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US 11,691,986 B2Granted
PTEFB inhibiting macrocyclic compounds
AssigneesBayer Aktiengesellschaft, Bayer Pharma Aktiengesellschaft
InventorsUlrich Lücking, Daniel Hog, Clara Christ, Ulrike Sack, Franziska Siegel, Philip Lienau, Nicolas Werbeck
Life of this patent
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Abstract
The present invention relates to novel modified macrocyclic compounds with improved tolerability of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
Claims20
A compound of general formula (10):
- wherein:
- Z is hydrogen or fluorine;
- L is a C3-C8-alkylene moiety,
- wherein said moiety is optionally substituted with:
- (i) one substituent selected from hydroxy, —NR8R9, C2-C3-alkenyl-, C2-C3-alkynyl-, C3-C4-cycloalkyl-, hydroxy-C1-C3-alkyl-, —(CH2)NR8R9, and/or
- (ii) one or two or three or four substituents, identically or differently, selected from halogen and C1-C3-alkyl-,
- or wherein:
- one carbon atom of said C3-C8-alkylene moiety forms a three- or four-membered ring together with a bivalent moiety to which it is attached, wherein said bivalent moiety is selected from —CH2CH2—, —CH2CH2CH2—, —CH2OCH2—;
- R1 is C1-C6-alkyl-, C3-C6-alkenyl-, C3-C7-cycloalkyl-, or heterocyclyl-;
- wherein said C1-C6-alkyl-, C3-C6-alkenyl-, C3-C7-cycloalkyl-, or heterocyclyl- is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of hydroxy, cyano, halogen, C1-C6-alkyl-, halo-C1-C3-alkyl-, C1-C6-alkoxy-, C1-C3-fluoroalkoxy-, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, —OP(═OH)2, —C(1)OH, and —C(═O)NH2;
- R2 is hydrogen, fluorine, chlorine, bromine, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, or C1-C3-fluoroalkoxy-;
- R3 and R4 are independently from each other, hydrogen, fluorine, chlorine, bromine, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, or C1-C3-fluoroalkoxy-;
- R8 and R9 are independently from each other, hydrogen, C1-C6-alkyl-, C3-C7-cycloalkyl-,
- heterocyclyl-, phenyl-, benzyl-, or heteroaryl-:
- wherein said C1-C6-alkyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl-, benzyl-, or
- heteroaryl- group is optionally substituted with one, two or three substituents, identically or differently, selected from the group consisting of halogen, hydroxy, C1-C3-alkyl-, C1-C3-alkoxy-, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, halo-C1-C3-alkyl-, and C1-C3-fluoroalkoxy-, or
- R8 and R9, together with the nitrogen atom they are attached to, form a cyclic amine;
- or a salt thereof.
15 more elements
A compound of general formula (21):
- Z is hydrogen or fluorine;
- IDC-138,C1
- L is a C3-C8-alkylene moiety,
- wherein said moiety is optionally substituted with:
- (i) one substituent selected from hydroxy, —NR8R9, C2-C3-alkenyl-, C2-C3-alkynyl-, C3-C4-cycloalkyl-, hydroxy-C1-C3-alkyl-, —(CH2)NR8R9, and/or
- (ii) one or two or three or four substituents, identically or differently, selected from halogen and C1-C3-alkyl-,
- or wherein:
- one carbon atom of said C3-C8-alkylene moiety forms a three- or four-membered ring together with a bivalent moiety to which it is attached, wherein said bivalent moiety is selected from —CH2CH2—, —CH2CH2CH2—, —CH2OCH2—;
- R1 is C1-C6-alkyl-, C3-C6-alkenyl-, C3-C7-cycloalkyl-, or heterocyclyl-;
- wherein said C1-C6-alkyl-, C3-C6-alkenyl-, C3-C7-cycloalkyl-, or heterocyclyl- is optionally substituted with one or two or three substituents, identically or differently, selected from the group consisting of hydroxy, cyano, halogen, C1-C6-alkyl-, halo-C1-C3-alkyl-, C1-C6-alkoxy-, C1-C3-fluoroalkoxy-, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, —OP(═O)(OH)2, —C(═O)OH, and —C(═O)NH2;
- R2 is hydrogen, fluorine, chlorine, bromine, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, or C1-C3-fluoroalkoxy-;
- R3 and R4 are independently from each other, hydrogen, fluorine, chlorine, bromine, cyano, C1-C3-alkyl-, C1-C3-alkoxy-, halo-C1-C3-alkyl-, or C1-C3-fluoroalkoxy-;
- R8 and R9 are independently from each other, hydrogen, C1-C6-alkyl-, C3-C7-cycloalkyl-,
- heterocyclyl-, phenyl-, benzyl-, or heteroaryl-:
- wherein said C1-C6-alkyl-, C3-C7-cycloalkyl-, heterocyclyl-, phenyl-, benzyl-, or heteroaryl- is optionally substituted with one, two or three substituents, identically or differently, selected from the group consisting of halogen, hydroxy, C1-C3-alkyl-, C1-C3-alkoxy-, —NH2, alkylamino-, dialkylamino-, acetylamino-, N-methyl-N-acetylamino-, cyclic amines, halo-C1-C3-alkyl-, and C1-C3-fluoroalkoxy-, or
- R8 and R9, together with the nitrogen atom they are attached to, form a cyclic amine;
- or a salt thereof.
14 more elements
Dependencies are inferred from the claim text.