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Name: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride, is researched, Molecular C20H28ClN3O6, CAS is 89396-94-1, about Imidapril: a review of its use in essential hypertension, type 1 diabetic nephropathy and chronic heart failure. Author is Robinson, Dean M.; Curran, Monique P.; Lyseng-Williamson, Katherine A..

A review. Imidapril (Tanatril), through its active metabolite imidaprilat, acts as an ACE inhibitor to suppress the conversion of angiotensin I to angiotensin II and thereby reduce total peripheral resistance and systemic blood pressure (BP). In clin. trials, oral imidapril was an effective antihypertensive agent in the treatment of mild to moderate essential hypertension. Some evidence suggests that imidapril also improves exercise capacity in patients with chronic heart failure (CHF) and reduces urinary albumin excretion rate in patients with type 1 diabetes mellitus. Imidapril was well tolerated, with a lower incidence of dry cough than enalapril or benazepril, and is a first choice ACE inhibitor for the treatment of mild to moderate essential hypertension. Pharmacol. Properties The active metabolite of imidapril is imidaprilat, which inhibits the conversion of angiotensin I to angiotensin II. Lowering of plasma and tissue angiotensin II levels results in peripheral vasodilation, reduced systemic BP, renoprotective effects in patients with type 1 diabetes, and decreased renal sodium and water retention. After multidose oral administration in patients with hypertension, steady-state maximum plasma concentrations of imidapril (≈30 ng/mL) and imidaprilat (≈20 ng/mL) are achieved in a median time of 2 and 5 h. In healthy men 25.5% of a single dose of imidapril 10mg was excreted in the urine within 24 h. Elimination occurs primarily through excretion in the urine (≈40%) and feces (≈50%); after oral administration in healthy volunteers, the terminal elimination half-life of imidaprilat is ≈24 h. Therapeutic Efficacy In randomized controlled trials, oral imidapril was effective in the treatment of adults with mild to moderate essential hypertension. In short-term (2- and 4-wk) dose-finding trials, imidapril dosages of 10-40 mg/day were significantly more effective than placebo, inducing 11-15mm Hg reductions in sitting diastolic BP (sDBP; primary endpoint). In comparative 12- and 24-wk trials, imidapril 5-20 mg/day induced reductions in mean sDBP of 10-15mm Hg that did not differ significantly from those induced by hydrochlorothiazide 12.5-50 mg/day or captopril 50-100 mg/day (primary endpoint), nor those induced by enalapril 5-10 mg/day or nifedipine sustained release (SR) 40-80 mg/day (secondary endpoint). In addition, reductions in sDBP and sitting systolic BP (co-primary endpoints) with imidapril did not differ from those induced by candesartan 4-16 mg/day. Favorable reductions in sDBP were maintained during 6-mo and 52-wk noncomparative trials. In patients with type 1 diabetes, the urinary albumin excretion rate (a marker of nephropathy) increased by 72% in placebo recipients, but declined by 41% in imidapril 5 mg/day and by 6% in captopril 37.5 mg/day recipients during a mean treatment period of 1.5 years. In patients with CHF, mean total exercise time increased from baseline in imidapril 2.5-10 mg/day recipients in a dose-related manner after 12-wk of treatment; a 9.7% increase with imidapril 10 mg/day was significantly greater than the change with placebo (+0.7%). Tolerability Overall, imidapril was relatively well tolerated, with an incidence of adverse events in pooled analyses of data from clin. trials and post-marketing surveillance (n = 6632) of 6.6%. The most commonly reported adverse events were cough, hypotension, dizziness and pharyngeal discomfort. During 2- and 4-wk trials, the overall incidence of adverse events was 26% and 40% in recipients of imidapril 2.5-40 mg/day compared with 35% and 37% in placebo recipients. In comparative trials, the incidence of treatment-related adverse events in imidapril vs. enalapril recipients in two 12-wk trials were 5.6% vs. 12.2% and 12.0% vs. 14.1%; in other 12-wk trials treatment-related adverse events were observed in 24.2% of imidapril vs. 41.7% of nifedipine SR, and 20.7% of imidapril vs. 46.4% of captopril recipients, while the overall incidence of adverse events in imidapril vs. candesartan recipients was 11.7% vs. 16.1%. The incidences of adverse events in a 24-wk trial were 46.0% with imidapril and 52.8% with hydrochlorothiazide. In longer-term trials, adverse events were reported by 61.6% of imidapril recipients in the 52-wk trial; however, only 1.7% of imidapril recipients in a 6-mo field trial experienced adverse events considered related to ACE inhibitor treatment. In prospective investigations in hypertensive patients, switching to imidapril did not reduce the incidence of cough (a class effect of ACE inhibitors) in a small open-label trial in hypertensive patients already experiencing ACE-inhibitor induced cough; however, in a large crossover trial, the incidence of cough with imidapril (15.2%) was less than half that with enalapril (38.6%). In addition, cough disappeared in 52.9% of enalapril recipients switched to imidapril, and in patients without cough during imidapril treatment, switching to enalapril induced cough in 20.9%. In contrast, in patients without cough during initial enalapril treatment, only 0.9% developed cough during subsequent imidapril treatment. In a second large, double-blind crossover trial, the incidence of cough was significantly lower in imidapril than benazepril recipients.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride( cas:89396-94-1 ) is researched.Recommanded Product: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride.Saruta, Takao; Omae, Teruo; Kuramochi, Morio; Iimura, Osamu; Yoshinaga, Kaoru; Abe, Keishi; Ishii, Masao; Watanabe, Tsutomu; Takeda, Tadanao published the article 《Imidapril hydrochloride in essential hypertension: A double-blind comparative study using enalapril maleate as a control》 about this compound( cas:89396-94-1 ) in Journal of Hypertension. Keywords: imidapril hydrochloride enalapril maleate antihypertensive. Let’s learn more about this compound (cas:89396-94-1).

The objective was to assess the value of using imidapril hydrochloride (ACE/TA-6366), a long-acting angiotensin converting enzyme (ACE) inhibitor developed in Japan, to treat patients with essential hypertension. A double-blind, comparative, phase III study was carried out using enalapril maleate as a control, with a 4-wk observation period and a 12-wk treatment period. Both drugs were started at a dose of 5 mg once a day, increasing to 10 mg in patients whose antihypertensive response was insufficient after 4 wk. The study included 231 outpatients aged 30-74 yr; of these, 108 in the imidapril group and 115 in the enalapril group were assessed. There were no differences in background factors between groups. An adequate antihypertensive effect was observed in 71.3% (77/108) in the imidapril group and in 66.1% (76/115) in the enalapril group, with no significant difference between groups. The pulse rate was unchanged in both groups. The drug had no adverse effects in 86.1% (93/108) of the imidapril group and 79.1% (91/115) of the enalapril group, with no significant difference between groups. Adverse drug effects were observed in 5.6% (6/108) of the imidapril group and 12.2% (14/115) of the enalapril group. Cough was the most frequent side effect, reported in 0.9% (1/108) of the imidapril group and 7.0% (8/115) of the enalapril group. Other side effects were reported in 4.6% (5/108) of the imidapril group and 5.2% (6/115) of the enalapril group. Abnormal laboratory values were observed in 3.7% (4/108) of the imidapril group and 0.9% (1/115) of the enalapril group. Imidapril showed excellent clin. efficacy and safety compared to enalapril. The low incidence of cough is of particular interest.

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Copper catalysis in organic synthesis – NCBI,
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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Analysis of Risk Factors in Human Bioequivalence Study That Incur Bioinequivalence of Oral Drug Products, published in 2009-02-28, which mentions a compound: 89396-94-1, Name is (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride, Molecular C20H28ClN3O6, Application of 89396-94-1.

In the study of human bioequivalence (BE), newly developed oral products sometimes fail to prove BE with a reference product due to the high variability in pharmacokinetic (PK) parameters after oral absorption. In this study, risk factors that incur bioinequivalence in BE study were analyzed by applying the Biopharmaceutics Classification System (BCS). Forty-four generic products were selected from a database of BE studies in the past 10 years at Towa Pharmaceutical Co., Ltd. (Osaka, Japan), and 90% confidence interval (CI) of AUC and Cmax in human BE study for all products were converted into coefficient of variation (CV90). Then, the required number of subjects to confirm BE was estimated from the 90% CI in human BE study of new products. It was found that both the permeability of drugs to human intestinal membrane (Peff) and the dose number calculated from their water solubility did not correlate well to CV90 and the estimated subject number in human BE study, suggesting the contribution of other factors to cause the variability in oral drug absorption. As the PK parameter of drugs, the value of AUC/dose was calculated and plotted against CV90 and the estimated subject number by classifying drugs into 4 BCS classes. For drugs in classes 1 and 3, AUC/dose gave a clear criterion to distinguish the drugs with a high risk of bioinequivalence, where drugs with low AUC/dose showed high CV90 and large number of subjects. It was suggested that the high metabolic clearance (for class 1 drug) and low oral absorption (for class 3 drug) could be significant factors to incur bioinequivalence in human BE study, although for drugs in classes 2 and 4, clear factors were not defined. Consequently, for drugs in BCS classes 1 and 3, risks in human BE study to incur bioinequivalence could be predicted by calculating the AUC/dose. In the case of generic drugs, since the parameter of AUC/dose is available before initiating human BE study, this finding is expected to promote an efficient and cost-saving strategy for the development of oral drug products.

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Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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From this literature《Pharmacological studies on TA-6366, a new ACE inhibitor: II. Effect of long-term administration from the pre-hypertensive stage on blood pressure, relative heart weight and ACE activity of various tissues in spontaneously hypertensive rats (SHRs)》,we know some information about this compound(89396-94-1)HPLC of Formula: 89396-94-1, but this is not all information, there are many literatures related to this compound(89396-94-1).

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 89396-94-1, is researched, Molecular C20H28ClN3O6, about Pharmacological studies on TA-6366, a new ACE inhibitor: II. Effect of long-term administration from the pre-hypertensive stage on blood pressure, relative heart weight and ACE activity of various tissues in spontaneously hypertensive rats (SHRs), the main research direction is TA6366 blood pressure heart ACE pharmacol.HPLC of Formula: 89396-94-1.

The long-term oral administration of TA-6366 (I) (5 mg/kg/day) from 4-wk old impeded the genetic hypertension development with only a slight decrease in heart rate in spontaneously hypertensive rats (SHRs). However, the lower dose (1 mg/kg/day) of TA-6366 did not affect the development, but it lowered blood pressure after the development was almost accomplished. Concomitantly, relative heart weights in both the groups were markedly decreased to almost the same degree. The reduction of ACE activity in the aorta, brain and lung of both groups was found at 24 h after the final administration, particularly at the 5 mg/kg/day dose; and that of the aorta was kept at almost the same low level even on the 9th day of withdrawal. After withdrawal of TA-6366 (5 mg/kg/day), the decrease in blood pressure was sustained at least for 10 wk. The beneficial effect of TA-6366 on the hypertension development in SHRs seems to be related to its strong and long-lasting ACE inhibition, especially in the vasculature.

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From this literature《UV derivative spectrophotometric and RP-HPLC methods for determination of imidapril hydrochloride in tablets and for its stability assessment in solid state》,we know some information about this compound(89396-94-1)COA of Formula: C20H28ClN3O6, but this is not all information, there are many literatures related to this compound(89396-94-1).

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Stanisz, Beata; Regulska, Katarzyna; Kolasa, Kinga researched the compound: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride( cas:89396-94-1 ).COA of Formula: C20H28ClN3O6.They published the article 《UV derivative spectrophotometric and RP-HPLC methods for determination of imidapril hydrochloride in tablets and for its stability assessment in solid state》 about this compound( cas:89396-94-1 ) in Acta Poloniae Pharmaceutica. Keywords: imidapril stability spectroscopy HPLC quality control. We’ll tell you more about this compound (cas:89396-94-1).

Two methods for determination of imidapril hydrochloride (IMD) in the form of tablets were developed and the stability-indicative determination of IMD in solid state formulations by means of the proposed methods was investigated. IMD is not a pharmacopeial raw material, therefore there is no official method for its determination and purity assessment. The following anal. techniques were adopted for IMD determination: reverse-phase high performance liquid chromatog. (RP-HPLC) and first derivative (1D) UV spectrophotometry. RP-HPLC anal. was performed with the use of LiChrosfer RP-18 column as a stationary phase and acetonitrile-methanol-phosphate buffer pH 2.0 (60:10:30 volume/volume/v) as a mobile phase. The proposed method showed good linearity (in a range 40.0 – 400.0 μg/mL), accuracy, precision and selectivity for: IMD, its degradation product, and for oxymetazoline as an internal standard (IS). Addnl., different spectrophotometric methods were tested, and the first derivative spectrophotometry was accepted for further research. This method showed good linearity (in a range 4.0 – 40.0 μg/mL), precision and accuracy. The proposed methods were successfully applied to the pharmaceutical dosage form containing the investigated compound without any interference from the excipients. Finally, the results of the suggested methods were statistically compared using t-Student and F-Snedecor tests in the assessment for their equivalence.

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Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

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From this literature《Effects of long-term administration of (4S)-1-methyl-3-{(2S)-2-[N-((1S)-1-ethoxycarbonyl-3-phenylpropyl)amino]propionyl}-2-oxoimidazolidine-4-carboxylic acid hydrochloride (TA-6366), a new angiotensin I converting enzyme (ACE) inhibitor, from the pre-hypertensive stage on morphological change and mechanical property related to sodium ion permeability in aorta of spontaneously hypertensive rats (SHRs)》,we know some information about this compound(89396-94-1)Electric Literature of C20H28ClN3O6, but this is not all information, there are many literatures related to this compound(89396-94-1).

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride, is researched, Molecular C20H28ClN3O6, CAS is 89396-94-1, about Effects of long-term administration of (4S)-1-methyl-3-{(2S)-2-[N-((1S)-1-ethoxycarbonyl-3-phenylpropyl)amino]propionyl}-2-oxoimidazolidine-4-carboxylic acid hydrochloride (TA-6366), a new angiotensin I converting enzyme (ACE) inhibitor, from the pre-hypertensive stage on morphological change and mechanical property related to sodium ion permeability in aorta of spontaneously hypertensive rats (SHRs).Electric Literature of C20H28ClN3O6.

Effects of TA-6366 (I) on morphol. change and mech. property related to sodium ion permeability in the aorta of spontaneously hypertensive rats (SHRs) were examined, as compared with those of enalapril and captopril. Ten-week oral administration of I (1 and 5 mg/kg/d) from 4 wk of age impeded aortic media-thickening together with a rise in blood pressure in SHRs. Concomitantly, aorta weights in both groups were markedly decreased. The higher dose of I almost fully suppressed the accelerated tension development induced by K+-free medium and decreased total sodium ion content in the aorta. These vascular effects of I were more prominent than those of enalapril and captopril at 5 mg/kg/d. The difference in potencies on the above vascular parameters between I and these drugs seemed to be mainly related to the difference in their antihypertensive activities. These results suggest that I has preventive effects against progression of vascular diseases, particularly atherosclerosis, accompanied with hypertension.

From this literature《Effects of long-term administration of (4S)-1-methyl-3-{(2S)-2-[N-((1S)-1-ethoxycarbonyl-3-phenylpropyl)amino]propionyl}-2-oxoimidazolidine-4-carboxylic acid hydrochloride (TA-6366), a new angiotensin I converting enzyme (ACE) inhibitor, from the pre-hypertensive stage on morphological change and mechanical property related to sodium ion permeability in aorta of spontaneously hypertensive rats (SHRs)》,we know some information about this compound(89396-94-1)Electric Literature of C20H28ClN3O6, but this is not all information, there are many literatures related to this compound(89396-94-1).

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In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Effects of angiotensin-converting enzyme inhibitors on the treatment of anemia with erythropoietin, published in 2001-11-30, which mentions a compound: 89396-94-1, Name is (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride, Molecular C20H28ClN3O6, Recommanded Product: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride.

The hypothesis that angiotensin-converting enzyme (ACE) inhibitors interfere with the treatment of anemia with recombinant human erythropoietin (rHuEPO) remains controversial. To test this hypothesis, a retrospective anal. was conducted in a large group of hemodialysis patients with renal anemia. The effects of ACE inhibitors in these patients were evaluated by measuring the weekly increment in hematocrit (ΔHct) values within 12 wk of the initiation of rHuEPO treatment. Results from 2213 rHuEPO naive patients were compared between patients receiving rHuEPO alone and patients receiving both rHuEPO and ACE inhibitors. Because of the demog. differences between the two groups, a propensity score was used to eliminate the influence of confounding factors and to match the patient population in these two patient groups. Multiple regression anal. also was performed. When the ΔHct values were compared directly between the two groups or were assessed by multiple regression anal., no effect of ACE inhibitors was observed (P = 0.941 and P = 0.308, resp.). When the effects of ACE inhibitors on the treatment of anemia with rHuEPO were analyzed in 329 patients extracted from each group by their propensity score, ΔHct did not differ between the two groups (P = 0.355). These results suggest that ACE inhibitors have no effect on the rHuEPO treatment for anemia in hemodialysis patients who were treated with a relatively low dose of ACE inhibitors and low-dose rHuEPO.

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Copper catalysis in organic synthesis – NCBI,
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Abdulla, Shabaan A.; Frag, Eman Y.; Ahmed, Heba E. published an article about the compound: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride( cas:89396-94-1,SMILESS:O=C([C@H](CN1C)N(C([C@@H](N[C@@H](CCC2=CC=CC=C2)C(OCC)=O)C)=O)C1=O)O.[H]Cl ).Product Details of 89396-94-1. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:89396-94-1) through the article.

An aqueous alk. degradation study was performed for imidapril hydrochloride (IMD) drug in the presence of its degradation products and an isocratic stability indicating method was presented using a HPLC technique. The separations were performed using an ACE Generix 5C8, 150 × 4.6 mm column and a mobile phase consisting of buffer solution (0.1 M potassium dihydrogen phosphate and 0.02 M tetra-N-Bu ammonium hydrogen sulfate of pH = 4.5 with 1 N HCl) and acetonitrile 60 : 40 (volume/volume). The wavelength of the detector was adjusted at 210 nm. The method showed high sensitivity concerning accuracy, precision, linearity and specificity within the acceptable range from 0.1 to 100 μg mL-1 and the limit of quantification was found to be 0.0211 μg mL-1 for IMD. The proposed method was used to determine the drug in its pharmaceutical formulation and to investigate the degradation kinetics of the drug’s alk.-stressed sample. The reactions were found to follow a first-order reaction. The activation energy could also be estimated The optimized stability indicating HPLC method was validated according to ICH guidelines.

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From this literature《LC-MS determination and bioavailability study of imidapril hydrochloride after the oral administration of imidapril tablets in human volunteers》,we know some information about this compound(89396-94-1)Related Products of 89396-94-1, but this is not all information, there are many literatures related to this compound(89396-94-1).

Yun, Ji Hye; Myung, Ja Hye; Kim, Hye Jin; Lee, Sibeum; Park, Jong-Sei; Kim, Won; Lee, Eun-Hee; Moon, Cheol Jin; Hwang, Sung-Joo published an article about the compound: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride( cas:89396-94-1,SMILESS:O=C([C@H](CN1C)N(C([C@@H](N[C@@H](CCC2=CC=CC=C2)C(OCC)=O)C)=O)C1=O)O.[H]Cl ).Related Products of 89396-94-1. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:89396-94-1) through the article.

The purpose of the present study was to develop a standard protocol for imidapril hydrochloride bioequivalence testing. For this reason, a specific LC-MS method was developed and validated for the determination of imidapril in human plasma. A solid-phase extraction cartridge, Sep-pak C18, was used to extract imidapril and ramipril (an internal standard) from deproteinized plasma. The compounds were separated using a XTerra MS C18 column (3.5 μm, 2.1×150 mm) and acetonitrile-0.1% formic acid (67:33, volume/volume) adjusted to pH 2.4 by 2 mmol/L ammonium formic acid, as mobile phase at 0.3 mL/min. Imidapril was detected as m/z 406 at a retention time of ca. 2.3 min, and ramipril as m/z 417 at ca. 3.6 min. The described method showed acceptable specificity, linearity from 0.5 to 100 ng/mL, precision (expressed as a relative standard deviation of less than 15%), accuracy, and stability. The plasma concentration-vs.-time curves of 8 healthy male volunteers administered a single dose of imidapril (10 mg), gave an AUC12hr of imidapril of 121.48±35.81 ng mL-1 h, and Cmax and Tmax values of 32.59±9.76 ng/mL and 1.75±0.27 h. The developed method should be useful for the determination of imidapril in plasma with sufficient sensitivity and specificity in bioequivalence study.

From this literature《LC-MS determination and bioavailability study of imidapril hydrochloride after the oral administration of imidapril tablets in human volunteers》,we know some information about this compound(89396-94-1)Related Products of 89396-94-1, but this is not all information, there are many literatures related to this compound(89396-94-1).

Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”

 

Extracurricular laboratory: Synthetic route of 89396-94-1

From this literature《Transverse comparison of mannitol content in marketed drug products: Implication for no-effect dose of sugar alcohols on oral drug absorption》,we know some information about this compound(89396-94-1)Synthetic Route of C20H28ClN3O6, but this is not all information, there are many literatures related to this compound(89396-94-1).

Matsui, Kazuki; Takeuchi, Susumu; Haruna, Yuka; Yamane, Miki; Shimizu, Takahiro; Hatsuma, Yoshiki; Shimono, Norihito; Sunada, Machiko; Hayakawa, Masakane; Nishida, Tomo; Ito, Shusei; Ide, Masashi; Seino, Maki; Sugihara, Masahisa; Minagawa, Yasushi; Tachiki, Hidehisa published the article 《Transverse comparison of mannitol content in marketed drug products: Implication for no-effect dose of sugar alcohols on oral drug absorption》. Keywords: mannitol content products oral drug delivery system absorption.They researched the compound: (S)-3-((S)-2-(((S)-1-Ethoxy-1-oxo-4-phenylbutan-2-yl)amino)propanoyl)-1-methyl-2-oxoimidazolidine-4-carboxylic acid hydrochloride( cas:89396-94-1 ).Synthetic Route of C20H28ClN3O6. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:89396-94-1) here.

Some of pharmaceutical excipients are known to affect oral drug absorption via various mechanisms. Among diverse excipients, sugar alcs. (e.g. mannitol and sorbitol) are regarded as critical excipients that significantly alter drug absorption by osmotic effect. This recognition is based on the previous findings that several grams of sugar alcs. exhibited clear impact on the bioavailability/bioequivalence of certain drugs. However, commonly administered oral drug products contain less amount of sugar alc., thus, such a significant impact on drug absorption is questionable. The purpose of this research was to retrospectively estimate the no-effect dose of mannitol that may not affect oral absorption of BCS class I and III drugs. Mannitol content in marketed oral drug products (16 active pharmaceutical ingredients, 132 drug products) was quantified by means of reverse engineering or questionnaire survey to 11 generic drug manufacturers headquartered in Japan. The transverse comparison suggested that “”practical”” amount of mannitol may not have significant impact on oral absorption of investigated mols. This implication can be utilized to determine a no-effect threshold of sugar alc. in the context of BCS-based biowaiver guideline as well as other guidelines such as formulation change and pharmaceutical line extension.

From this literature《Transverse comparison of mannitol content in marketed drug products: Implication for no-effect dose of sugar alcohols on oral drug absorption》,we know some information about this compound(89396-94-1)Synthetic Route of C20H28ClN3O6, but this is not all information, there are many literatures related to this compound(89396-94-1).

Reference:
Copper catalysis in organic synthesis – NCBI,
Special Issue “Fundamentals and Applications of Copper-Based Catalysts”