C07D279/18

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.

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##

A Process for the Preparation of Methylene Blue

Provided herein is a process for preparation of 3,7-bis-(dimethylamino)-phenothian-5-ium chloride: Formula (I). The said process comprises preparing 3,7-dibromophenothiazin-5-ium bromide wet Crude(III) from phenothiazine (II) along promoter, catalyst and brominating agent in presence of organic solvent; preparing 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide (IV) from 3,7-dibromophenothiazin-5-ium bromide; preparing 3,7-bis (Dimethylamino)-phenothiazin-5-ium chloride from 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide and subsequently purifying and removing metal content through metal scavenger from 3,7-bis-(dimethylamino)-phenothiazin-5-ium chloride (I). The present process eliminates the additional step of ion exchange column in the reaction and provides 99 to 99.5 percentage of product purity.

##STR00001##

A Process for the Preparation of Methylene Blue

Provided herein is a process for preparation of 3,7-bis-(dimethylamino)-phenothian-5-ium chloride: Formula (I). The said process comprises preparing 3,7-dibromophenothiazin-5-ium bromide wet Crude(III) from phenothiazine (II) along promoter, catalyst and brominating agent in presence of organic solvent; preparing 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide (IV) from 3,7-dibromophenothiazin-5-ium bromide; preparing 3,7-bis (Dimethylamino)-phenothiazin-5-ium chloride from 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide and subsequently purifying and removing metal content through metal scavenger from 3,7-bis-(dimethylamino)-phenothiazin-5-ium chloride (I). The present process eliminates the additional step of ion exchange column in the reaction and provides 99 to 99.5 percentage of product purity.

##STR00001##

CONJUGATES INCLUDING A DETECTABLE MOIETY
20230192658 · 2023-06-22 ·

Disclosed herein are detectable moieties and detectable conjugates comprising one or more detectable moieties. In some embodiments, the disclosed detectable moieties have a narrow wavelength and are suitable for multiplexing. Also disclosed are methods of labeling one or more targets within a biological specimen using any of the detectable conjugates and/or detectable moieties described herein.

Method for preparation of 3,7-bis-(dimethylamino)-phenothiazin-5-ium chloride or bromide

The present invention relates to: a process for preparing 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide or chloride; a method of converting 3,7-bis-(dimethylamino)-phenothiazin-5-ium bromide to 3,7-bis-(dimethylamino)-phenothiazin-5-ium chloride; and the purification of 7-bis-(dimethylamino)-phenothiazin-5-ium chloride by crystallization from aqueous solution of hydrochloric acid, leading to a pharmaceutically acceptable 3,7-bis-(dimethylamino)-phenothiazin-5-ium chloride (methylthioninium chloride, methylene blue, MTC) of formula I below reported. ##STR00001##

Method for prevention of premature polymerization
09796693 · 2017-10-24 · ·

The present invention relates to a method for prevention of premature polymerization during the preparation, purification, transportation and storage of a polymerizable compound with at least one conjugated unsaturated group in the presence of an azine dye-based compound as inhibitor. Further the present invention relates to methods of preparing such inhibitors as well as to the inhibitors itself, as well as to methods of improving solubility and stability of dissolved inhibitors.

Method for prevention of premature polymerization
09796693 · 2017-10-24 · ·

The present invention relates to a method for prevention of premature polymerization during the preparation, purification, transportation and storage of a polymerizable compound with at least one conjugated unsaturated group in the presence of an azine dye-based compound as inhibitor. Further the present invention relates to methods of preparing such inhibitors as well as to the inhibitors itself, as well as to methods of improving solubility and stability of dissolved inhibitors.

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 ΔEst≤0.3 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.