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US 2016/0108031 A1Published application
Inhibitors of nhr2 and/or runx1/eto-tetramerization
AssigneeHeinrich-Heine-Universitat Dusseldorf
InventorsAlexander Metz, Holger Gohlke, Julia Schanda, Christian Wichmann, Manuel Grez
Life of this patent
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Abstract
The invention relates to inhibitors of the NHR2 tetramerization and their use as tumor therapeutics (e.g. against acute myeloid leukemia (AML)), cytostatics, and diagnostic agents.
Claims18
A compound according to general formula (A),
- wherein
- RA0, RA1 and RA2, respectively independently, mean —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- or RA0 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- and RA1 and RA2 are vicinal and together with the carbon atoms to which they are attached form a ring and mean —O—CH2—O— or —O—CH(Rx)—O— or —O—C(Rx)2—O—;
- RA3, RA4, and RA5, respectively independently, mean —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —O(═O)Rx, —O(═O)H, —O(═O)OH, —O(═O)ORx, —O(═O)NH2, —O(═O)NHRx, —O(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORX)2;
- or RA3 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —O(═O)Rx, —O(═O)H, —O(═O)OH, —O(═O)ORx, —O(═O)NH2, —O(═O)NHRx, —O(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- and RA4 and RA5 are vicinal and together with the carbon atoms to which they are attached form a ring and mean —O—CH2—O— or —O—CH(Rx)—O—;
- RA6 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —O(═O)Rx, —O(═O)H, —O(═O)OH, —O(═O)ORx, —C(═O)NH2, —O(═O)NHRx, —O(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RA7 means —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —O(═O)Rx, —O(═O)H, —O(═O)OH, —O(═O)ORx, —C(═O)NH2, —O(═O)NHRx, —O(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- mA means 0, 1, 2, 3, 4, 5 or 6;
- or a physiologically acceptable salt and/or a prodrug thereof;
- or a compound according to general formula (B)
- wherein
- RB1 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —O(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RB2 and RB3, respectively independently, mean —F, —Cl, —Br, —I, —ON, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- XB1 and XB2, respectively independently, mean O, S or NH;
- mB means 1, 2, 3, 4, 5, or 6;
- and
- nB means 1, 2, 3, 4, 5, or 6;
- or a physiologically acceptable salt and/or a prodrug thereof;
- or a compound according to general formula (C)
- wherein
- AC means O, S, or NRC3;
- RC1 means —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —O(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RC2 means —H or —(CH2)1-6—XC—Rx;
- RC3 means —Rx;
- RC4 means —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- XC means O, S, or NH;
- and
- mC means 0, 1, 2, 3, 4, 5 or 6;
- or a physiologically acceptable salt and/or a prodrug thereof;
- or a compound according to general formula (D)
- wherein
- XD1 means O, S, or NRD3;
- XD2 means O or S;
- YD means —(CH2)0-6— or —C(═O)—(CH2)1-6—XD2—;
- AD1 means N, NH or CH;
- AD2 means N or C;
- AD3 means N or CH;
- RD1 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRX, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RD2 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRX, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RD3 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRX, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RD4 means —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, or —C(═O)N(Rx)2;
- or a physiologically acceptable salt and/or a prodrug thereof;
- or a compound according to general formula (E)
- wherein
- RE1 and RE2, respectively independently, mean —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —O(═O)Rx, —O(═O)H, —O(═O)OH, —O(═O)ORx, —O(═O)NH2, —O(═O)NHRx, —O(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORX)2;
- RE3 and RE4, respectively independently, mean —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —O(═O)Rx, —O(═O)H, —O(═O)OH, —O(═O)ORx, —O(═O)NH2, —O(═O)NHRx, —O(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORX)2;
- RE5 means —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —O(═O)Rx, —O(═O)H, —O(═O)OH, —O(═O)ORx, —O(═O)NH2, —O(═O)NHRx, —O(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- mE means 0, 1, 2, 3, 4, 5, or 6;
- and
- nE means 0, 1, 2, 3, 4, 5, or 6;
- or a physiologically acceptable salt and/or a prodrug thereof;
- or a compound according to general formula (F)
- wherein
- RF1 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RF2 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RF3 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RF4 means —H, —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- RF5, RF6 and RF7, respectively independently, mean —H, —F, —Cl, —Br, —I, —ON, —NO2, —CHO, ═O, —Rx, —O(═O)Rx, —O(═O)H, —O(═O)OH, —O(═O)ORx, —O(═O)NH2, —O(═O)NHRx, —O(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- XF means O, S, or NRF5;
- YF means —(CH2)1-6C(═O)NH—(CH2)1-6—;
- AF1 means O, S, or NRF6;
- AF2 means O, S, or NRF7;
- or a physiologically acceptable salt and/or a prodrug thereof;
- wherein in each case Rx, respectively independently, means —C1-8-aliphatic, —C3-12-cycloaliphatic, -aryl, heteroaryl, —C1-8-aliphatic-C3-12-cycloaliphatic, —C1-8-aliphatic-aryl, —C1-8-aliphatic-heteroaryl, —C3-8-cycloaliphatic-C1-8-aliphatic, —C3-8-cycloaliphatic-aryl or —C3-8-cycloaliphatic-heteroaryl;
- wherein in each case “aliphatic”, respectively independently, means a branched or unbranched, saturated or a mono- or polyunsaturated, unsubstituted or mono- or polysubstituted, aliphatic hydrocarbon residue;
- wherein in each case “cycloaliphatic”, respectively independently, means a saturated or a mono- or polyunsaturated, unsubstituted or mono- or polysubstituted, alicyclic, mono- or multicyclic hydrocarbon residue;
- wherein in each case with respect to “aliphatic” and “cycloaliphatic”, “mono- or polysubstituted”, respectively independently, means the mono- or polysubstitution of one or more hydrogen atoms by —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)N(Rx)2, —OH, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)—ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NHC(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 or —PO(ORx)2;
- wherein in each case “aryl”, respectively independently, means a carbocyclic ring system with at least one aromatic ring, but without heteroatoms in this ring, wherein, if necessary, the aryl residues can be condensed with further saturated, (partially) unsaturated or aromatic ring systems, and each aryl residue can be present in unsubstituted or mono- or polysubstituted form, wherein the aryl substituents can be the same or different and in any desired and possible position of the aryl;
- wherein in each case “heteroaryl”, respectively independently, means a 5-, 6- or 7-membered cyclic aromatic residue, which contains 1, 2, 3, 4 or 5 heteroatoms, wherein the heteroatoms, the same or different, are nitrogen, oxygen or sulphur, and the heterocycle can be unsubstituted or mono- or polysubstituted;
- wherein in the case of the substitution on the heterocycle the substituents can be the same or different and can be in any desired and possible position of the heteroaryl;
- and wherein the heterocycle can also be part of a bi- or polycyclic system;
- wherein in each case with respect to “aryl” and “heteroaryl”, “mono- or polysubstituted”, respectively independently, means the mono- or polysubstitution of one or more hydrogen atoms of the ring system by substituents selected from the group comprising —F, —Cl, —Br, —I, —CN, —NO2, —CHO, ═O, —Rx, —C(═O)Rx, —C(═O)H, —C(═O)OH, —C(═O)ORx, —C(═O)NH2, —C(═O)NHRx, —C(═O)—N(Rx)2, —OH, —O(CH2)1-2O—, —ORx, —OC(═O)H, —OC(═O)Rx, —OC(═O)ORx, —OC(═O)NHRx, —OC(═O)N(Rx)2, —SH, —SRx, —SO3H, —S(═O)1-2—Rx, —S(═O)1-2NH2, —NH2, —NHRx, —N(Rx)2, —N+(Rx)3, —N+(Rx)2O−, —NHC(═O)Rx, —NHC(═O)ORx, —NH—C(═O)NH2, —NHC(═O)NHRx, —NHC(═O)—N(Rx)2, —Si(Rx)3 and —PO(ORx)2;
- wherein if necessary N-ring atoms present can be respectively oxidized.
72 more elements
Inhibitors of NHR2 and/or RUNX1/ETO-tetramerization for use in the treatment or the prevention of acute myeloid leukemia.
Dependencies are inferred from the claim text.