Category: 1261686-95-6

On April 13, 2017, Gopalsamy, Ariamala; Narayanan, Arjun; Liu, Shenping; Parikh, Mihir D.; Kyne, Robert E.; Fadeyi, Olugbeminiyi; Tones, Michael A.; Cherry, Jonathan J.; Nabhan, Joseph F.; LaRosa, Gregory; Petersen, Donna N.; Menard, Carol; Foley, Timothy L.; Noell, Stephen; Ren, Yong; Loria, Paula M.; Maglich-Goodwin, Jodi; Rong, Haojing; Jones, Lyn H. published an article.SDS of cas: 1261686-95-6 The title of the article was Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA). And the article contained the following:

The C-5 substituted 2,4-diaminoquinazoline RG3039 (compound I), a member of a chem. series that was identified and optimized using an SMN2 promoter screen, prolongs survival and improves motor function in a mouse model of spinal muscular atrophy (SMA). It is a potent inhibitor of the mRNA Decapping Scavenger Enzyme (DcpS), but the mechanism whereby DcpS inhibition leads to therapeutic benefit is unclear. Compound I is a dibasic lipophilic mol. that is predicted to accumulate in lysosomes. To understand if the in-vivo efficacy is due to DcpS inhibition or other effects resulting from the physicochem. properties of the chemotype, the authors undertook structure based mol. design to identify DcpS inhibitors with improved physicochem. properties. Herein the authors describe the design, synthesis, in-vitro pharmacol. characterization of these DcpS inhibitors along with the in-vivo mouse CNS PK profile of PF-DcpSi (compound II), one of the analogs found to be efficacious in SMA mouse model. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).SDS of cas: 1261686-95-6

The Article related to mrna dcps inhibitor spinal muscular atrophy pharmacokinetics, Pharmacology: Structure-Activity and other aspects.SDS of cas: 1261686-95-6

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On November 14, 2019, Focken, Thilo; Burford, Kristen; Grimwood, Michael E.; Zenova, Alla; Andrez, Jean-Christophe; Gong, Wei; Wilson, Michael; Taron, Matt; Decker, Shannon; Lofstrand, Verner; Chowdhury, Sultan; Shuart, Noah; Lin, Sophia; Goodchild, Samuel J.; Young, Clint; Soriano, Maegan; Tari, Parisa K.; Waldbrook, Matthew; Nelkenbrecher, Karen; Kwan, Rainbow; Lindgren, Andrea; de Boer, Gina; Lee, Stephanie; Sojo, Luis; DeVita, Robert J.; Cohen, Charles J.; Wesolowski, Steven S.; Johnson, J. P.; Dehnhardt, Christoph M.; Empfield, James R. published an article.Computed Properties of 1261686-95-6 The title of the article was Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective NaV1.6 Inhibitors with Efficacy in Mouse Models of Epilepsy. And the article contained the following:

Nonselective antagonists of voltage-gated sodium (NaV) channels have been long used for the treatment of epilepsies. The efficacy of these drugs is thought to be due to the block of sodium channels on excitatory neurons, primarily NaV1.6 and NaV1.2. However, these currently marketed drugs require high drug exposure and suffer from narrow therapeutic indexes. Selective inhibition of NaV1.6, while sparing NaV1.1, is anticipated to provide a more effective and better tolerated treatment for epilepsies. In addition, block of NaV1.2 may complement the anticonvulsant activity of NaV1.6 inhibition. We discovered a novel series of aryl sulfonamides as CNS-penetrant, isoform-selective NaV1.6 inhibitors, which also displayed potent block of NaV1.2. Optimization focused on increasing selectivity over NaV1.1, improving metabolic stability, reducing active efflux, and addressing a pregnane X-receptor liability. We obtained compounds 30-32, which produced potent anticonvulsant activity in mouse seizure models, including a d.c. maximal electroshock seizure assay. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).Computed Properties of 1261686-95-6

The Article related to cns penetrant aryl sulfonamide preparation epilepsy odium channel, Pharmacology: Structure-Activity and other aspects.Computed Properties of 1261686-95-6

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Nitrile – Wikipedia,
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On December 7, 2016, Gao, Yuzhe; Wang, Guocheng published a patent.Electric Literature of 1261686-95-6 The title of the patent was Preparation of xanthines as DPP-IV inhibitors. And the patent contained the following:

The invention relates to xanthine derivatives (e.g., I) and their pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical preparations comprising them, and their as DPP-IV inhibitors for treating type II diabetes. For instance, the invention compound I was prepared via substitution of 8-bromo-3,9-dihydro-3-methyl-1H-purine-2,6-dione with 1-bromo-2-butyne followed by substitution with 2-(bromomethyl)-6-fluoro-benzonitrile, substitution with (R)-3-(Boc-amino)piperidine, and hydrolysis. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).Electric Literature of 1261686-95-6

The Article related to xanthine preparation antidiabetic dipeptidyl peptidase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Electric Literature of 1261686-95-6

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Nitrile – Wikipedia,
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On May 26, 2011, Kim, Seon Mi; Lee, Min Hee; Kim, Jae Sun; Jung, Hoe Chul; Lee, So Young; Lee, Soo Min; Kim, Eun Jeong; Park, Eui Sun; Park, Sung Hoon; Lee, Bong Yong; Um, Key An published a patent.COA of Formula: C8H5BrFN The title of the patent was Preparation of gonadotropin releasing hormone receptor antagonists. And the patent contained the following:

Compound I [X = N-containing non-aromatic heterocycle or substituted non-aromatic heterocycle; Y = -(CR9aR9b)r-Z-R4; B = NR1R2 or OR1 where r = 0, 1, 2, 3; n = 2, 3, 4; Z = direct bond, O, S, CO, etc.; D = Q1, Q2, Q3, etc. where E = O, S, NR8; R1, R2 = independently H, (un)substituted C1-10 alkyl, (un)substituted C3-10 cycloalkyl, (un)substituted C6-12 aryl, etc.; R3a, R3b = independently H, (un)substituted C1-10 alkyl, (un)substituted C3-10 cycloalkyl, C1-10 alkoxy, etc.; R4 = H, substituted C1-10 alkyl, C3-10 cycloalkyl, (un)substituted C6-12 aryl, etc.; R5 = H, halogen, (un)substituted C1-6 alkyl, (un)substituted C3-10 cycloalkyl, etc.; R6 = H, (un)substituted C1-6 alkyl, (un)substituted C3-10 cycloalkyl, etc.;R8 = H, cyano, (un)substituted C1-10 alkyl, etc.; R9a, R9b = independently H, acyl, hydroxy, halogen, etc.; its stereoisomers or pharmaceutically acceptable salts] was prepared For example, II was prepared in a multistep synthesis. Compound I was claimed useful as gonadotropin releasing hormone (“”GnRH””) (known as LH releasing hormone) receptor antagonists for treatment of prostatic cancer, uterine cancer, and breast cancer, etc. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).COA of Formula: C8H5BrFN

The Article related to preparation gonadotropin releasing hormone receptor antagonist, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.COA of Formula: C8H5BrFN

Referemce:
Nitrile – Wikipedia,
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On December 19, 2019, Focken, Thilo; Burford, Kristen Nicole; Lofstrand, Verner Alexander; Wilson, Michael Scott; Zenova, Alla Yurevna published a patent.Recommanded Product: 2-(Bromomethyl)-6-fluorobenzonitrile The title of the patent was Preparation of benzenesulfonamide compounds and their use as therapeutic agents. And the patent contained the following:

This invention is directed to benzenesulfonamide compounds of formula I, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels (Nav1.6), such as epilepsy and/or epileptic seizure disorders. Compounds of formula I wherein m and n are independently 1 and 2; R1, R3a, R3b and each R4 are independently H and alkyl; R2 is thiazolyl, isothiazolyl and isoxazolyl; R5 is halo; each R6 is independently halo and alkoxy, provided that at least one R6 is alkoxy; R7 is azabicyclo[2.2.1]heptanylalkyl; R7 is ((methyl)(prop-2-yl)amino)alkyl when n is 2; and stereoisomers, enantiomers, tautomers, mixtures, pharmaceutically acceptable salts, solvates and prodrugs thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their voltage-gated sodium channel inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of 0.015 μM, > 30.00 μM and 9.603 μM towards Nav1.6, Nav1.5 and Nav1.1, resp. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).Recommanded Product: 2-(Bromomethyl)-6-fluorobenzonitrile

The Article related to benzenesulfonamide preparation voltage gated sodium channel inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Recommanded Product: 2-(Bromomethyl)-6-fluorobenzonitrile

Referemce:
Nitrile – Wikipedia,
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On March 5, 2020, Focken, Thilo; Andrez, Jean-Christophe; Burford, Kristen Nicole; Dehnhardt, Christoph Martin; Grimwood, Michael Edward; Jia, Qi; Lofstrand, Verner Alexander; Wilson, Michael Scott; Zenova, Alla Yurevna; Wesolowski, Steven Sigmund; Sun, Shaoyi published a patent.Electric Literature of 1261686-95-6 The title of the patent was Preparation of heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors. And the patent contained the following:

This invention is directed to pyridine- and thiophene-sulfonamide compounds of formula I, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy and/ or epileptic seizure disorders. Compounds of formula I wherein A is (un)substituted pyridinediyl, (un)substituted thiophenediyl, (un)substituted thiazolediyl, etc.; R1 is (un)substituted aryl and (un)substituted (mono/bi)cyclic heteroaryl; R2 is (un)substituted 5- to 6-membered heteroaryl; R3 and R4 are independently H and alkyl; and individual stereoisomers, enantiomers, tautomers, mixtures, pharmaceutically acceptable salts, solvates and prodrugs thereof, are claimed. Example compound II was prepared by sulfamidation of 5,6-dichloropyridine-3-sulfonyl chloride with tert-Bu thiazol-4-ylcarbamate; the resulting tert-Bu ((5,6-dichloropyridin-3-yl)sulfonyl)(thiazol-4-yl)carbamate underwent amination with (S)-1-(5-chloro-2-fluorophenyl)ethan-1-amine hydrochloride to give tert-Bu (S)-((5-chloro-6-((1-(5-chloro-2-fluorophenyl)ethyl)amino)pyridin-3-yl)sulfonyl)(thiazol-4-yl)carbamate, which underwent hydrolysis to give compound II. The invention compounds were evaluated for their sodium channel inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of 2.820μM, 5.573μM and 5.003μM towards Nav1.6, Nav1.5 and Nav1.1, resp. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).Electric Literature of 1261686-95-6

The Article related to heteroaryl sulfonamide preparation sodium channel inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Electric Literature of 1261686-95-6

Referemce:
Nitrile – Wikipedia,
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On March 16, 2021, Levkov, Igor V.; Kysil, Andrii I.; Biitseva, Angelina V.; Shilin, Sergey V.; Saffon-Merceron, Nathalie; Yegorova, Tatyana V.; Voitenko, Zoia V. published an article.COA of Formula: C8H5BrFN The title of the article was Synthesis of 2-(methoxymethyl)isoindolin-1-imine derivatives via an unusual Delepine reaction. And the article contained the following:

The synthesis of 2-(methoxymethyl)isoindolin-1-imine derivatives via an unusual Delepine reaction was reported. The substrate substituents’ influence on the reaction course was studied, and a possible reaction mechanism proposed. The structure of 2-(methoxymethyl)isoindolin-1-imine was confirmed by X-ray diffraction anal. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).COA of Formula: C8H5BrFN

The Article related to methoxymethylisoindolinimine preparation, bromomethylbenzonitrile methanol delepine reaction, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.COA of Formula: C8H5BrFN

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On December 3, 2020, Grosse, Sandrine Celine; Deratt, Lindsey Graham; Vandyck, Koen; Raboisson, Pierre Jean-Marie Bernard; Pieters, Serge Maria Aloyssius; Kesteleyn, Bart Rudolf Romanie; Verschueren, Wim Gaston; Berke, Jan Martin; LeComte, Morgan Charles R.; Martinez Lamenca, Carolina; Jonckers, Tim Hugo Maria; Deng, Gang; Jiang, Yimin; Xu, Yanping; Cheng, Zhangling; Hu, Lili; Kuduk, Scott D. published a patent.COA of Formula: C8H5BrFN The title of the patent was Fused heterocyclic derivatives as antiviral agents and their preparation. And the patent contained the following:

The application describes fused heterocycle derivatives of formula I, pharmaceutical compositions comprising these compounds, chem. processes for preparing these compounds and their use in the treatment of diseases associated with HBV infection. Compounds of formula I wherein A is absent and CH2; X is CH2 and O; Y is NH and derivatives; W is CHR3 and CH:CH2; Z is CO and CS; R1 is (un)substituted 5- to 10-membered (mono/bi)cyclic ring optionally containing heteroatoms; R2 is H and (un)substituted C1-4 alkyl; R3 is H, F, OH, (un)substituted C1-4 alkyl, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of Et 2-(2-aminoethyl)-5-(3,4-dichlorobenzoyl)-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine-3-carboxylate bistrifluoroacetate. The invention compounds were evaluated for their antiviral activity. From the assay, it was determined that compound II exhibited an EC50 value 9.628渭M and a CC50 value of > 50渭M. The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).COA of Formula: C8H5BrFN

The Article related to heterocycle preparation antiviral, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.COA of Formula: C8H5BrFN

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Nitrile – Wikipedia,
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On August 5, 2015, Van Doremaele, Gerard; Berthoud, Alexandra; Quiroga Norambuena, Victor; Rupnicki, Leszek; Karbaum, Peter published a patent.Recommanded Product: 2-(Bromomethyl)-6-fluorobenzonitrile The title of the patent was Metal complex with a cyclic amidine ligand. And the patent contained the following:

The present invention relates to a metal complex, CyYMLjXn (Cy = cyclopentadienyl-type ligand; M = metal of group 4; L = neutral Lewis basic ligand wherein the number of said neutral ligands j = the range of 0 to the amount that satisfies the 18-electron rule; X = anionic ligand; n = integer denoting the number of anionic ligands X and is 1 or 2, preferably is 2; Y = cyclic amidine-containing ligand), wherein the amidine-containing ligand is covalently bonded to the metal M via the imine nitrogen atom. Thus, reaction of 2-cyclopentylisoindolin-1-imine hydrobromide with (C5Me5)3TiCl gave title polymerization catalyst, Me5CpTiCl2(NC(Ph)(c-C5H9N)). The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).Recommanded Product: 2-(Bromomethyl)-6-fluorobenzonitrile

The Article related to cyclic amidine titanium preparation polymerization catalyst, Organometallic and Organometalloidal Compounds: Groups Iiib, Ivb, Vb – Sc, Y, Lanthanides, Actinides, Ti, Zr, Hf, V, Nb, Ta and other aspects.Recommanded Product: 2-(Bromomethyl)-6-fluorobenzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts

On August 6, 2015, Van Doremaele, Gerardus Henricus Josephus; Berthoud, Alexandra; Quiroga Norambuena, Victor; Rupnicki, Leszek; Karbaum, Peter published a patent.Application In Synthesis of 2-(Bromomethyl)-6-fluorobenzonitrile The title of the patent was Metal complex with a cyclic amidine ligand. And the patent contained the following:

The present invention relates to a metal complex, CyYMLjXn (Cy = cyclopentadienyl-type ligand; M = metal of group 4; L = neutral Lewis basic ligand wherein the number of said neutral ligands j = the range of 0 to the amount that satisfies the 18-electron rule; X = anionic ligand; n = integer denoting the number of anionic ligands X and is 1 or 2, preferably is 2; Y = cyclic amidine-containing ligand), wherein the amidine-containing ligand is covalently bonded to the metal M via the imine nitrogen atom. Thus, reaction of 2-cyclopentylisoindolin-1-imine hydrobromide with (C5Me5)3TiCl gave title polymerization catalyst, Me5CpTiCl2(NC(Ph)(c-C5H9N)). The experimental process involved the reaction of 2-(Bromomethyl)-6-fluorobenzonitrile(cas: 1261686-95-6).Application In Synthesis of 2-(Bromomethyl)-6-fluorobenzonitrile

The Article related to cyclic amidine titanium preparation polymerization catalyst, Organometallic and Organometalloidal Compounds: Groups Iiib, Ivb, Vb – Sc, Y, Lanthanides, Actinides, Ti, Zr, Hf, V, Nb, Ta and other aspects.Application In Synthesis of 2-(Bromomethyl)-6-fluorobenzonitrile

Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts