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Compounds useful as inhibitors of protein kinases

A technology of compounds, solvates, in the field of compounds useful as protein kinase inhibitors

Inactive Publication Date: 2011-08-31
ABBOTT LAB INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, their affinity and selectivity or their pharmacological profiles are not yet satisfactory

Method used

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  • Compounds useful as inhibitors of protein kinases
  • Compounds useful as inhibitors of protein kinases
  • Compounds useful as inhibitors of protein kinases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0335] N-[(1S)-2-Hydroxy-1-phenylethyl]-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-3,6-dihydropyridine-1(2H )-formamide

Embodiment 1A

[0337] (S)-2-(tert-butyldimethylsilyloxy)-1-phenylethylamine (ethanamine)

[0338] (S)-2-amino-2-phenylethanol (1.04g, 7.61mmol), tert-butylchlorodimethylsilane (1.15g, 7.62mmol), triethylamine (2.15ml, 15.4mmol), N , N-dimethylpyridin-4-amine (23mg, 0.19mmol) / dichloromethane solution was stirred overnight at room temperature, quenched with saturated aqueous NaHCO3, extracted with dichloromethane, dried (Na 2 SO 4 ), filtered, and concentrated to give 1.85 g of a clear oil, which was used without purification.

Embodiment 1B

[0340] (S)-N-(2-(tert-butyldimethylsilyloxy)-1-phenethyl)-4-(1H-pyrrolo[2,3-b]pyridin-3-yl)- 5,6-Dihydropyridine-1(2H)-carboxamide

[0341] A solution of the product of Example 1A (127mg, 0.505mmol), triphosgene (52.1mg, 0.176mmol), and triethylamine (0.25ml, 1.8mmol) / dichloromethane (2ml) was stirred at room temperature for 2 hours. 3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-pyrrolo[2,3-b]pyridine (0.10 g, 0.50 mmol) was added and stirred at room temperature for 2 hours. N,N-Dimethylformamide (1 ml) was added to dissolve, and the mixture was stirred overnight, diluted with ethyl acetate, washed with water and brine, dried (Na 2 SO 4 ), filtered, concentrated and chromatographed (3% methanol / dichloromethane) to give the product as a clear gum (0.186 g, 0.391 mmol).

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Abstract

Disclosed herein are compounds of formula (I) or pharmaceutical acceptable salts thereof, wherein A, X<1>, X<2>, R<1>, R<2>, R<3>, m, n, and p are defined in the specification. Compositions including the compounds which can be useful for inhibiting Rho kinase (ROCK) and methods for using the compositions are also described.

Description

technical field [0001] Bicyclic compounds that are inhibitors of Rho kinase (ROCK), compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions are provided. Background technique [0002] An important large family of enzymes is the protein kinase enzyme family. Currently, there are approximately 500 different known protein kinases. ATP-Mg 2+ The transfer of the y-phosphate of the complex to the amino acid side chain catalyzes the phosphorylation of the amino acid side chain in various proteins. [0003] These enzymes control much of the intracellular signal processing whereby cellular function, growth, differentiation and destruction (apoptosis) are governed by reversible phosphorylation of the hydroxyl groups of serine, threonine and tyrosine residues in proteins. Research has shown that protein kinases are key regulators of many cellular functions, including signal transduction, regulation of transcripti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/454A61P9/00
CPCC07D471/04A61K31/437A61P1/04A61P11/00A61P13/08A61P13/10A61P13/12A61P15/08A61P15/10A61P17/06A61P19/02A61P19/10A61P21/04A61P25/00A61P25/08A61P25/14A61P25/16A61P25/18A61P25/22A61P25/24A61P25/28A61P27/02A61P29/00A61P31/04A61P31/12A61P31/18A61P35/00A61P35/04A61P37/08A61P9/00A61P9/04A61P9/10A61P9/12A61P3/10
Inventor A.瓦苏德文B.S.布朗R.G.克迪A.D.霍布森
Owner ABBOTT LAB INC
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