Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C33H38Cl3N3O4 |
| Molecular Weight | 647.032 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COCCC1=CC(CN(C2CC2)C(=O)[C@H]3CNCC[C@@H]3C4=CN=C(OCCOC5=C(Cl)C=C(C)C=C5Cl)C=C4)=C(Cl)C=C1
InChI
InChIKey=PGSRKJVMAOWDEC-SXOMAYOGSA-N
InChI=1S/C33H38Cl3N3O4/c1-21-15-29(35)32(30(36)16-21)43-14-13-42-31-8-4-23(18-38-31)26-9-11-37-19-27(26)33(40)39(25-5-6-25)20-24-17-22(10-12-41-2)3-7-28(24)34/h3-4,7-8,15-18,25-27,37H,5-6,9-14,19-20H2,1-2H3/t26-,27+/m1/s1
| Molecular Formula | C33H38Cl3N3O4 |
| Molecular Weight | 647.032 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 10:36:23 GMT 2023
by
admin
on
Sat Dec 16 10:36:23 GMT 2023
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| Record UNII |
TA1ATU85YC
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| Record Status |
Validated (UNII)
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| Record Version |
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SUB193110
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1007392-69-9
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TA1ATU85YC
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12001785
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
The median time to Cmax (tmax) for ACT-178882 was prolonged from 3.5 to 5.0 h by diltiazem whereas its apparent terminal half-life (t) was unaffected by diltiazem, 22.9 and 24.2 h for treatments A and B, respectively. Using treatment A as reference, the geometric mean ratio (90 % CI) was 1.62 (1.36-1.94) for Cmax and 2.02 (1.75-2.34) for AUC, indicating a significant interaction between ACT-178882 and diltiazem. One (7.1 %) and 3 (21.3 %) of 14 subjects reported an adverse event during treatment A and B, respectively, with headache being the most frequently reported, with three events.Concomitant administration of diltiazem doubled the exposure to ACT-178882 without affecting t1/2.
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ACTIVE MOIETY |
Dizziness and headache were the most frequently reported adverse events. No clinically relevant changes occurred for body weight, vital signs, clinical laboratory variables, and ECG although both enalapril and ACT-178882 tended to decrease systolic blood pressure. Following single doses of ACT-178882, t1/2 and tmax varied from 18.7 to 24.7 h and from 3 to 5 h, respectively, and food had no significant effect. Steady-state conditions were achieved after 4-6 days of dosing and accumulation was minimal. ACT-178882 pharmacokinetics were dose proportional.
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ACTIVE MOIETY |
Originator: Actelion Pharmaceuticals, Merck & Co; Developer: Actelion Pharmaceuticals; Class: Amide, Antihypertensive, Piperidine, Pyrimidine; Mechanism of Action: Renin inhibitor; Highest Development Phase: No development reported for Hypertension; Most Recent Events: 05 Feb 2013 Phase-I clinical trials in Hypertension in Switzerland (PO), 05 Feb 2013 Drug interactions & adverse events data from a phase I trial in Healthy volunteers released by Actelion Pharmaceuticals, 19 Jul 2012 ACT 178882 is available for licensing as of 19 Jul 2012. http://www.actelion.com/en/index.page
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