Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors

A compound, C1-C3 technology, used in anti-inflammatory agents, drug combinations, non-central analgesics, etc.

Inactive Publication Date: 2010-06-09
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The full function of mTOR kinase and the role of mTOR inhibition are not fully understood

Method used

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  • Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
  • Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors
  • Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors

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example

[1085] general method

[1086] The following general procedures will outline the synthesis of imidazopyrimidine analogs for each example.

[1087] Synthesis of 6-morpholin-4-yl-2-aryl-9H-purine (Scheme 1)

[1088] Step 1: To a solution of 2,6-dichloropurine (0.8 g, 4.23 mmol) dissolved in EtOH (40 mL) was added morpholine (1.5 eq). The reaction was stirred at room temperature for 12 hours, and the crude solid product was filtered off. with Et 2 The crude material was washed with O and dried in vacuo to give 0.75 g of a beige solid.

[1089] To the morpholine product from Step 1 (50 mg, 0.21 mmol) dissolved in DMF (0.5 mL) was added the desired arylboronic acid (1.5 eq), Na 2 CO 3 solution (2eq) and Pd(PPh 3 ) 4 (catalytic amount). The reaction was heated at 175 °C for 10 min under microwave irradiation. The crude reaction was then concentrated and purified via preparative HPLC using a Gilson instrument (see below).

[1090] Synthesis of 6-morpholin-4-yl-2-aryl-9-pipe...

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Abstract

The present invention relates to Imidazolopyrimidine Analogs, methods of making Imidazolopyrimidine Analogs, compositions comprising an Imidazolopyrimidine Analog, and methods for treating or preventing a PI3K-related disorder comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog. The invention also relates to methods for treating or preventing mTOR -related disorders comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog.

Description

technical field [0001] The present invention relates to imidazopyrimidine analogs; compositions comprising imidazopyrimidine analogs; and methods for treating or preventing PI3K-related diseases, which comprise administering an effective amount of imidazopyrimidine analogs. The present invention also relates to a method for treating or preventing mTOR-related diseases, which comprises administering an effective amount of imidazopyrimidine analogs. Background technique [0002] Phosphatidylinositol (hereinafter abbreviated as "PI") is a phospholipid in the cell membrane. In recent years, it has become increasingly understood that PI also plays an important role in intracellular signal transduction. It is well recognized in the art that phospholipase C, inter alia, degrades phosphatidylinositol diphosphate (4,5) (PI(4,5)P2) to diacylglycerol and inositol triphosphate (1,4,5), thereby Induces protein kinase C activation and intracellular calcium mobilization, respectively [M....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/34A61K31/52A61P35/00
CPCC07D473/34A61P1/00A61P1/18A61P13/08A61P13/12A61P17/06A61P19/00A61P19/02A61P19/10A61P27/02A61P29/00A61P3/00A61P35/00A61P35/02A61P35/04A61P37/02A61P43/00A61P9/00A61P9/10
Inventor 马修·格雷戈理·布尔萨维奇阿拉纳帕坎姆·穆登拜·文卡特桑帕维尔·沃伊切赫·诺瓦克萨布里纳·隆巴尔迪亚当·马修·吉尔伯特克里斯托弗·马丁·德恩哈特奥斯瓦尔多·多斯桑托斯埃弗伦·吉列尔莫·迪罗斯桑托斯纳塔夏·布罗伊曼斯塞米拉米斯·艾拉尔-卡劳斯蒂安陈泽成叶罗恩·库内拉·费尔黑珍约书亚·卡普兰阿里·扎斯科
Owner WYETH LLC
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