116 results about "Acridone" patented technology

Certain derivatives of acridones and benzothiadiazines have been found to have anti-cancer properties by virtue of their specific inhibition of the cyclin D dependent kinase CDK4. These molecules inhibit CDK4 activity more than they inhibit the activity of other such kinases (e.g. CDC2 and CDK2). This specificity results in an improved therapeutic index when used as drugs to treat susceptible cancers.

The present invention provides novel pyrrolo-[2,1-c][1,4]benzodiazepine hybrids useful as anti-tumour agents and a process for the preparation thereof.

The invention provides a preparation method of acridine compounds, and relates to the technical field of photoinitiator. The preparation method comprises the following steps of: taking substituted N-methyl anthranilic acid as initial raw material, generating substituted acridone under the condition of acid, carrying out reaction on substituted bromobenzene and magnesium to generate grignard reagent, carrying out reaction on substituted acridone and the grignard reagent to generate substituted 9-oxhydryl-9-phenylacridine, and reducing to obtain the substituted 9-phenylacridine compounds. Different from the conventional synthesis route, the preparation method of the acridine compounds provided by the invention has more operation steps compared with the conventional one-step method, thus being slightly lower in yield compared with the conventional synthesis route, however, the preparation condition is mild relatively, and the high-temperature and high-pressure reaction and the use of expensive heavy metal catalyst can be avoided, so that the preparation method is good in environment protection.

The invention provides an OLED device comprising a cathode, an anode, and having therebetween a layer containing an acridone compound including a diarylamine or carbazole substituent where the nitrogen of the acridone and the nitrogen of the diarylamine or carbazole are connected by an aromatic hydrocarbon linking group. OLED devices of the invention exhibit improved efficiency and drive voltage.

Disclosed are new acridone dye derivatives having characteristic fluorescence lifetimes. Also disclosed are methods for labelling target biological materials employing the acridone dyes and use of the labelled materials in biological assays. The acridone derivatives have the following structure:in which Z1 and Z2 represent the atoms necessary to complete one ring, two fused ring, or three fused ring aromatic or heteroaromatic systems, each ring having five or six atoms selected from carbon atoms and optionally no more than two atoms selected from oxygen, nitrogen and sulphur; R2, R3, R4 and R5 are selected from hydrogen, halogen, amide, hydroxyl, cyano, nitro, mono- or di-nitro-substituted benzyl, amino, mono- or di-C1-C4 alkyl-substituted amino, sulphydryl, carbonyl, carboxyl, C1-C6 alkoxy, acrylate, vinyl, styryl, aryl, heteroaryl, C1-C20 alkyl, aralkyl, sulphonate, sulphonic acid, quaternary ammonium, the group -E-F and the group —(CH2—)nY; R1 is selected from hydrogen, mono- or di-nitro-substituted benzyl, C1-C20 alkyl, aralkyl, the group -E-F and the group —(CH2—)nY; where E is a spacer group, F is a target bonding group; Y is selected from sulphonate, sulphate, phosphonate, phosphate, quaternary ammonium and carboxyl; and n is an integer from 1 to 6. The invention also relates to a set of different fluorescent acridone dye derivatives, each dye having a different fluorescence lifetime, the set of dyes being particularly useful for multiparameter analysis.

The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ═O, L is —H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula —N(RN)Q, wherein: RN is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.

This invention pertains to certain acridone and acridine compounds of the formula which inhibit telomerase, regulate cell proliferation, etc., and / or treat cancer, proliferative conditions, etc.: wherein either: (a) K is ═O, L is —H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each a group of the formula —N(RN)—W, wherein: RN is a nitrogen substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and, W is C1-17alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and, wherein, when K is a 9-substituent, K is a group of the formula —N(RN)—Q, wherein: RN is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit telomerase, to regulate cell proliferation, etc., and / or in the treatment of cancer, proliferative conditions, etc.

Dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds comprise sulfenates having the formula, t,0080where E is selected from the group consisting of somatostatin receptor binding molecules, heat sensitive bacterioendotoxin receptor binding molecules, neurotensin receptor binding molecules, bombesin receptor binding molecules, cholecystekinin receptor binding molecules, steroid receptor binding molecules, and carbohydrate receptor binding molecules, and dihydoxyindolecarboxylic acid; L and X are independently selected from the group consisting of —(R5)NOC—, —(R5)NOCCH2O—, —(R5)NOCCH2CH2O—, —OCN(R5)—, —HNC(═S)NH—, and HNC(═O)NH—; DYE is an aromatic or a heteroaromatic radical derived from the group consisting of cyanines, indocyanines, phthalocyanines, rhodamines, phenoxazines, phenothiazines, phenoselenazines, fluoresceins, porphyrins, benzoporphyrins, squaraines, corrins, croconiums, azo dyes, methine dyes, indolenium dyes, crellins, and hypocrellins; R1 to R5 are independently selected from the group comprising hydrogen, C1-C10 alkyl, C5-C10 aryl, C1-C10 polyhydroxyalkyl, and C1-C10 polyalkoxyalkyl; and Ar is an aromatic or heteroaromatic radical derived from the group consisting of benzenes, naphthalenes, naphthoquinones, diphenylmethanes, fluorenes, anthracenes, anthraquinones, phenanthrenes, tetracenes, naphthacenediones, pyridines, quinolines, isoquinolines, indoles, isoindoles, pyrroles, imidiazoles, oxazoles, thiazoles, pyrazoles, pyrazines, purines, benzimidazoles, furans, benzofurans, dibenzofurans, carbazoles, acridines, acridones, phenanthridines, thiophenes, benzothiophenes, dibenzothiophenes, xanthenes, xanthones, flavones, coumarins, and anthacylines. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effects at once using a dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.

The invention discloses a method for synthesizing acridone derivatives by means of palladium-copper co-catalysis. The method comprises the steps that on the condition that palladium chloride, copper pivalate and di-tert-butyl peroxide or oxygen co-exist, diphenylamine compounds including symmetric diphenylamine and asymmetric diphenylamine are dissolved in an anhydrous organic solvent, all the materials are mixed to be uniform, a reaction is conducted for 20 h to 30 h under the condition of 80 DEG C to 120 DEG C in a carbon monoxide atmosphere, separation and purification are conducted, and the acridone derivatives can be obtained. According to the method for synthesizing the acridone derivatives by means of palladium-copper co-catalysis, the preparation method is simple, the diphenylamine compounds which are simple and easy to obtain are used as the raw materials, and the acridone derivatives are directly constructed through C-H / C-H oxidative carbonylation; the preparation condition is mild, and the target product can be obtained in a high-selectivity mode at 80 DEG C to 120 DEG C; the acridone derivatives have good substrate applicability, the range of substrates is greatly expanded, and the acridone derivatives have a great application prospect in biological medicine and materials and the like.

The invention discloses a compound with acridone as the core and application of the compound to an organic electroluminescent device. The compound has acridone as the core, is not easy to crystallize between molecules and is not easy to aggregate, and has good film forming ability. When the compound is used as a luminescent layer material of an OLED luminescent device, current efficiency, power efficiency and external quantum efficiency of the device are all greatly improved. Meanwhile, life of the device is obviously prolonged.

The invention discloses 12-(2-fluorophenyl)-benzo [h][1,3] methylenedioxy [4,5-b] acridine-10,11-diketone and a synthesis method thereof, and belongs to the technical field of dihydroketoacridine derivatives. The method comprises the steps of uniformly mixing 3,4-methylenedioxy aniline, 2-fluorobenzaldehyde, 2-hydroxyl-1,4-naphthaquinone, a catalyst and toluene sulfonic acid, performing heating and stirring, controlling the temperature to be 115-130 DEG C, and performing a reaction for 3-5h. Fluorine atom and methylenedioxy structures are introduced into 12-(2-fluorophenyl)-benzo [h][1,3] methylenedioxy [4,5-b] acridine-10,11-diketone, so that 12-(2-fluorophenyl)-benzo [h][1,3] methylenedioxy [4,5-b] acridine-10,11-diketone has higher activity, and more facilitates absorption. The synthesis method has the characteristics that the synthesis method is simple to operate, high in yield, green and environment-friendly, and raw materials are easy to obtain.

The invention discloses acridone derivative containing galactose, a preparation method and application thereof, and belongs to the technical field of drug synthesis. The acridone derivative has the technical scheme points that the specific structure of acridone derivative is as follows. The invention further discloses a preparation method of the acridone derivative containing galactose, and application of the acridone derivative containing galactose to preparation of anti-cancer drugs. The method has the advantages that the method is simple to operate and wild in reaction conditions, ensures that adopted reagents are all industrial common reagents, is suitable for large-scale industrial preparation, pollution-free in synthesis steps, and less in by-products; the formed acridone derivativehas excellent biological activity and anti-cancer activity, and has good commercial application value.

The invention discloses novel compounds containing an acridone structure, and particularly relates to acridone derivatives and a synthesis method thereof, belonging to the technical field of organic chemical synthesis. The structure of the acridone derivatives is shown in the specification, wherein R1 and R2 are independently selected from H, methoxy, C1-10 alkyl and C1-10 haloalkyl. The compounds have higher fluorescence and can be used for organic luminescent materials.

The invention discloses a material with antibacterial performance, a preparation method and application thereof, wherein the material is polyimide and is formed by polymerizing a diamine monomer containing an acridone structure and a dianhydride monomer. According to the invention, acridone with a planar rigid structure and a polar group are creatively introduced into a polyimide main chain, wherein the planar rigid acridone structure is beneficial to regular stacking of molecular chains and induction of polymer crystallization, and the polar group can enhance the hydrogen-bond interaction ofthe molecular chains and promote the tight stacking of the molecular chains, so that polyimide has excellent barrier property, high glass-transition temperature and thermal stability and low thermal expansion coefficient; and the polyimide contains an acridone structure and a polar group, so that the polyimide is endowed with a certain antibacterial property.