Author: Jessica.F

On December 18, 2020, Bessho-Uehara, Manabu; Huang, Wentao; Patry, Wyatt L.; Browne, William E.; Weng, Jing-Ke; Haddock, Steven H. D. published an article.Formula: C26H21N3O3 The title of the article was Evidence for de novo Biosynthesis of the Luminous Substrate Coelenterazine in Ctenophores. And the article contained the following:

Coelenterazine is a key substrate involved in marine bioluminescence which is used for light-production by at least nine phyla. Some luminous animals, such as the hydromedusa Aequorea, lack the ability to produce coelenterazine endogenously and instead depend on dietary sources. Little is known about the source organisms or the metabolic process of coelenterazine biosynthesis. Here, we present evidence that ctenophores are both producers and suppliers of coelenterazine in marine ecosystems. Using biochem. assays and mass spectrometry analyses, we detected coelenterazine from cultured ctenophores fed with a non-luminous coelenterazine-free diet. We propose that ctenophores are an emerging model organism to study coelenterazine biosynthesis and the origins of bioluminescence. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Formula: C26H21N3O3

The Article related to beroe mnemiopsis bolinopsis pleurobrachia coelenterazine bioluminescence, biomolecules, biosynthesis, evolutionary developmental biology, evolutionary history, Microbial, Algal, and Fungal Biochemistry: Composition and Products and other aspects.Formula: C26H21N3O3

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 March 27, 2019, Smith, Eric L.; Harrington, Kim; Staehr, Mette; Masakayan, Reed; Jones, Jon; Long, Thomas J.; Ng, Khong Y.; Ghoddusi, Maj; Purdon, Terence J.; Wang, Xiuyan; Do, Trevor; Pham, Minh Thu; Brown, Jessica M.; De Larrea, Carlos Fernandez; Olson, Eric; Peguero, Elizabeth; Wang, Pei; Liu, Hong; Xu, Yiyang; Garrett-Thomson, Sarah C.; Almo, Steven C.; Wendel, Hans-Guo; Riviere, Isabelle; Liu, Cheng; Sather, Blythe; Brentjens, Renier J. published an article.Application of 55779-48-1 The title of the article was GPRC5D is a target for the immunotherapy of multiple myeloma with rationally designed CAR T cells. And the article contained the following:

The orphan G protein-coupled receptor, class C group 5 member D (GPRC5D), normally expressed only in the hair follicle, was previously identified as expressed by mRNA in marrow aspirates from patients with MM, but confirmation of protein expression remained elusive. Using quant. immunofluorescence, we determined that GPRC5D protein is expressed on CD138+ MM cells from primary marrow samples with a distribution that was similar to, but independent of, BCMA. Panning a human B cell-derived phage display library identified seven GPRC5D-specific single-chain variable fragments (scFvs). Incorporation of these into multiple CAR formats yielded 42 different constructs, which were screened for antigen-specific and antigen-independent (tonic) signaling using a Nur77-based reporter system. Nur77 reporter screen results were confirmed in vivo using a marrow-tropic MM xenograft in mice. CAR T cells incorporating GPRC5D-targeted scFv clone 109 eradicated MM and enabled long-term survival, including in a BCMA antigen escape model. GPRC5D(109) is specific for GPRC5D and resulted in MM cell line and primary MM cytotoxicity, cytokine release, and in vivo activity comparable to anti-BCMA CAR T cells. Murine and cynomolgus cross-reactive CAR T cells did not cause alopecia or other signs of GPRC5D-mediated toxicity in these species. Thus, GPRC5D(109) CAR T cell therapy shows potential for the treatment of advanced MM irresp. of previous BCMA-targeted therapy. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Application of 55779-48-1

The Article related to multiple myeloma chimeric antigen receptor t cell gprc5d, Immunochemistry: Other (Immunity, Immune Suppression, Tolerance, etc.) and other aspects.Application of 55779-48-1

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Jaiswal, Poonam B.; Tung, Jack K.; Gross, Robert E.; English, Arthur W. published an article in 2020, the title of the article was Motoneuron activity is required for enhancements in functional recovery after peripheral nerve injury in exercised female mice.Safety of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one And the article contains the following content:

Inhibitory luminopsins (iLMO2) integrate opto- and chemo-genetic approaches and allow for cell-type specific inhibition of neuronal activity. When exposed to a Renilla luciferase substrate, Coelenterazine (CTZ), iLMO2 generates bioluminescence-mediated activation of its amino-terminal halorhodopsin, resulting in neuronal inhibition. Moderate daily exercise in the form of interval treadmill-training (IT) applied following a peripheral nerve injury results in enhanced motor axon regeneration and muscle fiber reinnervation in female mice. We hypothesized that iLMO2 mediated inhibition of motoneuron activity during IT would block this enhancement. Unilateral i.m. injections of Cre-dependent AAV2/9-EF1a-DIO-iLMO2 (∼8.5 x 1013 vg/mL) were made into the gastrocnemius and tibialis anterior muscles of young female ChAT-IRES-Cre mice, thereby limiting iLMO2 expression specifically to their motoneurons. Four to six weeks were allowed for retrograde viral transduction after which a unilateral sciatic nerve transection (Tx) and repair was performed. Animals were randomized into four groups: IT only, IT + CTZ, CTZ only, and untreated (UT). Three weeks post Tx-repair, the maximal amplitude direct muscle responses (M-max) in both muscles in the IT only group were significantly greater than in UT mice, consistent with the enhancing effects of this exercise regimen. Inhibiting motoneuron activity during exercise by a single injection of CTZ, administered 30 min prior to exercise, completely blocked the enhancing effect of exercise. Similar treatments with CTZ in mice without iLMO2 had no effect on regeneration. Neuronal activity is required for successful enhancement of motor axon regeneration by exercise. The experimental process involved the reaction of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one(cas: 55779-48-1).Safety of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

The Article related to exercise nerve injury female, rrid:cvcl_0045, rrid:mgi:3689725, inhibitory luminopsin, m-response, motoneuron activity, sciatic nerve injury, treadmill training, Mammalian Pathological Biochemistry: Nervous System and Psychiatric Diseases and other aspects.Safety of 8-Benzyl-2-(4-hydroxybenzyl)-6-(4-hydroxyphenyl)imidazo[1,2-a]pyrazin-3(7H)-one

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

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