Month: November 2022

On September 3, 2020, Chen, Yi published a patent.Category: pyrazines The title of the patent was Preparation of pyrrolopyrazines and related heterocycles as inhibitors of BTK and mutants thereof for the treatment of neoplastic, autoimmune and inflammatory disorders. And the patent contained the following:

The invention relates to preparation of pyrrolopyrazines and related heterocycles as inhibitors of BTK and mutants thereof. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compds and pharmaceutical compositions with them. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Category: pyrazines

The Article related to pyrrolopyrazine preparation prodrug pharmaceutical anticancer immunomodulator antiinflammatory, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Category: pyrazines

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On May 17, 2007, Chen, Xin; Coate, Heather; Crew, Andrew Philip; Dong, Han-Qing; Honda, Ayako; Mulvihill, Mark Joseph; Tavares, Paula A.R.; Wang, Jing; Werner, Douglas S.; Mulvihill, Kristen Michelle; Siu, Kam W.; Panicker, Bijoy; Bharadwaj, Apoorba; Arnold, Lee D.; Jin, Meizhong; Volk, Brian; Weng, Qinghua; Beard, James David published a patent.Application In Synthesis of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone The title of the patent was Preparation of substituted imidazopyrazines and related compounds as mTOR inhibitors. And the patent contained the following:

The title compounds I [X1, X2 = N or C(E1)aa; X5 = N, C(E1)aa or N(E1)aa; X3, X4, X6, X7 = N or C, wherein at least one of X3-X7 = N or N(E1)aa; R3 = alkyl, cycloalkyl, aryl, etc.; Q1 = (un)substituted indolyl, benzothiazolyl, etc.; E1 = halo, CF3, OCF3, etc.; aa = 0-1; with provisos] that are inhibitors of mTOR useful in the treatment of cancer, were prepared and formulated. Thus, coupling 8-amino-3-cyclobutyl-1-iodoimidazo[3,4-a]pyrazine with 5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole afforded II. The exemplified compounds I showed activity against mTOR kinase as demonstrated in the assays described in this invention. The experimental process involved the reaction of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone(cas: 936901-72-3).Application In Synthesis of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

The Article related to imidazopyrazine preparation mtor frap protein kinase inhibitor antitumor, imidazotriazine preparation mtor frap protein kinase inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Application In Synthesis of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Feno, Simona; Di Marco, Giulia; De Mario, Agnese; Monticelli, Halenya; Reane, Denis Vecellio published an article in 2019, the title of the article was High-throughput screening using photoluminescence probe to measure intracellular calcium levels.Synthetic Route of 55779-48-1 And the article contains the following content:

Aequorin, a 22 kDa protein produced by the jellyfish Aequorea victoria, was the first probe used to measure Ca2+ concentrations ([Ca2+]) of specific intracellular organelles in intact cells. After the binding of Ca2+ to three high-affinity binding sites, an irreversible reaction occurs leading to the emission of photons that is proportional to [Ca2+]. While native aequorin is suitable for measuring cytosolic [Ca2+] after cell stimulation in a range from 0.5 to 10, it cannot be used in organelles where [Ca2+] is much higher, such as in the lumen of endoplasmic/sarcoplasmic reticulum (ER/SR) and mitochondria. However, some modifications made on aequorin itself or on coelenterazine, its lipophilic prosthetic luminophore, and the addition of targeting sequences or the fusion with resident proteins allowed the specific organelle localization and the measurements of intra-organelle Ca2+ levels. In the last years, the development of multiwell plate readers has opened the possibility to perform aequorin-based high-throughput screenings and has overcome some limitation of the standard method. Here we present the procedure for expressing, targeting, and reconstituting aequorin in intact cells and for measuring Ca2+ in the bulk cytosol, mitochondria, and ER by a high-throughput screening system. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Synthetic Route of 55779-48-1

The Article related to calcium cytosol mitochondria endoplasmic reticulum photoluminescence probe, aequorin, calcium, calcium probes, cytosol, er, high-throughput screening, mitochondria, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Synthetic Route of 55779-48-1

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Ishimoto, Tetsuya; Okada, Takuya; Fujisaka, Shiho; Yagi, Kunimasa; Tobe, Kazuyuki; Toyooka, Naoki; Mori, Hisashi published an article in 2022, the title of the article was A New Method for Albuminuria Measurement Using a Specific Reaction between Albumin and the Luciferin of the Firefly Squid Watasenia scintillans.Application In Synthesis of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one And the article contains the following content:

This study demonstrates that the luciferin of the firefly squid Watasenia scintillans, which generally reacts with Watasenia luciferase, reacted with human albumin to emit light in proportion to the albumin concentration The luminescence showed a peak wavelength at 540 nm and was eliminated by heat or protease treatment. We used urine samples collected from patients with diabetes to quantify urinary albumin concentration, which is essential for the early diagnosis of diabetic nephropathy. Consequently, we were able to measure urinary albumin concentrations by precipitating urinary proteins with acetone before the reaction with luciferin. A correlation was found with the result of the immunoturbidimetric method; however, the Watasenia luciferin method tended to produce lower albumin concentrations This may be because the Watasenia luciferin reacts with only intact albumin. Therefore, the quantification method using Watasenia luciferin is a new principle of urinary albumin measurement that differs from already established methods such as immunoturbidimetry and high-performance liquid chromatog. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Application In Synthesis of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

The Article related to watasenia albuminuria albumin luciferin immunoturbidimetry bioluminescence, watasenia scintillans, albumin, bioluminescence, diabetic nephropathy, luciferin, urine, Biochemical Methods: Other (Not Covered At Other Subsections) and other aspects.Application In Synthesis of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem