Inhibitors of protein kinases
AssigneeIngenium Pharmaceuticals GmbH
InventorsHeike Schauerte, Hans Allgeier, Michael A. Pleiss, Martin Augustin, Gisela Peraus, Gabriele Stumm, Philipp Wabnitz
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Abstract
The present invention relates to inhibitors of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to methods of preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases comprising the administration of an effective amount of at least one inhibitor of cyclin-dependent kinases. formula (I).
Claims10
A compound according to the general Formula I
- wherein
- R1 is —XSO2NR5R6 or —XSO2R8;
- X is a branched or unbranched C1-4 alkylene, wherein said C1-4 alkylene optionally can be bound to R5 or R6 to form a 5- or 6-membered heterocycle;
- R5 and R6 independently of each other are selected from the group consisting of hydrogen, C1-4alkyl, hydroxy-C1-4alkyl, C3-4alkenyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-4-alkyl, C4-7-heterocycloalkyl-C0-4alkyl, C4-7-aryl-C0-4alkyl, and C4-7-heteroaryl-C0-4alkyl;
- or
- wherein R5 and R6 together with the N-atom to which they are bound form a 5- to 8-membered heterocycloalkyl,
- wherein said cycloalkyl, heterocycloalkyl, aryl, heteroaryl or alkyl is further optionally substituted by up to 2 radicals selected from the group consisting of halo, hydroxy, aminocarbonyl, C1-4 alkyl, hydroxy-C1-4 alkyl, C1-4 alkyl-O—C1-4 alkyl, C1-4 alkyl-O—, and —NR5R6;
- R8 is C1-4 alkyl, hydroxy-C2-4alkyl, C3-4alkenyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-4alkyl, or C4-7-heterocycloalkyl-C0-4 alkyl;
- wherein said cycloalkyl, heterocycloalkyl or alkyl is further optionally substituted by up to 2 radicals selected from the group consisting of halo, hydroxy, C1-4 alkyl, hydroxy-C1-4 alkyl, C1-4 alkyl-O—C1-4 alkyl, C1-4 alkyl-O, and —NR5R6;
- R2 is one or two substituents independently selected from halogen and hydrogen;
- R3 can be 1 to 3 substituents each independently selected from the group consisting of hydrogen, halo, hydroxy, C1-4alkyl, C3-7cycloalkyl, C1-4 alkyl-cycloalkyl, C1-4 alkyl-heterocycloalkyl, —O-heterocycloalkyl, C1-4 alkoxy, C2-4 alkenyloxy, —OCF3, C2-4 alkanoyl, C1-4alkylsulfonyl, mono- and di-(C1-C4alkyl)sulfonamido, aminocarbonyl, mono- and di-(C1-C4alkyl)aminocarbonyl, aryl-C1-4 alkoxy, heteroaryl-C1-4 alkoxy, heterocycloalkyl-C1-4-alkoxy, heterocycloalkyl-C1-4-alkyl, heteroaryl-C1-4-alkyl, C1-4 alkyloxymethyl, hydroxy-C1-4alkyloxymethyl, cyano, —COOH, and C1-C4 alkoxycarbonyl, wherein the above mentioned substituents can be further substituted by radicals selected from the group consisting of C1-4-alkyl, hydroxyl-C0-4-alkyl, C1-4-alkoxy, aminocarbonyl, halo, and NR5R6;
- R4a and R4b are the same or different and each is independently hydrogen, C1-4 alkyl, or —NR′R″, wherein R′ and R″ are each independently hydrogen or C1-4 alkyl;
- and the N-oxide derivatives, protected derivatives, and the pharmaceutically acceptable salts of such compounds.
Dependencies are inferred from the claim text.