Tag: 200-300

On May 5, 2022, Chen, Yi published a patent.HPLC of Formula: 87486-34-8 The title of the patent was Synthesis of Pyridine BTK inhibitors treating cancers, autoimmune and inflammatory diseases. And the patent contained the following:

The synthesis of pyridine BTK inhibitors, I, wherein Q is a 5-9 membered aryl or heteroaryl ring; Q1 is a 5-7 membered heterocycloalkyl group; Q2 can be a 5-membered heteroaryl or Ph ring; Q3 can be a 6-membered heteroaryl group; Z can be absent, alkyl ether, amine, thioether, carbonyl, sulfonyl, sulfone, ester, or related moieties; L can be absent or an appropriate linker group; the warhead is an alkene or alkyne group; R can be independently H, D, alkyl, spiroalkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, or related groups; R1 can be H, halo, alkyl, haloalkyl, or hydroxyalkyl; R2 can be H, halo, or low alkyl; treating cancers, autoimmune and inflammatory diseases. Of note, II was synthesized and tested in an in vitro dialysis assay WT BTK with an IC50 of 7.0 nM, in pharmacokinetics, xenograft and arthritis studies. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).HPLC of Formula: 87486-34-8

The Article related to pyridine btk inhibitor preparation anticancer autoimmune inflammatory, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.HPLC of Formula: 87486-34-8

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

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 November 19, 2009, Crew, Andrew P.; Jin, Meizhong; Kadalbajoo, Mridula; Kleinberg, Andrew; Mulvihill, Mark J.; Wang, Jing published a patent.Name: 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone The title of the patent was Substituted imidazopyrazines and imidazotriazines as ACK1 inhibitors and their preparation. And the patent contained the following:

The invention relates to fused pyridine-based bicyclic compounds having the structure of formula I, pharmaceutically acceptable salts thereof, preparation, compositions, and disease treatment therewith. Compounds of formula I wherein A is CH and N; Q1 is X1Y1Z1, 1-phenylbenzimidazol-5-yl and carbazolyl; X1 is (un)substituted 5- to 10-membered cyclic ring; Y is CO, O, S, SO, SO2, etc.; Z1 is (un)substituted 5- to 10-membered cyclic ring and C1-6 alkoxy; R1 is SH and derivatives, (un)substituted C1-6 alkyl, (un)substituted 5,6-bicyclic aryl and (un)substituted 3- to 6-membered ring; and pharmaceutically acceptable salt thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). All the invention compounds were evaluated for their ACK1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.1759 μM. The experimental process involved the reaction of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone(cas: 936901-72-3).Name: 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

The Article related to imidazopyrazine imidazotriazine preparation ack1 inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Triazines and other aspects.Name: 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On January 2, 2014, Do, Steven; Hu, Huiyong; Kolesnikov, Aleksandr; Tsui, Vickie H.; Wang, Xiaojing published a patent.SDS of cas: 87486-34-8 The title of the patent was 5-Azaindazole compounds as Pim kinase inhibitors and their preparation. And the patent contained the following:

5-Azaindazole compounds of formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Compounds of formula I wherein R1 is (un)substituted 5- to 6-membered heteroaryl; R2 is (un)substituted Ph and (un)substituted 6-membered heteroaryl; and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their Pim kinase inhibitory activity (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 azaindazole preparation pim kinase inhibitors, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.SDS of cas: 87486-34-8

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 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 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 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 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