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Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses

A compound, diastereomer technology, applied in the field of stereoisomer-enriched compositions, can solve problems such as limiting the effectiveness of chemotherapeutic agents

Inactive Publication Date: 2013-04-17
RIGEL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These types of cancer cell adaptations severely limit the effectiveness of certain classes of chemotherapeutic agents

Method used

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  • Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
  • Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
  • Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses

Examples

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Embodiment

[0199] The invention is further illustrated by reference to the following examples, which describe the preparation of various compounds described herein, methods for assaying their biological activity, and methods for their use. Many modifications in materials and methods of practice will be apparent to those skilled in the art without departing from the scope of the invention.

[0200] Preparation of 4-(4-methylpiperazin-1-yl)-3-methylnitrobenzene

[0201] reaction:

[0202]

[0203] Procedure: Homogenous mixture of 4-fluoro-3-methylnitrobenzene 1 (20 g, 129 mmol) and N-methylpiperazine 3 (25.82 g, 258 mmol) in N-methylpyrrolidone (NMP) (10 mL) in N 2 Reflux (120° C.) for 24 hours. The reaction mixture was cooled to room temperature and poured into saturated NaCl solution (100 mL). The resulting solid was sonicated for approximately 30 seconds, filtered, washed with ice-cold water (2 x 10 mL), and dried under high vacuum to yield 4-(4-methylpiperazin-1-yl)-3-methyl N...

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Abstract

The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.

Description

[0001] Cross References to Related Applications [0002] This application claims priority under 35 U.S.C. §119(e) to Application Serial No. 60 / 628,199, filed November 15, 2004, the contents of which are hereby incorporated by reference. technical field [0003] The present invention relates to stereo-enriched 4N-(3-aminocarbonylbicyclo[2.2.1]hept-5-en-2-yl)-N2-substituted phenyl-2,4-pyrimidinediamine compounds exhibiting antiproliferative activity Compositions of isomers (stereo-isomerically enriched); prodrugs of these compounds, intermediates and synthetic methods for preparing these compounds and / or prodrugs; pharmaceutical compositions comprising these compounds and / or prodrugs; And the use of these compounds and / or prodrugs in a variety of conditions including, for example, the treatment of proliferative diseases such as tumors and cancers. Background technique [0004] Cancer is a diverse group of diseases characterized by the uncontrolled growth and spread of abnorma...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/506A61K31/4353C07D239/48C07D413/12
CPCA61K31/495C07D413/12C07D239/48A61P35/00A61P35/02A61P35/04A61P43/00A61K31/505A61K31/506C07B53/00C07B57/00C07D405/12C07D487/08
Inventor A·阿加德R·辛格H·李
Owner RIGEL PHARMA