FIELD: pharmaceutics.
SUBSTANCE: present invention relates to novel piperidine compound of general formula (I) or its pharmaceutically acceptable salt. Besides, present invention relates to novel agent for enhancing anti-tumour effect, agonist, which include taxane anticancer agent for combined therapy. In compounds of formula (I) R1 is carboxyl group of -C(=O)NR5R6 or oxadiazolyl group, optionally containing C1-C6alkyl group or trifluoromethyl group as substitute; R2 is halogen atom or C1-C6alkoxy group; R3 is phenyl group, optionally containing 1-3 identical or different groups selected from halogen atom, C1-C6alkyl group C1-C6alkoxy group and trifluoromethyl group as substitute; R4 is a hydrogen atom or C1-C6alkyl group; and R5 and6 are identical or different, and each denotes a hydrogen atom, C1-C6alkyl group or C3-C6cycloalkyl group, or R5 and R6 optionally form 3-6-member nitrogen containing heterocyclic group saturated together with nitrogen atom to which R5 and R6 are connected.
EFFECT: this compound has excellent aurora A selective inhibiting action and is suitable as orally administered anticancer drug.
24 cl, 23 tbl, 28 ex
| Title | Year | Author | Number |
|---|---|---|---|
| JAK KINASE-MODULATING QUINAZOLINE DERIVATIVES AND METHODS OF APPLYING THEREOF | 2010 |
|
RU2529019C2 |
| PYRAZOLE DERIVATIVES APPLIED AS PROTEIN KINASE INHIBITORS | 2001 |
|
RU2340611C2 |
| AURORA KINASE INHIBITORS AND USE THEREOF | 2020 |
|
RU2822464C2 |
| KINASE INHIBITORS APPLICABLE FOR TREATING MYELOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES | 2007 |
|
RU2482112C2 |
| DIAMINOHETEROCYCLIC CARBOXAMIDE COMPOUND | 2010 |
|
RU2526253C2 |
| NOVEL AURORA KINASE INHIBITOR AND USE THEREOF | 2020 |
|
RU2835080C1 |
| NEW NICOTINAMIDE DERIVATIVE OR SALT THEREOF | 2011 |
|
RU2560163C2 |
| PYRIDINONE PYRIDAZINONE DERIVATIVES AS INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE (PARP) | 2007 |
|
RU2472782C2 |
| QUINOLINE DERIVATIVES AND MELK INHIBITORS CONTAINING SAME | 2011 |
|
RU2582610C2 |
| NEW 2-HETEROARYL-SUBSTITUTE BENZIMIDAZOLE DERIVATIVE | 2004 |
|
RU2329261C2 |
