发明公开
- 专利标题： INHIBITORS OF IKK- SERINE-THREONINE PROTEIN KINASE
- 专利标题（中）： IKK-丝氨酸 - 苏氨酸蛋白激酶的抑制剂
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申请号： EP08737089.6申请日： 2008-04-23
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公开(公告)号： EP2297128A1公开(公告)日： 2011-03-23
- 发明人: MOFFAT, David, Festus, Charles , DAVIES, Stephen, John , CHARLTON, Michael, Hugh , HIRST, Simon, Christopher , ONIONS, Stuart, Thomas , WILLIAMS, Jonathon, Gareth
- 申请人： Chroma Therapeutics Ltd.
- 申请人地址： 93 Milton Park Abingdon Oxfordshire OX14 4RY GB
- 专利权人： Chroma Therapeutics Ltd.
- 当前专利权人： Chroma Therapeutics Ltd.
- 当前专利权人地址： 93 Milton Park Abingdon Oxfordshire OX14 4RY GB
- 代理机构： Walls, Alan James
- 国际公布： WO2009130434 20091029
- 主分类号： C07D333/38
- IPC分类号： C07D333/38 ; A61K31/381 ; A61P25/28 ; A61P37/00
摘要：
Cyclopentyl (2S,4
E )-2-amino-5-{3-[4-carbamoyl-5 (carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl (2S,4
E )-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl (2S,4
E )-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl
O -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl
O -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienylJphenyl}-L-homoserinate; Cyclopentyl
N -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and
tert -Butyl
N -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity.
E )-2-amino-5-{3-[4-carbamoyl-5 (carbamoylamino)-2-thienyl]phenyl}pent-4-enoate; Cyclopentyl 5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-norvalinate; Cyclopentyl (2S,4
E )-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl (2S,4
E )-2-amino-5-{5-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-2-methylphenyl}pent-4-enoate; Cyclopentyl
O -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]phenyl}-L-homoserinate; Cyclopentyl
O -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienylJphenyl}-L-homoserinate; Cyclopentyl
N -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate; and
tert -Butyl
N -{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]benzyl}-L-alaninate are hydrolysed to the corresponding carboxylic acids by intracellular carboxylesterases, and are useful for the inhibition of IKKβ activity.
公开/授权文献
- EP2297128B1 INHIBITORS OF IKK- SERINE-THREONINE PROTEIN KINASE 公开/授权日：2012-08-15
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