C07C225/36

OZONOLYSIS FOR ACTIVATION OF COMPOUNDS AND DEGRADATION OF OZONE
20210393674 · 2021-12-23 ·

Provided is an inactive compound that is activated by reaction with ozone into an active compound having a carbonyl oxygen. Also provided is a method of activating the above inactive compounds. Further provided is a method of treating a disease or condition in a subject using the above compound at a site that is not exposed to atmospheric ozone. Additionally provided is a method of determining internal ozonolysis in a subject using the above compound. Also provided is a molecule less than 1000 mw, having a double bond that is reactive with ozone, and forms a nontoxic compound after reacting with ozone. Further provided is a method of degrading ozone.

OZONOLYSIS FOR ACTIVATION OF COMPOUNDS AND DEGRADATION OF OZONE
20210393674 · 2021-12-23 ·

Provided is an inactive compound that is activated by reaction with ozone into an active compound having a carbonyl oxygen. Also provided is a method of activating the above inactive compounds. Further provided is a method of treating a disease or condition in a subject using the above compound at a site that is not exposed to atmospheric ozone. Additionally provided is a method of determining internal ozonolysis in a subject using the above compound. Also provided is a molecule less than 1000 mw, having a double bond that is reactive with ozone, and forms a nontoxic compound after reacting with ozone. Further provided is a method of degrading ozone.

Acetalanthraquinone derivatives useful for cellular staining

The present invention provides di-substituted acetalanthraquinone-based compounds of the Formulae (l)-(IV) that are useful for cellular staining and for light-based detection of biological material, e.g. fluorescence-based detection of biological material. These compounds may be used in hydrolysed or non-hydrolysed form. Also provided is a fluorescent complex that comprises a nucleic acid and an acetalanthraquinone-based compound of the invention; and a method of staining a biological sample comprising cells or other biological material containing nucleic acid, which method comprises contacting the biological sample with an acetalanthraquinone-based compound of the invention. In the Formulae (l)-(IV), A and B are each independently of formula —R.sup.aCH.sub.2CH(OR.sup.b).sub.2; or one of A and B is of formula —R.sup.aCH.sub.2CH(OR.sup.b).sub.2 and the other one is of formula: —NR.sup.b.sub.2. ##STR00001##

Acetalanthraquinone derivatives useful for cellular staining

The present invention provides di-substituted acetalanthraquinone-based compounds of the Formulae (l)-(IV) that are useful for cellular staining and for light-based detection of biological material, e.g. fluorescence-based detection of biological material. These compounds may be used in hydrolysed or non-hydrolysed form. Also provided is a fluorescent complex that comprises a nucleic acid and an acetalanthraquinone-based compound of the invention; and a method of staining a biological sample comprising cells or other biological material containing nucleic acid, which method comprises contacting the biological sample with an acetalanthraquinone-based compound of the invention. In the Formulae (l)-(IV), A and B are each independently of formula —R.sup.aCH.sub.2CH(OR.sup.b).sub.2; or one of A and B is of formula —R.sup.aCH.sub.2CH(OR.sup.b).sub.2 and the other one is of formula: —NR.sup.b.sub.2. ##STR00001##

Deuterated compounds and uses thereof

An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumour, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumour cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided. ##STR00001##

Deuterated compounds and uses thereof

An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumour, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumour cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided. ##STR00001##

DEUTERATED COMPOUNDS AND USES THEREOF

An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumour, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumour cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided.

##STR00001##

DEUTERATED COMPOUNDS AND USES THEREOF

An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumour, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumour cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided.

##STR00001##

Anthraquinone analogs and methods of making and using thereof

Rhein analogues that exhibit anti-proliferative activity, particular against cancer cells, are described herein. In some embodiments, the compounds contain a flat or planar ring system. Such rings system by facilitate non-covalent binding of the compounds to the DNA complex, such as by intercalation. In some embodiment, the compounds contain a flat or planar ring system as described above and one or more substituents which are alkylating moieties, electrophilic groups or Michael acceptors or groups which contain one or more alkylating moieties, electrophilic groups and/or Michael acceptors. The compounds described herein can also contain one more functional groups to improve the solubility of the compounds.

Anthraquinone analogs and methods of making and using thereof

Rhein analogues that exhibit anti-proliferative activity, particular against cancer cells, are described herein. In some embodiments, the compounds contain a flat or planar ring system. Such rings system by facilitate non-covalent binding of the compounds to the DNA complex, such as by intercalation. In some embodiment, the compounds contain a flat or planar ring system as described above and one or more substituents which are alkylating moieties, electrophilic groups or Michael acceptors or groups which contain one or more alkylating moieties, electrophilic groups and/or Michael acceptors. The compounds described herein can also contain one more functional groups to improve the solubility of the compounds.