DK2146779T3 - Sulfonylamid-derivater til behandling af unormal cellevækst. - Google Patents
Sulfonylamid-derivater til behandling af unormal cellevækst. Download PDFInfo
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- DK2146779T3 DK2146779T3 DK08719431.2T DK08719431T DK2146779T3 DK 2146779 T3 DK2146779 T3 DK 2146779T3 DK 08719431 T DK08719431 T DK 08719431T DK 2146779 T3 DK2146779 T3 DK 2146779T3
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Claims (24)
- (a) Sammensætning ifølge formel I:i eller et farmaceutisk acceptabelt salt deraf; hvorved A er en ring-enhed, som er udvalgt fra gruppen, som består af et: (a) 4- til 7-element carboclyl, (b) 4- til 7-element heterocyclyl, (c) phenyl, og (d) 5- til 6-element heteroaryl-ring, idet hvert af 4- til 7-element carbocyclyl og 4- til 7-element heterocyclyl i A-gruppen eventuelt kan indeholde én eller to olefiniske bindinger; og hvorved et eller to kulstof-ringatomer i hvert af 4- til 7-element carbocyclyl og 4- til 7-element heterocyclyl i A-gruppen uafhængigt eventuelt kan erstattes af ent eller to enheder, der uafhængigt vælges ud fra gruppen, som består af -C(O)-, -C(S)- og -C(=NR4)-; B er phenyl eller et 5- til 6-element heteroaryl; K er CH, C(NH2) eller N; Hvert R1 er uafhængigt valgt ud fra gruppen, der består af -H, halo, -CF3, -CN, -N02, -NR7R8, -NR7R8)(=CR9), -CR7(NR7R8)(=NR7 ), - NR7C(NR7C(0)R9, -C(0)R9,-C(0)C(0)R9, -C(0)OR10, -0C(0)R9, -or10, -OC(0)OR10, -S(0)jRn, -S(0)(=NR7)R8, -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Ci0)cycloalkyl, -(Cs-Cio)cycloalkenyl, -(Ce-Cio)bicycloalkyl, -(C6-Ci0)bicycloalkenyl, -(Ci-C9)heterocycloalkyl, -(C4- C9)heterocycloalkenyl, -(Ce-C^heterocycloalkyl, -(C6- C9)heterobicycloalkenyl, -(C6-Cio)aryl, og -(Ci-C9)heteroaryl; og hvorved hvert af de foregående -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C3-Ci0)cycloalkyl, -(C5-C io)cycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Cio)aryl og -(Ci-Cg)heteroaryl enheder af R1 i givet fald uafhængigt er-stattes af én, to eller tre R grupper; R2 og R3 er hver uafhængigt udvalgt fra gruppen, som består af -H,-halo, -OR10, -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Cio)aryl og -(Ci-C9)heteroaryl; og hvorved hvert af de foregående -(Cr C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cl0)cycloalkyl, -(C5-Cio)cykloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Cio)aryl og -(Ci-Cg)heteroaryl enheder i R2 og R3 i givet fald substitueres af én, to eller tre R grupper; R4 og R5 er hver uafhængigt udvalgt fra gruppen, som består af -H,-NR7R8-(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Ci0)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Cio)aryl og -(Ci-C9)heteroaryl; og hvorved hvert af de foregående (Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Ci0)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Cio)aryl og -(Ci-C9)heteroaryl enheder i R4 og R5 i givet fald substitueres af én, to eller tre R12 grupper; R6 er udvalgt fra gruppen, som består af -halo, -NR7R8, -OR10, -C(0)R9, -C02R10, -CONR7R8, -S(0)jRu, -NR7CONR7R8, og -NR8S02Rn, -N02, -CN, -CF3, -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C2-C6)perfluoralkyl, -(C2-C6)perfluoralkynyl, -(C3-C7)cycloalkyl, -(Cs-Ciojcycloalkenyl, -(C6-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(Ci-C9)heterocyclyl, -(Ci- Cio)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(Cg- C9)heterobicyckloalkenyl, -(C6-Cio)aryl, -(Ci-Cg)heteroaryl, -(Cg- Cio)perfluoraryl, og -(Ci-C9)perfluorheteroaryl; og hvorved hver af -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-C7)cycloalkyl, -(C5- Cio)cycloalkenyl, -(C6-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(Cr C9)heterocyclyl, -(Ci-Cio)heterocycloalkenyl, -(C6-cC9)heterol-enheder af R6-grupper er eventuelt substitueret af én, to eller tre R12-grupper; R7 og R8 er hver uafhængigt udvalgt fra gruppen, som består af -H, -OR10, -S(0)jRn, -NO2, -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkyl, -(C6-Cio)bicycloalkyl, -(Ce-Cio)bicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(C6-C9)heterobicycloalkenyl, -(C6-C10)aryl og -(Cl-C9)heteroaryl; og hvorved hvert af de foregående -(Ci-C6)alkyl, -(C2-Ce)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Ci0)aryl og -(Cr C9)heteroaryl-enheder af R og R i givet fald substitueres af én, to eller tre R12 -grupper; Hver R9 er uafhængigt valgt fra gruppen, der består af -H, -Halo, -NR13R14, -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Ci0)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C6-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(C6-C9)heterobicycloalkenyl, -(C6-Cio)aryl, og -(Ci-C6)heteroaryl; og hvorved hvert af de foregående (Ci-Ce)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Cio)aryl, og -(Ci-C9)heteroaryl enheder i R9 i gi-vet fald substitueres af een, to eller tre R grupper; Hver R10 er uafhængigt valgt fra gruppen, som består af -H, -(Ci-Cf,), -(C2-Ce)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C6-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(C6- C9)heterobicycloalkenyl, -(C6-Cio)aryl, og -(Ci-C9)heteroaryl; og hvorved hvert af de foregående -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Cio)aryl, og -(Ci-C9)heteroaryl-enheder i R10 i givet fald substitueres af én, to eller tre R12-grupper. Hver R11 er uafhængigt valgt fra gruppen som består af -H, -NR13R14, -C(0)R13, -CF3, -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C6-Ci0)cycloalkenyl, -(Ce-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(C2-Cg)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Cg)heterobicycloalkenyl, -(C6-Cio)aryl, og -(Ci-C9)heteroaryl; og hvorved Hver af de foregående (Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(Cs-Cmjcycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-Cio)aryl, og -(Ci-C9)heteroarylenheder i R11 i givet fald substitueres af én, to eller tre R12-grupper. Hver R12 er uafhængigt valgt fra gruppen, som består af -H, -C(0)R13, -0C(0)R13, -0C(0)0R13, -C(0)NR13R14, -NR13C(0)NR13R14, -NR13R14, -(NR13R14)(=NR13), -NR13C(NR13R14)(=N-C(0)R14, -NR13S(0)jR13, - S(0)jR13, -CF3 , -CN, -(CrC6)alkyl, -(C2-C6)alkenyl -(C2-C6)alkenyl, -(C2-Ce)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(Ce- Cio)cycloalkenyl, -(C6-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(Ce- C9)heterobicycloalkenyl, -(C6-Cio)aryl, og -(Ci-C9)heteroaryl; og hvorved hver af de foregående -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(Cs-Cio)cycloalkenyl, -(C6-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(C6-C9)heterobicycloalkenyl, -(C6-Cio)aryl, og -(Ci-C9)heteroaryl i R12 i givet fald substitueres af én, to eller tre grupper, som er udvalgt fra gruppe, der består af -halo, -CF3, -CN, -N02, -OH, -0((Ci-C6)alkyl), -C(0)R15, -C(0)NR15R16, -S(0)jR15, og S(0)jNR15R16, -(C3-Cio)cycloalkyl, -(C2-C9)heterocycloalkyl, -SH, -S((CrC6)alkyl), -NH2, -NHtfCrQdalkyl og -NKQ-CeJalkyltø R13 og R14 er hver uafhængigt udvalgt fra gruppen, som består af -H, -NR15C(0)R16, -CF3, -CN, -S(0)jR15, -(CrC6)alkyl, -(C2-C6)alkenyl, -(C2-Celalkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(Ce- Cio)bicycloalkyl, -(Ce-Ciolbicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(C6- C9)heterobicycloalkenyl, -(Ce-Cgjaryl, og -(Ci-C9)heteroaryl; og hvorved hvert af de foregående -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Ci0)cycloalkenyl, -(C6-Ci0)bicycloalkyl, -(C6- Cio)bicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(C6-C9)heterobicycloalkenyl, -(C6-Cg)aryl, og -(Ci-C9)heteroaryl i R13 og R14 i givet fald uafhængigt substitueres af én, to eller tre grupper, som er udvalgt fra gruppen, der består af -halo, -CF3, -CN, -N02, -OH, -0((Ci-C6)alkyl, -C(0)((Ci-C6)alkyl), -(C3-Cio)cycloalkyl, -(C2-C9)heterocycloalkyl, -SH, -S((Ci-C6)alkyl), -NH2, -NH((Ci-C6)alkyl) og -N((Ci-C6)alkyl)2; R15 og R16 er hver uafhængigt valgt fra gruppen, der består af -H, -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C6-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(C2- C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(C6-C9)heterobicycloalkenyl, og -(Ci-C9)heteroaryl; og hvorved hver af de foregående -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C6-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(C6-C9)heterobicycloalkenyl, og -(Ci-Cg)heteroaryl i R15 og R16 i givet fald uafhængigt substitueres af én eller to eller tre grupper, der består af -halo, -CF3, -CN, -NO2, -OH, -0((Ci-C6)alkyl), -C(0)((CrC6)alkyl, -(C3-C10)cycloalkyl, - (C2- C9)heterocycloalkyl, -NH2, -NH((Ci-C6)alkyl) og -N((Ci-C6)alkyl)2; hvorved eet eller to carbonring-atomer i hver af de førnævnte -(Ci-C6)alkyl, -(C2-C6)alkenyl, -(C2-C6)alkynyl, -(C3-Ci0)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C6-Cio)bicycloalkyl, -(C6-Cio)bicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(Οβ- C9)heterobicycloalkenyl, i R1 til R14 grupperne i givet fald og uafhængigt kan erstattes med -(CO)- eller -C(S)-; hvorved to grupper, som er fastgjort til samme tetravalente carbonatom i hver af de førnævnte -(Ci-Cejalkyl, -(C2-C6)alkenyl, -(Q-Cejalkynyl, -(C3- Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C6-Cio)bicycloalkyl, -(Ce-Cio)bicycloalkenyl, -(C2-C9)heterocycloalkyl, -(C4-C9)heterocycloalkenyl, -(C6-C9)heterobicycloalkyl, -(C6-C9)heterobicycloalkenyl, i R1 til R14 grupperne i givet fald kan forenes, så der dannes et ringsystem, der er udvalgt fra gruppen, som består af et -(C3-Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C2-Cgjheterocycloalkyl, -(C4-C9)heterocycloalkenyl, og hvorved J er et heltal fra 0 til 2; n er et heltal fra 1 til 3; og m er et heltal fra 0 til 3: hvorved alkyl, alkenyl, alkynyl, cycloalkyl, cycloal-kenyl, 4- til 7-element carbocyclyl, (C6-Cio)aryl, (Ci-Cg)heteoaryl, 5- til 6-element heteoaryl-ring, (C1 -Cgjheterocycloalkyl, (C4-Cg)heterocycloalkenyl og 4- til 7-element heterocyclylgrupper hver i givet fald kan substitueres med 1, 2 eller 3 fluoro, chloro, trifluoromethyl, -(Ci-C6)alkoxy, -(C6-Cio)aryloxy, trifluoromethoxy, difluoromethoxy eller -(Ci-C6)alkyl substituent(er).
- 2. Sammensætning ifølge krav 1, hvorved A er et phenyl.
- 3. Sammensætning ifølge krav 1, hvorved A er et 5- til 6-leddet heteroaryl.
- 4. Sammensætning ifølge et hvilket som helst af de foregående krav, hvorved hver R1 er uafhængigt udvalgt fra gruppen, der består af -H, halo, -CF3, -CN, -NO2, -NR7R8, -NR7R8)(=CR9), -CR7(NR7R8)(=NR7 ), -NR7C(NR7C(0)R9, -C(0)R9,-C(0)C(0)R9, -C(0)OR10, -0C(0)R9, -OR10, -OC(0)OR10, -S(0)jRn og -S(0)(=NR7)R8.
- 5. Sammensætning ifølge et hvilket som helst af kravene 1 til 4, hvorved R1 er -C(0)R9.
- 6. Sammensætning ifølge krav 5, hvorved R1 er -C(0)R9, og R9 er udvalgt fra gruppen, som består af -NR13R14, -(Ci-C6)alkyl og -(C3-Cio)cycloalkyl; hvorved hver af -(Ci-C6)alkyl, og -(C3-Cio)cycloalkyl i R9 -gruppen i givet fald substitueres af én til tre R12-grupper; og hvorved to grupper, der er fastgjort til samme tetravalente carbon-atom i — (Ci-Cejalkylet og -(C3-Cio)cycloalkylet i R9, i givet fald kan sammenføjes, så der dannes et ringsystem, der er udvalgt fra gruppen, som består af et -(C3- Cio)cycloalkyl, -(C5-Cio)cycloalkenyl, -(C2-C9)heterocycloalkyl, og -(C4-C9)heterocycloalkenyl.
- 7. Sammensætning ifølge krav 6, hvorved R1 er -C(0)R9, og R9 er -NR13R14.
- 8. Sammensætning ifølge krav 7, hvorved R1 er -C(0)R9, R9 er -NR13R14, og R13 og R14 er hver uafhængigt udvalgt fra gruppen, som består af -H og -(Ci-C6)alkyl; og hvorved -(Ci-C6)alkyl i R13 og R14 -grupperne i givet fald uafhængigt substitueres af én til tre grupper, der er udvalgt fra gruppen, som består af -halo, -CF3, -CN, -NO2, -OH, -0((Ci-C6)alkyl), -C(0)((Ci-C6)alkyl, -(C3-Ci0)cycloalkyl, - (C2- C9)heterocycloalkyl, -SH, S((Ci-C6)alkyl), -NH2, -N((Ci-C6)alkyl) og -N((Cr C6)alkyl)2.
- 9. Sammensætning ifølge et hvilket som helst af de foregående krav, hvorved R2 og R3 er hver uafhængigt udvalgt fra gruppen, som består af -H, -halo, og -OR10.
- 10. Sammensætning ifølge et hvilket som helst af kravene 1 til 8, hvorved R og R er hver uafhængigt udvalgt fra gruppen, der består af -H, -(Ci-C6)alkyl, -(C2-C6)alkenyl og -(C2-C6)alkynyl; og hvorved hver af de foregående -(Ci-C6)alkyl, -(C2-C6)alkynyl-enheder i R2 og R3 i givet fald uafhængigt substitueres af én til tre R12 grupper.
- 11. Sammensætning ifølge et hvilket som helst af de foregående krav, hvorved R4 og R5 er hver uafhængigt udvalgt fra gruppen, som består af -H, -(Ci-C6)alkyl, -(C2-C6)alkenyl og -(C2-C6)alkynyl; og hvorved hver af de foregående -(Ci-C6)alkyl, -(C2-C6)(alkenyl og -(C2-C6)alkynyl-enheder i R4 og R5 i givet fald uafhængigt substitueres af én til tre R12 grupper.
- 12. Sammensætning ifølge et hvilket som helst af de foregående krav, hvorved R6 er -CF3, K er CH, m er 1, og n er 1.
- 13. Sammensætning ifølge krav 1, hvorved enhedenrepræsenterer en enhed, der er udvalgt fra gruppen, som består af:
- 14. Sammensætning ifølge krav 1, og som er udvalgt fra gruppen, der består af (R)-N-(3-((2-(4-(l-aminoethyl)phenylamino)-5-(trifluoromethyl)pyrimidin-4- ylamino)pyridine-2-yl)-N-methylmethan-sulfonamid; N-(3-((2-(4-(aminomethyl)phenylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino) Methyl)pyridine-2-yl)-N-methylmethan-sulfonamid; N-[4-[{ {2-[methyl(methylsufonyl)amino]pyridine-3-yl}methyl)amino]-5-(trifluo-romethyl)pyrimidin-2-yl} amino)benzyl] acetamid; N-(3((2-(4-(hydroxymethyl)phenylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyridine-2-yl)-N-methylmethan-sulfonamid; og N-(3-((2-(4-(chloromethyl)phenylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyridine-2-yl)-N-methylmethan-sulfonamid; eller et farmaceutisk acceptabelt salt deraf.
- 15. Sammensætning ifølge krav 1, og som er udvalgt fra gruppen, der består af N-(3-((2-(4-(( 1,3-dihydroxypropan-2-ylamino)phenylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyridine-2-yl)-N-methylmethan-sulfonamid; eller et acceptabelt salt deraf; Tert-butyl 3-({4-[({2-[methyl(methylsulfonyl)amino]pyridin-3-yl}methyl)amino]-5 - (trifluoromethyl)pyrimidin-2-yl} amino)benzoat; 3-( {4- [({2- [methyl(methylsulfonyl)amino]pyridin-3-yl }methyl)amino]-5-(trifluoromethyl)pyrimidin-2-yl} amino)benzoesyre; N-cyclopropyl-3-({4-[({2-[methyl(methylsulfonyl)amino]pyridin-3-yl}methyl)amino]-5-(trifluoromethyl)pyrimidin-2-yl}amino)benzamid; og N-(3-((2-(4-(l-hydroxyetyl)phenylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)pyridin-2-yl)-N-methylmethansulfonamid; eller et farmaceutisk acceptabelt salt deraf.
- 16. Sammensætning ifølge krav 1, og som er udvalgt fra gruppen, der består af 2- fluoro-4-({4-[({2-[methyl(methylsulfonyl)amino]pyridin-3-yl}methyl)amino]-5-(trifluoromethyl)pyrimidin-2-yllamino)benzamid; 3- fluoro-4-({4-[({2-[methyl(methylsulfonyl)amino]pyridin-3-yl}methyl)amino]-5-(trifluoromethyl)pyrimidin-2-yllamino)benzamid; og N-methyl-4-({4-[({3-[methyl(methylsulfonyl)amino]pyrazin-2-yl}methyl)amino]-5-( trifluoromethyl)pyrimidin-2-yllamino)benzamid; eller et farmaceutisk acceptabelt salt deraf.
- 17. Sammensætning ifølge krav 1, og som er udvalgt fra gruppen, som består af 2-fbioro-4-({4-[({2-[methyl(methylsulfonyl)amino]pyridin-3-yl}methyl)amino]-5-( trifluoromethyl)pyrimidin-2-yllamino)benzamid format; 3-fluoro-4-({4-[({2-[methyl(methylsulfonyl)amino]pyridin-3-yl}methyl)amino]-5-(trifluoromethyl)pyrimidin-2-yl}amino)benzamid format; og N-methyl-4-({4-[({3-[methyl(methylsulfonyl)amino]pyrazin-2-yl}methyl)amino]-5-( trifluoromethyl)pyrimidin-2-yl}amino)benzamid hydrochlorid; 18. N-methyl-4-({4-[({3-[methyl(methylsulfonyl)amino]pyrazin-2-yl}methyl)amino] -5-( trifluoromethyl)pyrimidin-2-yl}amino)benzamid ifølge formlen:eller et farmaceutisk acceptabelt salt deraf. 19. N-methyl-4-({4-[({3-[methyl(methylsulfonyl)amino]pyrazin-2-yl}methyl)amino]-5-( trifluoromethyl)pyrimidin-2-yl}amino)benzamid hydrochlorid.
- 20. Farmaceutisk sammensætning, omfattende en sammensætning eller et salt ifølge et hvilket som helst af kravene 1 til 19 og et farmaceutisk acceptabelt hjælpestof, fortynding smiddel, bærestof eller excipiens.
- 21. Sammensætning eller salt ifølge et hvilket som helst af kravene 1 til 19 til anvendelse ved behandling af cancer i et pattedyr.
- 22. Sammensætning til anvendelse ifølge krav 21, hvorved canceren er udvalgt fra gruppen, som består af lungekræft, knoglekræft, bug spytkirtelkræft, hudkræft, kræft i hovedet eller nakken, cutan eller intraocular melanom, livmoderkræft, æggestokskræft, endetarmskræft, kræft i endetarmsåbningen, mavekræft, tyktarmskræft, brystkræft, carcinom i æggelederne, carcinom i endometrium, carcinom i halsen, carcinomi vagina, carcinom i vulva, Hodgkins sygdom, cancer i spiserøret, cancer i tyndtarmen, cancer i det indokrine system, cancer i skjoldbruskkirtlen, cancer i biskjoldbruskkirtlen, cancer i binyrerne, sarkom i blødt væv, cancer i urinrørskræft, cancer i penis, prostatakræft, kronisk eller akut leukæmi, lymfekræft, kræft i blæren, kræft i nyre eller urinleder, nyrecellecarcinom, carcinom i nyrebækkenet, svulster i centralnervesystemet (CNS), primært CNS-lymphom, rygradstumorer, hjernestamme-tumorer, hypofyse-adenom, eller en kombination af én eller flere af de foregående kræftformer.
- 23. Anvendelse af en sammensætning eller et salt ifølge et hvilket som helst af kravene 1 til 19 med henblik på fremstilling af et medikament til behandling afkræft i et pat tedyr.
- 24. Anvendelse ifølge krav 23, hvorved canceren er udvalgt fra gruppen, som består af lungekræft, knoglekræft, bugspytkirtelkræft, hudkræft, kræft i hovedet eller nakken, cutan eller intraocular melanom, livmoderkræft, æggestokskræft, endetarmskræft, kræft i endetarmsåbningen, mavekræft, tyktarmskræft, brystkræft, carcinom i æggelederne, carcinom i endometrium, carcinom i halsen, carcinomi vagina, carcinom i vulva, Hodgkins sygdom, cancer i spiserøret, cancer i tyndtarmen, cancer i det indokrine system, cancer i skjoldbruskkirtlen, cancer i biskjoldbruskkirtlen, cancer i binyrerne, sarkom i blødt væv, cancer i urinrørskræft, cancer i penis, prostatakræft, kronisk eller akut leukæmi, lymfekræft, kræft i blæren, kræft i nyre eller urinleder, nyrecellecarcinom, carcinom i nyrebækkenet, svulster i centralnervesystemet (CNS), primært CNS-lymphom, rygradstumorer, hjemestammetumorer, hypofyse-adenom, eller en kombination af én eller flere af de foregående kræftformer.
- 25. En kombination af en sammensætning eller salt ifølge et hvilket som helst af kravene til 19, og et kræftbekæmpelsesmiddel, et svulstbekæmpelsesmiddel eller et middel, som er nyttigt ved behandling af unormal cellevækst.
- 26. Farmaceutisk sammensætning, omfattende en terapeutisk effektiv mængde af sammensætning eller salt ifølge et hvilket som helst af kravene 1 til 19, et farmaceutisk acceptabelt bærestof og, eventuelt, i det mindste eet yderligere medicinsk eller farmaceutisk middel.
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