Richter Gedeon Nyrt.

Szegedi Tudomanyegyetem

Biotie Therapies Corporation

Magyar Tudományos Akadémia Természettudományi Kutatóközpont

Bioblocks Magyarorszag Gyogyszerkemiai Es Fejleszto Kft.

Ferenc Fülöp

Gábor Balogh

Ibolya Horváth

Zsolt Török

Sándor Bernáth

Botond Penke

Ákos Hunya

István Szatmári

David Smith

Marjo Pihlavisto

Zsolt Szakonyi

László Vígh

Tibor Soós

Petri Vainio

Gergely Szakács

József Toldi

László Vécsei

Szilárd Tóth

Dóra Türk

Veronika Pape

László Vigh

György Dormán

István Mándity

László Lázár

Roberta Ferenczi-Palkó

Sakari Alaranta

András Füredi

Balázs Olasz

The invention relates to C-3 substituted kynurenic acid derivatives with the general formula (I) wherein Ris Calkyl-, RRN&#x2014;Calkyl-, Caryl-Calkyl group; Ris H or Calkyl group; or Rand Rwith the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; Ris &#x2014;OH, Calkyl-O&#x2014;, &#x2014;NH, Calkyl-NH&#x2014;, Caryl-Calkyl-NH&#x2014; or &#x2014;NH&#x2014; &#x2014;(CH)&#x2014;NRRgroup wherein n is an integer from 1 to 3; Ris H, Calkyl-, Caryl group or a halogen atom; Ris H or Caryl group; R6 is Calkyl group; Ris Calkyl group; or Rand Rwith the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; Ris Calkyl group; Ris Calkyl group; Rand Rwith the nitrogen atom to which they are attached form a saturated or partially saturated 5-7 membered, optionally benzofused heterocyclic ring, optionally comprising additional N, O, S heteroatoms and optionally being substituted; and stereoisomers, tautomers and salts thereof. The invention relates to the pharmaceutical preparations comprising the compounds and stereoisomers, tautomers and pharmaceutically acceptable salts. The compounds of the invention have neuroprotective activity, may be used for the prevention and treatment of neurodegeneration, and for slowing down the development of the conditions and diseases associated with a decline in cognitive abilities. 

Types of C-3 substituted kynurenic acid derivatives with improved neuroprotective activity

The present invention is related to 8-hydroxy-quinoline derivatives having multidrug-resistance reversing activity with improved selectivity and increased cytotoxicity towards multidrug-resistant cancer cells, preparation thereof and use of the same in the treatment of cancer, especially multidrug-resistant variants thereof. 

MDR-reversing 8-hydroxy-quinoline derivatives

The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein Ris optionally substituted Caryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; Rand Rare independently hydrogen or Calkyl group; Rand Rare independently hydrogen, Calkyl group optionally substituted with amino, mono- or di(Calkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with Calkyl group or Calkoxy group; Ris Calkyl, Ccycloalkyl, CcycloalkylCalkyl or arylCalkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder mediated by heat shock proteins. 

1,4-dihydropyridine derivatives with HSP modulating activity

1,4-dihydropyridine derivatives with Hsp modulating activity

The invention relates to new morphine derivatives deuterated at the 7,8-position of the morphine ring, furthermore to a process for the preparation thereof, and to pharmaceutical compositions comprising them. The new deuterated morphine derivatives show high and selective &#x3bc;-opioid receptor binding activity leading to the benefit of higher analgesic activity at lower dosages inducing thereby reduced adverse effects compared to the hydrogenated derivatives. The compounds of the invention are useful for example in the treatment of pain or can be used as antitussive agents with a reduced risk of the possibility of drug abuse.

Deuterated morphine derivatives

The present invention is directed to carbocyclic hydrazino compounds that function as inhibitors of copper-containing amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-I (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases. The novel compounds have the general formula:or a pharmaceutically acceptable solvate, hydrate, or salt thereof wherein Rto Rare as defined herein.

Carbocyclic hydrazino inhibitors of copper-containing amine oxidases

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Szeged, Hungary

Ferenc Fülöp