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US 2023/0099567 A1Published application
Composition for treatment, prevention, or amelioration of lymphedema
AssigneeRappeler Co., Ltd.
InventorsJin-Mo Ku, Sukchan Lee, Hee Kang
Life of this patent
Estimating the term…
Abstract
Provided are a novel compound exhibiting the effect of treating, preventing or ameliorating lymphedema, and a composition including the same as an active ingredient, and may be applied as a medicament product, functional food or food supplement, or cosmetics. The compound used as an active ingredient compound according to the disclosure exhibits a remarkable ameliorating effect on lymphedema in various aspects such as TNFα production inhibitory activity, metabolic stability, solubility, and blood exposure.
Claims6
A compound of Formula 1 or Formula 2, or a pharmaceutically, food, or cosmetically acceptable salt thereof:
- wherein, in this formula,
- R1 and R2 are each independently one or more selected from a group consisting of —H, —OH, —OR3, —OCOR3, —NO2, —CN, —SH, —SR3, —COR4, —COOR4, —CONHR4, —CON(R4)2, —NH2, —NHR4, —N(R4)2, —NHCOR4, —N(R5)COR4, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, halogen, an allyloxy group, a C3-C7 cycloalkyl group, an allyl group, a heteroallyl group having at least one hetero atom and consisting of 3-7 atoms, and a heterocycloalkyl group having at least one hetero atom and consisting of 3-7 atoms,
- R3 are each independently selected from the group consisting of a C1-C6 alkyl group, a C3-C10 aryl group,
- R6 are each independently one or more selected from the group consisting of —H, —OH, —OR7, —NO2, —CN, a C1-C6 alkyl group, a C1-C6 alkoxy group, halogen, —NH2, —NHR7, and —N(R7)2,
- R7 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- R4 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- R5 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- provided that butein is excluded from the compound of Formula 1;
- wherein, in this formula,
- R8 and R9 are each independently one or more selected from the group consisting of —H, —OH, —OR10, —NO2, —CN, —SH, —SR10, —COR11, —COOR11, —CONHR11, —CON(R11)2, —NH2, —NHR11, —N(R11)2, —NHCOR11, —N(R12)COR11, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, halogen, an allyloxy group, a C3-C7 cycloalkyl group, an allyl group, a heteroallyl group having at least one hetero atom and consisting of 3-7 atoms, and a heterocycloalkyl group having at least one hetero atom and consisting of 3-7 atoms,
- R10 is each independently selected from the group consisting of a C1-C6 alkyl group, a C3-C10 aryl group,
- R13 is each independently one or more selected from the group consisting of —H, —OH, —NO2, —CN, a C1-C6 alkyl group, a C1-C6 alkoxy group, halogen, —NH2, —NHR14, and —N(R14)2,
- R14 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- R11 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group, and
- R12 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group.
12 more elements
A pharmaceutical composition for treating or preventing lymphedema, comprising a compound of Formula 1 or Formula 2, or pharmaceutically acceptable salt thereof:
- wherein, in this formula,
- R1 and R2 are each independently one or more selected from the group consisting of —H, —OH, —OR3, —OCOR3, —NO2, —CN, —SH, —SR3, —COR4, —COOR4, —CONHR4, —CON(R4)2, —NH2, —NHR4, —N(R4)2, —NHCOR4, —N(R5)COR4, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, halogen, an allyloxy group, a C3-C7 cycloalkyl group, an allyl group, a heteroallyl group having at least one hetero atom and consisting of 3-7 atoms, and a heterocycloalkyl group having at least one hetero atom and consisting of 3-7 atoms,
- R3 are each independently selected from the group consisting of a C1-C6alkyl group, a C3-C10 aryl group,
- R6 are each independently one or more selected from the group consisting of —H, —OH, —OR7, —NO2, —CN, a C1-C6 alkyl group, a C1-C6 alkoxy group, halogen, —NH2, —NHR7, and —N(R7)2,
- R7 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- R4 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- R5 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- provided that butein is excluded from the compound of Formula 1;
- [Formula 2]
- wherein, in this formula,
- R8 and R9 are each independently one or more selected from the group consisting of —H, —OH, —OR10, —NO2, —CN, —SH, —SR10, —COR11, —COOR11, —CONHR11, —CON(R11)2, —NH2, —NHR11, —N(R11)2, —NHCOR11, —N(R12)COR11, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, halogen, an allyloxy group, a C3-C7 cycloalkyl group, an allyl group, a heteroallyl group having at least one hetero atom and consisting of 3-7 atoms, and a heterocycloalkyl group having at least one hetero atom and consisting of 3-7 atoms,
- R10 is each independently selected from the group consisting of a C1-C6 alkyl group, a C3-C10 aryl group,
- R13 is each independently one or more selected from the group consisting of —H, —OH, —NO2, —CN, a C1-C6 alkyl group, a C1-C6 alkoxy group, halogen, —NH2, —NHR14, and —N(R14)2,
- R14 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- R11 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group, and
- R12 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group.
13 more elements
A method of treating or preventing lymphedema comprising administering to a subject a compound of Formula 1 or Formula 2, or a pharmaceutically acceptable salt thereof:
- wherein, in this formula,
- R1 and R2 are each independently one or more selected from the group consisting of —H, —OH, —OR3, —OCOR3, —NO2, —CN, —SH, —SR3, —COR4, —COOR4, —CONHR4, —CON(R4)2, —NH2, —NHR4, —N(R4)2, —NHCOR4, —N(R5)COR4, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, halogen, an allyloxy group, a C3-C7 cycloalkyl group, an allyl group, a heteroallyl group having at least one hetero atom and consisting of 3-7 atoms, and a heterocycloalkyl group having at least one hetero atom and consisting of 3-7 atoms,
- R3 are each independently selected from the group consisting of a C1-C6 alkyl group, a C3-C10 aryl group,
- R6 are each independently one or more selected from the group consisting of —H, —OH, —OR7, —NO2, —CN, a C1-C6 alkyl group, a C1-C6 alkoxy group, halogen, —NH2, —NHR7, and —N(R7)2,
- R7 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- R4 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- R5 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- provided that butein is excluded from the compound of Formula 1;
- wherein, in this formula,
- R8 and R9 are each independently one or more selected from the group consisting of —H, —OH, —OR10, —NO2, —CN, —SH, —SR10, —COR11, —COOR11, —CONHR11, —CON(R11)2, —NH2, —NHR11, —N(R11)2, —NHCOR11, —N(R12)COR11, a C1-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, halogen, an allyloxy group, a C3-C7 cycloalkyl group, an allyl group, a heteroallyl group having at least one hetero atom and consisting of 3-7 atoms, and a heterocycloalkyl group having at least one hetero atom and consisting of 3-7 atoms,
- R10 is each independently selected from the group consisting of a C1-C6 alkyl group, a C3-C10 aryl group,
- R13 is each independently one or more selected from the group consisting of —H, —OH, —NO2, —CN, a C1-C6 alkyl group, a C1-C6 alkoxy group, halogen, —NH2, —NHR14, and —N(R14)2,
- R14 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group,
- R11 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group, and
- R12 is selected from the group consisting of a C1-C6 alkyl group, an allyl group, and a heteroallyl group.
12 more elements
Dependencies are inferred from the claim text.