172215-93-9

Upstream product

• 6641-64-1 4,5-dichloro-2-nitroaniline 

Downstream Products

• 20066-83-5 2-Bromo-4-chloro-3-(4-chloro-3-trifluoromethyl-phenoxy)-6-nitro-phenylamine 
• 20066-81-3 2-Bromo-4-chloro-3-(2,4-dichloro-phenoxy)-6-nitro-phenylamine 
• 172215-94-0 3-bromo-4,5-dichlorophenylene-1,2-diamine 
• 20066-80-2 3-Bromo-4-(4-bromo-phenoxy)-5-chloro-benzene-1,2-diamine 
• 20074-12-8 3-Bromo-5-chloro-4-(4-chloro-3-trifluoromethyl-phenoxy)-benzene-1,2-diamine 
• 20074-02-6 4-Chlor-5-phenylthio-6-brom-1,2-phenylendiamin 
• 17011-00-6 3,4-Diamino-2-brom-6,4'-dichlordiphenylether 
• 20074-01-5 3-Bromo-5-chloro-4-(2,4,5-trichloro-phenoxy)-benzene-1,2-diamine 
• 20066-82-4 3-Bromo-5-chloro-4-(2,4-dichloro-phenoxy)-benzene-1,2-diamine 
• 20066-76-6 4-Chlor-5-phenoxy-6-brom-1,2-phenylendiamin 
• 1421703-65-2 C₂₄H₂₉Cl₂N₅O 
• 1421703-93-6 4-(5,6-dichloro-4-(dimethylcarbamoyl)-2-(isopropylamino)-1H-benzo[d]imidazol-1-yl)phenyl trifluoromethanesulfonate 
• 1421703-92-5 5,6-dichloro-1-(4-hydroxyphenyl)-2-(isopropylamino)-N,N-dimethyl-1H-benzo[d]imidazole-4-carboxamide 
• 1421703-91-4 5,6-dichloro-2-(isopropylamino)-1-(4-methoxyphenyl)-N,N-dimethyl-1H-benzo[d]imidazole-4-carboxamide 

Relevant academic research and scientific papers

Synthesis and antiviral evaluation of halogenated β-D- and -L- erythrofuranosylbenzimidazoles

A series of 2-substituted benzimidazole D- and L-erythrofuranosyl nucleosides were synthesized and tested for activity against herpesviruses and for cytotoxicity. The D-nucleosides 2,5,6-trichloro-1-(β-D- erythrofuranosyl)benzimidazole (8a) and 2-bromo-5,6-dichloro-1-(β-D- erythrofuranosyl)benzimidazole (8b) were prepared by coupling 1,2,3-tri-O- acetyl-β-D-erythrofuranose (D-6) with the appropriate benzimidazole, followed by removal of the acetyl protecting groups. The 2-isopropylamino (9), 2-cyclopropylamino (10), and 2-mercaptobenzyl (11) derivatives were synthesized by nucleophilic displacements of the C-2 chlorine in the benzimidazole moiety of 8a. The v-nucleoside 4-bromo-5,6-dichloro-2- isopropylamino-1-(β-v-erythrofuranosyl)benzimidazole (17) was prepared by coupling D-6 with the appropriate benzimidazole. The L-erythrofuranosyl derivatives, 5,6-dichloro-2-isopropylamino-1-(β-L- erythrofuranosyl)benzimidazole (21a), its 2-cyclopropylamino analogue (21b), and the 2-isopropylamino analogue (25), were prepared by coupling L-6 with the appropriate benzimidazole. Several of these new derivatives had very good activity against HCMV in plaque and yield reduction assays (IC50 = 0.05-19 μM against the Towne strain of HCMV) and DNA hybridization assays. Very little activity was observed against other herpesviruses. This pattern is similar to the antiviral activity profile observed for the corresponding ribofuranosides 2,5,6-trichloro-1-(β-D-ribofuranosyl)benzimidazole (4a), its 2-bromo analogue (4b), and the 2-cyclopropylamino analogue (4c). In comparison, 8a was 15-fold more active against HCMV than 4a, and 8b was 4- fold more active against HCMV than 4b. The 5,6-dichloro-2-isopropylamino-1- (βL-erythrofuranosyl)benzimidazole (21a) was less active than 4c, which is now in clinical trials for HCMV infection. Both 8a,b had comparable HCMV activity to 4c. Mode of action studies with the v-erythrose analogues established that 8b acted by inhibition of viral DNA processing whereas 9 and 10 may act via a different mechanism. The lack of a 5'-hydroxymethyl group in all members of this series established that antiviral activity occurred without 5'-phosphorylation, a feature required for the activity of most nucleoside analogues.

HETEROARYL RHEB INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same. Compositions comprising a compound of this invention or a pharmaceutically acceptable derivative thereof and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The amount of the compound in compositions of this invention is such that it is effective to measurably inhibit Rheb, in a biological sample or in a patient.

Optimization of a novel series of TRPV4 antagonists with in vivo activity in a model of pulmonary edema

High-throughput screening and subsequent hit optimization identified 1-piperidinylbenzimidazoles, exemplified by compound 1, as TRPV4 inhibitors. Lead optimization identified potent TRPV4 blocker 19, which has good target activity and pharmacokinetic properties. Inhibitor 19 was then profiled in an in vivo rat model, demonstrating its ability to inhibit TRPV4-mediated pulmonary edema.

L-benzimidazole nucleosides

The present invention relates to benzimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.