Comparison of two levonorgestrel-releasing intrauterine systems for the treatment of heavy menstrual bleeding: a randomised, controlled, phase 3 trial.

Purpose: To evaluate the levonorgestrel-releasing intrauterine system Donasert (also known as Levosert) compared with the reference product Mirena for the alleviation of heavy menstrual bleeding (HMB).

Materials And Methods: A phase 3 multicentre, non-inferiority, active-controlled study in non-menopausal women with HMB (menstrual blood loss [MBL] ≥ 80 mL) as the primary symptom randomised to either Donasert or Mirena and followed for 6 months. MBL was evaluated using a validated, modified version of the Wyatt pictogram.

Radiation exposure does not significantly contribute to the risk of recurrence of Chernobyl thyroid cancer.

Context: Papillary thyroid carcinoma (PTC) in patients exposed to environmental radioiodine after the Chernobyl accident is thought to have a relatively aggressive clinical course. Long-term results of treatment are not well known, especially in comparison with sporadic PTC.

Objective: The determination of risk factors for PTC recurrence in a controlled for baseline factors group of patients with radiation-related and sporadic PTC.

Nonsurgical management of thyroid abscess with sonographically guided fine needle aspiration.

Treatment of thyroid abscess commonly includes the surgical drainage along with systemic antibiotic therapy. Alternatives for open surgical intervention may be the conservative management with use needle aspiration or catheter drainage. We report here two cases of thyroid abscess treatment with 21-gauge needle aspiration under ultrasound guidance.

Synthesis of heterocyclic compounds possessing the 4H-thieno[3,2-b]pyrrole moiety.

A series of novel heterocyclic combinatorial libraries containing 4H-thieno[3,2-b]pyrrole, thieno[2',3':4,5]-pyrrol[1,2-d][1,2,4]triazine and thieno[2',3':4,5]pyrrolo[1,2-a]pyrazine heterocyclic moieties were obtained by parallel solution-phase synthesis. Key steps include different reactions of initial alkyl 4H-thieno[3,2-b]-pyrrole-5-carboxylates, such as alkylation with alkylating agents; transformation of the carboxylate group into different reactive functionalities, followed by reactions with electrophilic species; intramolecular cyclizations; and amide bond formation. Simple manual techniques for parallel reactions were coupled with easy purification procedures to give high-purity final products.

Liquid-phase parallel synthesis of combinatorial libraries of substituted 6-carbamoyl-3,4-dihydro-2H-benzo[1,4]thiazines.

In this work, we explored several original combinatorial derivatization patterns for the 3,4-dihydro-2H-1,4-benzothiazine scaffold. The synthesis begins with commercially available 4-chloro- and 4-fluoro-3-nitrobenzoates and employs a sequence of moderate and high-yielding reactions that display a relatively high substituent tolerance. Simple manual techniques for parallel reactions were coupled with easy workup and purification procedures to give high-purity final products.

Screening for caspase-3 inhibitors: a new class of potent small-molecule inhibitors of caspase-3.

From the authors' 650,000 compound collection, they have selected approximately 15,000 potential small-molecule protease inhibitors, which were subjected to high-throughput screening against caspase-3. The screening yielded a series of hits that belong to 11 different scaffolds. Based on the structure of one of the hits, a new class of the small-molecule inhibitors with a double electrophilic warhead, 8-sulfonyl-pyrrolo[3,4-c]quinoline-1,3-diones (SPQ), was synthesized and tested in follow-up mechanistic and anti-apoptosis assays.

New scaffolds for combinatorial synthesis. 1. 5-sulfamoylisatins and their reactions with 1,2-diamines.

3,3-Dichloro-5-(4-methylpiperidinosulfonyl)-2-indolinone (3) and 5-sulfamoylisatins 4 have been synthesized from 5-chlorosulfonyl-3,3-dichloro-2-indolinone (1). Compounds 4 are promising scaffolds for the solid- and liquid-phase syntheses of new combinatorial libraries of various heterocycles. Thus, the reactions of 4 with 1,2-diamines, such as o-phenylenediamine (5) and aminoguanidine hydrochloride (6), 1,2-diaminoimidazoles (9), and thiosemicarbazide led, respectively, to new heterocycles 7 and 8 and new combinatorial libraries of triazinoindoles 10 and 15.