Delving into the Latest Updates on Spirapril Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Cardiopril, Quadropril, Renpress

+ [9]

Target

ACE

Action

inhibitors

Mechanism

ACE inhibitors(Angiotensin-converting enzyme inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypertension

Inactive Indication-

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization

Novartis AG

Meda AB

Italfarmaco SpA

Inactive Organization

Schering Corp.

Drug Highest PhaseApproved

First Approval Date

Finland (22 Jul 1995),

Hypertension

Regulation-

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Structure/Sequence

Molecular FormulaC22H31ClN2O5S2

InChIKeyCLDOLNORSLLQDI-OOAIBONUSA-N

CAS Registry94841-17-5

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The MAPEC study was designed to investigate whether normalizing the circadian blood pressure profile towards a more dipper pattern (increasing the diurnal/nocturnal ratio of blood pressure) by the use of Chronotherapy (that is, taking into account the time of day of administration of antihypertensive medications) reduces cardiovascular risk.

Start Date01 Mar 2000

Sponsor / Collaborator

Universidade de Vigo

[+2]

100 Clinical Results associated with Spirapril Hydrochloride

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100 Translational Medicine associated with Spirapril Hydrochloride

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100 Patents (Medical) associated with Spirapril Hydrochloride

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215

Literatures (Medical) associated with Spirapril Hydrochloride

28 Nov 2024·Journal of Medicinal Chemistry

Proline Analogues in Drug Design: Current Trends and Future Prospects

Review

Author: Kubyshkin, Vladimir ; Mykhailiuk, Pavel K.

Proline analogues are versatile chemical building blocks that enable modular construction of small-molecule drugs and pharmaceutical peptides. Over the past 15 years, the FDA has approved over 15 drugs containing proline analogues in their structures, five in the last three years alone (daridorexant, trofinetide, nirmatrelvir, rezafungin, danicopan). This perspective offers an analysis of the most common types of proline analogues currently trending in drug design. We focus on examples of fluoroprolines, α-methylproline, bicyclic proline analogues, and aminoprolines, while also highlighting proline analogues that remain underrepresented. We supplement our analysis with physicochemical information regarding the specific molecular properties of these moieties. Additionally, we discuss several intriguing cases where nonproline residues were replaced with proline analogues as a strategy to eliminate unwanted hydrogen bond donor sites. In conclusion, we present some suggestions for the future exploration of this promising class of molecular entities in drug discovery.

01 Sep 2024·Hypertension Research

Risk of pneumonia-related hospitalization after initiating angiotensin-converting enzyme inhibitors compared with angiotensin II receptor blockers: a retrospective cohort study using LIFE Study data

Article

Author: Maeda, Megumi ; Fukuda, Haruhisa ; Murata, Fumiko ; Hieda, Michinari ; Uemura, Ryosuke

There is insufficient evidence that angiotensin-converting enzyme inhibitors (ACEIs) can reduce pneumonia by inducing a dry cough that confers a protective effect on the airway. To increase the evidence base on the clinical use of ACEIs for pneumonia prevention, this retrospective cohort study aimed to comparatively examine the risk of pneumonia-related hospitalization between ACEI initiators and angiotensin II receptor blocker (ARB) initiators using claims data from two Japanese municipalities. We identified persons who were newly prescribed any ACEI or ARB as their first antihypertensive agent between April 2016 and March 2020. The Fine-Gray method was applied to a Cox proportional hazards model to estimate the subdistribution hazard ratio (HR) of ACEI use (reference: ARB use) for pneumonia-related hospitalization, with death treated as a competing risk. Sex, age, comorbidities, medications, and pneumococcal immunization were included as covariates. The analysis was conducted on 1421 ACEI initiators and 9040 ARB initiators, and the adjusted subdistribution HR of ACEI use was estimated to be 1.21 (95% confidence interval: 0.89-1.65; P = 0.22). ACEI initiation did not demonstrate any significant preventive effect against pneumonia-related hospitalization relative to ARB initiation. There remains a lack of strong evidence on the protective effects of ACEIs, and further research is needed to ascertain the benefits of their use in preventing pneumonia. We conducted a large-scale retrospective cohort study using real-world healthcare data from a Japanese population. In this study, ACEI initiation did not indicate a significant preventive effect against pneumonia-related hospitalization.

01 Aug 2024·Data in Brief

Dataset for discovering new hypertension small molecules using machine learning-aided computational fragment-based design

Article

Author: Chude-Okonkwo, Uche A. K. ; Lehasa, Odifentse Mapula-e

This dataset demonstrates the use of computational fragmentation-based and machine learning-aided drug discovery to generate new lead molecules for the treatment of hypertension. Specifically, the focus is on agents targeting the renin-angiotensin-aldosterone system (RAAS), commonly classified as Angiotensin-Converting Enzyme Inhibitors (ACEIs) and Angiotensin II Receptor Blockers (ARBs). The preliminary dataset was a target-specific, user-generated fragment library of 63 molecular fragments of the 26 approved ACEI and ARB molecules obtained from the ChEMBL and DrugBank molecular databases. This fragment library provided the primary input dataset to generate the new lead molecules presented in the dataset. The newly generated molecules were screened to check whether they met the criteria for oral drugs and comprised the ACEI or ARB core functional group criterion. Using unsupervised machine learning, the molecules that met the criterion were divided into clusters of drug classes based on their functional group allocation. This process led to three final output datasets, one containing the new ACEI molecules, another for the new ARB molecules, and the last for the new unassigned class molecules. This data can aid in the timely and efficient design of novel antihypertensive drugs. It can also be used in precision hypertension medicine for patients with treatment resistance, non-response or co-morbidities. Although this dataset is specific to antihypertensive agents, the model can be reused with minimal changes to produce new lead molecules for other health conditions.

100 Deals associated with Spirapril Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
D03765	Spirapril Hydrochloride	C09AA11	DB01348

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Hypertension	Finland	-	22 Jul 1995

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ESH1989	Not Applicable	-	-	Spirapril 12.5 mg	(yzhzggzquu) = jfbaembvaf yixjjtcggt (wgxtszgdyi, ± 2)	-	18 Mar 1989
				Spirapril 25 mg	(yzhzggzquu) = rljyzzfkkl yixjjtcggt (wgxtszgdyi, ± 1)