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Thienopyrimidines useful as aurora kinase inhibitors

A technology of CR1AR1B and compounds, applied in the field of thienopyrimidines suitable for use as AURORA kinase inhibitors, can solve problems such as insufficient treatment

Inactive Publication Date: 2008-04-09
SUNESIS PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In particular, there is a need to develop compounds suitable for use as Aurora inhibitors, especially given that currently available treatments for most conditions involving Aurora activation are insufficient

Method used

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  • Thienopyrimidines useful as aurora kinase inhibitors
  • Thienopyrimidines useful as aurora kinase inhibitors
  • Thienopyrimidines useful as aurora kinase inhibitors

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0649] This example describes the synthesis of:

[0650]

[0651] Step 1: [2-(4-Amino-phenyl)-ethyl]-carbamic acid tert-butyl ester (compound 1.1; 1.0 mmol, according to Hah , J.M. et al., prepared by the procedure of J.Med.Chem 46, 2003, 1661) and triethylamine ("TEA"; 3.0 equivalents) in anhydrous tetrahydrofuran ("THF"; 5.0 mL). After the reaction was complete, the mixture was partitioned between water and ether. The organic layer was separated, washed with 1.0N HCl, saturated sodium bicarbonate and brine and dried. Purification by flash column chromatography on silica gel gave [2-(4-benzoylamino-phenyl)-ethyl]-carbamic acid tert-butyl ester (compound 1.2).

[0652] Step 2: Compound 1.2 (1.0 mmol) was treated with anhydrous 4.0 N HCl in dioxane (25 mL) at 0°C, stirred at room temperature for 2 hours and concentrated to dryness under reduced pressure. The crude amine salt 4-chloro-7-methylthieno[3,2-d]pyrimidine (1.0 equiv) and N,N-diisopropylethylamine ("DIEA"; 2.5 eq...

example 2

[0654] This example describes the synthesis of:

[0655]

[0656] where R 1 is as previously described. These compounds were prepared according to the procedure of Example 1 except that in Step 2 Instead of 4-chloro-7-methylthieno[3,2-d]pyrimidine. R 1 Illustrative examples of are found throughout this disclosure and in Table 1.

[0657] Table 1

[0658]

[0659]

example 3

[0661] This example describes the synthesis of:

[0662]

[0663] where R 1 is as previously described. These compounds were prepared according to the procedure of Example 1, except that in Step 2 Instead of 4-chloro-7-methylthieno[3,2-d]pyrimidine. R 1 Illustrative examples of are found throughout this disclosure and in Table 2.

[0664] Table 2

[0665]

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Abstract

The present invention provides a compound which is described commonly and is described in the subclass of the text and has the formula (I), wherein R<1>, R<2>, X<1>, X<2>, L<1>, L<2>, Y and Z are defined as the category and subclass of the text, the invention also provides the medical composition which is suitable to be used as protein kinase (such as Aurora) inhibitor and is suitable for treating the disease mediated by Aurora.

Description

[0001] priority [0002] This application claims priority to the following U.S. Provisional Patent Applications: 60 / 632,568, filed December 1, 2004, and 60 / 588,718, filed July 16, 2004, the entire contents of each of which are Incorporated herein by reference. technical field [0003] none Background technique [0004] In recent years, a better understanding of the structure of enzymes and other biomolecules associated with disease has greatly aided the search for new therapeutic agents. An important class of enzymes that are the subject of extensive research are protein kinases. [0005] Protein kinases constitute a large family of structurally related enzymes responsible for the control of a variety of signal transduction processes within cells. (See Hardie, G. and Hanks, S. The Protein Kinase Facts Book, I and II, Academic Press, San Diego, CA: 1995). Due to the conservation of the structure and catalytic function of protein kinases, it is believed that protein kinase...

Claims

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Application Information

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IPC IPC(8): C07D495/04A61K31/519
Inventor 威拉德·卢苏布拉马尼安·巴什卡兰约翰·D·奥斯洛布乔希·约伯恩钟民
Owner SUNESIS PHARMA INC
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