Month: October 2022

On December 17, 2020, Wang, Jin; Guo, Wen-Hao; Qi, Xiaoli; Wang, Luhua; Liu, Yang; Nomie, Krystle J. published a patent.Synthetic Route of 87486-34-8 The title of the patent was Preparation of small molecule proteolysis-targeting chimeras for use as Bruton tyrosine kinase inhibitors. And the patent contained the following:

Title compounds I [A = BTK binder; L = linker; B = E3 ligase binder], and their pharmaceutically acceptable salts, are prepared and disclosed as Bruton tyrosine kinase inhibitors. Thus, e.g., II was prepared by a multistep procedure (preparation given). Select I were evaluated in BTK inhibition assays, e.g., II demonstrated an IC50 value of 1.8 nM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Synthetic Route of 87486-34-8

The Article related to pyrimidinylpiperidine pyrazolo preparation bruton tyrosine kinase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Synthetic Route of 87486-34-8

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On March 4, 2021, Rathod, Rajendrasinh Jashvantsinh; Raut, Virendra Narendra; Βhatt, Tushar Bhupendrabhai; Savant, Pratit Viram; Joshi, Kiritkumar Parmeshkumar; Jarag, Tushar Mukund; Chimanwala, Sabbirhusen Yusufbhai; Sengupta, Prabal; Kadiyala, V. S. N. Murty; Chitturi, Trinadha Rao published a patent.SDS of cas: 936901-72-3 The title of the patent was Preparation of cycloalkylidene carboxylic acids and derivatives as BTK inhibitors. And the patent contained the following:

The present invention relates to novel cycloalkylidene carboxylic acids and derivatives thereof of formula I [Ra = N(R2)NR3R4, OH, NR15R16; ring Hy = II-VI; ring A = VII-VIII (wherein R5 = H, halo, OH, etc.; Y1 = CH, N; Y2 = CH and N; Y3 = CH and N; Y4 = N, O and S); W = absent, (CH2)1-2, NH, NHCH2; Y = O, S, NH, etc.; ring B = (un)substituted 6-10 membered aryl, cycloalkyl and 5-10 membered heteroaryl containing 1-3 heteroatoms each independently selected from N, O and S; R1 = H, halo, alkyl, etc.; R2 and R3 = (independently) H, hydroxyalkyl, and alkyl optionally substituted with cycloalkyl; or R2 and R3 together with N atoms to which they are attached form 4-7 membered heterocycloalkyl ring; R4 = C(O)alkyl, C(O)cycloalkyl, C(S)alkyl, etc.; R15 = H or alkyl; R16 = H, OH, alkyl, etc.; m = 1-3; n = 1-3; with the proviso] or pharmaceutically acceptable salts, stereoisomers or deuterated analogs, useful as Bruton tyrosine kinase (BTK) inhibitors. The present disclosure also relates to processes for their preparation, pharmaceutical compositions containing one or more such compounds, and to the use of such compounds and pharmaceutical compositions for the treatment of disorders involving mediation of BTK in humans. E.g., a multi-step synthesis of IX, starting from 3-bromo-1H-pyrazolo[3,4-d]pyrimidin-4-amine, was described. The inhibitory activity of exemplified compounds I was evaluated in the BTK assay employing the ADP-GloTM Platform (data given). The experimental process involved the reaction of 3-(8-Chloroimidazo[1,5-a]pyrazin-3-yl)cyclobutanone(cas: 936901-72-3).SDS of cas: 936901-72-3

The Article related to cycloalkylidene carboxylic acid preparation bruton tyrosine kinase btk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 936901-72-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

On May 18, 2017, Yasuda, Takuma; Park, In Seob; Yang, Yu Seok; Sumiya, Hiroshi; Fukushima, Yukio published a patent.Category: pyrazines The title of the patent was Dicyanopyrazine compound, luminescent material for light transmitter, and preparation method for 2,5-dicyano-3,6-dihalogenopyrazine. And the patent contained the following:

Dicyanopyrazine compound I [R3 = electron-donating group; R4 = H, (un)substituted aryl or electron-donating group; L3 = (un)substituted heteroarylene or (un)substituted arylene; L4 = single bond, (un)substituted heteroarylene or (un)substituted arylene; L3 and L4, together with carbon atoms to which each is attached, may combine to form a ring] and II [R5 = electron-donating group; R6 = H, (un)substituted aryl or electron-donating group; L5 = (un)substituted heteroarylene or (un)substituted arylene; L6 = single bond, (un)substituted heteroarylene or (un)substituted arylene] were provided. Organic electroluminescent device comprising an invention compound, e.g., III, showed maximum external quantum efficiency of higher than 5%. Further disclosed is a preparation method of 2,5-dicyano-3,6-dihalogenopyrazine. For example, treatment of 2,3-diamino-3-(phenylthio)acerylonitrile with citric acid-sodium citrate buffer (pH = 3.0) [1,2-dimethoxyethane, water, room temperature, 5 h, 45%] and halogenation [CuBr2, tert-Bu nitrite, acetonitrile, 70°, 5 h] afforded 2,5-dicyano-3,6-dibromopyrazine (67.0% yield). Of note, 2,5-dicyano-3,6-dihalogenopyrazine is a useful synthetic intermediate for dicyanopyrazine compound The experimental process involved the reaction of 3,6-Dibromopyrazine-2,5-dicarbonitrile(cas: 1391026-27-9).Category: pyrazines

The Article related to dicyanopyrazine light transmitter material, dicyanodihalogenopyrazine preparation cyclization halogenation, Optical, Electron, and Mass Spectroscopy and Other Related Properties: Luminescence and other aspects.Category: pyrazines

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

On May 10, 2013, Crawford, James John; Ortwine, Daniel Fred; Wei, Binqing; Young, Wendy B. published a patent.Application of 87486-34-8 The title of the patent was 8-Fluorophthalazin-1(2H)-one compounds as inhibitors of BTK activity and their preparation. And the patent contained the following:

8-Fluorophthalazin-1(2H)-one compounds of formula I, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting BTH 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 X1 is CR1 and N; X2 is CR2 and N; X3 is CR3 and N, provided that one or two of X1 – X3 are N; Y1 and Y2 are independently CH and N, provided that not both are N; R1, R2 and R3 are independently H, F, Cl, CN, Me, Et, etc.; R4 is F, F, Cl, CN, CH2OH, etc.; R6 is H, Me, Et, etc.; R8 is C6-20 aryl, C3-12 carbocyclyl, C1-20 heteroaryl, etc.; and stereoisomers, tautomers, or 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 IC70 value of 0.024 μM. The experimental process involved the reaction of 3,5-Dibromo-1-methylpyrazin-2(1H)-one(cas: 87486-34-8).Application of 87486-34-8

The Article related to fluorophthalazinone preparation btk inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Application of 87486-34-8

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 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