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Formulations of phospholipase enzyme inhibitors

A technology of active agent and solubilizer, applied in anti-inflammatory agents, non-central analgesics, non-active ingredients of oil/fat/wax, etc., can solve problems such as unpurified proteins

Inactive Publication Date: 2009-11-04
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the protein was not purified to homogeneity [see C.C. Leslie et al., Biochem. Biophys. Acta., 963: 476-492 (1988)]

Method used

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  • Formulations of phospholipase enzyme inhibitors
  • Formulations of phospholipase enzyme inhibitors
  • Formulations of phospholipase enzyme inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0176] 1. the preparation of the compound of formula I or formula II

[0177] Compounds of Formula I or II can be readily prepared from commercially available starting materials, compounds known in the literature, or readily available intermediates, using standard synthetic methods and schemes known to those skilled in the art. Standard synthetic methods and procedures for the preparation of organic molecules and functional group transformations and manipulations are readily available from the relevant scientific literature or standard works in the field. It is to be understood that where typical or preferred process conditions (ie, reaction temperatures, times, molar ratios of reactants, solvents, pressures, etc.) are given, other process conditions can also be used unless otherwise stated. Optimum reaction conditions may vary with the particular reactants or solvent used, but those skilled in the art can determine such conditions by routine optimization procedures. Those sk...

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Abstract

The present invention refers to formulations of inhibitors of phospholipase enzymes, such as cytosolic PLA2, compositions containing the same and processes for manufacture thereof.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of US Provisional Patent Application No. 60 / 855,569, filed October 31, 2006, which is incorporated herein by reference in its entirety. field of invention [0003] The present invention relates to phospholipases (e.g. cytosolic PLA 2 ) inhibitor formulations, compositions containing the same and methods for their preparation. Background of the invention [0004] Leukotrienes and prostaglandins are important mediators of inflammation, and they participate in the establishment of inflammatory responses in different ways. Leukotrienes recruit inflammatory cells such as neutrophils to sites of inflammation, facilitate extravasation of these cells and stimulate the release of tissue-damaging superoxide and proteases. Leukotrienes also play a pathophysiological role in asthma-induced hypersensitivity [see, eg, B. Samuelson et al., Science, 237:1171-76 (1987)]. Prostaglandins enhance th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4045A61K9/48A61K47/14A61K47/44A61P29/00
CPCA61K47/44A61K31/4045A61K47/14A61K9/4858A61P11/06A61P25/00A61P29/00A61P43/00
Inventor F·A·多纳休M·S·泰斯科尼M·S·库
Owner WYETH LLC
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