10133-22-9

Upstream product

• 14315-14-1 5-methylthianaphthene 
• 94-36-0 dibenzoyl peroxide 
• 20532-34-7 5-(hydroxymethyl)benzothiophene 
• 18441-43-5 5-methylbenzofuran 

Downstream Products

• 20532-34-7 5-(hydroxymethyl)benzothiophene 
• 10133-30-9 benzo[b]thiophene-5-carbaldehyde 
• 1643-19-2 tetrabutylammomium bromide 
• 1198790-98-5 sodium (1R,4S,5R)-1,4,5-trihydroxy-3-[(benzo[b]thiophen-5-yl)methoxy]cyclohex-2-en-1-carboxylate 
• 1233376-41-4 methyl (1R,4S,5R)-3-(benzo[b]thiophen-5-yl)methoxy-1,4,5-trihydroxycyclohex-2-en-1-carboxylate 
• 1319745-61-3 ethyl (1R,4S,5R)-3-(benzo[b]thiophen-5-yl)methoxyl-1,4,5-trihydroxycyclohex-2-ene-1-carboxylate 
• 1319745-73-7 ethyl (1R,4S,5R)-4,5-dibutyroxy-3-(benzo[b]thiophen-5-yl)methoxy-1-hydroxycyclohex-2-ene-1-carboxylate 
• 1319745-65-7 propyl (1R,4S,5R)-3-(benzo[b]thiophen-5-yl)methoxy-1,4,5-trihydroxycyclohex-2-ene-1-carboxylate 
• 1319745-74-8 propyl (1R,4S,5R)-3-(benzo[b]thiophen-5-ylmethoxy)-4,5-dibutyroxy-1-hydroxycyclohex-2-ene-1-carboxylate 
• 1319745-75-9 propyl (1R,4S,5R)-3-(benzo[b]thiophen-5-ylmethoxy)-4-butyroxy-1,5-dihydroxycyclohex-2-ene-1-carboxylate 
• 56540-52-4 benzo[b]thiophen-5-ylmethanamine 
• 96803-30-4 5-(2-hydroxyethyl)benzo[b]thiophene 
• 17381-54-3 (1-benzothiophen-5-yl)acetic acid 
• 348080-83-1 benzo[b]thiophene-5-methanesulfonyl chloride 

Relevant academic research and scientific papers

THERAPEUTIC COMPOUNDS AND METHODS TO TREAT INFECTION

Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.

METHOD FOR PRODUCING 5-(BROMOMETHYL)-1-BENZOTHIOPHENE

Provided is a method for industrially producing 5-(bromomethyl)-1-benzothiophene. The production method according to the present invention comprises: (1) a step for introducing 5-methyl-1-benzothiophene, a brominating agent, and a solvent into a reactor; (2) a step for emitting light having a wavelength range of 200-780 nm inside the reactor; and (3) a step for recovering 5-(bromomethyl)-1-benzothiophene from the reactor.

COMPETITIVE INHIBITORS OF TYPE II DEHYDROQUINASE ENZYME

The present invention is directed to a compound of formula (I), its diastereoisomers, its enantiomers or its pharmaceutically acceptable salts or solvates, formula (I), to procedures of obtaining the same, to intermediates thereof, and use as competitive inhibitors of the third enzyme of the shikimic acid pathway, the type II dehydroquinase.

Synthesis and biological evaluation of new nanomolar competitive inhibitors of Helicobacter pylori type II dehydroquinase. Structural details of the role of the aromatic moieties with essential residues

The shikimic acid pathway is essential to many pathogens but absent in mammals. Enzymes in its pathway are therefore appropriate targets for the development of novel antibiotics. Dehydroquinase is the third enzyme of the pathway, catalyzing the reversible dehydratation of 3-dehydroquinic acid to form 3-dehydroshikimic acid. Here we present the synthesis of novel inhibitors with high affinity for Helicobacter pylori type II dehydroquinase and efficient inhibition characteristics. The structure of Helicobacter pylori type II dehydroquinase in complex with the most potent inhibitor shows that the aromatic functional group interacts with the catalytic Tyr22 by π-stacking, expelling the Arg17 side chain, which is essential for catalysis, from the active site. The structure therefore explains the favorable properties of the inhibitor and will aid in design of improved antibiotics.

NOVEL INHIBITORS OF BETA-LACTAMASE

This invention provides novel β-lactamase inhibitors of the aryl- and heteroarylsulfonamidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammonium groups. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e.g., imipenem and ceftazidime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.

4-AMINO-PIPERIDINE DERIVATIVES AS MONOAMINE UPTAKE INHIBITORS

The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such,

(Hetero) Bicyclymethanesulfonylamino-substituted hydroxamic acid derivatives

Compounds of formula (I) wherein R is hydrogen, alkyl alkenyl, alkynyl, aryl, heteroaryl or heterocyclyl; and R1 is bicyclyl or heterobicyclyl; are useful in the treatment and prophylaxis of conditions mediated by s-CD23 or TNF.

Imidazole compounds

A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.

Piperidine derivatives having renin inhibiting activity

Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I wherein R1, R2, R3, R4, Q, X, Z, m and n are as described herein.

Catecholamine surrogates useful as β3 agonists

Compounds of the formula STR1 or pharmaceutically acceptable salts thereof wherein: A is a bond, --(CH 2) n -- or --CH(B)--, where n is an integer of 1 to 3 and B is --CN, --CON(R 9)R 9'' or --CO 2 R 7 ;R 1 is lower alkyl, aryl or arylalkyl;R 2 is hydrogen, hydroxy, alkoxy, --CH 2 OH, cyano, --C(O)OR 7, --CO 2 H, --CONH 2, tetrazole, --CH 2 NH 2 or halogen; STR2 R 3 is hydrogen, alkyl, heterocycle or R 4 is hydrogen, alkyl or B;R 5, R 5'', R 8, R 8'' or R 8"" are independently hydrogen, alkoxy, lower alkyl, halogen, --OH, --CN, --(CH 2) n NR 6 COR 7, --CON(R 6)R 6'', --CON(R 6)OR 6'', --CO 2 R 6, --SR 7, --SOR 7, --SO 2 R 7, --N(R 6)SO 2 R 1, --N(R 6)R 6'', --NR 6 COR 7, --OCH 2 CON(R 6)R 6'', --OCH 2 CO 2 R 7 or aryl; orR 5 and R 5'' or R 8 and R 8'' may together with the carbon atoms to which they are attached form an aryl or heterocycle;R 6 and R 6'' are independently hydrogen or lower alkyl; andR 7 is lower alkyl;R 9 is hydrogen, lower alkyl, alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl; or R 9 and R 9'' may together with the nitrogen atom to which they are attached form a heterocycle; with the proviso that when A is a bond or --(CH 2) n and R 3 is hydrogen or unsubstituted alkyl, then R 4 is B or substituted alkyl. These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.