Brock University

Smart Brain S.r.o.

Biotechnologicky Ustav Av Cr, V.v.i.

Springtide Ventures S.r.o.

Mitotax S.r.o.

Ustav Molekularni Genetiky Av Cr, V.v.i.

Biotechnology Ustav Av Cr, V.v.i.

Kkcg Ag

Institute of Biotechnology Cas, V.v.i.

Lukas Werner

Tomas Hudlicky

Ales Machara

Mary Ann Endoma-Arias

Jan Stursa

Hannes Leisch

Jiri Neuzil

Robert James Carroll

Sona Hubackova

Martina Wernerova

Marta Dvorakova

David R Adams

Robert Carroll

Lucie Janeckova

Vit Karafiat

Michal Dvorak

Kristyna Blazkova

Jirí Neuzil

The present invention relates to compounds of general formula (I) in particular for use in the treatment of senescence-related diseases, such as idiopathic pulmonary fibrosis, sarcopenia, diabetes, obesity, osteoarthritis, chronic inflammations, glaucoma, cataracts, radiation-induced oral mucosis, renal transplantation, prostatic hyperplasia. 

Method for treatment of senescence-related disorders

The present invention relates to 1-acyl-lysophosphatidyl derivatives of general formula I; in which R is C4 to C30 aliphatic hydrocarbyl chain, R1 is selected from H or C1 to C10 alkyl, preferably C1 to C6 alkyl, R2 is selected from H, C10 to C30 acyl or C1 to C10 alkyl, preferably C1 to C6 alkyl, and R3, when present, is selected from H or C1 to C10 alkyl, preferably C1 to C6 alkyl. These derivatives are intended for the treatment of cancer, in particular melanoma, hepatocarcinoma or GIT carcinomas.

Phospholipid derivatives and their use as medicaments

Compounds for treatment of senescence-related disorders

The subject of the invention are new mitochondrially targeted E/Z isomers of aliphatic triphenylphosphonium derivatives of tamoxifen where the aliphatic chain is alkyl or alkenyl, and their corresponding tertiary amine salts and/or their mixture (MitoTAX). Alkyl triphenylphosphonium derivatives of tamoxifen have the general formula (I), where n=8 to 12 and where Z is selected from the group of organic salts or inorganic salts. Alkenyl triphenylphosphonium derivatives of tamoxifen have the general formula IA, where n=6 to 10 and where Z has the above mentioned meaning. These compounds are applicable for the treatment of neoplastic disease, especially those with high HER2 protein levels. The drug for the treatment of neoplastic diseases according to the invention contains at least one E/Z isomer of aliphatic triphenylphosphonium derivatives of tamoxifen of the general formula (I) and/or IA or their corresponding salts of tertiary amine.

Tamoxifen derivatives for treatment of neoplastic diseases, especially with high HER2 protein level

The present invention provides a method for the N-demethylation and N-functionalization of an N-methylated heterocycle such as a morphine alkaloid or tropane alkaloid. The method comprises reacting the heterocycle with an functionalization agent in the presence of a transition metal catalyst in air or in the presence of an oxidant.

Methods for one-pot N-demethylation/N-functionalization of morphine and tropane alkaloids

A high-yielding method for the N-demethylation of oxycodone- and oxymorphone-N-oxides by the reaction of these compounds with cyclodehydration reagents has been performed. This method has been utilized to improve the synthesis of various morphine analogs, such as naltrexone, nalbuphone and naloxone.

Processes and intermediates in the preparation of morphine analogs via N-demethylation of N-oxides using cyclodehydration reagents

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The present application describes processes for the synthesis of morphinane and morphinone compounds, useful as pharmaceutical agents. Also included are novel intermediates useful in the preparation of these compounds. The process comprises quaternization of oripavine to provide a mixture of the R- and S-isomeric (at the nitrogen) quaternary salts. The R-isomer is readily isolated and converted to various N-(R)-morphinane and N-(S)-morphinone compounds. The R-isomer, S-isomer or a mixture of R- and S-isomers may be demethylated and converted to various morphinane and morphinone compounds.

Processes for the preparation of morphinane and morphinone compounds

The present application relates to processes for the preparation of intermediates useful in the manufacture of oseltamivir and the HPOsalt of oseltamivir, Tamiflu&#xae;. The application further relates to novel intermediate and compounds and oseltamivir analogs and to pharmaceutical compositions comprising said analog compounds. The application further relates to a method of using the novel analogs of oseltamivir to treat or prevent influenza.

Process and compounds for the manufacture of oseltamivir and analogs thereof, and new antiviral agents

Growing community of inventors

Kadan, Czechia

Lukas Werner