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US 2017/0283396 A1Published application
Diaminoheteroaryl substituted indazoles
AssigneeBayer Pharma Aktiengesellschaft
InventorsChristoph-Stephan HILGER, Marion HITCHCOCK, Hans BRIEM, Gerhard SIEMEISTER, Amaury Ernesto FERNANDEZ-MONTALVAN, Jens SCHRÖDER, Simon HOLTON, Cornelia PREUßE, Karsten DENNER
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Abstract
Compounds of formula (I) which are inhibitors of Bub 1 kinase, processes for their production and their use as pharmaceuticals.
Claims18
1-15. (canceled)
16:
- A compound of formula (I)
- wherein:
- X is CR6 or N;
- Y is CH or N;
- R1 is hydrogen, halogen, or 1-3C-alkyl;
- R2 and R3 are independently hydrogen, halogen, cyano, hydroxy, 1-6C-haloalkyl, 1-6C-haloalkoxy, or 1-6C-alkoxy;
- R4 is independently hydrogen, hydroxy, halogen, cyano, 1-6C-alkyl, 2-6C-alkenyl, 2-6C-alkynyl, 1-6C-haloalkyl, 1-6C-hydroxyalkyl, 1-6C-alkoxy, —O-(2-4C-alkylen)-O—C(O)-(1-4C-alkyl), 1-6C-haloalkoxy, —C(O)OR9, —C(O)-(1-6C-alkyl), —C(O)NR10R11, 3-7C-cycloalkyl, —S(O)2NH-(3-6C-cycloalkyl), —S(O)2NR10R11, or heteroaryl, which is optionally substituted independently one or more times with cyano, 1-4C-alkyl, 1-4C-haloalkyl, or 1-4C-haloalkoxy,
- wherein two of R2, R3, and (R4)n, when positioned ortho to each other, are optionally taken together with the two carbon atoms to which they are attached to form a heterocyclic 5-, 6-, or 7-membered ring containing 1 or 2 heteroatoms selected from O and N, and optionally containing an additional double bond and/or optionally substituted by an oxo (═O) group and/or an 1-4C-alkyl group;
- n is 0, 1, 2, or 3;
- R5 is
- (a) hydrogen,
- (b) —C(O)-(1-6C-alkyl),
- (c) —C(O)-(1-6C-alkylen)-O-(1-6C-alkyl),
- (d) —C(O)NH-(1-6C-alkyl), or
- wherein the * is the point of attachment;
- R6 is
- (a) hydrogen,
- (b) hydroxy,
- (c) cyano,
- (d) 1-6C-alkoxy optionally substituted independently one or more times with
- (d1) OH,
- (d2) —O-(1-6C-alkyl),
- (d3) —C(O)NR10R11,
- (d4) —NR12R13,
- (d5) —S-(1-6C-alkyl),
- (d6) —S(O)-(1-6C-alkyl),
- (d7) —S(O)2-(1-6C-alkyl),
- (d8) —S(O)2NR10R11,
- (d9) heterocyclyl, which is optionally substituted with oxo (═O), or
- (d10) heteroaryl, which is optionally substituted independently one or more times with cyano, 1-4C-alkyl, 1-4C-haloalkyl, 1-4C-haloalkoxy, C(O)NR10R11, or (1-4C-alkylen)-O-(1-4C-alkyl);
- (e) —O-heteroaryl optionally substituted with CN,
- wherein the * is the point of attachment,
- (g) —O-(2-6C-alkylen)-O-(1-6C-alkyl), which is optionally substituted with hydroxy,
- (h) —NR12R13,
- (i) —NHS(O)2-(1-6C-alkyl), or
- (j) —NHS(O)2-(1-6C-haloalkyl),
- or
- R5 and R6 form a 6-membered ring together with the nitrogen atom to which R5 is attached and together with the pyrimidine ring carbon atoms to which R5—NH and R6 are attached, which optionally contains one additional heteroatom selected from the group consisting of O, S, and N, and which is optionally substituted by an oxo (═O) group;
- R7 is
- (a) hydrogen,
- (b) 1-4C-alkyl, which is optionally substituted with heteroaryl,
- (c) 1-4C-haloalkyl,
- (d) 2-4C-hydroxyalkyl, or
- wherein the * is the point of attachment;
- R8 is independently hydrogen, halogen, hydroxy, 1-4C-alkyl, 1-4C-hydroxyalkyl, 1-4C-haloalkyl, 1-4C-haloalkoxy, C(O)OR9, or C(O)NR10R11;
- m is 0, 1, 2, 3, or 4;
- R9 is
- (a) hydrogen, or
- (b) 1-4C-alkyl, which optionally is substituted with hydroxy;
- R10 and R11 are independently hydrogen, 1-4C-alkyl, or 2-4C-hydroxyalkyl,
- or
- R10 and R11 are taken together with the nitrogen atom to which they are attached to form a 4-6-membered heterocyclic ring optionally containing one additional heteroatom selected from the group consisting of O, S, and N, and which is optionally substituted with 1-2 fluorine atoms or C(O)OR9;
- and
- R12 and R13 are independently hydrogen, 1-4C-alkyl, 2-4C-hydroxyalkyl, —C(O)-(1-6C-alkyl), —C(O)-(1-6C-alkylen)-O-(1-6C-alkyl), —C(O)H, or C(O)OR9,
- or
- R12 and R13 are taken together with the nitrogen atom to which they are attached to form a 4-6-membered heterocyclic ring optionally containing one additional heteroatom selected from the group consisting of O, S, and N, and which is optionally substituted by an oxo (═O) group,
- or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer, or stereoisomer.
54 more elements
17:
- The compound of formula (I) according to claim 16,
- wherein:
- X is CR6 or N;
- Y is CH or N;
- R1 is hydrogen, halogen, or 1-3C-alkyl;
- R2 and R3 are independently hydrogen, halogen, cyano, hydroxy, 1-3C-haloalkyl, 1-3C-haloalkoxy, or 1-3C-alkoxy;
- R4 is independently hydrogen, hydroxy, halogen, cyano, 1-3C-alkyl, 2-3C-alkenyl, 2-3C-alkynyl, 1-3C-haloalkyl, 1-3C-hydroxyalkyl, 1-3C-alkoxy, —O-(2-4C-alkylen)-O—C(O)-(1-4C-alkyl), 1-3C-haloalkoxy, —C(O)OR9, —C(O)-(1-3C-alkyl), —C(O)NR10R11, 3-7C-cycloalkyl, —S(O)2NH-(3-6C-cycloalkyl), or —S(O)2NR10R11;
- n is 0 or 1;
- R5 is
- (a) hydrogen,
- (b) —C(O)-(1-3C-alkyl),
- (c) —C(O)-(1-3C-alkylen)-O-(1-3C-alkyl),
- (d) —C(O)NH-(1-3C-alkyl), or
- wherein the * is the point of attachment;
- R6 is
- (a) hydrogen,
- (b) hydroxy,
- (c) cyano,
- (d) 1-3C-alkoxy optionally substituted independently one or more times with
- (d1) OH,
- (d2) —O-(1-3C-alkyl),
- (d3) —C(O)NR10R11,
- (d4) —NR12R13,
- (d5) —S-(1-3C-alkyl),
- (d6) —S(O)-(1-3C-alkyl),
- (d7) —S(O)2-(1-3C-alkyl),
- (d8) —S(O)2NR10R11,
- (d9) heterocyclyl, which is optionally substituted with oxo (═O), or
- (d10) heteroaryl, which is optionally substituted independently one or more times with cyano, 1-4C-alkyl, 1-4C-haloalkyl, 1-4C-haloalkoxy, C(O)NR10R11, or (1-4C-alkylen)-O-(1-4C-alkyl);
- (e) —O-heteroaryl optionally substituted with CN,
- wherein the * is the point of attachment,
- (g) —O-(2-3C-alkylen)-O-(1-3C-alkyl), which is optionally substituted with hydroxy,
- (h) —NR12R13,
- (i) —NHS(O)2-(1-3C-alkyl), or
- (j) —NHS(O)2-(1-3C-haloalkyl),
- or
- R5 and R6 form a 6-membered ring together with the nitrogen atom to which R5 is attached and together with the pyrimidine ring carbon atoms to which R5—NH and R6 are attached, which optionally contains one additional heteroatom selected from the group consisting of O, S, and N, and which is optionally substituted by an oxo (═O) group;
- R7 is
- (a) hydrogen,
- (b) 1-4C-alkyl, which is optionally substituted with heteroaryl,
- (c) 1-4C-haloalkyl,
- (d) 2-4C-hydroxyalkyl, or
- wherein the * is the point of attachment;
- R8 is hydrogen, halogen, hydroxy, 1-4C-alkyl, 1-4C-hydroxyalkyl, 1-4C-haloalkyl, 1-4C-haloalkoxy, C(O)OR9, or C(O)NR10R11;
- m is 0 or 1;
- R9 is
- (a) hydrogen, or
- (b) 1-4C-alkyl, which optionally is substituted with hydroxy;
- R10 and R11 are independently hydrogen, 1-4C-alkyl, or 2-4C-hydroxyalkyl,
- or
- R10 and R11 are taken together with the nitrogen atom to which they are attached to form a 4-6-membered heterocyclic ring optionally containing one additional heteroatom selected from the group consisting of O, S, and N, and which is optionally substituted with 1-2 fluorine atoms or C(O)OR9;
- and
- R12 and R13 are independently hydrogen, 1-4C-alkyl, 2-4C-hydroxyalkyl, —C(O)-(1-3C-alkyl), —C(O)-(1-3C-alkylen)-O-(1-3C-alkyl), —C(O)H, or C(O)OR9,
- or
- R12 and R13 are taken together with the nitrogen atom to which they are attached to form a 4-6-membered heterocyclic ring optionally containing one additional heteroatom selected from the group consisting of O, S, and N, and which is optionally substituted by an oxo (═O) group,
- or an N-oxide, a salt, a tautomer, or a stereoisomer of said compound, or a salt of said N-oxide, tautomer, or stereoisomer.
53 more elements
18:
- The compound of formula (I) according to claim 16,
- wherein:
- X is CR6 or N;
- Y is CH or N;
- R1 is hydrogen, halogen, or 1-3C-alkyl;
- R2 and R3 are independently hydrogen, halogen, cyano, hydroxy, 1-3C-haloalkyl, 1-3C-haloalkoxy, or 1-3C-alkoxy;
- R4 is independently hydrogen, hydroxy, halogen, cyano, 1-3C-alkyl, 2-3C-alkenyl, 2-3C-alkynyl, 1-3C-haloalkyl, 1-3C-hydroxyalkyl, 1-3C-alkoxy, 1-3C-haloalkoxy, —C(O)OR9, —C(O)-(1-3C-alkyl), —C(O)NR10R11, or —S(O)2NR10R11;
- n is 0 or 1;
- R5 is
- (a) hydrogen,
- (b) —C(O)-(1-3C-alkyl),
- (c) —C(O)-(1-3C-alkylen)-O-(1-3C-alkyl),
- (d) —C(O)NH-(1-3C-alkyl), or
- wherein the * is the point of attachment;
- R6 is
- (a) hydrogen,
- (b) hydroxy,
- (c) cyano,
- (d) 1-3C-alkoxy optionally substituted independently one or more times with
- (d1) OH,
- (d2) —O-(1-3C-alkyl),
- (d3) —C(O)NR10R11,
- (d4) —NR12R13,
- (d5) —S-(1-3C-alkyl),
- (d6) —S(O)-(1-3C-alkyl),
- (d7) —S(O)2-(1-3C-alkyl)
- (d8) —S(O)2NR10R11,
- (d9) heterocyclyl, which is optionally substituted with oxo (═O), or
- (d10) heteroaryl, which is optionally substituted independently one or more times with cyano, 1-4C-alkyl, 1-4C-haloalkyl, 1-4C-haloalkoxy, C(O)NR10R11, or (1-4C-alkylen)-O-(1-4C-alkyl);
- (e) —O-heteroaryl optionally substituted with CN,
- wherein the * is the point of attachment,
- (g) —O-(2-3C-alkylen)-O-(1-3C-alkyl), which is optionally substituted with hydroxy,
- (h) —NR12R13,
- (i) —NHS(O)2-(1-3C-alkyl), or
- (j) —NHS(O)2-(1-3C-haloalkyl),
- or
- R5 and R6 form a 6-membered ring together with the nitrogen atom to which R5 is attached and together with the pyrimidine ring carbon atoms to which R5—NH and R6 are attached, which optionally contains one additional oxygen atom, and which is optionally substituted by an oxo (═O) group;
- R7 is
- (a) hydrogen,
- (b) 1-4C-alkyl, which is optionally substituted with heteroaryl,
- (c) 1-4C-haloalkyl,
- (d) 2-4C-hydroxyalkyl, or
- wherein the * is the point of attachment;
- R8 is hydrogen, halogen, hydroxy, 1-4C-alkyl, 1-4C-hydroxyalkyl, 1-4C-haloalkyl, 1-4C-haloalkoxy, C(O)OR9, or C(O)NR10R11;
- m is 0:
- R9 is
- (a) hydrogen, or
- (b) 1-4C-alkyl, which optionally is substituted with hydroxy;
- R10 and R11 are independently hydrogen, 1-4C-alkyl, or 2-4C-hydroxyalkyl,
- or
- R10 and R11 are taken together with the nitrogen atom to which they are attached to form a 4-6-membered heterocyclic ring optionally containing one additional heteroatom selected from the group consisting of O, S, and N, and which is optionally substituted with 1-2 fluorine atoms or C(O)OR9;
- and
- R12 and R13 are independently hydrogen, 1-4C-alkyl, 2-4C-hydroxyalkyl, —C(O)-(1-3C-alkyl), —C(O)-(1-3C-alkylen)-O-(1-3C-alkyl), —C(O)H, or C(O)OR9,
- or
- R12 and R13 are taken together with the nitrogen atom to which they are attached to form a 4-6-membered heterocyclic ring optionally containing one additional oxygen atom,
- or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer, or stereoisomer.
53 more elements
19:
- The compound of formula (I) according to claim 16,
- wherein:
- X is CR6 or N;
- Y is CH or N;
- R1 is hydrogen;
- R2 and R3 are independently hydrogen or halogen;
- R4 is independently hydrogen or 1-3C-alkoxy;
- n 0 or 1;
- R5 is
- (a) hydrogen,
- (b) —C(O)-(1-3C-alkyl),
- (c) —C(O)-(1-3C-alkylen)-O-(1-3C-alkyl),
- (d) —C(O)NH-(1-3C-alkyl), or
- wherein the * is the point of attachment;
- R6 is
- (a) hydrogen,
- (d) 1-3C-alkoxy optionally substituted independently one or more times with
- (d1) OH, or
- (d2) —O-(1-3C-alkyl),
- (h) NR12R13,
- (i) —NHS(O)2-(1-3C-alkyl), or
- (j) —NHS(O)2-(1-3C-haloalkyl),
- or
- R5 and R6 form a 6-membered ring together with the nitrogen atom to which R5 is attached and together with the pyrimidine ring carbon atoms to which R5—NH and R6 are attached, which optionally contains one additional oxygen atom, and which is optionally substituted by an oxo (═O) group;
- R7 is
- (a) hydrogen, or
- wherein the * is the point of attachment;
- R8 is hydrogen;
- m is 0;
- and
- R12 and R13 are independently hydrogen or —C(O)-(1-3C-alkylen)-O-(1-3C-alkyl),
- or
- R12 and R13 are taken together with the nitrogen atom to which they are attached to form a 4-6-membered heterocyclic ring optionally containing one additional oxygen atom,
- or an N-oxide, a salt, a tautomer, or a stereoisomer of said compound, or a salt of said N-oxide, tautomer, or stereoisomer.
31 more elements
20:
- The compound of formula (I) according to claim 16,
- wherein:
- X is CR6 or N;
- Y is CH or N;
- R1 is hydrogen;
- R2 and R3 are independently hydrogen or fluorine;
- R4 is independently hydrogen or 1-3C-alkoxy;
- n is 0 or 1;
- R5 is
- (a) hydrogen,
- (b) —C(O)—CH3,
- (c) —C(O)-(methylen)-O-(methyl),
- (d) —C(O)NH-(1-3C-alkyl), or
- wherein the * is the point of attachment;
- R6 is
- (a) hydrogen,
- (d) 1-3C-alkoxy optionally substituted independently one or more times with
- (d1) OH, or
- (d2) —O-(methyl),
- (h) —NR12R13,
- (i) —NHS(O)2-(1-3C-alkyl), or
- (j) —NHS(O)2—(CF3),
- or
- R5 and R6 form a 6-membered ring together with the nitrogen atom to which R5 is attached and together with the pyrimidine ring carbon atoms to which R5—NH and R6 are attached, which optionally contains one additional oxygen atom, and which is optionally substituted by an oxo (═O) group;
- R7 is
- (a) hydrogen, or
- wherein the * is the point of attachment;
- R8 is hydrogen;
- m is 0;
- and
- R12 and R13 are independently hydrogen or —C(O)-(1-3C-alkylen)-O-(1-3C-alkyl),
- or
- R12 and R13 are taken together with the nitrogen atom to which they are attached to form a 6-membered heterocyclic ring containing one additional oxygen atom,
- or an N-oxide, a salt, a tautomer, or a stereoisomer of said compound, or a salt of said N-oxide, tautomer, or stereoisomer.
31 more elements
21:
- The compound of formula (I) according to claim 16, which is selected from the group consisting of:
- 2-[1-(2-fluorobenzyl)-1H-indazol-3-yl]-N-(pyridin-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(2-fluorobenzyl)-1H-indazol-3-yl]-N,N′-di(pyridin-4-yl)pyrimidine-4,6-diamine;
- N-{2-[1-(2-fluorobenzyl)-1H-indazol-3-yl]-6-(pyridin-4-ylamino)pyrimidin-4-yl}acetamide;
- N-{2-[1-(2-fluorobenzyl)-1H-indazol-3-yl]-6-(pyridin-4-ylamino)pyrimidin-4-yl}-2-methoxyacetamnide;
- N-{6-(dipyridin-4-ylamino)-2-[1-(2-fluorobenzyl)-1H-indazol-3-yl]-pyrimidin-4-yl}acetamide;
- N-{6-(dipyridin-4-ylamino)-2-[1-(2-fluorobenzyl)-1H-indazol-3-yl]pyrimidin-4-yl}-2-methoxyacetamnide;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-N-(pyridin-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-methoxy-N-(pyridin-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(morpholin-4-yl)-N-(pyridin-4-yl)pyrimidine-4,6-diamine;
- 1-{2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(morpholin-4-yl)-6-(pyridin-4-ylamino)pyrimidin-4-yl}-3-ethylurea;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-N-(pyrimidin-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-methoxy-N-(pyrimidin-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(morpholin-4-yl)-N-(pyrimidin-4-yl)pyrimidine-4,6-diamine;
- 1-{2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(morpholin-4-yl)-6-(pyrimidin-4-ylamino)pyrimidin-4-yl}-3-ethylurea;
- 6-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-N-(pyridin-4-yl)-1,3,5-triazine-2,4-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(2-methoxyethoxy)-N-(pyridin-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(2-methoxyethoxy)-N-(pyrimidin-4-yl)pyrimidine-4,6-diamine;
- N-{4-amino-2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-6-(pyridin-4-ylamino)pyrimidin-5-yl}-2-methoxyacetamnide;
- N-{4-amino-2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-6-(pyrimidin-4-ylamino)pyrimidin-5-yl}-2-methoxyacetamnide;
- N-{4-amino-2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-6-(pyridin-4-ylamino)pyrimidin-5-yl}ethanesulfonamide;
- N-{4-amino-2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-6-(pyridin-4-ylamino)pyrimidin-5-yl}-1,1,1-trifluoromethanesulfonamide
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-4-(pyridin-4-ylamino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-4-(pyrimidin-4-ylamino)-6H-pyrimido[5,4-b][1,4]oxazin-7(8H)-one;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-N,N′-di(pyridine-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-methoxy-N,N′-di(pyridin-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(morpholin-4-yl)-N,N′-di(pyridin-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(morpholin-4-yl)-N,N′-di(pyrimidin-4-yl)pyrimidine-4,6-diamine;
- 6-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-N,N′-di(pyridin-4-yl)-1,3,5-triazine-2,4-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(2-methoxyethoxy)-N,N′-di(pyridin-4-yl)pyrimidine-4,6-diamine;
- 2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-5-(2-methoxyethoxy)-N,N′-di(pyrimidin-4-yl)pyrimidine-4,6-diamine;
- N-{2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-4,6-bis(pyridin-4-ylamino)pyrimidin-5-yl}-2-methoxyacetamide;
- N-{2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-4,6-bis-(pyrimidin-4-ylamino)pyrimidin-5-yl}-2-methoxyacetamide;
- N-{2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-4,6-bis(pyridin-4-ylamino)pyrimidin-5-yl}ethanesulfonamide;
- N-{2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-4,6-bis(pyridin-4-ylamino)pyrimidin-5-yl}-1,1,1-trifluoromethanesulfonamide;
- 2-({4-amino-2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-6-(pyridin-4-ylamino)pyrimidin-5-yl}oxy)ethanol;
- and
- 2-({2-[1-(4-ethoxy-2,6-difluorobenzyl)-1H-indazol-3-yl]-4,6-bis-(pyridin-4-ylamino)pyrimidin-5-yl}oxy)ethanol,
- or an N-oxide, a salt, a tautomer, or a stereoisomer of said compound, or a salt of said N-oxide, tautomer, or stereoisomer.
36 more elements
22:
- A pharmaceutical composition comprising at least one compound of formula (I) according to claim 16, or an N-oxide, a salt, a tautomer, or a stereoisomer of said compound, or a salt of said N-oxide, tautomer, or stereoisomer, together with at least one pharmaceutically acceptable auxiliary.
23:
- A method of treating haemotological tumours, solid tumours, and/or metastases thereof comprising administering to a mammal in need thereof a therapeutically effective amount of the composition according to claim 22.
24:
- A combination comprising one or more first active ingredients selected from a compound of formula (I) according to claim 16, or an N-oxide, a salt, a tautomer, or a stereoisomer of said compound, or a salt of said N-oxide, tautomer, or stereoisomer, and one or more second active ingredients selected from chemotherapeutic anti-cancer agents and target-specific anti-cancer agents.
25:
- A compound selected from:
- wherein R1, R2, R3, R4, R6, and n have the meanings according to claim 16;
- wherein R1, R2, R3, R4, and n have the meanings according to claim 16;
- wherein R1, R2, R3, R4, and n have the meanings according to claim 16;
- and
- wherein R1, R2, R3, R4, and n have the meanings according to claim 16.
3 more elements
26:
- A method for treatment or prophylaxis of a hyperproliferative disease or disorder responsive to induction of apoptosis comprising administering to a mammal in need thereof a therapeutically effective amount of the compound of formula (I) according to claim 16, or an N-oxide, a pharmaceutically acceptable salt, a tautomer, or a stereoisomer of said compound, or a pharmaceutically acceptable salt of said N-oxide, tautomer, or stereoisomer.
27:
- The method according to claim 26, wherein the hyperproliferative disease or disorder responsive to induction of apoptosis is a haematological tumour, a solid tumor, or metastases thereof.
28:
- The method according to claim 26, wherein the hyperproliferative disease or disorder responsive to induction of apoptosis is a tumour selected from gastric-, pancreatic-, cervical-, breast-, non-small cell lung-, prostate-, colon-, and melanoma tumours, or metastases thereof.
29:
- A method for treatment or prophylaxis of disorders and diseases associated with excessive or abnormal angiogenesis comprising administering to a mammal in need thereof a therapeutically effective amount of the compound of formula (I) according to claim 16, or an N-oxide, a pharmaceutically acceptable salt, a tautomer or a stereoisomer of said compound, or a pharmaceutically acceptable salt of said N-oxide, tautomer, or stereoisomer.
30:
- The method according to claim 29, wherein the disorders and diseases associated with excessive or abnormal angiogenesis are selected from the group consisting of diabetic retinopathy, ischemic retinal-vein occlusion, retinopathy of prematurity, age-related macular degeneration (AMD), neovascular glaucoma, psoriasis, retrolental fibroplasias, angiofibroma, inflammation, rheumatoid arthritis (RA), restenosis, in-stent restenosis, and vascular graft restenosis.
31:
- A method for treatment or prophylaxis of disorders associated with aberrant mitogen extracellular kinase activity comprising administering to a mammal in need thereof a therapeutically effective amount of the compound of formula (I) according to claim 16, or an N-oxide, a pharmaceutically acceptable salt, a tautomer, or a stereoisomer of said compound, or a pharmaceutically acceptable salt of said N-oxide, tautomer, or stereoisomer.
32:
- The method according to claim 31, wherein the disorders associated with aberrant mitogen extracellular kinase activity are selected from the group consisting of stroke, heart failure, hepatomegaly, cardiomegaly, diabetes, Alzheimer's disease, cystic fibrosis, symptoms of xenograft rejections, septic shock, and asthma.