Tag: 200-300

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 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 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 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 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 July 1, 2019, Yang, Jianhong; Du, Jiatian; Huang, Chong; Wang, Tianqi; Huang, Luyi; Yang, Shengyong; Li, Linli published an article.COA of Formula: C5H4Br2N2O The title of the article was Discovery of 5-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrazin-2(1H)-one derivatives as new potent PB2 inhibitors. And the article contained the following:

PB2 is an important subunit of influenza RNA-dependent RNA polymerase (RdRP) and has been recognized as a promising target for the treatment of influenza. We herein report the discovery of a new series of PB2 inhibitors containing the skeleton 5-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrazin-2(1H)-one. Compound I is the most potent one, which showed KD values of 0.11 μM and 0.19 μM in surface plasmon resonance (SPR) and isothermal titration calorimetry (ITC) assays, resp. In antiviral activity and cellular cytotoxicity assays, compound I showed an EC50 value of 1.025 μM and a CC50 value greater than 100 μM. Mol. docking was also used to predict the binding mode of I with PB2. Collectively, this study provides a promising lead compound for subsequent anti-influenza drug discovery targeting PB2. 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 fluoropyrrolopyridinyl pyrazinone preparation pb2 inhibitor antiinfluenza antiviral activity, influenza a virus, pb2, small molecule inhibitor, structure-activity relationship and other aspects.COA of Formula: C5H4Br2N2O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On July 28, 2016, Chen, Yi published a patent.Product Details of 87486-34-8 The title of the patent was Preparation of substituted [(6-phenyl-4-methyl-3-oxo-3,4-dihydropyrazin-2-yl)amino]benzene derivatives as selective Bruton’s tyrosine kinase inhibitors. And the patent contained the following:

The invention provides compounds I [R0 and R1 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, etc.; L = N(Rd)(CH2)m; Rd = H, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; m = 0-4; R2 = H or alkyl; R3 = H, halo, alkyl, or hydroxyalkyl; R4 = W, X, Y or Z; R5, R6, R7, R8, R9, R10, R11 and R12 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, halo, or alkoxy], or their N-oxides, pharmaceutically acceptable salts, solvates, polymorphs or tautomers. For example, compound II was prepared by coupling of compound III (preparation given) with compound IV (preparation given) followed by hydrolysis. The Kd value of compound II for Bruton’s tyrosine kinase (BTK) was 0.86 nM, which clearly shows that compound II is a highly potent BTK inhibitor. The invention compounds are useful as inhibitors of Bruton’s tyrosine kinase for the treatment of neoplastic disease, autoimmune disease and inflammatory disorder. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Product Details of 87486-34-8

The Article related to phenylmethyloxodihydropyrazinylaminobenzene compound preparation bruton tyrosine kinase inhibitor, neoplastic disease autoimmune disease inflammatory disorder treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Product Details of 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On April 9, 2015, Chen, Yi published a patent.Formula: C5H4Br2N2O The title of the patent was Preparation of substituted [(6-phenyl-4-methyl-3-oxo-3,4-dihydropyrazin-2-yl)amino]benzene derivatives as inhibitors of bruton’s tyrosine kinase. And the patent contained the following:

The present invention provides compounds I [R0 and R1 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, etc.; L = N(Rd)(CH2)m; Rd = H, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; m = 0-4; R2 = H or alkyl; R3 = H, halo, alkyl, or hydroxyalkyl; R4 = W, X, Y or Z; R5, R6, R7, R8, R9, R10, R11 and R12 = independently H, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, halo, or alkoxy], or their N-oxides, pharmaceutically acceptable salts, solvates, polymorphs or tautomers. For example, compound II was prepared by coupling of compound III (preparation given) with compound IV (preparation given) followed by hydrolysis. The Kd value of compound II for bruton’s tyrosine kinase (BTK) was 0.86 nM, which clearly shows that compound II is a highly potent BTK inhibitor. The invention compounds are useful as inhibitors of bruton’s tyrosine kinase for the treatment of neoplastic disease, autoimmune disease and inflammatory disorder. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Formula: C5H4Br2N2O

The Article related to phenylmethyloxodihydropyrazinylaminobenzene compound preparation bruton tyrosine kinase inhibitor, neoplastic disease autoimmune disease inflammatory disorder treatment, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Formula: C5H4Br2N2O

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On March 24, 2005, Heeres, Jan; de Jonge, Marc R.; Koymans, Lucien M. H.; Daeyaert, Frits F. D.; Vinkers, Maarten; Van Aken, Koen J. A.; Arnold, Edward; Das, Kalyan; Kilonda, Amuri; Hoornaert, Georges J.; Compernolle, Frans; Cegla, Marek; Azzam, Rasha A.; Andries, Koen; de Bethune, Marie-Pierre; Azijn, Hilde; Pauwels, Rudi; Lewi, Paul J.; Janssen, Paul A. J. published an article.Reference of 3,5-Dibromo-1-methylpyrazin-2(1H)-one The title of the article was Design, Synthesis, and SAR of a Novel Pyrazinone Series with Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitory Activity. And the article contained the following:

A series of novel pyrazinones designed as non-nucleoside reverse transcriptase inhibitors (NNRTIs) was synthesized and their anti-HIV structure-activity relationship (SAR) was studied. Optimization of activity was guided by mol. modeling, which in turn was based on x-ray structures of HIV-1 reverse transcriptase-bound 4-[[4-[(2,4,6-trimethylphenyl)amino]-2-pyrimidinyl]amino]benzonitrile (dapivirine). An example compound thus prepared and studied was 3-[(4-chlorophenyl)amino]-5-(2,4-dimethylphenoxy)-1-methyl-2(1H)-pyrazinone (I). The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Reference of 3,5-Dibromo-1-methylpyrazin-2(1H)-one

The Article related to design synthesis structure activity pyrazinone nonnucleoside hiv reverse transcriptase, mol modeling phenylamino phenoxy pyrazinone hiv reverse transcriptase dapivirine, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of 3,5-Dibromo-1-methylpyrazin-2(1H)-one

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On March 20, 2008, Whitney, James A.; Di Paolo, Julie; Valleca, Mark A.; Brittelli, David R.; Currie, Kevin S.; Darrow, James W.; Kropf, Jeffrey E.; Lee, Tony; Gallion, Steven L.; Mitchell, Scott A.; Pippen, Douglas A.I.; Blomgren, Peter A.; Stafford, Douglas Gregory published a patent.COA of Formula: C5H4Br2N2O The title of the patent was Preparation of substituted amides as Btk kinase inhibitors. And the patent contained the following:

Methods of inhibiting Btk activity by inhibiting phosphorylation of Y551 of Btk, methods of treating patients by inhibiting Btk activity by inhibiting phosphorylation of Y551 of Btk, chem. entities that bind to Btk and inhibited complexes are provided. Thus, the title compounds I [R = (un)substituted cycloalkyl, aryl, heteroaryl; M = a bond, CH:CH; Q = CR10R11NR12, NR12CR10R11, NR13CO, CONR13, NR14CONR15 (R10, R11 = H, alkyl, haloalkyl; R12-R15 = H, alkyl, haloalkyl, etc.); Z = (un)substituted phenylene, pyridylidene; W = (un)substituted heteroaryl other than imidazo[1,2-a]pyrazine; D = hydrogen bond donor other than H; with the proviso] were prepared E.g., a multi-step synthesis of II, starting from 3,5-dibromo-1H-pyridin-2-one, was given. Exemplified compounds I were tested in the Btk assay and certain of those compounds exhibited an IC50 value less than or equal to 1 μM. Some of the compounds I were tested in the B-cell proliferation assay and exhibited an IC50 value less than or equal to 10 μM. 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 amide preparation bruton’s tyrosine kinase btk kinase inhibitor, y551 btk phosphorylation inhibitor amide preparation, b cell proliferation inhibitor amide preparation, 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