Month: October 2022

On February 13, 2020, Ngu, Khehyong published a patent.Reference of 5-Chlorobenzo[b]thiophene-3-carbaldehyde The title of the patent was Benzimidazoles as inhibitors of PAD enzymes and their preparation. And the patent contained the following:

The invention provides compounds of formula I or a pharmaceutically acceptable salt thereof, useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders. Compounds of formula I wherein ring A is 4- to 15-membered heterocyclyl; B is (un)substituted indolyl, (un)substituted azaindolyl, (un)substituted benzothienyl and (un)substituted phenyl; R1 is substituted C3-6 cycloalkyl, (CH2)2-4R5a, substituted (CH2)1-4-C3-6 cycloalkyl, etc.; R3 is H, F, Cl, Br, etc.; R8 is independently H, F, Cl, CN, etc.; R5a is CONH2 and derivatives, NH2 and derivatives, NHCO2H and derivatives, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their PAD4 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of 0.014μM. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Reference of 5-Chlorobenzo[b]thiophene-3-carbaldehyde

The Article related to benzimidazole preparation pad inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Reference of 5-Chlorobenzo[b]thiophene-3-carbaldehyde

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On August 27, 2015, Chen, Shuhui; Zhu, Wenyuan; Wang, Jianfei; Li, Jian; Wei, Yuquan; Yu, Luoting; Tao, Xin published a patent.COA of Formula: C9H9BrO2S The title of the patent was Thiophene-imidazole derivatives as hepatitis c virus inhibitors and their preparation, pharmaceutical compositions and use in the treatment of chronic hepatitis C virus infection. And the patent contained the following:

Disclosed is thiophene-imidazole derivatives, e.g., I, as hepatitis C virus (HCV) inhibitors or variant derivatives thereof and compositions thereof. The invention further relates to the application in preparing chronic hepatitis C virus infection drugs. Particularly, the invention relates to a series of compounds used as NS5A inhibitors and compositions thereof and uses thereof for drug preparation Compound I was prepared by using cyclization, cross-coupling and condensation as the key steps. All the invention compounds were evaluated for their hepatitis c virus and NS5A inhibitory activity. From the assay, it was determined that example compound I exhibited the EC50 and CC50 values of 0.001 – 0.1 nM and > 10 nM against HCV 1b. The experimental process involved the reaction of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid(cas: 188240-63-3).COA of Formula: C9H9BrO2S

The Article related to thiophene imidazole preparation ns5a inhibitor treatment chronic hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.COA of Formula: C9H9BrO2S

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On August 26, 2015, Chen, Shuhui; Zhu, Wenyuan; Wang, Jianfei; Li, Jian; Wei, Yuquan; Yu, Luoting; Tao, Xin published a patent.Reference of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid The title of the patent was Thiophene-imidazole derivatives as hepatitis c virus inhibitors and their preparation, pharmaceutical compositions and use in the treatment of chronic hepatitis C virus infection. And the patent contained the following:

The invention discloses a series of thiophene or its variant derivative and composition as hepatitis C virus inhibitor, and relating to its application in preparation chronic HCV infection treatment medicine.In particular it relates to the series compound as NS5A inhibitor and composition thereof and pharmaceutical applications. Disclosed is thiophene-imidazole derivatives, e.g., I, as hepatitis C virus (HCV) inhibitors or variant derivatives thereof and compositions thereof. The invention further relates to the application in preparing chronic hepatitis C virus infection drugs. Particularly, the invention relates to a series of compounds used as NS5A inhibitors and compositions thereof and uses thereof for drug preparation Compound I was prepared by using cyclization, cross-coupling and condensation as the key steps. All the invention compounds were evaluated for their hepatitis c virus and NS5A inhibitory activity. From the assay, it was determined that example compound I exhibited the EC50 and CC50 values of 0.001 – 0.1 nM and > 10 nM against HCV 1b. The experimental process involved the reaction of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid(cas: 188240-63-3).Reference of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid

The Article related to thiophene imidazole preparation ns5a inhibitor treatment chronic hepatitis c, Heterocyclic Compounds (More Than One Hetero Atom): Imidazoles and other aspects.Reference of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On September 5, 1984, Ward, Robert William; Smith, Stephen Allan; Markwell, Roger Edward published a patent.Related Products of 16296-68-7 The title of the patent was Benzofuran- and benzothiophenecarboxylic acid derivatives. And the patent contained the following:

The title compounds I [X = O, S, SO, SO2, X1 = CH2; X = CH2, X1 = O; R = Ph, alkylphenyl, alkoxyphenyl, CF3C6H4, BrC6H4, ClC6H4, FC6H4, pyrrolyl, N-alkylpyrrolyl, furyl, thienyl, (un)substituted by Me, Cl, or Br; R1,R3 = H, alkyl; R2 = H, F, Cl, Br; R4 = H, alkyl] were prepared Thus, II (R2 = Br, R4 = R5 = H) was prepared by ring contraction of 6-bromo-4-chromanone with Tl(NO3)3, esterified, and subjected to Friedel-Crafts acylation with BzCl to give II (R2 = Br, R4 = Et, R5 = Bz) which was debrominated and saponified to II (R2 = R4 = H, R5 = Bz, III). At 5 mg/kg orally the phenylquinone writhing test in mice III gave analgesia in 90% of the animals. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Related Products of 16296-68-7

The Article related to benzofurancarboxylate preparation analgesic, benzothiophenecarboxylate, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenothiophenes and other aspects.Related Products of 16296-68-7

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On June 15, 2011, Capek, Petr; Zhang, Yan; Barlow, Deborah J.; Houseknecht, Karen L.; Smith, Garry R.; Dickerson, Tobin J. published an article.Recommanded Product: 16296-68-7 The title of the article was Enhancing the Pharmacokinetic Properties of Botulinum Neurotoxin Serotype A Protease Inhibitors through Rational Design. And the article contained the following:

Botulinum neurotoxin (BoNT), the etiol. agent that causes the neuroparalytic disease botulism, has become a highly studied drug target in light of the potential abuse of this toxin as a weapon of bioterrorism. In particular, small mol. inhibitors of the light chain metalloprotease of BoNT serotype A have received significant attention and a number of small mol. and biol. inhibitors have been reported. However, all small mols. reported have been identified from either primary screens or medicinal chem. follow-up studies, and the pharmacokinetic profiles of these compounds have not been addressed. In this study, we have removed the pharmacol. liabilities of one of the best compounds reported to date, 2,4-dichlorocinnamate hydroxamic acid, and in the process uncovered a related class of benzothiophene hydroxamic acids that are significantly more potent inhibitors of the BoNT/A light chain, while also possessing greatly improved ADME properties, with the best compound showing the most potent inhibition of BoNT/A light chain reported (Ki = 77 nM). Using a strategy of incorporating traditional drug development filters early into the discovery process, potential liabilities in BoNT/A lead compounds have been illuminated and removed, clearing the path for advancement into further pharmacol. optimization and in vivo efficacy testing. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Recommanded Product: 16296-68-7

The Article related to botulinum neurotoxin serotype a protease inhibitor chlorocinnamate benzothiophene hydroxamate, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenothiophenes and other aspects.Recommanded Product: 16296-68-7

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On September 12, 2013, Zhong, Zhaojin; Li, Zhuorong; Zhang, Dajun; Li, Yuhuan; Wang, Zhen; Gao, Rongmei; Shen, Jiajia published a patent.SDS of cas: 16296-68-7 The title of the patent was Preparation of phenyl oxazole derivatives as inosine monophosphate dehydrogenase inhibitors. And the patent contained the following:

Disclosed are Ph oxazolyl derivatives I [wherein R1 = H, halo, OH, alkyl, or alkoxy; R2 = absence, H, (un)substituted alkyl, CO2H, or sulfonyl; R = H, CN, (un)substituted alkyl, alkoxy, or aryloxy, etc.; p = 0-1; m = 0-3; n = 0-6] as an inosine monophosphate dehydrogenase (IMPDH) inhibitors for treating viral infection, neoplasm, and immune disease. For example, 3-methoxy-4-(oxazole-5-yl)aniline was reacted with 5-chloro-2-thiophenecarboxaldehyde to give II in 96.9% yield. In biol. test, II at 10 μg/mL showed 74.9% inhibition against IMPDH. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).SDS of cas: 16296-68-7

The Article related to preparation oxazole inosine monophosphate dehydrogenase inhibitor impdh human, treatment viral infection neoplasm immune disease, Heterocyclic Compounds (More Than One Hetero Atom): Oxazoles, Isoxazoles and other aspects.SDS of cas: 16296-68-7

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On May 6, 2021, Wang, Jianfei; Zhang, Yang; Zhu, Wenyuan; Li, Jian; Chen, Shuhui published a patent.Product Details of 188240-63-3 The title of the patent was Uricosuric agent, synthetic method therefor, and pharmaceutical application thereof. And the patent contained the following:

A compound of a uricosuric agent used as a uric acid transporter (URAT1) inhibitor, and application thereof in preparation of a medication for treating a disease related to abnormal uric acid levels. The experimental process involved the reaction of 3-Bromo-4,5,6,7-tetrahydrobenzo[c]thiophene-1-carboxylic acid(cas: 188240-63-3).Product Details of 188240-63-3

The Article related to uricosuric agent uric acid transporter inhibitor preparation, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Product Details of 188240-63-3

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On January 9, 2003, Basarab, Gregory; Eyermann, Joseph; Gowravaram, Madhusudhan; Green, Oluyinka; MacPherson, Lawrence; Morningstar, Marshall; Nguyen, Thanh published a patent.SDS of cas: 16296-68-7 The title of the patent was Preparation of pyrazolo[3,4-d]pyrimidines for inhibiting H. pylori infections. And the patent contained the following:

Title compounds I [wherein R1 and R2 = independently H, NH2, or (un)substituted (cyclo)alkyl, (cyclo)alkenyl, alkynyl, aryl, alkoxy, or heterocyclyl; R3 = (un)substituted monocyclic or bicyclic ring system comprising 0-3 heteroatoms independently selected from N, O, or S; R4 = (un)substituted alkyl or (di)alkylamino, with exceptions; Y = CH2, CHCH3, SO, or SO2; and pharmaceutically acceptable salts thereof] were prepared For example, 6-hydrazino-1-isobutyl-3-methylpyrimidine-2,4-(1H,3H)-dione (4-step preparation given) was condensed with 1-naphthaldehyde in MeOH to give the hydrazone. Cyclocondensation with N-(4-formylphenyl)acetamide in DMF afforded II. Compounds of the invention exhibited glutamate racemase (MurI) activity with IC50 values of < 400 μM. Thus, I and pharmaceutical compositions containing them are useful in the treatment or prophylaxis of Helicobacter pylori (H. pylori) infection (no data). The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).SDS of cas: 16296-68-7

The Article related to pyrazolopyrimidine preparation antibacterial helicobacter pylori, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.SDS of cas: 16296-68-7

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On June 16, 2016, Jones, Michael L.; Lilly, John C.; Ankala, Sudha V.; Singleton, Scott F. published a patent.Formula: C9H5ClOS The title of the patent was Preparation of quinazolinones, indazoles and other heterocyclic compounds as SOS inhibitors and antibiotic potentiators. And the patent contained the following:

The invention relates to preparation of quinazolinones of formula I, indazoles of formula II , wherein all the variables are as defined in the disclosure, and other heterocyclic compounds as SOS inhibitors and their use as antibiotics and as antibiotic potentiators. The example compound III was prepared by multistep synthesis according to the procedure shown and was tested for its antibacterial and SOS response-inhibiting activity (data disclosed). The compounds may act as colistin potentiators and SOS inhibitors. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Formula: C9H5ClOS

The Article related to quinazolinone indazole preparation sos inhibitor antibiotic potentiator combination chemotherapy, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Formula: C9H5ClOS

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

On November 30, 2010, Hanna-Elias, Amir; Manallack, David T.; Levit, Alla; Nguyen, William; Ayad, Fadi; Perera, Glen; Shapiro, Marina; Irving, Helen R.; Coupar, Ian M.; Iskander, Magdy N. published an article.Related Products of 16296-68-7 The title of the article was Synthesis, testing and structure-activity studies on a library of 5-HT4 ligands. And the article contained the following:

Several indole derivatives and analogs comprising a range of related structural classes were designed, synthesized and tested as ligands for the 5-HT4 receptor. Within each series, binding experiments showed compounds with good affinity demonstrating high percentage displacement values at 1 μM. The most potent of these (I) had a pKi of 8.54 demonstrating very good affinity. These indole analogs were combined with 55 ligands that were previously produced to explore the structure-activity relationships of these 5-HT4 ligands. A CoMFA (Comparative Mol. Field Anal.) anal. was used to extend an earlier simple pharmacophore to suggest two new mol. features beyond the primary amino binding site. The pharmacophore confirmed that a newly described tetrahydroquinoline analog was able to match the basic requirements of the model and the pharmacol. of this mol. is provided in more detail. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Related Products of 16296-68-7

The Article related to indole derivative preparation 5ht4 ligand structure activity relationship pharmacophore, comparative mol field analysis indole derivative serotonin receptor binding, Heterocyclic Compounds (One Hetero Atom): Indoles, Indolizines, Carbazoles, and Other Arenopyrroles and other aspects.Related Products of 16296-68-7

Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem