CH, CR 2 or C-COOR 21 ,
R 4 represents Ar 1 -B-(W) x , in which
W represents C=O, S, SO, SO 2 or C=N-OH,
x represents 0 or 1,
B represents a single bond or (CH 2 )p in which p represents 1 or 2, the group (CH 2 )p being optionally substituted by alkyl C1 to
Ar 1 represents phenyl, naphthyl or benzofurazanyl, Ar 1 being optionally substituted by one or more of X, CX 3 , OCH n X 3-n , hydroxy, alkyl C 1 to C6, Oalkyl C 1 to C6, nitro, amino, carboxy, -SCH 2 Ar 2 , -OCH 2 Ar 2 or -OCOAr 2 in which
X represents halogen,
n represents 0,1, 2 or 3, and
Ar 2 represents phenyl or phenyl substituted by hydroxy, halogen, alkyl C 1 to C6 or Oalkyl C 1 to C6, and
R 3 and R 1 are as defined in the specification.
There are also described processes for the preparation of compounds of formula I and pharmaceutical, eg cardiovascular, compositions containing them.
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