Category: 87486-34-8

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 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

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

On April 23, 2015, Bennett, Michael John; Betancort, Juan Manuel; Boloor, Amogh; Kaldor, Stephen W.; Stafford, Jeffrey Alan; Veal, James Marvin published a patent.Recommanded Product: 3,5-Dibromo-1-methylpyrazin-2(1H)-one The title of the patent was Heterocyclic compounds as bromodomain inhibitors and their preparation. And the patent contained the following:

The invention relates to substituted heterocyclic compounds of formula I, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease. Compounds of formula I wherein R2 is Me, ET, CH2CF3, etc.; X5 is CR5 and N; X6 is CR6 and N; X7 is CR7 and N; X8 is CR8 and N;, provided that no more than two of X5 – X8 are N; R5, R6 and R7 are independently H, halo, OH, CN, amino, alkyl, etc.; R8 is H, halo and alkyl; Ra is substituted Ph and substituted heteroaryl; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cross-coupling of 4-bromo-2-methylisoquinolin-1(2H)-one with (3-methoxyphenyl)boronic acid. The invention compounds were evaluated for their BRD4 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value in the range of > 0.5 μM to ≤ 5.0 μM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Recommanded Product: 3,5-Dibromo-1-methylpyrazin-2(1H)-one

The Article related to heterocycle preparation bromodomain inhibitor, Heterocyclic Compounds (One Hetero Atom): Quinolines and Isoquinolines and other aspects.Recommanded Product: 3,5-Dibromo-1-methylpyrazin-2(1H)-one

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 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 21, 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 Preparation of indole derivatives for use as kinase inhibitors. And the patent contained the following:

Title compounds I [R1 = alkyl, cycloalkyl, (un)substituted aryl, etc.; R2 = substituted pyrazine or imidazopyrazine; X = CH2 or CH2CH2], and their pharmaceutically acceptable salts, are prepared and disclosed as kinase inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated in BTK TR-FRET kinase activity assays (data given). 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 indole preparation kinase inhibitor, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Safety of 3,5-Dibromo-1-methylpyrazin-2(1H)-one

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On February 17, 2022, Bushaboina, Mallesh; Chen, Xin; Cheung, Atwood Kim; Culshaw, Andrew James; Hurley, Timothy Brian; Labbe-Giguere, Nancy; Miltz, Wolfgang; Orain, David; Patel, Tajesh; Rajagopalan, Srinivasan; Roehn, Till; Sandham, David Andrew; Thoma, Gebhard; Tichkule, Ritesh Bhanudasji; Waelchli, Rudolf published a patent.Recommanded Product: 87486-34-8 The title of the patent was Preparation of heteroaryl substituted spiropiperidinyl derivatives as LTC4S inhibitors and pharmaceutical uses thereof. And the patent contained the following:

The invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The invention further provides a combination of pharmacol. active agents and a pharmaceutical composition Compounds of formula I wherein R1 is (un)substituted phenyl; R2 is H and F; X1 is CH2 and O; R4 is (un)substituted (mono/bi)cyclic heteroaryl; and a pharmaceutically acceptable salt thereof, are claimed. Example compound II was prepared by oxidation of 2-(4-fluorophenyl)-1-hydrazinecarbothiomide; the resulting (E)-amino(2-(4-fluorophenyl)hydrazono)methanesulfonic acid underwent amination with 1-(4-chloro-3-fluorophenyl)-1,9-diazaspiro[5.5]undecane-2-one to give 1-(4-chloro-3-fluorophenyl)-N’-(4-fluorophenyl)-2-oxo-1,9-diazaspiro[5.5]undecane-9-carboximidehydrazide, which underwent cyclization to give compound II. The invention compounds were evaluated for their LTC4S inhibitory activity (data given). 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 heteroaryl spiropiperidine preparation ltc4s inhibitor, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Recommanded Product: 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem