Substituted beta-amino acid inhibitors of methionine aminopeptidase-2

A technology of substituents and alkyl groups, applied in the field of organic compounds

Inactive Publication Date: 2001-08-15
ABBOTT LAB INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the process is not fully understood, it is thought to involve a complex interplay of molecules that stimulate and inhibit the growth of endothelial cells, the primary cells of capillaries

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0322] (2RS,3S,1’S)-N-((1-ethoxycarbonyl)ethyl)-3-amino-2-hydroxy-5-(methylthio)pentanoyl

[0323] Amine hydrochloride

Embodiment 1A

[0325] A solution of N-(tert-butoxycarbonyl)-L-methionine (12.47 g, 50 mmol) and REDAL (50 mmol) in dry toluene (125 mL) was stirred at 0 °C for 30 min, then at room temperature for 1 Hour. The mixture was treated with Rochelle's saline solution and extracted with ether. The extract was sequentially treated with brine and NaHCO 3 Washed with aqueous solution, dried (MgSO 4 ), concentrated to give a colorless syrup (9.05 g).

Embodiment 1B

[0327] A solution of the product of Example 1A (9.05 g, 38.5 mmol), sulfur trioxide pyridine complex (30.64 g, 192.5 mmol) and triethylamine (26.8 mL, 192.5 mmol) in DMSO (30 mL) was stirred at room temperature for 30 minutes , cooled to 0°C, followed by water (20 mL) and saturated KHSO 4 Work up with aqueous solution (120 mL) and extract with ethyl acetate. The extract was sequentially washed with saturated KHSO 4 Washed with aqueous solution and brine, dried (MgSO 4 ), concentrated to give a colorless syrup (9.00 g).

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PUM

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Abstract

A class of substituted beta -amino acids are potent inhibitors of methionine aminopeptidase type 2 (MetAP2) and are thus useful in inhibiting angiogenesis and disease conditions which depend upon angiogenesis for their development such as diabetic retinopathy, tumor growth, and conditions of inflammation. Pharmaceutical compounds containing the compounds and methods of inhibiting methionine aminopeptidase-2, and angiogenesis are also disclosed.

Description

field of invention [0001] The present invention relates to biologically active organic compounds, compositions containing the same, and medical methods of treatment. More specifically, the present invention relates to a class of substituted β-amino acids and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the compounds and methods for treating pathological symptoms caused by or accompanied by angiogenesis . Background of the invention [0002] Angiogenesis is the fundamental process by which new blood vessels are formed, which is essential for a variety of normal body activities such as reproduction, development and wound repair. Although the process is not fully understood, it is thought to involve a complex interplay of molecules that stimulate and inhibit the growth of endothelial cells, the primary cells of capillaries. Under normal conditions, these molecules appear to persist in the microvasculature that remains dormant (that is, wit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/16A61K31/18A61K31/198A61K31/22A61K31/221A61K31/223A61K31/341A61K31/357C07D295/12A61K31/36A61K31/381A61K31/40A61K31/4015A61K31/403A61K31/4035A61K31/404A61K31/4045A61K31/415A61K31/4164A61K31/4166A61K31/4184A61K31/426A61K31/4402A61K31/4406A61K31/4409A61K31/4418A61K31/4468A61K31/451A61K31/454A61K31/472A61K31/5355A61K31/5375A61K31/55A61P9/00A61P19/02A61P27/02A61P29/00A61P35/00C07CC07C235/16C07C237/12C07C237/14C07C311/19C07C323/60C07D207/27C07D209/16C07D209/48C07D211/58C07D211/82C07D213/40C07D213/61C07D213/74C07D217/06C07D231/12C07D231/40C07D233/61C07D233/72C07D233/95C07D235/14C07D265/30C07D277/20C07D277/46C07D277/56C07D295/18C07D295/185C07D307/10C07D307/52C07D317/58C07D319/18C07D333/20C07D333/38
CPCY02P20/55C07C323/60
Inventor R·A·克赖格J·肯金M·卡韦L·L·林奇J·帕特尔G·S·舍帕尔德王结义
Owner ABBOTT LAB INC
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