Costunolide derivatives
AssigneeHutchison Medipharma Enterprises Limited
InventorsWei-Guo Su, Hong Jia, Xiaoqiang Yan, Jifeng Duan, Tao Wang, Yu Cai, Weihan Zhang
Life of this patent
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Abstract
Disclosed are methods for inhibiting TNFα expression, IL-1β expression, iNOS expression, and NF-κB activity and methods for treating autoimmune disease, cancer, or atherosclerosis with a compound of the following formula:
Claims21
A method of inhibiting TNFα expression, IL-1β expression, or iNOS expression in a subject in need thereof, comprising administering to the subject an effective amount of a compound of the following formula:
- wherein
- X is CH2;
- Y is NR1R2 or OCONR1R2, or X is C(O) and Y is NR1R2;
- in which R1 is alkyl, cycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl;
- and R2 is H, alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl, or R1, R2, and N to which they are attached, taken together, form a saturated or unsaturated 3-8 membered ring, optionally substituted with R1′, OR2′, NR2′R3′, SR2′, C(O)R2′, CO2R2′, C(O)NR2′R3′, R1′ being alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl, and each of R2′ and R3′, independently, being H, alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl;
- and
- Z is a bond;
- or a pharmaceutically acceptably salt thereof.
A method of inhibiting NF-κB in a subject in need thereof comprising administering to the subject an effective amount of a compound of the following formula:
- wherein
- X is CH2;
- Y is NR1R2 or OCONR1R2 or X is C(O) and Y is NR1R2;
- in which R1 is alkyl, cycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl;
- and R2 is H, alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl, or R1, R2, and N to which they are attached, taken together, form a saturated or unsaturated 3-8 membered ring, optionally substituted with R1′, OR2′, NR2′R3′, SR2′, C(O)R2′, CO2R2′, C(O)NR2′R3′, R1′ being alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl, and each of R2′ and R3′, independently, being H, alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl;
- and
- Z is a bond;
- or a pharmaceutically acceptably salt thereof.
A method of treating autoimmune disease, cancer, or atherosclerosis comprising administering to a subject in need thereof an effective amount of the a compound of the following formula:
- wherein
- X is CH2;
- Y is NR1R2 or OCONR1R2, or X is C(O) and Y is NR1R2;
- in which R1 is alkyl, cycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl;
- and R2, is H, alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl, or R1, R2, and N to which they are attached, taken together, form a saturated or unsaturated 3-8 membered ring, optionally substituted with R1′, OR2′, NR2′R3′, SR2′, C(O)R2′, CO2R2′, C(O)NR2′R3′, R1′ being alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl, and each of R2′ and R3′, independently, being H, alkyl, cycloalkyl, heterocycloalkyl, alkenyl, alkynyl, aryl, or heteroaryl;
- and
- Z is a bond;
- or a pharmaceutically acceptably salt thereof.
Dependencies are inferred from the claim text.