Patent classifications
C07D279/18
Substituted phenothiazines as mitochondrial agents
The invention provides compounds formula (I) and salts thereof: ##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.6 and Y have any of the values defined in the specification. The compounds are useful for treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
PHOTOSENSITIZER AND DERIVATIVES AND APPLICATION THEREOF
A photosensitizer and derivative, application thereof. The photosensitizer has the structure of general formula I, wherein X is S or Se, Y is organic or inorganic ion, R.sub.1 and R.sub.2 are independently selected from H, alkyl, alkoxy, alkyl amido, alkyl azide and the like; R.sub.3 is selected from H, alkyl, alkoxy, amino sulfonyl, hydroxyl, carboxyl and the like, and L.sub.1 is a linker selected from (CH.sub.2).sub.n1 or (CH.sub.2CH.sub.2O).sub.n2. The derivatives are molecular medicines with drug molecules of anticancer and chemotherapy or tumor targeting function connected to the said photosensitizer. The photosensitizer has excellent near infrared characteristics and low dark toxicity and is used in the field of photodynamic tumor therapy. The introduction of benzophenothiazine or benzophenoselenazine into derivatives with tumor-targeting function could improve the specific uptake of photosensitizer in tumor tissues. Moreover, clinical anticancer drugs can be introduced into the structure of benzophenothiazine or benzophenoselenazine to achieve the purpose of combining therapy of photodynamic therapy and chemotherapy.
##STR00001##
THERAPEUTIC COMPOUNDS
The invention provides compounds having the general formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables R.sup.1, R.sup.2, R.sup.3, R.sup.4, subscript m and n, have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
THERAPEUTIC COMPOUNDS
The invention provides compounds having the general formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables R.sup.1, R.sup.2, R.sup.3, R.sup.4, subscript m and n, have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Azulene ring-containing compound, its use, and an organic photoelectric device including the same
The present disclosure provides an azulene ring-containing compound, its use, and an organic photoelectric device including the same. The azulene ring-containing compound is a compound comprising a structure of Formula I. The organic photoelectric device includes an anode, a cathode, and one or more organic thin film layers located between the anode and the cathode; and at least one of the organic thin film layers contains the above-mentioned azulene ring-containing compound comprising the structure of Formula I. The azulene ring-containing compound provided by the present disclosure has an energy level difference Est0.3 eV between the lowest singlet state S.sub.1 and the lowest triplet state T.sub.1, and has a light-emitting mechanism of a thermally activated delayed fluorescent material, and can be used as a thermally activated delayed fluorescent material for organic photoelectric device, so that the light-emitting efficiency of the device is improved.
Azulene ring-containing compound, its use, and an organic photoelectric device including the same
The present disclosure provides an azulene ring-containing compound, its use, and an organic photoelectric device including the same. The azulene ring-containing compound is a compound comprising a structure of Formula I. The organic photoelectric device includes an anode, a cathode, and one or more organic thin film layers located between the anode and the cathode; and at least one of the organic thin film layers contains the above-mentioned azulene ring-containing compound comprising the structure of Formula I. The azulene ring-containing compound provided by the present disclosure has an energy level difference Est0.3 eV between the lowest singlet state S.sub.1 and the lowest triplet state T.sub.1, and has a light-emitting mechanism of a thermally activated delayed fluorescent material, and can be used as a thermally activated delayed fluorescent material for organic photoelectric device, so that the light-emitting efficiency of the device is improved.
MEDICAL METHODS UTILISING HIGH PURITY DIAMINOPHENOTHIAZINIUM COMPOUNDS
This disclosure pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as diaminophenothiaziniumcompounds) including Methythioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: nitrosylation (NOS); nitrosyl reduction (NR); thiosulfonic acid formation (TSAF); oxidative coupling (OC); Cr(VI) reduction (CR); isolation and purification of zwitterionic intermediate (IAPOZI); ring closure (RC); chloride salt-formation (CSF); one of: sulphide treatment (ST); dimethyldithiocarbamate treatment (DT); carbonate treatment (CT); ethylenediaminetetraacetic acid treatment (EDTAT); organic extraction (OE); and recrystallisation (RX). Also disclosed resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment and diagnosis, etc., for example, for tauopathies, Alzheimer's disease (AD), skin cancer, melanoma, viral diseases, bacterial diseases, or protozoal diseases.
MEDICAL METHODS UTILISING HIGH PURITY DIAMINOPHENOTHIAZINIUM COMPOUNDS
This disclosure pertains generally to the field of chemical synthesis and purification, and more specifically to methods of synthesizing and purifying certain 3,7 diamino-phenothiazin-5-ium compounds (referred to herein as diaminophenothiaziniumcompounds) including Methythioninium Chloride (MTC) (also known as Methylene Blue). In one embodiment, the method comprises the steps of, in order: nitrosylation (NOS); nitrosyl reduction (NR); thiosulfonic acid formation (TSAF); oxidative coupling (OC); Cr(VI) reduction (CR); isolation and purification of zwitterionic intermediate (IAPOZI); ring closure (RC); chloride salt-formation (CSF); one of: sulphide treatment (ST); dimethyldithiocarbamate treatment (DT); carbonate treatment (CT); ethylenediaminetetraacetic acid treatment (EDTAT); organic extraction (OE); and recrystallisation (RX). Also disclosed resulting (high purity) compounds, compositions comprising them (e.g., tablets, capsules), and their use in methods of inactivating pathogens, and methods of medical treatment and diagnosis, etc., for example, for tauopathies, Alzheimer's disease (AD), skin cancer, melanoma, viral diseases, bacterial diseases, or protozoal diseases.
METHODS OF SYNTHESIS AND/OR PURIFICATION OF DIAMINOPHENOTHIAZINIUM COMPOUNDS
Disclosed are methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (diaminophenothiazinium compounds) including Methylthioninium Chloride (MTC) (Methylene Blue), and the resulting high purity characterized by a purity greater than 98%, and very low levels of heavy metals and organic impurities Azure A, B, C and MVB. Also disclosed are methods of treatment of a tauopathy or methemoglobinemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of the high-purity diaminophenothiazinium compound.
METHODS OF SYNTHESIS AND/OR PURIFICATION OF DIAMINOPHENOTHIAZINIUM COMPOUNDS
Disclosed are methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (diaminophenothiazinium compounds) including Methylthioninium Chloride (MTC) (Methylene Blue), and the resulting high purity characterized by a purity greater than 98%, and very low levels of heavy metals and organic impurities Azure A, B, C and MVB. Also disclosed are methods of treatment of a tauopathy or methemoglobinemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of the high-purity diaminophenothiazinium compound.