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US 6,713,449 B1Granted
E2F activity inhibitory compounds
AssigneeKyowa Hakko Kogyo Co., Ltd.
InventorsKenji Shibata, Motoo Yamasaki, Tetsuo Yoshida, Tamio Mizukami
Life of this patent
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Abstract
E2F-inhibiting compounds are represented by the formula: R1—A—R2 wherein A represents a peptide sequence comprising a partial amino acid sequence having at least 12 continuous residues in the sequence of the dimerization region or DNA binding region of the E2F family, which are useful as a therapeutic agent of diseases such as tumor and arteriosclerosis, for which abnormal cellular growth is implicated.
Claims6
A compound represented by the formula (I):
- R1—A—R2 (I)
- wherein R1 represents substituted or unsubstituted alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroarylcarbonyl, substituted or unsubstituted alkoxycarbonyl, substituted or unsubstituted aryloxycarbonyl, or substituted or unsubstituted heteroaryloxycarbonyl;
- R2 represents substituted or unsubstituted alkoxy, or substituted or unsubstituted amino;
- and
- A represents a peptide sequence comprising 12 continuous residues in the sequence of the dimerization region or DNA binding region of each E2F family, or a pharmaceutically acceptable salt thereof.
2 more elements
A compound represented by the formula (I):
- R1—A—R2 (I)
- wherein R1 represents substituted or unsubstituted alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroarylcarbonyl, substituted or unsubstituted alkoxycarbonyl, substituted or unsubstituted aryloxycarbonyl, substituted or unsubstituted heteroaryloxycarbonyl or a hydrogen atom;
- R2 represents hydroxy, substituted or unsubstituted alkoxy, or substituted or unsubstituted amino;
- and
- A represents a peptide sequence that is at least 12 continuous residues from the dimerization region or DNA binding region of each E2F family, with the proviso that said peptide sequence is not an intact protein which is a member of E2F family or DP family, or
- a pharmaceutically acceptable salt thereof.
3 more elements
A compound represented by the formula (I):
- R1—A—R2 (I)
- wherein R1 represents substituted or unsubstituted alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroarylcarbonyl, substituted or unsubstituted alkoxycarbonyl, substituted or unsubstituted aryloxycarbonyl, substituted or unsubstituted heteroaryloxycarbonyl or a hydrogen atom;
- R2 represents substituted or unsubstituted alkoxy, or substituted or unsubstituted amino;
- and
- A represents a peptide sequence comprising 12 continuous residues in the sequence of the dimerization region or DNA binding region of each E2F family, or
- a pharmaceutically acceptable salt thereof.
3 more elements
A compound represented by the formula (I):
- R1—A—R2 (I)
- wherein R1 represents substituted or unsubstituted alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroarylcarbonyl, substituted or unsubstituted alkoxycarbonyl, substituted or unsubstituted aryloxycarbonyl, or substituted or unsubstituted heteroaryloxycarbonyl;
- R2 represents hydroxy, substituted or unsubstituted alkoxy, or substituted or unsubstituted amino;
- and
- A represents a peptide sequence comprising 12 continuous residues in the sequence of the dimerization region or DNA binding region of each E2F family, or
- a pharmaceutically acceptable salt thereof.
3 more elements
Dependencies are inferred from the claim text.