Pyrazine derivatives, Methods of use, and methods for preparing same

a technology of pyrazine and derivatives, which is applied in the field of methods for producing pyrazine derivatives, can solve the problems of undesirable for a number of medical uses, markers and methods suffer from drawbacks, etc., and achieve the effect of rapid renal clearan

Inactive Publication Date: 2010-01-14
MEDIBEACON
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006]Among the various aspects of the present invention are pyrazine derivatives that may be detected in vivo and used in a number of medical procedures (e.g., renal function monitoring). Without being bound by a particular theory, the pyrazine derivatives described herein may be designed to be hydrophilic and / or have rigid functionality, thus allowing for rapid renal clearance while providing desired pharmacokinetic properties for monitoring renal function.

Problems solved by technology

[14] Unfortunately, these markers and methods suffer from drawbacks such as the use of radioactivity and / or ionizing radiation.
These limitations make them undesirable for a number of medical uses (e.g., real-time, bedside renal function monitoring).

Method used

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  • Pyrazine derivatives, Methods of use, and methods for preparing same
  • Pyrazine derivatives, Methods of use, and methods for preparing same
  • Pyrazine derivatives, Methods of use, and methods for preparing same

Examples

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example 1

Protocol for Assessing Renal Function

[0143]An example of an in vivo renal monitoring assembly 10 is shown in FIG. 1 and includes a light source 12 and a data processing system 14. The light source 12 generally includes or is interconnected with an appropriate device for exposing at least a portion of a patient's body to light therefrom. Examples of appropriate devices that may be interconnected with or be a part of the light source 12 include, but are not limited to, catheters, endoscopes, fiber optics, ear clips, hand bands, head bands, forehead sensors, surface coils, and finger probes. Indeed, any of a number of devices capable of emitting visible and / or near infrared light of the light source may be employed in the renal monitoring assembly 10.

[0144]Still referring to FIG. 1, the data processing system 14 of the renal monitoring assembly 10 may be any appropriate system capable of detecting spectral energy and processing data indicative of the spectral energy. For instance, the ...

example 2

Synthesis of Representative Pyrazine PEG Analogues

[0148]Unless otherwise noted, all reagents in this Example were used as supplied. Organic extracts were dried over anhydrous Na2SO4 and filtered using a fluted filter paper (P8). Solvents were removed on a rotary evaporator under reduced pressure. RP-LC / MS (ESI, positive ion mode) analyses were carried out on a Waters Micromass ZQ system equipped with a PDA detector using either a BDS Hypersil C18 3 μm (50 mm×4.6 mm) or a ThermoElectron Hypersil Gold C18 3 μm (4.6 mm×50 mm) column. Compounds were injected using a gradient condition (5 to 50-95% B / 6 min) with a flow rate of 1 mL / min (mobile phase A: 0.05% TFA in H2O; mobile phase B: 0.05% TFA in CH3CN). Chemical shifts are expressed in parts per million (δ) relative to TMS (δ=0) as an internal standard and coupling constants (J) are reported in Hz.

A. Diethyl 3,6-bis(benzylamino)pyrazine-2,5-dicarboxylate (7)

[0149]

[0150]To a well-stirred red suspension of diethyl 3,6-diaminopyrazine-2,...

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Abstract

The present invention relates to methods for producing N,N′-alkylated diaminopyrazines.

Description

RELATED APPLICATIONS[0001]This application claims priority to U.S. provisional application Ser. Nos. 61 / 080,207 and 61 / 082,296 filed on 11 Jul. 2008 and 21 Jul. 2008 (respectively), both of which are entitled “Pyrazine Derivatives, Methods of Use, and Methods for Preparing Same,” and both of which are incorporated by reference herein to the extent their teachings are not inconsistent with that of the present application.FIELD[0002]The present invention relates to methods for producing pyrazine derivatives, and particularly, methods for producing N,N′-alkylated diaminopyrazines.INTRODUCTION[0003]The ability to continuously monitor renal function via the glomerular filtration rate (GFR) in the clinic is currently an unmet medical need.[1-5] Monitoring of renal function is important to reduce the risk of acute renal failure caused by clinical, physiological, and pathological conditions. It is particularly important in the cases of critically ill or injured patients, since these patient...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): C07D241/10
CPCC07D241/28A61P13/12A61P43/00
InventorDORSHOW, RICHARD B.FRESKOS, JOHNNEUMANN, WILLIAM L.POREDDY, AMRUTA REDDYRAJAGOPALAN, RAGHAVAN
OwnerMEDIBEACON