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Fluoro-substituted compounds as kinase inhibitors and methods of use thereof

A compound and solvate technology, applied in the field of pharmaceutically active compounds and compound intermediates for the treatment of various tumor diseases, can solve problems such as genome instability and high cell division rate

Inactive Publication Date: 2012-07-04
JIANGSU MEDOLUTION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mutations render c-Kit function independent of Scf activation, leading to high cell division rates and possibly genome instability

Method used

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  • Fluoro-substituted compounds as kinase inhibitors and methods of use thereof
  • Fluoro-substituted compounds as kinase inhibitors and methods of use thereof
  • Fluoro-substituted compounds as kinase inhibitors and methods of use thereof

Examples

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preparation example Construction

[0075] Novel starting materials and / or intermediates and processes for their preparation are likewise subject of the present invention. In selected embodiments, such starting materials are used and reaction conditions are selected to obtain one or more desired compounds.

[0076] The starting materials of the present invention are known, commercially available or can be synthesized by methods known in the art or methods analogous thereto. Many starting materials may be prepared according to known methods, in particular using the methods described in the schemes and examples. During the synthesis of starting materials, functional groups are protected in some cases with suitable protecting groups when necessary.

[0077] Methods involving the use of protecting groups can be employed. In particular, if one or more functional groups (such as carboxyl, hydroxyl, amino or mercapto) are protected or need to be protected during the preparation of the compounds of the invention becau...

Embodiment 1-14

[0139] Embodiment 1-14 (method A)

[0140]

Embodiment 1

[0141] The preparation of embodiment 1.4-((4-methylpiperazin-1-yl) methyl) methyl benzoate

[0142]

[0143] Into a 250-mL three-neck round bottom flask was placed methyl 4-formylbenzoate (4.92 g, 30.0 mmol, 1.00 equiv) in CH 3 Solution in CN (100 mL), 1-methylpiperazine (3.6 mL, 1.30 equiv) and CF 3 COOH (2.5 mL, 1.10 equiv). The resulting solution was stirred at room temperature for 15 min, then NaBH was added in several portions 3 CN (3.78 g, 60.0 mmol, 2.00 equiv). The resulting solution was stirred overnight at room temperature. The reaction was terminated by adding 10 mL of water. The resulting mixture was concentrated in vacuo. The residue was applied to a silica gel column and eluted with dichloromethane / methanol (80:1). 4 g of methyl 4-((4-methylpiperazin-1-yl)methyl)benzoate were obtained as a white solid.

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Abstract

The present invention provides for novel compounds of Formula I and pharmaceutically acceptable salts and solvates thereof which have kinase inhibitor activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating and preventing a Bcr-Abl, c-Kit or PDGF-R mediated disorder for which one or more kinase inhibitor is indicated, including neoplasia such as chronic myelogenous leukemia or gastrointestinal stromal tumors. The present invention also provides for processes of making the compounds of Formula I, including salts and solvates thereof, and pharmaceutical compositions comprising the same.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to US Provisional Application No. 61 / 270,786, filed July 14, 2009, which is incorporated herein by reference. field of invention [0003] The present invention generally relates to the field of medicines, and more specifically, relates to pharmaceutically active compounds, pharmaceutical compositions and methods of use for treating various tumor diseases. The invention also relates to intermediates and processes for the preparation of such compounds. Background of the invention [0004] Protein kinases represent a large family of enzymes that catalyze the phosphorylation of target protein substrates. Phosphorylation is generally the transfer reaction of a phosphate group from ATP to a protein substrate. Common points of attachment of phosphate groups to protein substrates include, for example, tyrosine, serine or threonine residues. For example, protein tyrosine kinases (PTKs) are en...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/14A61K31/505A61P35/00A61P35/02
CPCC07D401/04A61P35/00A61P35/02
Inventor 张大为
Owner JIANGSU MEDOLUTION
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