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Formulations of oxabicycloheptanes and oxabicycloheptenes

A technology of alkyl and alkenyl, applied in the field of No. 565, No. WO2010/0

Active Publication Date: 2015-12-30
莱克斯特生物技术公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, in PCT International Application Publication Nos. WO2008 / 097561, WO2009 / 020565, WO2010 / 014141, WO2010 / 014220, WO2010 / 014254, WO2010 / 147612 and WO2012 / 162535 The PP2A inhibitors described have not been explored in human clinical trials

Method used

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  • Formulations of oxabicycloheptanes and oxabicycloheptenes
  • Formulations of oxabicycloheptanes and oxabicycloheptenes
  • Formulations of oxabicycloheptanes and oxabicycloheptenes

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0382] Stability study of example 1.LB-100 in normal saline and sodium bicarbonate

[0383] 1.1 Purpose

[0384] To determine the stability of LB-100 stored at room temperature and under refrigeration in saline and 4.2% sodium bicarbonate formulations.

[0385] 1.2 Materials and methods

[0386] 1.2.1 Preparations

[0387] LB-100 (Ash Stevens, Inc., Riverview, MI) was stored refrigerated and is considered stable under such storage conditions.

[0388] The vehicles used to prepare the LB-100 formulation were normal saline (0.9% Sodium Chloride Injection USP) (Baxter, Deerfield, IL) and 4.2% Sodium Bicarbonate, which Prepared by diluting 8.4% Sodium Bicarbonate Injection (Seneca Medical, Tiffin OH) 2-fold with Milli-Q water.

[0389] The saline formulation and the 4.2% sodium bicarbonate formulation were each prepared as follows at a target LB-100 concentration of 1.00 mg / mL. Weigh approximately 20 mg LB-100 into a tared glass vial. Vehicle is added to obtain the desired...

example 2

[0398] Example 2. Stability of LB-100 in glutamate, triethanolamine and phosphate buffer

[0399] 2.1 Purpose

[0400] To compare the long-term storage stability of LB-100 in the following formulations:

[0401] 1mg / mLLB-100 in glutamic acid buffered saline, pH8.5±0.1;

[0402] 1mg / mLLB-100 in glutamate buffer, pH10.5±0.1;

[0403] 1mg / mLLB-100 in triethanolamine buffer, pH7.0±0.1;

[0404] 1 mg / mL LB-100 in triethanolamine buffer, pH 9.0±0.1; and

[0405] 1mg / mLLB-100, in phosphate buffer, pH8.0±0.1.

[0406] 2.2 Materials and methods

[0407] 2.2.1 Preparations

[0408] 2.2.1.10.1 M glutamate solution

[0409] 28.1 g ± 0.1 g L-glutamate monosodium salt monohydrate was weighed out and added to 1500 mL nanopure water. The mixture was mixed until all the salts were dissolved to form a 0.1 mL stock solution of glutamic acid monosodium salt monohydrate.

[0410] Adjust the pH of 750 mL of the stock solution of L-glutamic acid monosodium salt monohydrate to 8.5 ± 0.1 us...

example 3

[0450] Example 3. Pharmaceutical compositions comprising LB-100

[0451] The following protocol was used to manufacture 42 L of a pharmaceutical composition comprising 1 mg / mL LB-100 and 0.1 M monosodium glutamate, pH 10.5.

[0452] 3.1 Materials

[0453] Table 11. Formulation ingredients

[0454]

[0455] Table 12. Container and Closure Components

[0456]

[0457] Table 13. Filtration and plumbing components

[0458]

[0459] 3.2 Preparation process

[0460] Add approximately 34kg of sterile water for injection USP to the 40L hyaluronic acid bottle. Sodium L-glutamate monohydrate was then added to the acid bottle and mixed for a minimum of ten minutes. The pH of the resulting mixture was adjusted to a pH in the range 10.4-10.6 with sodium hydroxide and / or hydrochloric acid. The target pH for this pH adjustment step is 10.5. Continue mixing the mixture until all the solids in the acid bottle have dissolved.

[0461] Next, add LB-100 to the acid bottle and m...

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PUM

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Abstract

The invention relates to a pharmaceutical composition comprising a protein phosphatase 2A (PP2A) inhibitor and monosodium glutamate.

Description

[0001] This application claims priority to US Provisional Application No. 61 / 810,053, filed April 9, 2013, the contents of which are hereby incorporated by reference. [0002] Throughout this application, reference is made to various publications. The disclosures of these documents are hereby incorporated by reference in their entirety into this application in order to more fully describe the state of the art to which this invention pertains. Background technique [0003] PCT International Application Publication Nos. WO2008 / 097561, WO2009 / 020565, WO2010 / 014141, WO2010 / 014220, WO2010 / 014254, WO2010 / 147612 and WO2012 / 162535 describe small proteins Phosphatase 2A (PP2A) inhibitors and their use for the treatment of various conditions, including cancer, neurodegenerative diseases, and diseases characterized by loss of protein function. [0004] One of the PP2A inhibitors described in PCT International Application Publication No. WO2008 / 097561, LB-100, has been tested in animal m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/34A61K31/4525A01N43/90
CPCA61K31/34A61K31/4525A61K31/197A61K31/496A61P21/00A61P25/00A61P25/14A61P25/16A61P25/28A61P27/02A61P3/00A61P35/00A61P35/02A61P3/06A61P43/00A61P7/04A61P9/10A61P3/10A61K2300/00A61K9/0019
Inventor 约翰·S·科瓦奇米奇·L·韦尔斯
Owner 莱克斯特生物技术公司
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