205055-10-3

Usage

Uses

Used in Research and Development:
Benzo[b]thiophene, 6-fluoro(9CI) is used as a building block in the synthesis of various organic compounds, contributing to the development of new chemical entities with potential applications in different fields.
Used in Pharmaceutical Production:
Benzo[b]thiophene, 6-fluoro(9CI) serves as a precursor in the production of pharmaceuticals, aiding in the creation of new drugs with potential therapeutic benefits.
Used in Agrochemical Production:
Benzo[b]thiophene, 6-fluoro(9CI) is also utilized as a precursor in the development of agrochemicals, which are essential for enhancing crop protection and productivity.
Used in Medicine and Drug Discovery:
Due to its potential biological and pharmacological activities, Benzo[b]thiophene, 6-fluoro(9CI) is being studied for its applications in the field of medicine, with the aim of discovering new drugs for the treatment of various diseases and conditions.

Upstream product

• 550998-52-2 6-fluorobenzo[b]thiophene-2-carboxylic acid methyl ester 
• 1098607-88-5 6-fluoro-1-benzothiophen-3(2H)-one 
• 501944-64-5 3-fluorobenzenethioacetaldehyde diethyl acetal 
• 212078-68-7 6-fluorobenzo[b]thiophene-2-carboxylic acid ethyl ester 
• 1550-35-2 2,4-difluorobenzaldehyde 
• 142329-23-5 6-fluorobenzo[b]thiophene-2-carboxylic acid 

Downstream Products

• 324769-21-3 C₂₇H₃₂FNO₄SSi 
• 324769-20-2 1-benzyl-3-methyl-4-hydroxy-4-(2-trimethylsilyl-6-fluorobenzothien-7-yl)piperidine 
• 212078-69-8 1-(6-fluorobenzo[b]thiophen-2-yl)-3-(1-triphenylmethyl-1H-imidazol-4-yl)-propan-1-ol 

Relevant academic research and scientific papers

Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?

The syntheses and antiplasmodial activities of various substituted aminoquinolines coupled to an adamantane carrier are described. The compounds exhibited pronounced in vitro and in vivo activity against Plasmodium berghei in the Thompson test. Tethering a fluorine atom to the aminoquinoline C(3) position afforded fluoroaminoquinolines that act as intrahepatocytic parasite inhibitors, with compound 25 having an IC50 = 0.31 μM and reducing the liver load in mice by up to 92% at 80 mg/kg dose. Screening our peroxides as inhibitors of liver stage infection revealed that the tetraoxane pharmacophore itself is also an excellent liver stage P. berghei inhibitor (78: IC50 = 0.33 μM). Up to 91% reduction of the parasite liver load in mice was achieved at 100 mg/kg. Examination of tetraoxane 78 against the transgenic 3D7 strain expressing luciferase under a gametocyte-specific promoter revealed its activity against stage IV-V Plasmodium falciparum gametocytes (IC50 = 1.16 ± 0.37 μM). To the best of our knowledge, compounds 25 and 78 are the first examples of either an 4-aminoquinoline or a tetraoxane liver stage inhibitors.

Pharmaceutical compounds

This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, m and n have the values defined in claim 1, their preparation and use as pharmaceuticals.

Indole derivatives for the treatment of depression and anxiety

The present invention provides compounds of formula (I): which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotine.

An improved synthesis of substituted benzo[b]thiophenes using microwave irradiation

An easy and high-yielding method for the synthesis of substituted benzo[b]thiophenes using microwave irradiation is described.

C17,20-lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors.

Novel nonsteroidal C(17,20)-lyase inhibitors were synthesized using de novo design based on its substrate, 17 alpha-hydroxypregnenolone, and several compounds exhibited potent C(17,20)-lyase inhibition. However, in vivo activities were found to be short-lasting, and in order to improve the duration of action, a series of benzothiophene derivatives were evaluated. As a result, compounds 9h, (S)-9i, and 9k with nanomolar enzyme inhibition (IC(50)=4-9 nM) and 9e (IC(50)=27 nM) were identified to have powerful in vivo efficacy with extended duration of action. The key structural determinants for the in vivo efficacy were demonstrated to be the 5-fluoro group on the benzothiophene ring and the 4-imidazolyl moiety. Superimposition of 9k and 17 alpha-hydroxypregnenolone demonstrated their structural similarity and enabled rationalization of the pharmacological results. In addition, selected compounds were also identified to be potent inhibitors of human enzyme with IC(50) values of 20-30 nM.

Fused ring compounds, process for producing the same and use thereof

To provide a novel compound of the formula: [wherein A1 ix a 5 or 6-membered ring which may be substituted by a group not containing a cyclic group, A2 is an aromatic ring which may be substituted, X is a divalent group, Y is a nitrogen atom or a methine group, Z is an ethenylene which may be substituted or ethynylene, R is a heterocyclic group which may be substituted, provided that 3,4-dihydro-6-[3-(1H-imidazol-1-yl)-1-propenyl]-2(1H)-quinolone and 2-[3-[5-ethyl-6-methyl-2-(benzyloxy)-3-pyridyl]-1-propenyl]benzoxazole are excluded.], or a salt thereof which has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating mammals suffering from, for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.

Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds

The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

Substituted sulfonic acid N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds

The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.

SUBSTITUTED SULFONIC ACID N-[(AMINOIMINOMETHYL)PHENYLALKYL]-AZAHETEROCYCLAMIDE COMPOUNDS

The compounds of formula I exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.