NITROGEN-CONTAINING HETEROCYCLIC COMPOUND OR ITS SALT Russian patent published in 2017 - IPC C07D213/74 C07D239/48 C07D239/49 C07D401/12 C07D401/14 C07D403/12 C07D405/12 C07D409/12 A61K31/506 A61K31/5377 A61P35/02 

Abstract RU 2632253 C2

FIELD: chemistry.

SUBSTANCE: invention relates to compound of the general formula [1]-(1): , where R2ais a hydrogen atom or a C1-6alkyl group, which may be substituted by one or more substituents selected from a halogen atom; an amino-group; a C1-6alkylamino-group, which may be substituted by one or more halogen atoms, di(C1-6alkyl) amino-group, which may be substituted by one or more hydroxy-group, a C1-6alkylaminocarbonyl and di(C1-6alkyl) amino-group, or morpholinyl or piperazinyl group, which may be substituted by one or more substituents selected from hydroxy-group, a C1-6alkyl group and a hydroxy-C1-6alkyl group, R4a is a hydrogen atom or a C1-6alkyl group, which may be substituted by one or more phenyl groups, R17a is a hydrogen atom or a C1-6alkyl group, which may be substituted by one or more substituents selected from a halogen atom, the hydroxyl group, and a C1-6alkoxygroup, provided that R17a together with R4a, the nitrogen atom, to which R4a is attached, and the carbon atom, to which R17a is attached, may form a nitrogen-containing divalent azetidinyl, pyrrolidinyl, piperidinyl, or azepanyl group, which may be substituted by one or more substituents selected from the atom of the halogen atom, a hydroxyl group, a C1-3alkyl group or a C1-6alkoxy group; R17b and R18b are the same or different and are a hydrogen atom or a C1-6alkyl group, which may be substituted by one or more substituents selected from the atom of the halogen atom, a hydroxyl group and a C1-6alkoxy group, provided that R17b and R18b together with the carbon atom, to which they are attached, can form C(=O), or R17b and R18b together with the carbon atom, to which they are attached, may form a tetrahydropyrandyl group; R9a is a C1-6alkoxy group, pyrrolidinyl, piperidinyl, piperazinyl, pyrazolidine, triazoline, or morpholinyl group, which may be substituted by one or more substituents selected from the atom of the halogen atom and a C1-3alkyl group, or N(R15)(R16), where R15 is a hydrogen atom or a C1-6alkyl group, and R16 is a C1-6alkyl group, which may be substituted by one or more groups selected from a halogen atom, a cyano group, a C3-6cycloalkyl group, a phenyl group, which may be substituted by one or more halogen atoms, a C1-6alkoxy group, di(C1-6alkyl) amino-group, and a morpholinyl, a tetrahydropyranyl, or a thiophenol group, a C3-8cycloalkyl group, a phenyl group, which may be substituted by one or more groups selected from a halogen atom, a cyano group, a C1-6alkyl group, a C1-6alkoxy group, or a pyridinyl or chinolyl group, which may be substituted by one or more C1-6alkoxy group, or R15 and R16 may form a cyclic amino-group, which may be substituted by one or more groups selected from halogen and a C1-3alkyl group, and R12a is a C1-6alkyl group, which may be substituted by one or more groups selected from the hydroxy groups, di(C1-6alkyl) amino-group or a pyridinyl, a morpholinyl, or a pyrrolidinyl group, a phenyl group, which may be substituted by one or more groups selected from the halogen atom; a cyano group; an amino-group, which may be protected by the acyl group; a carbamoyl group, which may be substituted by one or more groups selected from the C1-6alkyl groups and the C3-8cycloalkyl group; a C1-6alkyl group, which may be substituted by one or more groups selected from halogen and the triazoline group; a C1-6alkoxy group, which may be substituted with halogen; or pyrazolidine, triazoline, or thiazolidine group which may be substituted by one or more groups selected from C1-6alkyl group and ceanography, or pyridyloxy, izohinolinove, talinolol, isoxazolidine, isothiazolinone, thiadiazolidine, indazolinone, benzothiazolyl, chinolyl, benzoxazolyl, or pyrazolopyrimidinyl group, which may be substituted by one or more groups selected from halogen, a C1-6alkyl group, which may be substituted by one or more C1-6alkoxy group, a C1-6alkoxy group, a C1-6alkyl amino-group, a C1-6alkoxy carbonyl group, or a morpholinyl group; X2a is a C1-6alkylene group, which may be substituted by one or more substituents selected from exography and the C1-6alkyl group, a divalent C2-6alicyclic hydrocarbon group, or a divalent aromatic hydrocarbon group, which may be substituted by one or more groups selected from halogen, a C1-6alkyl group, which may be substituted by halogen and the C1-6alkoxy group, and X3a is a C2-6alkynyl amino-group, or N(R22)-C(=O), where R22 is a hydrogen atom.

EFFECT: compounds are an inhibitor of Fms-like tyrosine kinase 3, which can be used as a therapeutic agent for acute myelogenous leukemia.

21 cl, 261 tbl, 70 ex

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RU 2 632 253 C2

Authors

Takasaki Masaru

Tsudzino Tosiyaki

Tanabe Sintarou

Ookubo Megumi

Sato Kimikhiko

Khirai Atsusi

Terada Dajsuke

Inuki Sinsuke

Midzumoto Sinsuke

Dates

2017-10-04Published

2013-04-16Filed