Author: Jessica.F

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

On August 10, 2016, Wang, Xuehai; Wu, Chengde; Xu, Yong; Shen, Chunli; Li, Lie; Hu, Guoping; Yue, Yang; Li, Jian; Guo, Diliang; Shi, Nengyang; Huang, Lu; Chen, Shuhui; Tu, Ronghua; Yang, Zhongwen; Zhang, Xuwen; Xiao, Qiang; Tian, Hua; Yu, Yanping; Chen, Hailiang; Sun, Wenjie; He, Zhenyu; Shen, Jie; Yang, Jing; Tang, Jing; Zhou, Wen; Yu, Jing; Zhang, Yi; Liu, Quan published a patent.SDS of cas: 87486-34-8 The title of the patent was Btk inhibitor. And the patent contained the following:

Provided are a series of heterocyclic compounds as BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or pro-drug thereof. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).SDS of cas: 87486-34-8

The Article related to heterocycle preparation btk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.SDS of cas: 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On July 21, 2016, Wang, Xuehai; Wu, Chengde; Xu, Yong; Shen, Chunli; Li, Li’e; Hu, Guoping; Yue, Yang; Li, Jian; Guo, Diliang; Shi, Nengyang; Huang, Lu; Chen, Shuhui; Tu, Ronghua; Yang, Zhongwen; Zhang, Xuwen; Xiao, Qiang; Tian, Hua; Yu, Yanping; Chen, Hailiang; Sun, Wenjie; He, Zhenyu; Shen, Jie; Yang, Jing; Tang, Jing; Zhou, Wen; Yu, Jing; Zhang, Yi; Liu, Quan published a patent.Name: 3,5-Dibromo-1-methylpyrazin-2(1H)-one The title of the patent was Btk inhibitor. And the patent contained the following:

Provided are a series of heterocyclic compounds as BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or pro-drug thereof. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Name: 3,5-Dibromo-1-methylpyrazin-2(1H)-one

The Article related to heterocycle preparation btk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Name: 3,5-Dibromo-1-methylpyrazin-2(1H)-one

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On December 31, 2021, Choi, Sunju; Matta, Hittu; Gopalakrishnan, Ramakrishnan; Natarajan, Venkatesh; Gong, Songjie; Jeronimo, Alberto; Kuo, Wei-Ying; Bravo, Bryant; Chaudhary, Preet M. published an article.COA of Formula: C26H21N3O3 The title of the article was A novel thermostable beetle luciferase based cytotoxicity assay. And the article contained the following:

Cytotoxicity assays are essential for the testing and development of novel immunotherapies for the treatment of cancer. We recently described a novel cytotoxicity assay, termed the Matador assay, which was based on marine luciferases and their engineered derivatives In this study, we describe the development of a new cytotoxicity assay termed ‘Matador-Glo assay’ which takes advantage of a thermostable variant of Click Beetle Luciferase (Luc146-1H2). Matador-Glo assay utilizes Luc146-1H2 and D-luciferin as the luciferase-substrate pair for luminescence detection. The assay involves ectopic over-expression of Luc146-1H2 in the cytosol of target cells of interest. Upon damage to the membrane integrity, the Luc146-1H2 is either released from the dead and dying cells or its activity is preferentially measured in dead and dying cells. We demonstrate that this assay is simple, fast, specific, sensitive, cost-efficient, and not labor-intensive. We further demonstrate that the Matador-Glo assay can be combined with the marine luciferase-based Matador assay to develop a dual luciferase assay for cell death detection. Finally, we demonstrate that the Luc146-1H2 expressing target cells can also be used for in vivo bioluminescence imaging applications. 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).COA of Formula: C26H21N3O3

The Article related to luciferase thermostability isolation beetle anticancer agent cytotoxicity, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.COA of Formula: C26H21N3O3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On July 17, 2014, Boruah, Anima; Hosahalli, Subramanya; Panigrahi, Sunil Kumar published a patent.Safety of 3,5-Dibromo-1-methylpyrazin-2(1H)-one The title of the patent was Substituted 2-pyrazinone derivatives as kinase inhibitors. And the patent contained the following:

The present invention provides novel substituted 2-pyrazinone derivatives (I) as protein kinase inhibitors that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting kinase enzyme, more particularly BTK enzyme. The present invention also provides methods for synthesizing and administering the kinase inhibitor compounds The present invention also provides pharmaceutical formulations comprising at least one of the kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Safety of 3,5-Dibromo-1-methylpyrazin-2(1H)-one

The Article related to btk kinase inhibitor pyrazinone derivative preparation cancer autoimmune inflammation, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Safety of 3,5-Dibromo-1-methylpyrazin-2(1H)-one

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Sepehrirad, Shahrzad; Amanlou, Arash; Bagherzadeh, Kowsar; Azizian, Homa; Amanlou, Massoud published an article in 2021, the title of the article was Library-based lead compound discovery for CS-1 protein in multiple myeloma: homology modelling, molecular dynamic simulations, virtual screening and molecular docking.Quality Control of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one And the article contains the following content:

The signaling lymphocytic activation mol. F7 (CS-1) enables the selective killing of the myeloma cells with minimal side effects on the healthy tissue. In this study, we have modelled the 3D structure of CS-1 followed by performing mol. dynamic simulations. To develop a potential CS-1 modulator, a virtual screening of the ‘Bioactive Compound Database’was conducted. The screening results have given three interacting regions. The best representative structure of each class and mode of action were revealed. Our study suggests compounds ICG-001, Avanafil, and BPTES, as novel drug candidates at the CS-1 protein target. The mol. dynamic simulation study reveals that the resulted compounds provide different binding patterns over the CS-1 Ig-like V-type domain in which Avanafil and BPTES provide stable interactions with their binding environment located at the bc-hi loops clefts and bc-fg loops clefts, resp. In contrast, compound ICG-001 shows more flexible and transient non-binding interaction due to the vast binding region over β-sheet strands consisting of H, C and D during the simulation timeline. We conclude that the identified compounds seem to be the best candidates to design a series of new compounds with the ability to bind to CS-1 with potential binding activity to its target. 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).Quality Control of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

The Article related to lead protein multiple myeloma mol docking simulation virtual screening, cs protein multiple myeloma mol docking simulation virtual screening, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.Quality Control of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On January 31, 2011, Di Paolo, Julie A.; Huang, Tao; Balazs, Mercedesz; Barbosa, James; Barck, Kai H.; Bravo, Brandon J.; Carano, Richard A. D.; Darrow, James; Davies, Douglas R.; DeForge, Laura E.; Diehl, Lauri; Ferrando, Ronald; Gallion, Steven L.; Giannetti, Anthony M.; Gribling, Peter; Hurez, Vincent; Hymowitz, Sarah G.; Jones, Randall; Kropf, Jeffrey E.; Lee, Wyne P.; Maciejewski, Patricia M.; Mitchell, Scott A.; Rong, Hong; Staker, Bart L.; Whitney, J. Andrew; Yeh, Sherry; Young, Wendy B.; Yu, Christine; Zhang, Juan; Reif, Karin; Currie, Kevin S. published an article.COA of Formula: C5H4Br2N2O The title of the article was Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis. And the article contained the following:

Bruton’s tyrosine kinase (Btk) is a therapeutic target for rheumatoid arthritis, but the cellular and mol. mechanisms by which Btk mediates inflammation are poorly understood. Here we describe the discovery of CGI1746, a small-mol. Btk inhibitor chemotype with a new binding mode that stabilizes an inactive nonphosphorylated enzyme conformation. CGI1746 has exquisite selectivity for Btk and inhibits both auto- and transphosphorylation steps necessary for enzyme activation. Using CGI1746, we demonstrate that Btk regulates inflammatory arthritis by two distinct mechanisms. CGI1746 blocks B cell receptor-dependent B cell proliferation and in prophylactic regimens reduces autoantibody levels in collagen-induced arthritis. In macrophages, Btk inhibition abolishes FcγRIII-induced TNFα, IL-1β and IL-6 production Accordingly, in myeloid- and FcγR-dependent autoantibody-induced arthritis, CGI1746 decreases cytokine levels within joints and ameliorates disease. These results provide new understanding of the function of Btk in both B cell- or myeloid cell-driven disease processes and provide a compelling rationale for targeting Btk in rheumatoid arthritis. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).COA of Formula: C5H4Br2N2O

The Article related to brutons tyrosine kinase inhibitor cgi1746 inflammatory cytokine rheumatoid arthritis, Pharmacology: Effects Of Inflammation Inhibitors and Immune Agents and other aspects.COA of Formula: C5H4Br2N2O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem