Abstract: 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.
Type:
Grant
Filed:
March 29, 2018
Date of Patent:
August 16, 2022
Assignees:
USTAV MOLEKULARNI GENETIKY AV CR, V.V.I., SMART BRAIN S.R.O.
Inventors:
Michal Dvorak, Marta Dvorakova, Vit Karafiat, Jan Stursa, Lukas Werner, Lucie Janeckova
Abstract: Compounds of general formula I are disclosed. The meaning of individual substituents is described in the claims. The compounds are useful in treatment of cancers, due to their multi-modal mechanism of action.
Type:
Application
Filed:
June 11, 2020
Publication date:
August 11, 2022
Applicants:
INSTITUTE OF BIOTECHNOLOGY CAS, V.V.I., SMART BRAIN S.R.O.
Inventors:
Jaroslav TRUKSA, Lukas WERNER, Jan STURSA, Kristyna BLAZKOVA, Cristian Adrian SANDOVAL ACUNA
Abstract: 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.
Abstract: The deferoxamine derivatives of general formula I and pharmaceutically acceptable salts thereof, at least one of R1 and R2 is a substituent of formula II. The novel derivatives are particularly suitable as medicaments, preferably for the treatment of cancer. Pharmaceutical preparations of compounds of formula I and a metal, preferably gallium, are also provided resulting in even more active medicaments or contrast agents. Combinations with other agents, resulting in synergistic effects are provided.
Type:
Application
Filed:
July 13, 2018
Publication date:
March 12, 2020
Applicants:
BIOTECHNOLOGICKY USTAV AV CR, V.V.I, SMART BRAIN S.R.O.
Inventors:
JAROSLAV TRUKSA, Lukas WERNER, Jan STURSA
Abstract: 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.