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COMPOUNDS FOR THE TREATMENT OF NF-KB-RELATED DISEASES OR DISORDERSCM Patents

Índice de la ficha

Updated at
24/07/2026
Numero publicacion
EP.3656762.A1
Fecha publicacion
27/05/2020
Numero solicitud
EP20180382856
Fecha presentacion
26/11/2018

En detalle

Resumen

[0001] The invention relates to a family of fungal compounds which are inhibitors of NF-κB inducing kinase and are thus useful in the treatment of NF-κB-related diseases or disorders such as inflammatory or autoimmune diseases or disorders.

Reivindicaciones

1. Compound of formula (I) <img class="EMIRef" id="655143965-ib0006" /> wherein R<1> is selected from -C(=O)OR<a>, -C(=O)NHR<a>, -C(=O)N(R<a>)<2>, -C(=O)R<a>, and-CH<2>OR<a>, wherein each R<a> is independently selected from hydrogen, and substituted or unsubstituted alkyl, alkenyl or alkynyl group; R<2> is selected from R<c>, -OR<c>, -NHR<c> and -N(R<c>)<2>, wherein each R<c> is independently selected from hydrogen, and substituted or unsubstituted alkyl, alkenyl or alkynyl group; R<3>, R<4> and R<5> 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-κB-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 R<1> is -C(=O)OR<a>, and R<a> is as defined in claim 1. 3. The compound for use according to any preceding claim, wherein R<2> is-OR<c>, and R<c> is as defined in claim 1. 4. The compound for use according to any preceding claim, wherein R<3> is selected from substituted or unsubstituted C<1-6> alkyl, C<2-6> alkenyl and C<2-6> alkynyl. 5. The compound for use according to any preceding claim, wherein R<4> is selected from substituted or unsubstituted C<1-6> alkyl, C<2-6> alkenyl and C<2-6> alkynyl. 6. The compound for use according to any preceding claim, wherein R<5> is selected from substituted or unsubstituted C<3-9> alkyl, C<3-9> alkenyl and C<3-9> 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 <img class="EMIRef" id="655143965-ib0007" /> or a pharmaceutically acceptable salt, stereoisomer, or solvate thereof. 9. The compound for use according to any preceding claim, which is <img class="EMIRef" id="655143965-ib0008" /> or a pharmaceutically acceptable salt or solvate thereof. 10. The compound for use according to any preceding claim, wherein the NF-κB-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-κB-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 GVHD; liver injury and liver fibrosis; dermatitis; systemic lupus erythematosus; and psoriasis. 12. The compound for use according to claim 11, wherein the NF-κB-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-κB-related disease or disorder is rheumatoid arthritis or multiple sclerosis. 14. The compound for use according to claim 11, wherein the NF-κB-related disease or disorder is rheumatoid arthritis. 15. The compound for use according to claim 11, wherein the NF-κB-related disease or disorder is multiple sclerosis.

Etiquetas

Inventores
Fernández Medarde AntonioVinuesa Navarro María de los ÁngelesSánchez López José MaríaCañedo Hernández Librada MaríaFresno Escudero ManuelSánchez -Valdepeñas Villegas Carmen María
Solicitantes
Inst Biomar SaUniversidad Autónoma de Madrid
Clasificacion ipc
A61K 31/ 403 A IA61P 29/ 00 A IC07D 209/ 52 A I
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