Delving into the Latest Updates on Laboratorios Salvat SA with Synapse

Overview

Tags

Eye Diseases

Skin and Musculoskeletal Diseases

Cardiovascular Diseases

Small molecule drug

Disease domain score

A glimpse into the focused therapeutic areas

Technology Platform

Most used technologies in drug development

Targets

Most frequently developed targets

Disease Domain	Count

Endocrinology and Metabolic Disease	2
Infectious Diseases	2

Top 5 Drug Type	Count

Small molecule drug	13

Top 5 Target	Count

Bacterial DNA gyrase x GR x Topoisomerase IV	1
fungal CYP51A1	1

Background and purpose: Highly selective M3 muscarinic receptor antagonists may represent a better treatment for overactive bladder syndrome, diminishing side effects. Cardiac side effects of non‐selective antimuscarinics have been associated with activity at M2 receptors as these receptors are mainly responsible for muscarinic receptor‐dependent bradycardia. We have investigated a novel antimuscarinic, SVT‐40776, highly selective for M3 over M2 receptors (Ki = 0.19 nmol·L−1 for M3 receptor affinity). This study reports the functional activity of SVT‐40776 in the bladder, relative to its activity in atria.Experimental approach: In vitro and ex vivo (oral dosing) inhibition of mouse detrusor and atrial contractile responses to carbachol were used to study the functional activity of SVT‐40776. The in vivo efficacy of SVT‐40776 was characterized by suppression of isovolumetric spontaneous bladder contractions in anaesthetized guinea pigs after intravenous administration.Key results: SVT‐40776 was the most potent in inhibiting carbachol‐induced bladder contractions of the anti‐cholinergic agents tested, without affecting atrial contractions over the same range of concentrations. SVT‐40776 exhibited the highest urinary versus cardiac selectivity (199‐fold). In the guinea pig in vivo model, SVT‐40776 inhibited 25% of spontaneous bladder contractions at a very low dose (6.97 µg·kg−1 i.v), without affecting arterial blood pressure.Conclusions and implications: SVT‐40776 is a potent inhibitor of M3 receptor‐related detrusor contractile activity. The absence of effects on isolated atria preparations represents an interesting characteristic and suggests that SVT‐40776 may lack unwanted cardiac effects; a feature especially relevant in a compound intended to treat mainly elderly patients.British Journal of Pharmacology (2009) doi:10.1111/j.1476‐5381.2008.00082.x

01 Apr 2007·Journal of Medicinal ChemistryQ1 · MEDICINE

Discovery of Diaryl Imidazolidin-2-one Derivatives, a Novel Class of Muscarinic M3 Selective Antagonists (Part 1)

Q1 · MEDICINE

Article

Author: Fernández, Andrés G. ; Radice, Luigi ; Raveglia, Luca F. ; Rizzi, Andrea ; Villetti, Gino ; Radaelli, Stefano ; Scarpitta, Francesca ; La Porta, Elena ; Civelli, Maurizio ; Guala, Matilde ; Scudellaro, Roberta ; Santoro, Enza ; Misiano, Paola ; Fossati, Claudia ; Dondio, Giulio M. ; Delcanale, Maurizio ; Salcedo, Carolina ; Amari, Gabriele ; Armani, Elisabetta ; Petrillo, Paola ; Peretto, Ilaria ; Imbimbo, Bruno P. ; Patacchini, Riccardo ; Giardina, Giuseppe A. M. ; Bigogno, Chiara ; Giardini, Alessandra ; Forlani, Roberto ; Bergamaschi, Marco

Pharmacophore-based structural identification, synthesis, and structure-activity relationships of a new class of muscarinic M3 receptor antagonists, the diaryl imidazolidin-2-one derivatives, are described. The versatility of the discovered scaffold allowed for several structural modifications that resulted in the discovery of two distinct classes of compounds, specifically a class of tertiary amine derivatives (potentially useful for the treatment of overactive bladder by oral administration) and a class of quaternary ammonium salt derivatives (potentially useful for the treatment of respiratory diseases by the inhalation route of administration). In this paper, we describe the synthesis and biological activity of tertiary amine derivatives. For these compounds, selectivity for the M3 receptor toward the M2 receptor was crucial, because the M2 receptor subtype is mainly responsible for adverse systemic side effects of currently marketed muscarinic antagonists. Compound 50 showed the highest selectivity versus M2 receptor, with binding affinity for M3 receptor Ki = 4.8 nM and for M2 receptor Ki = 1141 nM. Functional in vitro studies on selected compounds confirmed the antagonist activity toward the M3 receptor and functional selectivity toward the M2 receptor.

01 May 1999·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

In Vitro Susceptibilities of Clinical Yeast Isolates to the New Antifungal Eberconazole Compared with Their Susceptibilities to Clotrimazole and Ketoconazole

Q2 · MEDICINE

Article

Author: Torres-Rodríguez, Josep M. ; Mendez, Raúl ; Lagunas, Carme ; López-Jodra, Olga ; Jimenez, Teresa ; Espasa, Mateu ; Morera, Yolanda

ABSTRACT The antifungal activity of eberconazole, a new imidazole derivative, against 124 clinical isolates of Candida comprising eight different species and to 34 isolates of Cryptococcus neoformans was compared to those of clotrimazole and ketoconazole. MICs of eberconazole, determined by the National Committee for Clinical Laboratory Standards standardized microbroth method, were equal to or lower than those of other azoles, especially for Candida krusei and Candida glabrata , which are usually resistant to triazoles.

100 Deals associated with Laboratorios Salvat SA

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100 Translational Medicine associated with Laboratorios Salvat SA

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Pipeline

Pipeline Snapshot as of 05 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Preclinical

8

1

Phase 2 Clinical

NDA/BLA

2

Approved

Other

8

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Eberconazole Nitrate ( fungal CYP51A1 )	Tinea Pedis More	Approved
Ciprofloxacin Hydrochloride/Fluocinolone Acetonide ( Bacterial DNA gyrase x GR x Topoisomerase IV )	Otitis Media More	Approved
SVT-19971	Sepsis More	NDA/BLA
SVT-15652	Otitis Externa More	NDA/BLA
SVT-18651	Eczema More	Phase 2