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Use of PPAR agonists to treat ruminants

A ruminant and agonist technology, applied in the field of PPAR agonist, treatment of ruminant diseases related to lower blood sugar concentration, and treatment of feline fatty liver, can solve complex interactions, do not know PPAR expression milk production or quality, issues of limited knowledge

Inactive Publication Date: 2008-02-13
PFIZER PROD INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the interplay of biological processes described is complex and knowledge of the important genes, enzymes and endogenous substrates required to optimize energy balance in dairy cows is limited
Furthermore, since NEFAs are key substrates for milk and glucose biosynthesis, it is not known how improvements in PPAR expression would affect milk production or quality, lipolysis, or gluconeogenesis

Method used

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  • Use of PPAR agonists to treat ruminants
  • Use of PPAR agonists to treat ruminants
  • Use of PPAR agonists to treat ruminants

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0121] Twelve lactating cows were selected to study the pharmacokinetic and pharmacodynamic properties of 2 PPARα agonists - Compound "X" and Compound "Y". Both compounds were administered by IV and SC routes as indicated in the table below.

[0122] treat

dosage

Cow No.

T1 compound "X"

T2 compound "X"

T3 compound "Y"

T4 compound "Y"

0.5mg / kg IV

0.5mg / kg SC

0.5mg / kg IV

0.5mg / kg SC

3

3

3

3

[0123] All animals were bled one day, and 15 minutes prior to compound administration. Blood samples were collected from IV-treated animals 5 and 10 minutes after compound administration. Blood samples were collected from all animals at 0.5, 1, 2, 4, 6, 24, 30, 48, 54, and 72 hours after compound administration. Samples were analyzed for glucose concentration using a Dade Behring Dimension RXL Serum Chemistry Analyzer. Treatment with both compounds, regardless of route of administration, caused...

Embodiment 2

[0127] Ten lactating cows fed a low starch / high fat diet were selected to study the effect of dosing on circulating glucose levels. Animals were fed a low-starch / high-fat diet for one week prior to dosing and remained on the same diet throughout the study.

[0128] treat

dosage

Cow No.

T1 saline

T2 Compound A

3.0mL SC

0.5mg / kg SC

5

5

[0129] All animals were bled 5 minutes prior to compound administration. Blood samples were collected from all animals at 2, 4, 6, 8, 24, 32, and 48 hours after compound administration. In this example, Compound A is the PPAR alpha agonist (3S)-3-[3-(1-carboxy-1-methyl-ethoxy)-phenyl]-piperidine-1-carboxylic acid 4- Trifluoromethyl-benzyl ester.

[0130]

[0131] Samples were analyzed for glucose concentration using an Olympus AU640 analyzer. Treatment with compounds elicited a transient increase in glucose relative to saline controls. The results are shown in Figure 2.

[0...

preparation Embodiment

[0224] In the following formulations, "active ingredient" means a compound used in the present invention.

[0225] Formulation 1: Solution for parenteral administration

[0226] A solution of the active ingredient is prepared as follows:

[0227] Element

Amount (mg / 5ml)

active ingredient

Potassium hydroxide

Sodium dihydrogen phosphate

Sodium hydrogen phosphate

Methylparaben

water

1-750

0.1-75

0-50

0-100

0-40

up to 5ml

[0228] or

[0229] Formulation 1a: Solution for Parenteral Administration

[0230] A solution of the active ingredient is prepared as follows:

[0231] Element

Amount (mg / 5ml)

active ingredient

Potassium hydroxide

sodium hydroxide

Sodium dihydrogen phosphate

Sodium hydrogen phosphate

pvp

Methylparaben

water

1-750

0-75

0-75

0-50

0-100

0-50

0-40

up to 5...

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PUM

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Abstract

The use of a PPAR agonist in the manufacture of a medicament to increase ruminant serum glucose concentrations, and preferably, the use for the palliative, prophylactic or curative treatment of ruminant disease associated with reduced serum glucose concentration. The ruminant disease associated with reduced serum glucose concentration includes fatty liver syndrome, dystocia, immune dysfunction, impaired immune function, toxification, primary ketosis, secondary ketosis, downer cow syndrome, indigestion, inappetence, retained placenta, displaced abomasum, mastitis, (endo-)-metritis, infertility, low fertility, lameness, subacute rumen acidosis and inadequate nutrient intake associated with stress e.g. heat, poor housing, overcrowding, shipping, dominance or illness.

Description

technical field [0001] The invention described herein relates to the novel use of peroxisome proliferator-activated receptor (PPAR) agonists for increasing serum glucose levels in ruminants. In particular, the present invention provides the use of a PPAR agonist for the treatment of diseases in ruminants associated with decreased blood glucose concentrations. As a separate aspect, the present invention also provides the use of a PPAR agonist in the treatment of fatty liver in felines. Background technique [0002] Peroxisome proliferator-activated receptors (PPARs) are involved in many biological processes and disease conditions including hypercholesterolemia, dyslipidemia, and diabetes. PPARs are members of the nuclear receptor superfamily of transcription factors, which includes steroid, thyroid, and vitamin D receptors. They play a role in controlling the expression of proteins that regulate lipid and carbohydrate metabolism and are activated by fatty acids and fatty ac...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61K31/451A61P1/00A61P1/16A61P3/00A61P15/00A61P37/00A23K1/16A23K1/18
CPCA23K1/1612A61K31/47A61K31/19A61K31/192A23K1/1813A61K31/451A61K31/422A61K31/4709A61K31/427A23K20/111A23K50/10A61P1/00A61P1/16A61P15/00A61P3/00A61P3/06A61P37/00
Inventor L·F·戈策M·E·小克尔里A·P·里基茨P·C·陶布
Owner PFIZER PROD INC
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