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1. WO2020109297 - COMPOUNDS FOR THE TREATMENT OF NF-KB–RELATED DISEASES OR DISORDERS

Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

[ EN ]

CLAIMS

1. Compound of formula (I)


wherein

R1 is selected from -C(=0)0Ra, -C(=0)NHRa, -C(=0)N(Ra)2, -C(=0)Ra, and -CH2ORa,

wherein each Ra is independently selected from hydrogen, and substituted or unsubstituted alkyl, alkenyl or alkynyl group;

R2 is selected from Rc, -ORc, -NHRC and -N(RC)2,

wherein each Rc is independently selected from hydrogen, and substituted or unsubstituted alkyl, alkenyl or alkynyl group;

R3, R4 and R5 are each independently selected from substituted or unsubstituted alkyl, alkenyl and alkynyl group;

X is H or halogen;

or a pharmaceutically acceptable salt, stereoisomer, or solvate thereof;

for use in the treatment of a NF-KB-related disease or disorder, with the proviso that the disease or disorder is not cancer.

2. The compound for use according to claim 1 , wherein R1 is -C(=0)0Ra, and Ra is as defined in claim 1.

3. The compound for use according to any preceding claim, wherein R2 is - ORc, and Rc is as defined in claim 1.

4. The compound for use according to any preceding claim, wherein R3 is selected from substituted or unsubstituted Ci-6 alkyl, C2-6 alkenyl and C2-6 alkynyl.

5. The compound for use according to any preceding claim, wherein R4 is selected from substituted or unsubstituted C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl.

6. The compound for use according to any preceding claim, wherein R5 is selected from substituted or unsubstituted C3-9 alkyl, C3-9 alkenyl and C3-9 alkynyl.

7. The compound for use according to any preceding claim, wherein X is halogen.

8. The compound for use according to any preceding claim, which is


or a pharmaceutically acceptable salt, stereoisomer, or solvate thereof.

9. The compound for use according to any preceding claim, which is

or a pharmaceutically acceptable salt or solvate thereof.

10. The compound for use according to any preceding claim, wherein the NF- kB-related disease or disorder is an inflammatory or autoimmune disease or disorder.

11. The compound for use according to any preceding claim, wherein the NF- kB-related disease or disorder is selected from rheumatoid arthritis; multiple sclerosis; asthma; inflammatory bowel disease; colonic inflammation; chronic obstructive pulmonary disease; diabetes and obesity, in particular diabetes- or obesity-associated inflammation; transplantation rejection, in particular GVFID; liver injury and liver fibrosis; dermatitis; systemic lupus erythematosus; and psoriasis.

12. The compound for use according to claim 11 , wherein the NF-KB-related disease or disorder is selected from rheumatoid arthritis, multiple sclerosis, asthma, inflammatory bowel disease, transplantation rejection, psoriasis, dermatitis, systemic lupus erythematosus and type 2 diabetes.

13. The compound for use according to claim 11 , wherein the NF-KB-related disease or disorder is rheumatoid arthritis or multiple sclerosis.

14. The compound for use according to claim 11 , wherein the NF-KB-related disease or disorder is rheumatoid arthritis.

15. The compound for use according to claim 11 , wherein the NF-KB-related disease or disorder is multiple sclerosis.