54 results about "Phthalazines" patented technology

The invention relates to a phthalazinone derivative and its preparation method and use in medicine, and specifically, relates to a novel phthalazinone derivative shown in the general formula I, a preparation method of the novel phthalazinone derivative, a novel phthalazinone derivative-containing pharmaceutical composition, and a use of the novel phthalazinone derivative-containing pharmaceutical composition utilized as a treatment agent and especially utilized as a poly(ADP-ribose)polymerase(PAPR) inhibitor.

The present invention relates to both a novel method of preparing hydralazine hydrochloride and to a novel method of preparing hydrazine derivatives of compounds containing a pyridazine ring, including, for example, pyridazines, phthalazines and other compounds containing the pyridazine ring.

The invention relates to the field of medicinal chemistry, relates to pyridazinone BTK inhibitors and an application thereof, and concretely relates to pyridazinone BTK inhibitors represented by formula (I), a preparation method thereof, a medicinal composition containing the compounds, and a use of the compounds or the medicinal composition in the treatment of Bruton's tyrosine kinase-related diseases.

The invention discloses an iridium complex-containing phosphorescent material and a preparation method thereof and application thereof in mercury ion detection, and belongs to the technical field of photoelectric phosphorescent materials. The iridium complex-containing phosphorescent material comprises a main ligand and an auxiliary ligand, wherein the main ligand is a 4-substituted phthalazine derivative; and the auxiliary ligand is an N-(diphenyl thiophosphino)-P, P-diphenylphosphino thioamide derivative. Through ligand exchange of Hg2+ and the auxiliary ligand of an iridium complex, the color, ultraviolet absorption and phosphorescence spectrum of the iridium complex are changed so as to achieve an aim of detecting the Hg2 + by a phosphorescent chemical sensor. The invention phosphorescent chemical sensor has the advantages of visible Hg2 + recognition, high phosphorescent response speed, ratiometric response, high sensitivity, good selectivity and applicability to Hg2 + detection in a variety of environments.

The invention belongs to the field of medicinal chemistry, and discloses a 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound having antitumor activity as well as a synthesizing method and application of the 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound. The 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound has a structure as shown in a general formula I, wherein R1 refers to H, methyl or phenyl; R2 refers to 4-fluorophenyl, 4-chloroanilino, 4-bromophenyl, 4-methoxyphenyl, 4-hydroxydiphenyl, 2-fluorophenyl, 3-trifluoromethyl)phenyl]amino, naphthylamine-1-yl, pyrrolidone-1-yl, piperidine-1-yl, 3,5-dimethyl piperidine-1-yl, morpholine-4-yl, or piperazidine-1-yl. The preliminary in-vitro antitumor activity finds that the serial compounds have obvious inhibit and killing effects on multiple tumor cells, and the 3, 6 modified-[1, 2, 4] triazole [3, 4-alpha] phthalazine compound can act as an active ingredient to be applied to clinical prevention and cancer treatment after being developed into a novel medicament.

The invention relates to a 4-pyridine substituted phthalazinone compound, a preparation method, a pharmaceutical composition and an application thereof, the structure of the 4-pyridine substituted phthalazinone compound is shown as a formula I, the compound of the formula I has improved pharmaceutical physicochemical properties and in-vivo pharmacokinetic properties, oral bioavailability is high,druggability is good, The compound is a non-nucleoside small-molecule HBV virus inhibitor which is novel in structure and can be orally taken.

The invention discloses a synthesis method of a phthalazine derivative. In the method, phthalylhydrazine and dimedone or 1,3-cyclohexanedione react with aromatic aldehyde or aliphatic aldehyde in the conditions that the ionic liquid [BSO3HMIm]HSO4 is used as a catalyst, PEG (polyethylene glycol) 600 is used as a solvent and the temperature is 100-160 DEG C; and the phthalazine derivative is synthesized from three components in one pot. The synthesis method has the advantages of low cost, good application prospect and the like, and is efficient, non-toxic and environment-friendly; and the catalyst and solvent are easily recycled and can be recycled.

The invention discloses a PARP inhibitor containing a phthalazine-1(2H)-ketone structure as well as a preparation method and medical application of the PARP inhibitor. A compound as shown in a generalformula (I) or a pharmaceutically acceptable salt thereof are described in the specification. The invention provides novel PARP inhibitors containing phthalazine-1(2H)-ketone structures, and the PARPinhibitors can be used as single therapeutic agents for tumors or combined with other anti-tumor drugs, so that the effects of improving the curative effect of the existing anti-tumor drugs and reducing the dosage and toxicity are achieved.

A compound of formula (I)

wherein A, R¹, R³, and R²⁴ are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, I_Kur-associated disorders, and other disorders mediated by ion channel function.

The invention discloses a phthalazinopyrrole compound and a preparation method thereof. The phthalazinopyrrole compound has potential antibacterial, anti-inflammatory and anti-tumour activities. The preparation method of the compound comprises the following steps: under the nitrogen protection condition, dissolving phthalazine derived 1,3-dipole and allene ester into an organic solvent, adding an organic phosphine catalyst, stirring, and carrying out cycloaddition reaction, so that the phthalazinopyrrole compound can be obtained.

The present invention discloses serial new 1-amido-4-(pyridyl-4-methylene) phthalazine derivatives and their medicinal salts, hydrates, solvolytes, precursors, precursor derivatives, and compositions, and their preparation process and pharmacological use, especially in preparing medicines for treating hypertrophic diseases, such as tumor, inflammatory rheumatism, rheumatoid diseases, etc and diseases caused by vascularization disorder, such as eye' s maculopathy, retinopathy, etc.

The invention belongs to the field of drug synthesis, relates to an arylphthalazine compound with a structure shown in a general formula (I) and its pharmaceutically acceptable salt and especially relates to an arylphthalazine compound containing piperazine, pyrrolidine or azetidine and its preparation method and use in medical science. An in-vitro Hedgehog signal path target gene Gli inhibition activity test proves that the compound has good Hedgehog signal path inhibition activity. The compound can be used for preparation of a novel anti-tumor drug.

The present specification provides crystalline forms of 4-[3-(3-[(cyclopropylamino)methyl]azetidine-1-carbonyl)-4-fluorobenzyl]phthalazin-1 (2H)-one hydrochloride, methods of preparing the same, and pharmaceutical compositions comprising the same.

The present invention relates to a method for solubilizing 5-amino-2,3-dihydro-1,4- phthalazinedione or salts thereof, to the solubilisate produced by this method and respective uses in pharmaceuticaldosage forms. A phosphatidylcholine-based solubilization method is disclosed.

The invention discloses a phthalazone compound crystal form N and a preparation method thereof, and belongs to the field of the medical chemistry, and specifically relates to a new crystal form of a compound [2(1H)-butyl-2-enoyl-3,4- dihydroisoquinoline-5-yl]-carbamic acid-4-[8-fluoro-(2H)-phthalazine-1-ketone] benzyl methanesulfonate with a tumor effect, a preparation method of the compound, a composition containing the crystal form, and application of the crystal form or the composition containing the crystal form in the medicine preparation. The N crystal form has good physical-chemical stability and particle size distribution uniformity, and is suitable for preparing the medicine preparation.

The invention discloses a phthalazine derivative, a preparation method and applications thereof, and belongs to the field of medicinal chemistry, wherein the phthalazine derivative prepared by the invention is a good PARP and HDAC double-target inhibitor. According to the invention, by using a design method based on a medicine splicing principle, the basic functional groups of a marketed medicineolaparib (PARP inhibitor) are reserved while a functional group structure capable of acting with HDAC protein is introduced into the tail part, so the designed brand-new compound can simultaneously inhibit PARP and HDAC, the advantages of the two inhibitors can be simultaneously provided, the combined effect of the two inhibitors can be completely provided, the low-toxicity and high-efficiency targeting antitumor inhibitor can be obtained, the application of the phthalazine derivative in the development of drugs for preventing and/or treating PARP and HDAC related diseases is developed, and the phthalazine derivative has great application value.

The invention discloses preparation and performance research of a phthalazine-based aggregation-induced emission molecule, belongs to a material chemistry technology, and particularly relates to a D-A-D structure molecule which is designed and synthesized by taking phthalazine as a center and has an aggregation-induced emission effect. The structural formula of the prepared luminescent material is shown in the description. The preparation comprises the steps of mixing 1, 4-dichlorophthalazine, 4-(diphenylamino) phenylboronic acid and tetrakis (triphenylphosphine) palladium in a tetrahydrofuran solution and a potassium carbonate solution; reacting at 80 DEG C for 12 hours; and after the reaction is finished, extracting the product with DCM, washing the organic phase with water for multiple times, drying with anhydrous magnesium sulfate, carrying out suction filtration, spin-drying the filtrate, and separating and purifying with silica gel column chromatography to obtain the final product. The luminescent material with the aggregation-induced emission effect is prepared from phthalazine molecules and triphenylamine. The raw materials are easily available and the synthesis method is simple. When the luminescent material is aggregated in a poor solvent, fluorescence enhancement can be seen, the phenomenon of fluorescence aggregation-induced quenching can be effectively avoided, and the material has relatively high thermal stability and is expected to be applied to a solid luminescent material.