发明名称 PAR-2 agonist
摘要 The present invention relates to a pharmaceutical composition for preventing/treating conditions associated with PAR-2. The present invention also relates to a method for preventing/treating the condition using the pharmaceutical composition and use for manufacturing the pharmaceutical composition. The pharmaceutical composition comprises a compound represented by the following general formula (1), salt or solvate thereof and a pharmaceutically acceptable carrier: Ar—CO—AA1—AA2—AA3—AA4—NH—X—Y (1) wherein, Ar represents a phenyl group or an aromatic heterocyclic group optionally having substituent(s): AA1 represents a hydrophobic amino acid: AA2 represents an amino acid absent of substituent(s) having more than two carbon atoms: AA3 represents an amino acid absent of substituent(s) having more than two carbon atoms: AA4 represents a basic amino acid: X represents a straight chain or branched bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms: Y represents basic substituent(s); straight chain, branched, or cyclic bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms; or an aromatic hydrocarbon group having 6 to 10 carbon atoms. The compound represented by the general formula (1) has dramatically improved PAR-2 activation potency compared to peptide comprised of 6 amino acids (Tethered receptor agonist peptide: TRAP) in spite of reduction of the number of amino acid.
申请公布号 US8133864(B2) 申请公布日期 2012.03.13
申请号 US20060909931 申请日期 2006.03.29
申请人 ISHIWATA HIROYUKI;KABEYA MOTOTSUGU;KANKE TORU;KOWA COMPANY, LTD. 发明人 ISHIWATA HIROYUKI;KABEYA MOTOTSUGU;KANKE TORU
分类号 A61K38/08;C07K5/083;C07K5/087 主分类号 A61K38/08
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