TY - CONF AU - Pusztai, Gyöngyvér AU - Poszávácz, László AU - Vincze, Anna AU - Marton, András AU - Ahmed, Qasim Abdulhussein AU - Halász, Judit AU - Dancsó, András AU - Simig, Gyula AU - Balogh, György Tibor AU - Volk, Balázs TI - Tiadiazinoindol-dioxid származékok: új gyűrűrendszerek szintézise, fizikokémiai és korai fázisú farmakokinetikai jellemzése T2 - Heterociklusos és Elemorganikus Kémiai Munkabizottság ülése 2025 PY - 2025 UR - https://m2.mtmt.hu/api/publication/36280671 ID - 36280671 LA - Hungarian DB - MTMT ER - TY - JOUR AU - Pusztai, Gyöngyvér AU - Poszávácz, László AU - Vincze, Anna AU - Marton, András Dénes AU - Abdulhussein, Ahmed Qasim AU - Halász, Judit AU - Dancsó, András AU - Simig, Gyula AU - Balogh, György Tibor AU - Volk, Balázs TI - Thiadiazino-indole, thiadiazino-carbazole and benzothiadiazino-carbazole dioxides: synthesis, physicochemical and early ADME characterization of representatives of new tri-, tetra- and pentacyclic ring systems and their intermediates JF - BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY J2 - BEILSTEIN J ORG CHEM VL - 21 PY - 2025 SP - 2220 EP - 2233 PG - 14 SN - 1860-5397 DO - 10.3762/bjoc.21.169 UR - https://m2.mtmt.hu/api/publication/36391850 ID - 36391850 N1 - This work was prepared in the framework of 2020-1.1.2-PIACI-KFI-2020-00039 project with the support of the Ministry of Culture and Innovation from the National Research, Development and Innovation Fund (Hungary). AB - Motivated by the in vivo anxiolytic activity of previously described 1,2,3-benzothiadiazine 1,1-dioxides, we aimed at elaborating a synthetic procedure for the preparation of their pyrrole-fused counterparts, 2,9-dihydro[1,2,3]thiadiazino[5,6- g ]indole 1,1-dioxide derivatives. The simple and versatile process led, via Fischer indole cyclization of the corresponding hydrazones, to a wide structural variety of new tri-, tetra- and pentacyclic ring systems. The structural characterization of ( E )- and ( Z )-hydrazones was supported by 2D NMR techniques, while that of the target compounds by single-crystal X-ray measurements. The hydrazone intermediates and the new title compounds were subjected to a physicochemical and early ADME characterization study, in the framework of which log P , p K a and log k values were calculated. Following that, kinetic solubility and in vitro gastrointestinal membrane-specific permeability measurements were carried out to assess the lead-likeness of the compounds. Subsequently, the metabolic stability of the most promising derivatives was also determined using human liver microsomes. LA - English DB - MTMT ER - TY - JOUR AU - Poszávácz, László AU - Porcs-Makkay, Márta AU - Halász, Judit AU - Mórász, Tamás AU - Nagy, Tamás AU - Kátainé Fadgyas, Katalin AU - Simig, Gyula AU - Volk, Balázs TI - Points of Interest in the Chemistry of the Levomepromazine Drug Substance: Recycling of Undesired Enantiomer, Identification of New Phenothiazine Dimers, Synthesis of a Pharmacopeial Impurity, and an Unexpected Rearrangement JF - ORGANIC PROCESS RESEARCH & DEVELOPMENT J2 - ORG PROCESS RES DEV VL - 28 PY - 2024 IS - 1 SP - 281 EP - 292 PG - 12 SN - 1083-6160 DO - 10.1021/acs.oprd.3c00368 UR - https://m2.mtmt.hu/api/publication/34483970 ID - 34483970 LA - English DB - MTMT ER - TY - GEN AU - Poszávácz, László AU - Porcs-Makkay, Márta AU - Halász, Judit AU - Kátainé Fadgyas, Katalin AU - Nagy, Tamás AU - Simig, Gyula AU - Volk, Balázs TI - A levomepromazine hatóanyaggal kapcsolatos érdekességek – ami a „tankönyvekből” kimaradt PY - 2024 PG - 31 UR - https://m2.mtmt.hu/api/publication/35721751 ID - 35721751 LA - Hungarian DB - MTMT ER - TY - JOUR AU - Poszávácz, László AU - Nagy, Tamás AU - Kátainé Fadgyas, Katalin AU - Volk, Balázs TI - New, scalable process for the preparation of 5-acetyl-1H-pyrazole-3-carboxylic acid, a key intermediate of darolutamide JF - SYNTHESIS-STUTTGART J2 - SYNTHESIS-STUTTGART VL - 55 PY - 2023 IS - 13 SP - 2061 EP - 2069 PG - 9 SN - 0039-7881 DO - 10.1055/a-2016-4337 UR - https://m2.mtmt.hu/api/publication/33585454 ID - 33585454 AB - A new, efficient process for the synthesis of 5-acetyl-1H-pyrazole-3-carboxylic acid, a versatile building block and the key intermediate of darolutamide, using diethyl pyrazole-3,5-dicarboxylate as the starting material is described. Contrary to the synthetic routes known from the literature, this procedure does not apply explosive diazo reagents, moreover it is simple and safe, thereby suitable for scale-up. LA - English DB - MTMT ER - TY - GEN AU - Poszávácz, László AU - Szilágyi, Bence AU - Nagy, Tamás AU - Egyed, Attila AU - Kátainé Fadgyas, Katalin AU - Keserű, György Miklós AU - Mándity, István AU - Volk, Balázs TI - „Semmi sem olyan egyszerű, mint amilyennek látszik”. Darolutamid intermedier generikus szemmel PY - 2022 UR - https://m2.mtmt.hu/api/publication/33106229 ID - 33106229 N1 - előadó: Nagy Tamás LA - Hungarian DB - MTMT ER - TY - JOUR AU - Hunyadi, Dávid AU - Poszávácz, László TI - Crystalline form of 8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid JF - THE IP.COM JOURNAL J2 - IP DOT COM JOURNAL PY - 2018 PG - 8 SN - 1533-0001 UR - https://m2.mtmt.hu/api/publication/33685230 ID - 33685230 LA - English DB - MTMT ER - TY - PAT AU - Gacsályi, István AU - Bózsing, D AU - Kertész, Sz AU - Megyeri, K AU - Barkóczy, J AU - Molnárné Samu, Erika AU - Poszávácz, László AU - Antoni, Ferenc András AU - Volk, Balázs TI - Quinazoline derivatives, process for the preparation thereof and pharmaceutical compositions comprising the same PY - 2015 UR - https://m2.mtmt.hu/api/publication/3102668 ID - 3102668 N1 - Chem Abstr. 2015, 236307 LA - English DB - MTMT ER - TY - JOUR AU - Volk, Balázs AU - Gacsályi, István AU - Pallagi, Katalin AU - Poszávácz, László AU - Gyönös, Ildikó AU - Szabó, Éva AU - Bakó, Tibor AU - Spedding, M AU - Simig, Gyula AU - Szénási, Gábor TI - Optimization of (Arylpiperazinylbutyl)oxindoles Exhibiting Selective 5-HT(7) Receptor Antagonist Activity JF - JOURNAL OF MEDICINAL CHEMISTRY J2 - J MED CHEM VL - 54 PY - 2011 IS - 19 SP - 6657 EP - 6669 PG - 13 SN - 0022-2623 DO - 10.1021/jm200547z UR - https://m2.mtmt.hu/api/publication/1846147 ID - 1846147 N1 - Megjegyzés-27433218 N1 CAPLUS AN 2011:1183946(Journal; Online Computer File) Megjegyzés-27433224 N1 CAPLUS AN 2011:1183946(Journal; Online Computer File) Megjegyzés-27433229 N1 CAPLUS AN 2011:1183946(Journal; Online Computer File) Megjegyzés-27433212 N1 CAPLUS AN 2011:1183946(Journal; Online Computer File) Chemical Research Division, EGIS Pharmaceuticals Plc., P.O. Box 100, Budapest, H-1475, Hungary Preclinical Research Division, EGIS Pharmaceuticals Plc., P.O. Box 100, Budapest, H-1475, Hungary Les Laboratoires Servier, 22 rue Garnier, 92578 Neuilly-sur-Seine, France Cited By :36 Export Date: 31 May 2021 CODEN: JMCMA Correspondence Address: Volk, B.; Chemical Research Division, P.O. Box 100, Budapest, H-1475, Hungary; email: volk.balazs@egis.hu Chemicals/CAS: oxindole, 59-48-3; Anti-Anxiety Agents; Antidepressive Agents; Indoles; Ligands; Piperazines; Receptor, Serotonin, 5-HT1A, 112692-38-3; Receptors, Adrenergic, alpha-1; Receptors, Serotonin; Serotonin Antagonists; serotonin 7 receptor AB - A series of (arylpiperazinylbutyl)oxindoles as highly potent 5-HT(7) receptor antagonists has been studied for their selectivity toward the 5-HT(1A) receptor and alpha(1)-adrenoceptor. Several derivatives exhibited high 5-HT(7)/5-HT(1A) selectivity, and the key structural factors for reducing undesired alpha(1)-adrenergic receptor binding have also been identified. Rapid metabolism, a common problem within this family of compounds, could be circumvented with appropriate substitution patterns on the oxindole carbocycle. Contrary to expectations, none of the compounds produced an antidepressant-like action in the forced swimming test in mice despite sufficiently high brain concentrations. On the other hand, certain analogues showed significant anxiolytic activity in two different animal models: the Vogel conflict drinking test in rats and the light-dark test in mice. LA - English DB - MTMT ER - TY - GEN AU - Poszávácz, László AU - Bertha, Ferenc AU - Simig, Gyula AU - Fetter, József TI - Novel Synthesis of Naratriptan via N-benzyl-indole-5-carbaldehyde PY - 2009 UR - https://m2.mtmt.hu/api/publication/33706675 ID - 33706675 LA - English DB - MTMT ER -