Amide compound, and Pin1 inhibitor, therapeutic agent for inflammatory diseases and therapeutic agent for cancer that use the same
AssigneesHiroshima University, Tokyo University of Pharmacy & Life Sciences, The University of Tokyo
InventorsTomoichiro Asano, Yusuke Nakatsu, Hisanaka Ito, Takayoshi Okabe
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Abstract
The purpose of the invention is to develop, as drug-candidate compounds, a group of novel compounds having the activity of inhibiting functions of Pin1. The invention provides: a compound represented by formula (I) or a salt thereof; and a Pin1 inhibitor, a pharmaceutical composition, a therapeutic or prophylactic agent for inflammatory diseases, a therapeutic or prophylactic agent for cancer, and a therapeutic or prophylactic agent for adiposity that use said compound/salt.
Claims22
A compound represented by Formula (I), or a salt thereof:
- wherein m represents an integer of 0 to 2, and n represents an integer of 0 to 1, provided that 0≤m+n≤2;
- R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted amino group;
- R2 represents an optionally substituted fluorenyl group, a substituted naphthyl group, or an optionally substituted group represented by any one of the following structures:
- R3 represents 0 to 7 identical or different substituents attached to the naphthyl group;
- and
- X represents a single bond, —CH2— group, or —NH— group.
A Pin1 inhibitor comprising a compound represented by Formula (I) or a salt thereof:
- wherein m represents an integer of 0 to 2, and n represents an integer of 0 to 1, provided that 0≤m+n≤2;
- R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted amino group;
- R2 represents an optionally substituted fluorenyl group, a substituted naphthyl group, or an optionally substituted group represented by any one of the following structures:
- R3 represents 0 to 7 identical or different substituents attached to the naphthyl group;
- and
- X represents a single bond, —CH2— group, or —NH— group.
A therapeutic agent for the treatment of an inflammatory disease associated with fibrosis, comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient:
- wherein m represents an integer of 0 to 2, and n represents an integer of 0 to 1, provided that 0≤m+n≤2;
- R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted amino group;
- R2 represents an optionally substituted fluorenyl group, a substituted naphthyl group, or an optionally substituted group represented by any one of the following structures:
- R3 represents 0 to 7 identical or different substituents attached to the naphthyl group;
- and
- X represents a single bond, —CH2— group, or —NH— group.
A therapeutic agent for the treatment of cancer, comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient:
- wherein m represents an integer of 0 to 2, and n represents an integer of 0 to 1, provided that 0≤m+n≤2;
- R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted amino group;
- R2 represents an optionally substituted fluorenyl group, a substituted naphthyl group, or an optionally substituted group represented by any one of the following structures:
- R3 represents 0 to 7 identical or different substituents attached to the naphthyl group;
- and
- X represents a single bond, —CH2— group, or —NH— group.
A therapeutic agent for the treatment of obesity, comprising a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient:
- wherein m represents an integer of 0 to 2, and n represents an integer of 0 to 1, provided that 0≤m+n≤2;
- R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group, or an optionally substituted amino group;
- R2 represents an optionally substituted fluorenyl group, a substituted naphthyl group, or an optionally substituted group represented by any one of the following structures:
- R3 represents 0 to 7 identical or different substituents attached to the naphthyl group;
- and
- X represents a single bond, —CH2— group, or —NH— group.
Dependencies are inferred from the claim text.