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Pyrazolopyridinamines as MKNK1 and MKNK2 inhibitors

A compound, C2-C6- technology, applied in the direction of anti-inflammatory agents, organic chemistry, drug combination, etc., can solve the problems of pyrazolopyridinamine compounds that have not been disclosed to treat or prevent different diseases

Inactive Publication Date: 2017-10-13
BAYER PHARMA AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Substituted pyrazolopyridinamine compounds of general formula (I) that are not disclosed in the prior art for the treatment or prevention of different diseases

Method used

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  • Pyrazolopyridinamines as MKNK1 and MKNK2 inhibitors
  • Pyrazolopyridinamines as MKNK1 and MKNK2 inhibitors
  • Pyrazolopyridinamines as MKNK1 and MKNK2 inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0581] (RS) N,N-Dimethyl-4-(pyrazolo[1,5-a]pyridin-5-ylamino)-5,6,7,8-tetrahydro[1]benzothieno[ 2,3-d]pyrimidine-7-carboxamide

[0582]

Embodiment 1a

[0586] (RS)-4-Chloro-N,N-dimethyl-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-7-carboxamide

[0587]

[0588] will contain 4.54 g (16.90 mmol) of (RS)-4-chloro-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine-7-carboxylic acid (prepared according to WO2013174744) , 182 mL N,N-dimethylformamide, 8.83 mL N-ethyl-N-isopropylpropan-2-amine, 42.2 mL N-methylmethylamine solution (2M, in tetrahydrofuran) and 40.2 mL 2,4,6-tripropyl-1,3,5,2,4,6-trioxatriphosphorinane 2,4,6-trioxide solution (50%, in N,N- dimethylformamide) was stirred at 23°C for 1 hour. The mixture was poured into water, ice was added, the precipitate was washed with water and ether, and dried to give 3.44 g (65%) of the title compound.

Embodiment 2

[0590] (7S)-4-(pyrazolo[1,5-a]pyridin-5-ylamino)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidine -7-Formic acid

[0591]

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PUM

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Abstract

The present invention relates to substituted pyrazolopyridinamine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative and / or angiogenesis disorder, inflammatory disease and disease associated with inflammatory pain, as a sole agent or in combination with other active ingredients.

Description

technical field [0001] The present invention relates to substituted pyrazolopyridinamine compounds of general formula (I) as described and defined herein, processes for the preparation of said compounds, intermediate compounds for the preparation of said compounds, compounds comprising said compounds Pharmaceutical compositions and combinations, and the use of said compounds as single agents or in combination with other active ingredients for the manufacture of drugs for the treatment or prophylaxis of diseases, especially hyperproliferative, angiogenic disorders, inflammatory diseases or associated with inflammatory pain Diseases). Background of the invention [0002] The present invention relates to chemical compounds that inhibit MKNK1 kinase (also known as MAP kinase-interacting kinase, Mnk1 ) and / or MKNK2 kinase (also known as MAP kinase-interacting kinase, Mnk2). Human MKNKs comprise a set of four proteins encoded by two genes (gene symbols: MKNK1 and MKNK2) through a...

Claims

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Application Information

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IPC IPC(8): C07D519/00A61K31/5377A61K31/519A61P35/00A61P29/00A61P37/00
CPCC07D519/00C07D495/04A61P37/00A61P29/00A61P35/00A61K31/437A61K31/519
Inventor A.吉泽U.克拉尔K.格雷厄姆G.克特绍D.聚尔兹勒P.利瑙K.彼得森J.莱弗兰克N.施密特
Owner BAYER PHARMA AG
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