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Substituted triazolopyridine

A technology of substituents and general formulas, applied in the field of intermediate compounds for the preparation of said compounds, can solve problems such as no records

Inactive Publication Date: 2016-01-20
BAYER IP GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] However, the above background art is silent on specific triazolopyridine compounds of general formula (I) of the present invention, stereoisomers, tautomers thereof as described and defined herein and hereinafter referred to as "compounds of the present invention" , N-oxide, hydrate, solvate or salt, or their mixture, or their pharmacological activity

Method used

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  • Substituted triazolopyridine
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  • Substituted triazolopyridine

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Experimental program
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Effect test

Embodiment 11

[0303] N-(4-{2-[(2-cyanophenyl)amino]-5-methyl[1,2,4]triazolo[1,5-a]pyridin-6-yl}phenyl) -2-Phenylacetamide

[0304]

[0305] To a stirring solution of Int2.3 (90 mg) in DMF (3 mL) was added potassium carbonate (256 mg), phenylacetic acid (55 mg) and TBTU (424 mg). The mixture was stirred at room temperature for 15h. The mixture was concentrated in vacuo, water was added and the mixture was extracted with ethyl acetate. The organic phase was washed with water and saturated sodium chloride solution, dried (sodium sulfate) and the solvent was removed in vacuo. The solid was obtained by silica gel chromatography, which was recrystallized from ethanol. Obtained: 39 mg of the title compound.

[0306] 1 H-NMR(300MHz,DMSO-d 6 ): δ[ppm]=2.61(s,3H), 3.64(s,2H), 7.12(td,1H), 7.19-7.25(m,1H), 7.27-7.33(m,4H), 7.37(d, 2H), 7.49 (s, 2H), 7.59-7.66 (m, 1H), 7.66-7.75 (m, 3H), 8.02 (d, 1H), 9.50 (s, 1H), 10.30 (s, 1H).

[0307] In addition, the compound of formula (I) of the present invention...

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Abstract

The present invention relates to triazolopyridine compounds of general formula (I) as inhibitors of monopolar spindle 1 kinase (Mps-1 or TTK), processes for the preparation of said compounds, pharmaceutical compositions and combinations comprising said compounds, Said compound is used for the purposes of preparing the pharmaceutical composition of treating or preventing proliferative disease and is used for preparing the intermediate compound of said compound, in general formula (I) R1, R2, R3, R4 and R5 are as described in specification sheet and stated in the claims.

Description

[0001] The present invention relates to triazolopyridine compounds of the general formula (I) as described and defined herein, methods for preparing the compounds, pharmaceutical compositions and combinations comprising the compounds, and the compounds for the treatment or prevention of diseases The use of the pharmaceutical composition and the intermediate compound for the preparation of the compound. Background of the invention [0002] The present invention relates to compounds that inhibit Mps-1 (unipolar spindle 1) kinase (also known as tyrosine threonine kinase, TTK). Mps-1 is a dual-specific Ser / Thr kinase that plays an important role in the activation of mitotic checkpoints (also called spindle checkpoints, spindle assembly checkpoints), thereby ensuring proper separation of chromosomes during mitosis [AbrieuA et al., Cell, 2001, 106, 83-93]. Every dividing cell needs to ensure that the replicated chromosomes are equally divided into two daughter cells. After entering m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/04A61K31/437A61P35/00
CPCC07D471/04A61P1/04A61P11/00A61P13/08A61P13/10A61P13/12A61P15/00A61P17/00A61P21/00A61P25/00A61P29/00A61P35/00A61P35/02A61P35/04A61P37/02A61P43/00A61P5/00A61P9/00
Inventor V·舒尔策M·科皮茨D·科泽蒙德B·巴德尔P·利瑙H·布里姆S·霍尔顿G·西迈斯特S·佩克特A·M·温内尔
Owner BAYER IP GMBH