Compositions and systems for renal function determination

A compound, CH2 technology, applied in drug combinations, urinary system diseases, compound screening/testing, etc., can solve problems such as difficult re-evaluation of measurement values ​​and calculations, delays, inaccuracies, etc.

Pending Publication Date: 2019-11-22
MEDIBEACON
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Often, doses of medications are adjusted for renal function, so can be equally inaccurate, equally delayed, and difficult to reassess the measurements and calculations on which dosing is based

Method used

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  • Compositions and systems for renal function determination
  • Compositions and systems for renal function determination
  • Compositions and systems for renal function determination

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0144] Preparation of 3,6-diamino-N2,N2,N5,N5-tetrakis(2-methoxyethyl)pyrazine-2,5-dicarboxamide

[0145]

[0146] At room temperature, 3,6-diaminopyrazine-2,5-dicarboxylic acid (200 mg, 1.01 mmol), bis-2-(methoxyethyl)amine (372 μL, 335.5 mg, 2.52 mmol), HOBt·H 2 A mixture of O (459 mg, 3.00 mmol) and EDC·HCl (575 mg, 3.00 mmol) was stirred together in DMF (20 mL) for 1 h. The mixture was concentrated to dryness and the residue was partitioned with EtOAc and water. The layers were separated and washed with saturated NaHCO 3 The EtOAc solution was washed with brine. The solution was washed with anhydrous Na 2 SO 4 Dry, filter and concentrate. By radial flash chromatography (SiO 2 ,10 / 1CHCl 3 -MeOH) to afford 228.7 mg (53% yield) of Example 1 as an orange foam: 1 H NMR (300MHz, CDCl 3 ),4.92(s,4H),3.76(apparent t,J=5.4Hz,4H),3.70(apparent t,J=5.6Hz,4H),3.64(apparent t,J=5.4Hz,4H) ,3.565(apparent t,J=5.4Hz),3.67(s,6H),3.28(s,6H). 13 C NMR (75MHz, CDCl 3 )δ167.6(s...

Embodiment 2

[0148] 3,6-Diamino-N 2 ,N 5 -Bis(2,3-dihydroxypropyl)pyrazine-2,5-dicarboxamide

[0149]

[0150] Step 1. 3,6-Diamino-N 2 ,N 5 -Synthesis of bis((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)pyrazine-2,5-dicarboxamide

[0151]

[0152] 3,6-diaminopyrazine-2,5-dicarboxylic acid (350 mg, 1.77 mmol), racemic (2,2-dimethyl-1,3-dioxolane-4- base) methylamine (933μL, 944mg, 7.20mmol), HOBt·H 2 A mixture of O (812 mg, 5.3 mmol) and EDC·HCl (1.02 g, 5.32 mmol) was stirred together in DMF (20 mL) for 16 hours. The mixture was concentrated to dryness and the residue was partitioned with EtOAc and water. The layers were separated and washed with saturated NaHCO 3 The EtOAc solution was washed with brine. The solution was washed with anhydrous Na 2 SO 4 Drying, filtration and concentration afforded 665 mg (88% yield) of the bisamide diastereometric pair as a yellow solid: 1 NMR (300MHz, CDCl 3 )δ8.38(t, J=5.8Hz, 2H), 6.55(s, 4H), 4.21(quintet, J=5.8Hz, 2H), 3.98(dd, J=8.4Hz, 6....

Embodiment 3

[0155] (2S,2’S)-2,2’-((3,6-diaminopyrazine-2,5-dicarbonyl)bis-(azanediyl))-bis(3-hydroxypropionic acid)

[0156]

[0157] Step 1. 2,2'-((3,6-Diaminopyrazine-2,5-dicarbonyl)bis(azanediyl))(2S,2'S)-bis(3-(benzyloxy)propionic acid) Synthesis of Dimethyl Ester

[0158]

[0159] Sodium 3,6-diaminopyrazine-2,5-dicarboxylate (300mg, 1.24mmol), L-Ser(OBn)-OMe·HCl salt (647mg, 2.64mmol), HOBt·H 2 A mixture of O (570 mg, 3.72 mmol) and EDC·HCl (690 mg, 3.60 mmol) in DMF (25 mL) was treated with TEA (2 mL). The resulting mixture was stirred for 16 hours and concentrated. Carry out aftertreatment according to the method for Example 1, obtain the bisamide of 370mg (51% productive rate), be bright yellow powder: 1 NMR (300MHz, CDCl 3 ):8.47(d,J=8.74Hz,2H),7.25-7.37(complex m,10H),5.98(bs,4H),4.85(dt,J=8.7,3.3Hz,2H),4.56(ABq,J =12.6, Hz, △v=11.9Hz, 4H), 3.99 (half of ABq of d, J=8.7, 3.3, △v vague, 2H), 3.76-3.80 (half of ABq – vague, 2H), 3.78(s,6H). 13 C NMR (75MHz, CDCl 3 )δ...

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Abstract

The present disclosure relates to systems and methods for determining the renal glomerular filtration rate or assessing the renal function in a patient in need thereof. The system includes a computingdevice, a power supply, one or more sensors, and at least one tracer agent that fluoresces when exposed to electromagnetic radiation. The electromagnetic radiation is detected using the sensors, andthe rate in which the fluorescence decreases in the patient is used to calculate the renal glomerular filtration rate in the patient.

Description

Background technique [0001] The field disclosed herein relates generally to methods and pharmaceutical compositions comprising pyrazine derivatives for assessing renal function in a patient in need thereof. [0002] Acute renal failure (ARF) is a common condition among patients admitted to general surgery hospitals. About half of patients who develop ARF die directly from ARF or from complications related to the underlying medical condition, while survivors experience significantly increased morbidity and prolonged hospital stay. Early diagnosis is generally considered important because kidney failure is often asymptomatic and often requires careful follow-up of markers of kidney function in the blood. Active monitoring of renal function in patients is required in order to minimize the risk of acute renal failure caused by various clinical, physiological and pathological conditions. Such dynamic monitoring is often particularly important in the case of critically ill or inju...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/00A61P13/12C07D241/20
CPCA61K49/0004A61K49/0054C09B57/00A61K49/0021C07D241/26A61B5/0071A61B5/201A61B5/1495A61B5/0093A61P13/12A61B5/7203A61B5/6815A61B5/6813
Inventor 马丁·P·德布赖采尼拉加万·拉贾戈帕兰理查德·B·多尔休威廉·L·诺伊曼托马斯·E·罗格斯
Owner MEDIBEACON
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