Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C20H18N6O3S2 |
| Molecular Weight | 454.525 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=NC=CC=C1OC2=CC(SC3=NC=CC=C3)=CN=C2NC4=NC(=NS4)[C@H](O)CO
InChI
InChIKey=PCOMIRCNMMNOAP-CQSZACIVSA-N
InChI=1S/C20H18N6O3S2/c1-12-15(5-4-8-21-12)29-16-9-13(30-17-6-2-3-7-22-17)10-23-19(16)25-20-24-18(26-31-20)14(28)11-27/h2-10,14,27-28H,11H2,1H3,(H,23,24,25,26)/t14-/m1/s1
| Molecular Formula | C20H18N6O3S2 |
| Molecular Weight | 454.525 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:06:02 UTC 2023
by
admin
on
Sat Dec 16 09:06:02 UTC 2023
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| Record UNII |
P8B61X2X2D
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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| Code System | Code | Type | Description | ||
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P8B61X2X2D
Created by
admin on Sat Dec 16 09:06:02 UTC 2023 , Edited by admin on Sat Dec 16 09:06:02 UTC 2023
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25235269
Created by
admin on Sat Dec 16 09:06:02 UTC 2023 , Edited by admin on Sat Dec 16 09:06:02 UTC 2023
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AMG-151 FREE BASE
Created by
admin on Sat Dec 16 09:06:02 UTC 2023 , Edited by admin on Sat Dec 16 09:06:02 UTC 2023
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PRIMARY | Official Title: A Phase 1, Double-blind, Randomized, 2-Way Crossover, Placebo-controlled Study to Investigate the Effect of AMG 151 on 24-hour Ambulatory Blood Pressure and Glucose Levels in Subjects With Type 2 Diabetes Mellitus.Purpose: This is a phase 1, randomized, double-blind, placebo-controlled, 2-way crossover study to evaluate the effect of AMG 151 on 24-hour ambulatory blood pressure and glucose levels in subjects with type 2 diabetes mellitus who are on a stable regimen of metformin alone, metformin and a dipeptidyl peptidase-4 inhibitor (DPP4), metformin and a thiazolidinedione (TZD), or metformin, a DPP4, and a TZD for a minimum of 3 months prior to randomization. | ||
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1138669-65-4
Created by
admin on Sat Dec 16 09:06:02 UTC 2023 , Edited by admin on Sat Dec 16 09:06:02 UTC 2023
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1304015-76-6
Created by
admin on Sat Dec 16 09:06:02 UTC 2023 , Edited by admin on Sat Dec 16 09:06:02 UTC 2023
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NO STRUCTURE GIVEN | |||
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300000042394
Created by
admin on Sat Dec 16 09:06:02 UTC 2023 , Edited by admin on Sat Dec 16 09:06:02 UTC 2023
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| Related Record | Type | Details | ||
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TARGET -> ACTIVATOR |
ALLOSTERIC INHIBITOR
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Originator: Array BioPharma; Class: Antihyperglycaemic, Small molecule; Mechanism of Action: Glucokinase stimulant; Highest Development Phase: Discontinued for Type 2 diabetes mellitus; Most Recent Events: 07 Aug 2013 ARRY 403 is no longer licensed to Amgen worldwide, 19 Apr 2013 Amgen terminates phase I trial in Type-2 diabetes mellitus in USA (NCT01755442), 01 Nov 2012 Amgen initiates enrolment in a phase I trial for Type-2 diabetes mellitus in USA (NCT01755442)
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ACTIVE MOIETY |
Patients received oral AMG 151 at 50, 100 or 200mg twice daily, AMG 151 at 100, 200 or 400mg once daily or matching placebo for 28 days. A significant linear dose-effect trend was observed with the twice-daily regimen (p=0.004) for change in FPG to day 28. No trend was observed with the once-daily regimen. A higher incidence of hypoglycaemia and hypertriglyceridaemia was observed with AMG 151 administration. AMG 151 significantly reduced FPG when administered twice daily but not when administered once daily in patients with type 2 diabetes treated with metformin.
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