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DRUGS FOR INHIBITING P38 AND USES THEREOFCM Patents

Índice de la ficha

Updated at
24/07/2026
Numero publicacion
EP.2774613.A1
Fecha publicacion
10/09/2014
Numero solicitud
EP20120846045

En detalle

Resumen

[0001] The invention relates to the use thereof in the treatment of the disease which shows the disease, which is relieved by suppressing the activation of the compound and p38 MAPK or the biological activity for example, the inflammation disease or the pain having the benzoxadiazolyl amine structure suppressing the activation or the biological activity of the p38 mitogen activated protein kinase (MAPK; the mitogen-activated protein kinase).

Reivindicaciones

1. Use of a compound of formula (I): <img class="EMIRef" id="468680164-ib0020" /> where n represents 0 or 1; X represents -CH<2> - or -C(O)-; R<1> and R<2> are independently selected from the group consisting of H, halogen, NO<2> , CF<3> and CN; R<3> and R<6> are independently selected from the group consisting of halogen, OH, optionally substituted C<1> -C<6> alkyl, optionally substituted C<1> -C<6> alkoxy, C<1-6> haloalkyl, NH<2> , NO<2> and CN; R<4> , R<5> and R<7> are independently selected from the group consisting of H, halogen, OH, optionally substituted C<1> -C<6> alkyl, optionally substituted C<1> -C<6> alkoxy, C<1-6> haloalkyl, NH<2> , NO<2> and CN; or a salt or solvate thereof, in the preparation of a medicinal product. 2. Use according to claim 1, where n is 0. 3. Use according to any of the preceding claims, where R<4> , R<5> and R<7> are independently selected from the group consisting of H, halogen, OH, methyl, methoxy, CF<3> , NH<2> , NO<2> and CN. 4. Use according to claim 3, where at least one of R<4> , R<5> and R<7> is H. 5. Use according to claim 4, where R<7> is H. 6. Use according to any of the preceding claims, where R<1> and R<2> are independently selected from the group consisting of H, Cl, NO<2> and CF<3> . 7. Use according to claim 6, where at least one of R<1> and R<2> is NO<2> . 8. Use according to any of the preceding claims, where R<3> and R<6> are independently selected from the group consisting of halogen, OH, methyl, methoxy, CF<3> , NH<2> , NO<2> and CN. 9. Use according to any of the preceding claims, where the compound of formula (I) is a compound of formula (Ia): <img class="EMIRef" id="468680164-ib0021" /> where n, X, R<1> -R<7> are as defined in claims 1 to 8, or a salt or solvate thereof. 10. Use according to any of claims 1 to 8, where the compound of formula (I) is a compound of formula (Ib): <img class="EMIRef" id="468680164-ib0022" /> where n, X, R<1> -R<7> are as defined in claims 1 to 8, or a salt or solvate thereof. 11. Use according to claim 9, where the compound of formula (Ia) is selected from the group consisting of: <img class="EMIRef" id="468680164-ib0023" /> and or a salt or solvate thereof. 12. Use according to claim 10, where the compound of formula (Ib) is selected from the group consisting of: <img class="EMIRef" id="468680164-ib0024" /> or a salt or solvate thereof. 13. Use according to any of the preceding claims in the preparation of a medicinal product for the prevention and/or treatment of a p38 MAPK-regulated disease. 14. Use according to claim 13, where the p38 MAPK regulated disease is an inflammatory disease, a heart disease, cancer, a neurodegenerative disease, a metabolic disease and/or pain. 15. Use according to claim 14, where the pain is selected from inflammatory pain, neuropathic pain, pain associated with neurodegeneration and pain associated with multiple sclerosis. 16. Use according to claim 14, where the metabolic disease is obesity or diabetes. 17. Use according to claim 14, where the neurodegenerative disease is multiple sclerosis or amyotrophic lateral sclerosis. 18. A pharmaceutical composition comprising a compound of formula (I) as defined in claims 1 to 12, or a salt or solvate thereof, and a pharmaceutically acceptable carrier. 19. A compound of formula (I) <img class="EMIRef" id="468680164-ib0025" /> where n represents 0 or 1; X represents -CH<2> - or -C(O)-; R<1> and R<2> are independently selected from the group consisting of H, halogen, NO<2> , CF<3> and CN; R<3> and R<6> are independently selected from the group consisting of halogen, OH, optionally substituted C<1> -C<6> alkyl, optionally substituted C<1> -C<6> alkoxy, C<1-6> haloalkyl, NH<2> , NO<2> and CN; R<4> , R<5> and R<7> are independently selected from the group consisting of H, halogen, OH, optionally substituted C<1> -C<6> alkyl, optionally substituted C<1> -C<6> alkoxy, C<1-6> haloalkyl, NH<2> , NO<2> and CN; or a salt or solvate thereof, with the proviso that the compound of formula (I) is not (5-chloro-2-methyl-phenyl)-(7-chloro-4-nitro-benzo[1,2,5]oxadiazol-5-yl)-amine or (7-chloro-4-nitro-benzo[1,2,5]oxadiazol-5-yl)-(2,5-dimethyl-phenyl)-amine. 20. The compound according to claim 19, where the compound of formula (I) is a compound of formula (Ia) <img class="EMIRef" id="468680164-ib0026" /> where n, X, R<1> -R<7> are as defined in claim 19, or a salt or solvate thereof. 21. The compound according to claim 20, where the compound of formula (Ia) is a compound of formula (Ia') <img class="EMIRef" id="468680164-ib0027" /> where n, X, R<1> -R<7> are as defined in claim 20, or a salt or solvate thereof. 22. The compound according to any of claims 19 to 21, where n is 0. 23. The compound according to any of claims 19 to 22, where R<4> , R<5> and R<7> are independently selected from the group consisting of H, halogen, OH, methyl, methoxy, CF<3> , NH<2> , NO<2> and CN. 24. The compound according to claim 23, where at least one of R<4> , R<5> and R<7> is H. 25. The compound according to claim 24, where R<7> is H. 26. The compound according to any of claims 19 to 25, where R<1> and R<2> are independently selected from the group consisting of H, Cl, NO<2> and CF<3> . 27. The compound according to claim 26, where R<1> is NO<2> or chlorine. 28. The compound according to any of claims 26 to 27, where R<2> is H. 29. The compound according to any of claims 19 to 28, where R<3> and R<6> are independently selected from the group consisting of halogen, OH, methyl, methoxy, CF<3> , NH<2> , NO<2> and CN. 30. The compound according to any of claims 19 to 29, where the compound of formula (I) is selected from the group consisting of: <img class="EMIRef" id="468680164-ib0028" /> and or a salt or solvate thereof.

Etiquetas

Inventores
Mayor Menendez FedericoMurga Montesinos CristinaCampos Muelas Pedro ManuelHeijnen Jacoba JohanaKavelaars Anna Maria Agnes AntoniusMorreale de Leon AntonioGil Redondo RubenAnna Maria Agnes Antonius KavelaarsAntonio Morreale de LeónCristina Murga MontesinosFederico Mayor MéndezJacoba Johana HeijnenPedro Manuel Campos MuelasRubén Gil RedondoMayor Menéndez FedericoMorreale de León AntonioGil Redondo RubénHeijnen Jacoba Johannaフェデリコ、マヨール、メネンデスクリスティーナ、ムルガ、モンテシノスペドロ、マヌエル、カンポス、ムエラスヤコバ、ヨハナ、エイジネンアナ、マリナ、アグネス、アントニウス、カベラールスアントニオ、モレアレ、デ、レオンルーベン、ヒル、レドンドMayor Ménendez FedericoMayor Mendez Federico
Solicitantes
Universidad Autónoma de Madridウニベルシダッド・アウトノマ・デ・マドリッド
Clasificacion ipc
A61K 31/ 4245 A IC07D 271/ 12 A IA61P 21/ 02 A IA61P 25/ 00 A IA61P 25/ 04 A IA61P 29/ 00 A IA61P 3/ 00 A IA61P 3/ 04 A IA61P 3/ 10 A IA61P 35/ 00 A IA61P 43/ 00 A IA61P 9/ 00 A IC07D 271/ 08 A I
Clasificacion cpc
4C056/AA014C056/AB024C056/AC044C056/AD034C056/AE034C056/AF014C086/AA014C086/AA024C086/AA034C086/BC714C086/MA014C086/MA044C086/NA144C086/ZA024C086/ZA084C086/ZA364C086/ZA704C086/ZA944C086/ZB114C086/ZB264C086/ZC204C086/ZC214C086/ZC35A61K31/4245A61P21/02A61P25/00A61P25/04A61P29/00A61P3/00A61P3/04A61P3/10A61P35/00A61P43/00&111A61P9/00C07D271/08
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