Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C34H34N4O4 |
| Molecular Weight | 562.6582 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CN1C2=C(C=CC(=C2)C(=O)NC3(CCC3)C(=O)NC4=CC=C(\C=C\C(O)=O)C=C4)C(C5CCCC5)=C1C6=CC=CC=N6
InChI
InChIKey=JBSNALXXNTWUEC-SFQUDFHCSA-N
InChI=1S/C34H34N4O4/c1-38-28-21-24(13-16-26(28)30(23-7-2-3-8-23)31(38)27-9-4-5-20-35-27)32(41)37-34(18-6-19-34)33(42)36-25-14-10-22(11-15-25)12-17-29(39)40/h4-5,9-17,20-21,23H,2-3,6-8,18-19H2,1H3,(H,36,42)(H,37,41)(H,39,40)/b17-12+
| Molecular Formula | C34H34N4O4 |
| Molecular Weight | 562.6582 |
| Charge | 0 |
| Count |
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| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Optical Activity | NONE |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:38:20 GMT 2023
by
admin
on
Sat Dec 16 11:38:20 GMT 2023
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| Record UNII |
3WV68DY85W
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| Record Status |
Validated (UNII)
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| Record Version |
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Common Name | English | ||
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Code | English |
| Code System | Code | Type | Description | ||
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494856-61-0
Created by
admin on Sat Dec 16 11:38:20 GMT 2023 , Edited by admin on Sat Dec 16 11:38:20 GMT 2023
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3WV68DY85W
Created by
admin on Sat Dec 16 11:38:20 GMT 2023 , Edited by admin on Sat Dec 16 11:38:20 GMT 2023
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56949326
Created by
admin on Sat Dec 16 11:38:20 GMT 2023 , Edited by admin on Sat Dec 16 11:38:20 GMT 2023
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BILB-1941
Created by
admin on Sat Dec 16 11:38:20 GMT 2023 , Edited by admin on Sat Dec 16 11:38:20 GMT 2023
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PRIMARY | Official Title: A Multinational Randomised, Double-blind, Placebo Controlled Study to Evaluate the Antiviral Pharmacodynamic Effect, Safety, and Pharmacokinetics of Escalating Doses of BILB 1941 ZW Oral Solution Administered Q8H for Five Days to Patients With Chronic Hepatitis C Genotype 1 Virus Infection.Purpose: To assess the antiviral effect, safety and pharmacokinetics of rising doses of 10 mg, 20 mg, 40 mg, 60 mg, 80 mg, 100 mg, 150 mg, 200 mg, 300 mg, 450 mg, 650 mg, 900 mg oral BILB 1941 ZW administered Q8H in a polyethyleneglycol 400 (PEG 400): distilled water: Tromethamine (TRIS) drinking solution for five days to patients with chronic HCV genotype 1 infection. |
| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Originator: Boehringer Ingelheim; Class: Antiviral; Mechanism of Action: Hepatitis C virus NS 5 protein inhibitor; Highest Development Phase: Discontinued for Hepatitis C; Most Recent Events: 01 Oct 2014 Discontinued - Phase-I for Hepatitis C (In volunteers) in Germany (PO, tablet), 01 Oct 2014 Discontinued - Phase-II for Hepatitis C in France, Germany and Spain (PO, solution), 01 Apr 2006 Boehringer Ingelheim completes a phase II trial in Hepatitis C in France, Germany and Spain (NCT02254707)
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ACTIVE MOIETY |
VL decreased by > or =1 log10 IU/ml in 2/8, 2/8, 1/8, 2/7, 0/8, 2/8 and 4/5 patients on 60, 80, 100, 150, 200, 300 and 450 mg, respectively. No response was seen with placebo. HCV subtype 1b showed better response than 1a, the effect of other covariables including prior interferon treatment was not significant. NS5B population sequencing and phenotyping identified baseline samples with reduced BILB 1941 susceptibility, but did not detect an on-treatment emergence of resistant mutants. Plasma drug levels were linear until 300 mg. No serious adverse events (AEs) were reported. AEs were mainly gastrointestinal-related (most frequent diarrhoea) and frequency increased with dose. On 450 mg, all five active-treated patients discontinued (four for gastrointestinal intolerance and one for increased aspartate aminotransferase and alanine aminotransferase levels) and the trial was discontinued.
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