USE OF MALEIMIDE DERIVATIVES FOR PREVENTING AND TREATING CANCER

The present invention is related to a compound of formula (I) a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, a metabolite thereof or a prodrug thereof; for use in a method for the treatment and/or prevention of cancer, wherein X is selected from the group consisting of N-R1, O and S; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl, arylalkyl and hydrogen; R2 is selected from the group consisting of indolyl, substituted indolyl, azaindolyl and substituted azaindolyl; and R3 is selected from the group consisting of aryl, substituted aryl, unsubstituted heteroaryl, heterocyclyl and substituted heterocyclyl.

Use of maleimide derivatives for preventing and treating leukemia

The present invention is related to a compound of formula (I): a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, a metabolite thereof or a prodrug thereof; for use in a method for the treatment and/or prevention of leukemia, wherein X is selected from the group consisting of N—R 1 , O and S; R 1 is selected from the group consisting of alkyl, cycloalkyl, aryl, arylalkyl and hydrogen; R 2 is selected from the group consisting of indolyl, substituted indolyl, azaindolyl and substituted azaindolyl; and R 3 is selected from the group consisting of aryl, substituted aryl, unsubstituted heteroaryl, heterocyclyl and substituted heterocyclyl.

Use of maleimide derivatives for preventing and treating cancer

The present invention is related to a compound of formula (I) a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, a metabolite thereof or a prodrug thereof; for use in a method for the treatment and/or prevention of cancer, wherein X is selected from the group consisting of N—R 1 , O and S; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl, arylalkyl and hydrogen; R 2 is selected from the group consisting of indolyl, substituted indolyl, azaindolyl and substituted azaindolyl; and R 3 is selected from the group consisting of aryl, substituted aryl, unsubstituted heteroaryl, heterocyclyl and substituted heterocyclyl.

Use of Maleimide Derivatives for Preventing and Treating Cancer

The present invention is related to a compound of formula (I): 1102-. (canceled)104. The method of claim 103 , wherein the compound is 3-(4-acetylphenyl)-4-(2-methyl-1H-indol-3-yl)-1H-pyrrole-2 claim 103 ,5-dione.105. The method of claim 103 , further comprising administering a second therapeutic agent claim 103 , wherein the second therapeutic agent is a chemotherapeutic agent.106vinca. The method of claim 105 , wherein the chemotherapeutic agent is selected from the group consisting of cytarabine claim 105 , etoposide claim 105 , mitoxantron claim 105 , cyclophosphamide claim 105 , retinoic acid claim 105 , daunorubicin claim 105 , doxorubicin claim 105 , idarubicin claim 105 , azacytidine claim 105 , decitabine claim 105 , a tyrosine-kinase inhibitor claim 105 , a antineoplastic antibody claim 105 , alkaloids and steroids.107. The method of claim 106 , wherein the chemotherapeutic agent is a tyrosine kinase inhibitor claim 106 , wherein the tyrosine kinase inhibitor is selected from the group consisting of sorafenib claim 106 , dasatinib claim 106 , nilotinib claim 106 , nelarabine and fludarabine claim 106 , or wherein the chemotherapeutic agent is alemtuzumab.108. The method of claim 103 , wherein the compound has an antiproliferative effect on cells of the cancer. The present invention relates to a chemical compound of formula (I), its use in the treatment of a disease, a pharmaceutical composition comprising the compound, and a method for the treatment of a disease.Cancer is the second leading cause of death in many countries, exceeded only by heart disease. Despite recent advances in cancer diagnosis and treatment, surgery and radiotherapy may be curative if a cancer is found early, but current drug therapies for metastatic disease are mostly palliative and seldom offer a long-term cure. Even with new chemotherapies entering the market, the need continues for new drugs effective in monotherapy or in combination with existing agents as first line therapy, and ...

USE OF MALEIMIDE DERIVATIVES FOR PREVENTING AND TREATING LEUKEMIA

The present invention is related to a compound of formula (I): a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, a metabolite thereof or a prodrug thereof; for use in a method for the treatment and/or prevention of leukemia, wherein X is selected from the group consisting of N—R, O and S; Ris selected from the group consisting of alkyl, cycloalkyl, aryl, arylalkyl and hydrogen; Ris selected from the group consisting of indolyl, substituted indolyl, azaindolyl and substituted azaindolyl; and Ris selected from the group consisting of aryl, substituted aryl, unsubstituted heteroaryl, heterocyclyl and substituted heterocyclyl. 2. The compound of claim 1 , wherein{'sup': '2', 'Rcomprises one, two, three, four, five or six substituents, whereby each and any of the substituents is individually and independently selected from the group comprising halogen, alkyl, alkenyl, alkynyl, acyl, formyl, cycloalkyl, aryl, haloalkyl, polyfluoroalkyl, alkylthio, arylthio, monoalkylamino, dialkylamino, monoarylamino, diarylamino, alkylarylamino, alkylimido, hydroxy, alkoxy, aryloxy, carboxyl, alkoxycarbonyl, aryloxycarbonyl, cyano, amino, amido, acylamino, nitro, alkylsulfinyl, arylsulfinyl, alkylsulfonyl, arylsulfonyl, alkylsulfinamido, arylsulfinamido, alkylsulfonamido and arylsulfonamido.'}3. The compound of any one of to claim 1 , wherein{'sup': '3', 'Rcomprises one, two, three, four, five, six or seven substituents, whereby each and any of the substituents is individually and independently selected from the group comprising hydrogen, alkyl, alkenyl, alkynyl, aryl, acyl, formyl, halogen, haloalkyl, alkylthio, monoalkylamino, dialkylamino, monoarylamino, diarylamino, alkylarylamino, hydroxy, alkoxy, aryloxy, carboxyl, alkoxycarbonyl, aryloxycarbonyl, cyano, amino, amido, acylamino, nitro, alkylsulfinyl, arylsulfinyl, alkylsulfonyl, arylsulfonyl, alkylsulfinamido, arylsulfinamido, alkylsulfonamido and arylsulfonamido.'}4. The compound of any one of to ...

USE OF MALEIMIDE DERIVATIVES FOR PREVENTING AND TREATING CANCER

The present invention is related to a compound of formula (I) a pharmaceutically acceptable salt thereof, a hydrate thereof, a solvate thereof, a metabolite thereof or a prodrug thereof; for use in a method for the treatment and/or prevention of cancer, wherein X is selected from the group consisting of N—R, O and S; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl, arylalkyl and hydrogen; Ris selected from the group consisting of indolyl, substituted indolyl, azaindolyl and substituted azaindolyl; and Ris selected from the group consisting of aryl, substituted aryl, unsubstituted heteroaryl, heterocyclyl and substituted heterocyclyl. 6. The compound of any one of to , wherein X is O.9. The compound of claim 8 , wherein each and any of the substituents is individually and independently selected from the group consisting of fluoro claim 8 , chloro claim 8 , methyl claim 8 , trifluoromethyl claim 8 , vinyl claim 8 , acetyl claim 8 , acetamido claim 8 , methoxy claim 8 , formyl claim 8 , ethoxycarbonyl and ydimethylamidocarbonyl.11. The compound of claim 8 , wherein Ris substituted phenyl and each and any of the substituents is individually any independently selected from the group consisting of alkyl claim 8 , substituted alkyl claim 8 , alkoxy claim 8 , substituted alkoxy claim 8 , alkynly and halogen.15. The compound of any of to claim 8 , preferably any one of to claim 8 , more preferably any one of to claim 8 , wherein each and any of indolyl claim 8 , substituted indolyl claim 8 , azaindolyl and substituted azaindolyl of Ris individually and independently either unprotected or protected at N claim 8 , preferably at N of the 5-membered ring.27. The compound of claim 26 , wherein each and any of the substituents is individually and independently selected from the group consisting of fluoro claim 26 , chloro claim 26 , methyl claim 26 , trifluoromethyl claim 26 , vinyl claim 26 , acetyl claim 26 , acetamido claim 26 , methoxy claim 26 , formyl ...

Use of maleimide derivatives for preventing and treating cancer