129121-41-1

Upstream product

• 1747-60-0 6-methoxybenzothiazol-2-ylamine 
• 26278-79-5 2-amino-6-hydroxybenzothiazole 
• 352-33-0 1-Chloro-4-fluorobenzene 
• 36160-82-4 4-(4-fluorophenoxy)aniline 
• 100-00-5 4-chlorobenzonitrile 
• 371-41-5 4-Fluorophenol 
• 2561-25-3 4-(4-fluorophenoxy)-1-nitrobenzene 

Downstream Products

• 352527-98-1 1-(6-(4'-Fluorophenoxy)-2-benzothiazolyl)-3-ethylurea 

Relevant academic research and scientific papers

AGRICULTURAL CHEMICALS

The present invention relates to picolinic acid derivatives that are useful in treating fungal diseases ofplants.

Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels

Both N- and T-type calcium ion channels have been implicated in pain transmission and the N-type channel is a well-validated target for the treatment of neuropathic pain. An SAR investigation of a series of substituted aminobenzothiazoles identified a subset of five compounds with comparable activity to the positive control Z160 in a FLIPR-based intracellular calcium response assay measuring potency at both CaV2.2 and CaV3.2 channels. These compounds may form the basis for the development of drug leads and tool compounds for assessing in vivo effects of variable modulation of CaV2.2 and CaV3.2 channels.

Synthesis and anticonvulsant activity evaluation of 7-alkoxy[1,2,4] triazolo[3,4-b]benzothiazol-3(2H)-ones

A new series of 7-alkoxy[1,2,4]triazolo[3,4-b]benzothiazol-3(2H)-ones were synthesized and evaluated for their anticonvulsant activities. Among these compounds, 7-propoxy[1,2,4]triazolo[3,4-b]benzothiazol-3(2H)-one (4c) and 7-butoxy[1,2,4]triazolo[3,4-b]benzothiazol-3(2H)-one (4d) showed the highest activity against maximal electroshock (MES)-induced tonic extension [effective dose (ED)50: 11.4 and 13.6 mg/kg, respectively]. It is worth mentioning that compound 4d showed especially low neurotoxicity, which led to a high protective index (PI >51). The orally anticonvulsant activity data of compound 4d further confirmed its efficacy, in an MES test, and its high safety with a PI value of 50.2. In addition, the potency of compound 4h against seizures induced by pentylenetetrazole, 3-mercaptopropionic acid, and bicuculline in the chemical-induced seizure tests suggested that compound 4d may exert its anticonvulsant activity through affecting the GABAergic system.

Benzothiazole derivatives

The present invention is directed to a compound of formula (I), racemic-diastereomeric mixtures thereof, optical isomers thereof, prodrugs thereof, isotopes thereof or pharmaceutically-acceptable salts of said compound, isomers, prodrugs and isotopes, wherein the variables are defined herein. The compounds of this invention are useful as inhibitors of serine/threonine and tyrosine kinases. In particular, compounds of this invention are useful as inhibitors of tyrosine kinases that are important in hyperproliferative diseases, especially in cancer and in the process of angiogenesis.

1,5-benzothiazepine derivatives, their preparation and their use in the treatment of cardiovascular disorders

Compounds of formula (I): STR1 in which: R 1 is aryl or aromatic heterocyclic; R 2 and R 3 are hydrogen, alkyl, alkoxy, halogen, phenyl, phenoxy, C 1 -C 6 alkylthio, phenylthio, C 1 -C 6 haloalkyl, cyano or nitro, or together are alkylene optionally containing oxygen; R 4 is hydrogen, aliphatic acyl, cycloalkylcarbonyl, cycloalkoxycarbonyl, aromatic acyl, alkoxycarbonyl or benzyloxycarbonyl; R 5 and R 6 are alkyl; and X is oxygen, sulfur or methylene, have calcium channel blocking activity and can serve for the treatment or prophylaxis of cardiovascular diseases and disorders. They may be prepared by reacting a corresponding compound where R 4 is hydrogen and the aminoethyl group is replaced by hydrogen with a compound providing the aminoethyl group and the, if required, acylating the product.