Invention Application
- Patent Title: INHIBITORS OF IKK-BETA SERINE-THERONINE PROTEIN KINASE
- Patent Title (中): IKK-BETA丝氨酸蛋白激酶激酶的抑制剂
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Application No.: US12989022Application Date: 2008-04-23
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Publication No.: US20110039920A1Publication Date: 2011-02-17
- Inventor: David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Jonathon Gareth Williams , Stuart Thomas Onions
- Applicant: David Festus Charles Moffat , Stephen John Davies , Michael Hugh Charlton , Simon Christopher Hirst , Jonathon Gareth Williams , Stuart Thomas Onions
- Applicant Address: GB Abingdon, Oxfordshire
- Assignee: CHROMA THERAPEUTICS LTD.
- Current Assignee: CHROMA THERAPEUTICS LTD.
- Current Assignee Address: GB Abingdon, Oxfordshire
- International Application: PCT/GB2008/001434 WO 20080423
- Main IPC: A61K31/381
- IPC: A61K31/381 ; C07D333/38 ; C12N9/99 ; A61P35/00 ; A61P37/06 ; A61P29/00 ; A61P19/02 ; A61P3/10 ; A61P11/06 ; A61P1/04 ; A61P25/28

Abstract:
Cyclopentyl(2S,4E)-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,4E)-2-amino-5-{3-[4-carbamoyl-5-(carbamoylamino)-2-thienyl]-5-methylphenyl}pent-4-enoate; Cyclopentyl(25,4E)-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-thienyl]phenyl}-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.
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