Design and baseline characteristics of the finerenone in reducing cardiovascular mortality and morbidity in diabetic kidney disease trial

Background: Among people with diabetes, those with kidney disease have exceptionally high rates of cardiovascular (CV) morbidity and mortality and progression of their underlying kidney disease. Finerenone is a novel, nonsteroidal, selective mineralocorticoid receptor antagonist that has shown to reduce albuminuria in type 2 diabetes (T2D) patients with chronic kidney disease (CKD) while revealing only a low risk of hyperkalemia. However, the effect of finerenone on CV and renal outcomes has not yet been investigated in long-term trials. Patients and Methods: The Finerenone in Reducing CV Mortality and Morbidity in Diabetic Kidney Disease (FIGARO-DKD) trial aims to assess the efficacy and safety of finerenone compared to placebo at reducing clinically important CV and renal outcomes in T2D patients with CKD. FIGARO-DKD is a randomized, double-blind, placebo-controlled, parallel-group, event-driven trial running in 47 countries with an expected duration of approximately 6 years. FIGARO-DKD randomized 7,437 patients with an estimated glomerular filtration rate >= 25 mL/min/1.73 m(2) and albuminuria (urinary albumin-to-creatinine ratio >= 30 to <= 5,000 mg/g). The study has at least 90% power to detect a 20% reduction in the risk of the primary outcome (overall two-sided significance level alpha = 0.05), the composite of time to first occurrence of CV death, nonfatal myocardial infarction, nonfatal stroke, or hospitalization for heart failure. Conclusions: FIGARO-DKD will determine whether an optimally treated cohort of T2D patients with CKD at high risk of CV and renal events will experience cardiorenal benefits with the addition of finerenone to their treatment regimen. Trial Registration: EudraCT number: 2015-000950-39; ClinicalTrials.gov identifier: NCT02545049

4b,5,6,9-Tetrahydro-7<i>H</i>-dibenzo[<i>c</i>,<i>e</i>]pyrrolo[1,2-<i>a</i>]azepin-7-one

A simple approach to synthesize 4b,5,6,9-tetrahydro-7H-dibenzo[c,e]pyrrolo[1,2-a]azepin- 7-one has been developed, based on a three-step transformation of 2-(2-bromophenyl)cyclopropane-1,1-diester. The key stage in this method is an intramolecular cross-coupling of 1-(2-bromobenzyl)-5-(2-bromophenyl)pyrrolidin-2-one under continuous flow conditions in an H-Сube-Pro using commercially available supported Pd catalysts

Synthesis of Imidazo[2,1‑<i>b</i>]thiazoles via Copper-Catalyzed A³‑Coupling in Batch and Continuous Flow

A straightforward method for the synthesis of functionalized imidazo­[2,1-<i>b</i>]­thiazoles starting from benzaldehydes, 2-aminothiazoles, and alkynes under copper­(I,II) catalysis was developed. The protocol allows the construction of a variety of aryl-substituted imidazo­[2,1-<i>b</i>]­benzothiazoles, -[2,1-<i>b</i>]­thiazoles, and -[2,1-<i>b</i>]­[1,3,4]­thiadiazoles. The reactions were easy to perform affording most of the desired products in 33–93% yields. The intensification of the process in a continuous-flow reactor increases the products’ yields up to quantitative

Synthesis of Imidazo[2,1‑<i>b</i>]thiazoles via Copper-Catalyzed A³‑Coupling in Batch and Continuous Flow

A straightforward method for the synthesis of functionalized imidazo­[2,1-<i>b</i>]­thiazoles starting from benzaldehydes, 2-aminothiazoles, and alkynes under copper­(I,II) catalysis was developed. The protocol allows the construction of a variety of aryl-substituted imidazo­[2,1-<i>b</i>]­benzothiazoles, -[2,1-<i>b</i>]­thiazoles, and -[2,1-<i>b</i>]­[1,3,4]­thiadiazoles. The reactions were easy to perform affording most of the desired products in 33–93% yields. The intensification of the process in a continuous-flow reactor increases the products’ yields up to quantitative