Author: Jessica.F

On August 14, 2018, Mercado, Rocio; Fu, Rueih-Sheng; Yakutovich, Aliaksandr V.; Talirz, Leopold; Haranczyk, Maciej; Smit, Berend published an article.Safety of 3,6-Dibromopyrazine-2,5-dicarbonitrile The title of the article was In Silico Design of 2D and 3D Covalent Organic Frameworks for Methane Storage Applications. And the article contained the following:

We present a database of 69,840 largely novel covalent organic frameworks assembled in silico from 666 distinct organic linkers and 4 established synthetic routes. Due to their light weights and high internal surface areas, the frameworks are promising materials for CH4 storage applications. To assess their CH4 storage performance, we used grand-canonical Monte Carlo simulations to calculate their deliverable capacities. We demonstrate that the best structure, composed of C-C bonded triazine linkers in the tbd topol., has a predicted 65-bar deliverable capacity of 216 v STP/v, better than the best CH4 storage materials published to date. Using our approach, we also discovered other high-performing materials with 300 structures with calculated deliverable capacities >190 v STP/v and 10% of these outperforming 200 v STP/v. To encourage screening studies of these materials for other applications, all structures and their properties were made available on the Materials Cloud. The experimental process involved the reaction of 3,6-Dibromopyrazine-2,5-dicarbonitrile(cas: 1391026-27-9).Safety of 3,6-Dibromopyrazine-2,5-dicarbonitrile

The Article related to silico design twodimensional threedimensional covalent organic framework methane storage, Electrochemical, Radiational, and Thermal Energy Technology: Energy Handling, Transport, and Storage and other aspects.Safety of 3,6-Dibromopyrazine-2,5-dicarbonitrile

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On October 10, 2002, Janssen, Paul Adriaan Jan; Van Aken, Koen Jeanne Alfons; Lewi, Paulus Joannes; Koymans, Lucien Maria Henricus; De Jonge, Marc Rene; Heeres, Jan; Daeyaert, Frederik Frans Desire; Hoornaert, Georges Joseph Cornelius; Compernolle, Frans Josef Cornelius; Kilonda, Amuri published a patent.COA of Formula: C5H4Br2N2O The title of the patent was Preparation of HIV inhibiting pyrazinones. And the patent contained the following:

The title compounds [I; R1 = H, OH, CN, etc.; R2 = H, halo, SH, etc.; R3, R4 = (un)substituted Ph, pyridyl, pyrimidinyl, etc.; X = O, N:N, NHNH, NR14, alkanediyl, etc.; R14 = H, aryl, formyl, etc.], useful in inhibiting HIV replication, were prepared Thus, refluxing 5-bromo-3-(4-cyanophenylamino)-1,6-dimethyl-2(1H)-pyrazinone (preparation given) with 4-hydroxy-3,5-dimethylbenzonitrile in the presence of cesium carbonate, copper(I) chloride, 1-naphthoic acid and mol. sieves 4Å in toluene for 6 days afforded II which showed IC50 of 0.0063 μM against HIV-1. 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 pyrazinone preparation hiv1 inhibition aids, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.COA of Formula: C5H4Br2N2O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On August 4, 2017, Boruah, Anima; Subramanya, Hosahalli published a patent.COA of Formula: C5H4Br2N2O The title of the patent was Substituted 2-pyrazinone derivatives as kinase inhibitors and their preparation. And the patent contained the following:

The invention provides substituted 2-pyrazinone derivatives of formula I as protein kinase inhibitors, and pharmaceutically acceptable salts thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The invention also provides methods for synthesizing and administering the protein kinase inhibitor compounds The invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. Compounds of formula I wherein dashed bonds are single and double bonds; A is absent, CH, CH2, and CHCH2; X is N, C and CH; R1 is H and (un)substituted C1-6 alkyl; R2 is H, OH, acyl, (un)substituted C1-6 alkyl; R1R2 can be taken together to form (un)substituted heterocyclyl; R3 and R7 are independently H, acyl, (un)substituted C1-6 alkyl, (un)substituted aryl, etc.; R4 and R5 are independently H, halo, CN, OH, NO2, etc.; R3R4 can be taken together to form (un)substituted carbocyclic or (un)substituted heterocyclic ring; R6 is H, halo, CN, OH, NO2, etc.; m and p are independently 0 to 2; and pharmaceutically acceptable salts, derivatives, pro-drugs, isomers, stereoisomers, solvates and biol. active metabolites thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their protein kinase inhibitory activity (some data given). 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 pyrazinone preparation protein kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.COA of Formula: C5H4Br2N2O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On April 28, 2022, Weiss, Matthew M.; Zheng, Xiaozhang; Zhu, Xiao published a patent.Computed Properties of 87486-34-8 The title of the patent was Preparation of trifunctional compounds as IRAK4 degraders and uses thereof. And the patent contained the following:

The present application relates to novel trifunctional compounds, which function to recruit IRAK and BTK to E3 ubiquitin ligase for degradation, and methods of preparation and uses thereof. Compounds of formula I-IV wherein LBM is E3 ubiquitin ligase binding moiety; IBM is IRAK binding moiety capable of binding to one or more of IRAK1, IRAK2, IRAK3, IRAK4, preferably IRAK4; BBM is a BTK-binding moiety capable of binding to BTK; A is a bivalent moiety that connects LBM to IBM; B is a bivalent moiety that connects LBM to BBM; G is a bivalent moiety that connects IBM to BBM; D is a bivalent moiety that connects LBM to X; E is a bivalent moiety that connects IBM to X; F is a bivalent moiety that connects BBM to X; and X is a trivalent moiety that connects D, E, and F; and pharmaceutically acceptable salts thereof, are claimed. Example compound V was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their targeted degradation of IRAK4 (data given). From the assay, it was determined that example compound V exhibited DC50 value of <1μM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Computed Properties of 87486-34-8

The Article related to trifunctional compound preparation irak4 degrader, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Computed Properties of 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On February 17, 2022, Chen, Yi published a patent.SDS of cas: 87486-34-8 The title of the patent was Preparation of heterocyclic compounds as BTK inhibitors, and dosage form compositions comprising an inhibitor of BTK and mutants thereof. And the patent contained the following:

Provided herewith are pharmaceutical tablet compositions comprising an organic acid (such as fumaric acid) and a compound of formula I, or an N-oxide thereof, solvate, polymorph, tautomer, stereoisomer, an isotopic form, or a prodrug of said compound of formula I or N-oxide thereof: wherein the compound of formula I is an inhibitor of Bruton’ s tyrosine kinase. Compounds of formula I wherein Q3 is 5-membered heteroaryl; m and n are independently 0, 1, 2, 3 and 4; R1 and R5 are independently H, D, alkyl,spiroalkyl, alkenyl, etc.; and their tablet compositions comprising organic acids, N-oxides, polymorphs, tautomers, stereoisomers, isotopic forms, and prodrugs, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were formulated as tablets and tested for pharmacokinetic properties (data given). 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 heterocyclyl preparation btk inhibitor dosage form, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On June 7, 2007, Mulvihill, Kristen Michelle; Castelhano, Arlindo L. published a patent.Category: pyrazines The title of the patent was Process for the preparation of substituted imidazo[1,5-a]pyrazines. And the patent contained the following:

The title compounds [I; X = Cl, Br, I; e.g., 3-(1-bromo-8-chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone] are prepared by the halogenation of 3-(8-chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone with either N-chloro-, N-bromo-, or N-iodosuccinimide (e.g., NBS) in a compatible solvent (e.g., DMF) at 0-60°. The experimental process involved the reaction of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone(cas: 936901-72-3).Category: pyrazines

The Article related to bromochloroimidazopyrazinylcyclobutanone preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Category: pyrazines

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On May 10, 2013, Crawford, James John; Ortwine, Daniel Fred; Wei, Binqing; Young, Wendy B. published a patent.Recommanded Product: 87486-34-8 The title of the patent was Heteroarylpyridone and azapyridone compounds as inhibitors of BTK activity and their preparation. And the patent contained the following:

The invention relates to heteroarylpyridone and azapyridone compounds of formula I and stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathol. conditions, are disclosed. Compounds of formula I wherein X1is CR1 and N; X2 is CR2 and N; X3 is CR3 and N, where one or two of X1 – X2 are N; R1, R2 and R4 are independently H, F, Cl, NH2, etc.; R4 is H, F, Cl, CN, CH2OH, etc.; R5 is (un)substituted C6-20 aryl, C3-12 carbocyclyl, C1-20 heteroaryl, etc.; R6 is H, Me, Et, etc.; R7 is (un)substituted tricyclic azacyclyl; Y1 and Y2 are independently CH and N, provided that not both of Y1 and Y2 are N; and stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their BTK inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.132 μM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Recommanded Product: 87486-34-8

The Article related to heteroarylpyridone azapyridone preparation btk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On August 31, 1983, Vekemans, J.; Pollers-Wieers, C.; Hoornaert, G. published an article.SDS of cas: 87486-34-8 The title of the article was A new synthesis of substituted 2(1H)-pyrazinones. And the article contained the following:

The hydrohalides of 2-sec-aminoalkanenitriles on treatment with oxalyl halides in o-Cl2C6H4 at 80-100° give 3,5-dihalo-2(1H)-pyrazinones, e.g. I, of which the 3-halo substituent is easily replaced by nucleophiles. A reaction mechanism for the pyrazinone synthesis is proposed. 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 pyrazinone, aminoalkanenitrile cyclization oxalyl chloride, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On January 15, 2009, Barr, Sharon; Buck, Elizabeth; Eyzaguirre, Alexandra; Russo, Suzanne; Bhagwat, Shripad published a patent.Electric Literature of 936901-72-3 The title of the patent was Preparation of imidazo[1,5-a]pyrazin-8-amine for use in combination therapy of cancers and cancer metastasis. And the patent contained the following:

The present invention provides a method for treating tumors or tumor metastases in patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an anti-cancer agents or treatment that elevates pAkt levels in tumor cells and mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. Examples of such anti-cancer agents or treatments include doxorubicin, cisplatin, or ionizing radiation. The invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of the anti-cancer agent melphalan or 5-FU, and mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. The invention also provides a pharmaceutical composition comprising an anti-cancer agent or treatment that elevates pAkt levels in tumor cells and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. Example compound I was prepared by cross-coupling of 8-amino-3-cyclobutyl-1-iodoimidazol[3,4-a]pyrazine with 5-(4,4,5,5-tetramethyl-1,3,2-dioxoborolan-2-yl)-1H-indole. The invention compounds were evaluated in various biol. tests (some data given). The experimental process involved the reaction of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone(cas: 936901-72-3).Electric Literature of 936901-72-3

The Article related to imidazopyrazinamine preparation mtor kinase inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 936901-72-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On September 20, 2007, Buck, Elizabeth A.; Griffin, Graeme; Barr, Sharon M. published a patent.Safety of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone The title of the patent was Imidazo[1,5-a]pyrazin-8-amine in combined treatment with an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors. And the patent contained the following:

The invention provides a method for manufacturing a medicament intended for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in combination with an EGFR kinase inhibitor, characterized in that an mTOR inhibitor is used, and wherein the inhibitors are intended for administration either simultaneously or sequentially, and with or without administration of addnl. agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also provides a method for manufacturing a medicament intended for treating tumors or tumor metastases in a patient in combination of an EGFR kinase inhibitor, characterized in that an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases is used, and wherein the inhibitors are intended for administration either simultaneously or sequentially, and with or without administration of addnl. agents or treatments, such as other anti-cancer drugs or radiation therapy. The invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA). Example compound I was prepared by cross-coupling of 8-amino-3-cyclobutyl-1-iodoimidazol[3,4-a]pyrazine with 5-(4,4,5,5-tetramethyl-1,3,2-dioxoborolan-2-yl)-1H-indole. All the invention compounds were evaluated for their EGFR kinase inhibitory activity (some data given). The experimental process involved the reaction of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone(cas: 936901-72-3).Safety of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

The Article related to imidazopyrazinamine preparation egfr kinase inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem