发明名称 |
N-(Isoxazol-5-yl)-sulfonamide derivatives and their use as endothelin antagonists |
摘要 |
<p>Isoxazoles of formula (I) below have good affinity for endothelin receptors, and are selective for ETA over ETB. <CHEM> wherein R<1> is either a)a phenyl group; or b)an optionally benzo-fused 5- or 6-membered heterocyclic group with one to three heteroatoms in the heterocyclic ring, which heteroatoms are independently selected from N, O and S; or CHR<6>CHR<7>Ph, CR<6>:CR<7>Ph; each of which groups (a) (b) and (c) is optionally substituted by up to three substituents each independently selected from: i)halo; ii)C1-6 alkyl optionally substituted by OH, halogen, NR<4>R<5> OCOR<4> or CO2R<4>; iii)CN; iv)O(C1-8 alkyl optionally substituted by one or more halogen); and v)CO2R<4>; R<2> is aryl<1> or het<1>, R<3> is H, C1-6 alkyl, C(O)R<4>, CONHaryl<1>, CONHhet<1>, aryl<1> and het<1> Such compounds are useful in the treatment of conditions mediated by endothelin.</p> |
申请公布号 |
EP1160248(A1) |
申请公布日期 |
2001.12.05 |
申请号 |
EP20010304626 |
申请日期 |
2001.05.25 |
申请人 |
PFIZER INC.;PFIZER LIMITED |
发明人 |
BANKS, BERNARD JOSEPH;CHUBB, NATHAN ANTHONY LOGAN;ESHELBY, JAMES JOHN;PACEY, MICHAEL STEPHEN;SCHULZ, DARREN JOHN |
分类号 |
A61P9/12;C07D413/14;A61K31/506;A61P7/04;A61P9/10;A61P11/00;A61P11/08;A61P13/08;A61P13/12;A61P15/10;A61P25/00;A61P27/06;A61P35/00;A61P37/08;A61P43/00;C07D231/52;C07D401/12;C07D403/12;C07D403/14;C07D405/04;C07D405/14;C07D409/04;C07D409/14;(IPC1-7):C07D413/14;A61K31/415 |
主分类号 |
A61P9/12 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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