Month: November 2022

On December 3, 2020, Castro, Alfredo C. published a patent.Application of 386704-04-7 The title of the patent was Sulfamides as TEAD inhibitors and their preparation, pharmaceutical compositions and use in the treatment of cancer. And the patent contained the following:

The invention provides sulfamide compounds I, compositions thereof, and methods of using the same. Compounds of formula I wherein L1 is (un)substituted (un)branched C1-6 alkylene, etc.; ring A is Ph, (un)substituted 5- to 6-membered heteroaryl, etc.; R2 is H, (un)substituted 4- to 6-membered heteroaryl, etc.; R4 is H, halo, -SO2NH2 and derivatives, -CONH2 and derivatives; R6 is H, (un)substituted C1-6 alkyl, etc.; and their pharmaceutically acceptable salts as TEAD inhibitors in the treatment of cancer thereof, are claimed. Example compound II was prepared by using etherification and cross-coupling as the key steps. All the invention compounds were evaluated for their TEAD inhibitory activity. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7

The Article related to sulfamide preparation tead inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Application of 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On January 19, 2017, Duan, Wenhu; Geng, Meiyu; Yan, Wei; Ding, Jian; Ai, Jing; Zhao, Bin; Fan, Jun; Peng, Xia; Chen, Yi published a patent.Formula: C7H8FNO The title of the patent was Preparation of 3-(heteroaryl)indazole derivatives useful as FGFR1 inhibitor for the treatment of cancer. And the patent contained the following:

The invention relates to 3-(heteroaryl)indazole derivatives of formula I, method for their preparation and their use as FGFR1 inhibitor for the treatment of cancer. Compounds of formula I, wherein R1, R2, R3 are independently H and halo; R9 is (un)substituted 5- to 7-membered heteroaryl; R8 and R10 are independently H, halo, C1-3alkyl and C1-3alkoxy; R4, R5, R6 and R7 are independently H, halo, (un)substituted C1-8alkyl, etc.; M is CH2, CH, N, O and S; W is O and NH; dotted bond is single or double bond and can not be same, are claimed. Example compound II was prepared via a multistep procedure (procedure given). All the invention compounds were evaluated for their FGFR1 inhibitory activity. From the assay, it was determined that example compound II exhibited IC50 value of < 10 nM towards FGFR1. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Formula: C7H8FNO

The Article related to heteroarylindazole preparation fgfr1 inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Formula: C7H8FNO

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On January 11, 2017, Duan, Wenhu; Geng, Meiyu; Yan, Wei; Ding, Jian; Ai, Jing; Zhao, Bin; Fan, Jun; Peng, Xia; Chen, Yi published a patent.Electric Literature of 87674-15-5 The title of the patent was Preparation of 3-(heteroaryl)indazole derivatives useful as FGFR1 inhibitor for the treatment of cancer. And the patent contained the following:

The invention relates to 3-(heteroaryl)indazole derivatives of formula I, method for their preparation and their use as FGFR1 inhibitor for the treatment of cancer. Compounds of formula I, wherein R1, R2, R3 are independently H and halo; R9 is (un)substituted 5- to 7-membered heteroaryl; R8 and R10 are independently H, halo, C1-3alkyl and C1-3alkoxy; R4, R5, R6 and R7 are independently H, halo, (un)substituted C1-8alkyl, etc.; M is CH2, CH, N, O and S; W is O and NH; dotted bond is single or double bond and can not be same, are claimed. Example compound II was prepared via a multistep procedure (procedure given). All the invention compounds were evaluated for their FGFR1 inhibitory activity. From the assay, it was determined that example compound II exhibited IC50 value of < 10 nM towards FGFR1. The experimental process involved the reaction of 1-(3-Fluoropyridin-4-yl)ethanol(cas: 87674-15-5).Electric Literature of 87674-15-5

The Article related to heteroarylindazole preparation fgfr1 inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 87674-15-5

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Turkiewicz, Anna; Steliga, Teresa; Kluk, Dorota; Gminski, Zbigniew published an article in 2021, the title of the article was Biomonitoring Studies and Preventing the Formation of Biogenic H2S in the Wierzchowice Underground Gas Storage Facility.Electric Literature of 4719-04-4 And the article contains the following content:

The article discusses the results of biomonitoring research at the Underground Gas Storage (UGS). Hydrogen sulfide, as one of the products of microbiol. reaction and transformation, as well as a product of chem. reactions in rocks, is a subject of interest for global petroleum companies. The materials used in this research work were formation waters and stored natural gas. The biomonitoring of reservoir waters and cyclical analyses of the composition of gas stored at UGS Wierzchowice enabled the assessment of the microbiol. condition of the reservoir environment and individual storage wells in subsequent years of operation. Investigations of the formation water from individual wells of the UGS Wierzchowice showed the presence of sulfate reducing bacteria bacteria (SRB), such as Desulfovibrio and Desulfotomaculum genera and bacteria that oxidize sulfur compounds In the last cycles of UGS Wierzchowice, the content of hydrogen sulfide and sulfides in the reservoir waters ranged from 1.22 to 15.5 mg/dm3. The monitoring of natural gas received from UGS production wells and observation wells, which was carried out in terms of the determination of hydrogen sulfide and organic sulfur compounds, made it possible to observe changes in their content in natural gas in individual storage cycles. In the last cycles of UGS Wierzchowice, the content of hydrogen sulfide in natural gas from production wells ranged from 0.69 to 2.89 mg/dm3, and the content of organic sulfur compounds converted to elemental sulfur ranged from 0.055 to 0.130 mg Sel./Nm3. A higher hydrogen sulfide content was recorded in natural gas from observation wells in the range of 2.02-25.15 mg/Nm3. In order to explain the causes of hydrogen sulfide formation at UGS Wierzchowice, isotopic analyses were performed to determine the isotope composition of δ34SH2S, δ34SSO4, δ18OSO4 in natural gas samples (production and observation wells) and in the deep sample of reservoir water. The results of isotope tests in connection with microbiol. tests, chromatog. analyses of sulfur compounds in natural gas collected from UGS Wierzchowice and an anal. of the geol. structure of the Wierzchowice deposit allow us to conclude that the dominant processes responsible for the formation of hydrogen sulfide at UGS Wierzchowice are microbiol., consisting of microbial sulfate reduction (MSR). The presented tests allow for the control and maintenance of hydrogen sulfide at a low level in the natural gas received from the Wierzchowice Underground Gas Storage facility. The experimental process involved the reaction of 2,2′,2”-(1,3,5-Triazinane-1,3,5-triyl)triethanol(cas: 4719-04-4).Electric Literature of 4719-04-4

The Article related to biogenic hydrogen sulfide wierzchowice underground gas storage biomonitoring, Electrochemical, Radiational, and Thermal Energy Technology: Energy Handling, Transport, and Storage and other aspects.Electric Literature of 4719-04-4

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On July 2, 2020, Okuda, Yasuhiro; Imafuku, Kazuto; Tsuchida, Yoshiyuki; Seo, Tomoyo; Akashi, Haruo; Orita, Akihiro published an article.COA of Formula: C10H22S The title of the article was Process-Controlled Regiodivergent Copper-Catalyzed Azide-Alkyne Cycloadditions: Tailor-made Syntheses of 4- and 5-Bromotriazoles from Bromo(phosphoryl)ethyne. And the article contained the following:

We developed a regiodivergent syntheses of 4- and 5-bromo-substituted 1,2,3-triazoles in copper-catalyzed azide-alkyne cycloadditions (CuAACs) by taking advantage of bromo(phosphoryl)ethyne as a bromoethyne equivalent A one-shot dephosphorylative CuAAC afforded 4-bromotriazoles, which was transformed into a histone deacetylase 8 (HDAC8)-selective inhibitor, NCC-149. However, the direct CuAAC catalyzed by CuI/Cu(OAc)2 provided 5-bromo-4-phosphoryltriazoles. The consecutive nucleophilic substitution of the bromo group with thiols followed by MeOK-promoted dephosphorylation gave 5-thio-substituted triazoles. The experimental process involved the reaction of 1-Decanethiol(cas: 143-10-2).COA of Formula: C10H22S

The Article related to bromotriazole regiodivergent preparation copper catalyzed click cycloaddition bromophosphorylethyne, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.COA of Formula: C10H22S

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On March 17, 2016, Viet, Andrew Quoc; Wurtz, Nicholas R. published a patent.Recommanded Product: 72364-46-6 The title of the patent was Thioether triazolopyridine and triazolopyrimidine inhibitors of myeloperoxidase. And the patent contained the following:

The invention provides compounds of formula I as myeloperoxidase (MPO) and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments. Compounds of formula I wherein ring A is substituted Ph and (un)substituted 5-to 6-membered heteroaryl; X is CH and N; Y is substituted hydrocarbon linker and substituted hydrocarbon-heteroatom linker; R1 is CN, OH, C1-4 (halo)alkyl, etc. ; and stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs and solvates thereof, are claimed. Example compound II was prepared by thiolation of 7-chloro-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine with 1-phenylethylthiol. The invention compounds were evaluated for their myeloperoxidase and/or eosinophil peroxidase inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value ranged from 0.001 μM to 0.01 μM. The experimental process involved the reaction of (2-Fluorophenyl)methanethiol(cas: 72364-46-6).Recommanded Product: 72364-46-6

The Article related to preparation thioether triazolopyridine triazolopyrimidine inhibitor myeloperoxidase eosinophil peroxidase, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Recommanded Product: 72364-46-6

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On March 15, 2018, Sato, Takahiro; Nagayama, Yukiho; Yoshino, Yasuhiro; Inoue, Tsutomu; Kato, Hiroshige; Amata, Junichiro; Inaba, Masato; Yamoto, Noriko; Taniguchi, Tetsuya published a patent.HPLC of Formula: 386704-04-7 The title of the patent was Preparation of heterocyclic compounds having erythropoietin-production acceleration activity. And the patent contained the following:

Disclosed are compounds I [X = oxygen atom, nitrogen atom, sulfur atom, etc.; R1-R3 = independently H or alkyl; R4 = H, alkyl or aryl-alkyl; R5 = alkyl, alkenyl, alkynyl, etc. (wherein alkyl, alkenyl and alkynyl are optionally substituted with halo, methoxy, trifluoromethoxy, etc.); or pharmaceutically acceptable salts thereof] and pharmaceutical composition Thus, compound II was prepared via reaction of 2,4-dimethylbenzyl alc. with methanesulfonyl chloride followed by in-situ treatment with [(7-benzyloxy-5-mercapto[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl)amino]acetic acid tert-Bu ester and de-esterification. The invention compounds, e.g., II, promoted erythropoietin (EPO) production in Hep3B cells. Of note, compounds I are useful for the treatment of anemia. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).HPLC of Formula: 386704-04-7

The Article related to heterocycle preparation erythropoietin production promoter, antianemic agent triazolopyridine erythropoietin production acceleration, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.HPLC of Formula: 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On December 25, 2007, Xu, Hao; Han, Guozhi; Sha, Fei; Xu, Jian; Yao, Cheng published an article.Application of 2160-93-2 The title of the article was Synthesis of N-(tert-butyl)piperazine. And the article contained the following:

A method for the synthesis of the title compound is reported here. The synthetic sequence involved a condensation of tert-butylamine (i.e., 2-methyl-2-propanamine) with ethylene oxide, chlorination, cyclization, hydrogenation, debenzylation. The target product was characterized by 1H NMR and MS and its purity was also tested by GC. Exptl. result showed that the reactant in this synthesis route was easily available and it could be applied to industrial production (no data). The experimental process involved the reaction of 2,2′-(tert-Butylazanediyl)diethanol(cas: 2160-93-2).Application of 2160-93-2

The Article related to dimethylethyl piperazine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 2160-93-2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On March 12, 2020, Becker, Christopher; Li, Xiaolin; Lu, Peichao; Rajapaksa, Naomi Samadara; Tully, David Charles; Wang, Xiaojing Michael; Zhao, Qian published a patent.Recommanded Product: 1-[(Dibenzylamino)methyl]cyclopropanol The title of the patent was Preparation of pyridopyrazinedione compounds as antiviral agents for treating particularly herpes viruses. And the patent contained the following:

The invention is related to the preparation of compounds I [Cy = (un)substituted Ph, pyridinyl, pyrimidinyl, or a 5-8 membered cycloalkyl; R1, R2 = independently H, C1-3 alkyl; or R1CR2 = 3-6 membered cycloalkyl ring; R3 = 0-2 optional substituents on the ring to which -L-W is directly attached; R4 = H, halo, C1-3 alkyl; R5 = H, halo, CN, C1-3 alkoxy, etc.; L = C1-C4 straight chain or branched alkylene linker, or L = C1-C4 straight chain or branched alkylene linker or a bond when W is an optionally substituted ring; W = H, OH, an optionally substituted ring selected from 3-6 membered cycloalkyl, Ph, 5-6-membered heterocyclyl containing one or two N, O or S heteroatoms as ring members, and 5-membered heteroaryl containing up to 4 heteroatoms selected from N, O and S as ring members that is optionally fused to Ph, etc.; Y = (CH2)0-2] their pharmaceutically acceptable salts, to pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses. Thus, II (m.p. = 186°) was prepared by reaction of Bu 1,6-dioxo-2,3,4,6-tetrahydro-1H-pyrido[1,2-a]pyrazine-7-carboxylate (preparation given) with [1-(cyclopropylsulfonyl)cyclopropyl]methyl Methanesulfonate (preparation given) in DMF in the presence of NaH, acidulation of III•Na, activation of the acid III with oxalyl chloride, amidation with 4-(aminomethyl)benzonitrile hydrochloride. The exemplified compounds of the invention were studied in an CMV polymerase, CMV-luciferase and HSV polymerase assays (some data given). The activity of I against human herpes viruses CMV HSV-1, VZV and EBV was evaluated [Ec50 values of 24(±7) nM, 32(±12), 20(±8) and 12(±), resp]. The experimental process involved the reaction of 1-[(Dibenzylamino)methyl]cyclopropanol(cas: 428855-17-8).Recommanded Product: 1-[(Dibenzylamino)methyl]cyclopropanol

The Article related to pyridopyrazinedione preparation herpes antiviral, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 1-[(Dibenzylamino)methyl]cyclopropanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On July 11, 2019, Qian, Wenyuan; Yang, Chundao; Xu, Guanghai; Li, Jie; Li, Jian; Chen, Shuhui published a patent.SDS of cas: 386704-04-7 The title of the patent was Preparation of isoindolinone and derivatives thereof as CSF-1R inhibitors. And the patent contained the following:

The present invention relates to a type of isoindolinone derivatives and use thereof in the preparation of a medicament for treating diseases associated with a novel colony stimulating factor 1 receptor (CSF-1R) inhibitor. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).SDS of cas: 386704-04-7

The Article related to isoindolinone preparation colony stimulating factor receptor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts