公开(公告)号：US11414443B2

公开(公告)日：2022-08-16

申请号：US16500552

申请日：2018-03-29

申请人： USTAV MOLEKULARNI GENETIKY AV CR, V.V.I. ,  SMART BRAIN S.R.O.

发明人： Michal Dvorak ,  Marta Dvorakova ,  Vit Karafiat ,  Jan Stursa ,  Lukas Werner ,  Lucie Janeckova

IPC分类号： C07F9/10 ,  A61P35/00 ,  A61K9/00 ,  A61K31/704

摘要： 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.

公开(公告)号：US11014949B2

公开(公告)日：2021-05-25

申请号：US16465882

申请日：2017-11-15

申请人： SPRINGTIDE VENTURES S.R.O. ,  SMART BRAIN S.R.O. ,  BIOTECHNOLOGICKY USTAV AV CR, V.V.I. ,  MITOTAX S.R.O.

发明人： Sona Hubackova ,  Lukas Werner ,  Jan Stursa ,  Jiri Neuzil

IPC分类号： C07F9/54

摘要： 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.

公开(公告)号：US20210179646A1

公开(公告)日：2021-06-17

申请号：US17188111

申请日：2021-03-01

申请人： SPRINGTIDE VENTURES S.R.O. ,  SMART BRAIN S.R.O. ,  BIOTECHNOLOGICKY USTAV AV CR, V.V.I. ,  MITOTAX S.R.O.

发明人： Sona HUBACKOVA ,  Lukas WERNER ,  Jan STURSA ,  Jiri NEUZIL

IPC分类号： C07F9/54

摘要： 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 inflammation, glaucoma, cataracts, radiation-induced oral mucosis, renal transplantation, prostatic hyperplasia.

公开(公告)号：US20200079805A1

公开(公告)日：2020-03-12

申请号：US16465882

申请日：2017-11-15

申请人： SPRINGTIDE VENTURES S.R.O. ,  SMART BRAIN S.R.O. ,  BIOTECHNOLOGICKY USTAV AV CR, V.V.I. ,  MITOTAX S.R.O.

发明人： Sona HUBACKOVA ,  Lukas WERNER ,  Jan STURSA ,  Jiri NEUZIL

IPC分类号： C07F9/54

摘要： 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.

公开(公告)号：US11591352B2

公开(公告)日：2023-02-28

申请号：US17188111

申请日：2021-03-01

申请人： SPRINGTIDE VENTURES S.R.O. ,  SMART BRAIN S.R.O. ,  BIOTECHNOLOGICKY USTAV AV CR, V.V.I. ,  MITOTAX S.R.O.

发明人： Sona Hubackova ,  Lukas Werner ,  Jan Stursa ,  Jiri Neuzil

IPC分类号： C07F9/54

摘要： 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.

公开(公告)号：US09896466B2

公开(公告)日：2018-02-20

申请号：US14786710

申请日：2014-04-07

申请人： Smart Brain S.R.O. ,  Biotechnologicky Ustav Av Cr, V.V.I. ,  Jiri Neuzil ,  KKCG AG

发明人： Jiri Neuzil ,  Jan Stursa ,  Lukas Werner

IPC分类号： C07F9/54 ,  A61K31/135

CPC分类号： C07F9/5456 ,  C07F9/5442 ,  C07F9/5449

摘要： 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.

公开(公告)号：US20220251124A1

公开(公告)日：2022-08-11

申请号：US17612123

申请日：2020-06-11

申请人： INSTITUTE OF BIOTECHNOLOGY CAS, V.V.I. ,  SMART BRAIN S.R.O.

发明人： Jaroslav TRUKSA ,  Lukas WERNER ,  Jan STURSA ,  Kristyna BLAZKOVA ,  Cristian Adrian SANDOVAL ACUNA

IPC分类号： C07F9/54 ,  C07D249/08 ,  C07F9/6518 ,  C07F9/6506 ,  A61K49/04 ,  A61K31/675 ,  A61K31/4196 ,  A61P35/00

摘要： 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.

公开(公告)号：US20200078379A1

公开(公告)日：2020-03-12

申请号：US16613644

申请日：2018-07-13

申请人： BIOTECHNOLOGICKY USTAV AV CR, V.V.I. ,  SMART BRAIN S.R.O.

发明人： JAROSLAV TRUKSA ,  Lukas WERNER ,  Jan STURSA

IPC分类号： A61K31/66 ,  A61K31/704 ,  A61K33/00 ,  A61K31/337 ,  A61K31/513 ,  A61K33/243 ,  A61P35/00

摘要： 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.