59 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.

Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being phthalazinyl, pyrazinyl, pyridazinyl, or quinoxalinyl. Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine, or dopamine.

The present invention relates to novel compounds of the formula (I), wherein Het, A, Q, X1, X2, X3, R1 and R2 are defined in the specification, which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.

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 present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof:wherein R1 and R2 are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; X represents a cyano group, a nitro group, a halogen atom, a hydroxyimino group which may be substituted or a heteroaryl group which may be substituted; Y represents a heteroaryl group, an aryl group which may be substituted, an alkynyl group which may substituted, an alkenyl group, an alkyl group, an optionally substituted saturated or unsaturated 4- to 8-membered amine ring, and the cyclic amine compound is a monocyclic compound, bicyclic compound or a spiro compound; l is an integer of 1 to 3; provided that the case where l is 1 or 2, X is a cyano group, a nitro group or a chlorine atom, R1 is a chlorine atom, R2 is a methoxy group and Y is a 5- or 6-membered amine ring substituted with a hydroxyl group is excluded.

The invention relates to a phthalazine or benzo phthalazine derivative and a preparation method thereof. The structure of the compound is shown in the specification, wherein R is-OCH3C6H4,-CH3C6H4,-C6H5,-ClC6H4, p-CF3C6H4 or o-C5H4N. The phthalazine or benzo phthalazine derivative is synthesized by the reaction of cycloaddition reaction and inverse cycloaddition reaction for loss of a molecule of nitrogen, the reaction is in accordance with the atom economic reaction requirements, provides a new thinking way for construction of phthalazine or benzo phthalazine skeletons, and enriches synthetic methods of organic heterocyclic compounds, the synthetic method of the phthalazine or benzo phthalazine derivative is not reported in the literature. From the analysis of performance test, the phthalazine or benzo phthalazine derivative has certain absorption and emission spectra, and the quantum yield of the benzo phthalazine derivative is higher.

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 present invention comprises a new class of compounds useful for the prophylaxis and treatments of protein kinase mediated diseases, including inflammation and related conditions.

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.

Phthalazinediones that function as intracellular redox modulators in the redox therapy of certain stressed cells are provided. By buffering aberrant redox states, phthalazinediones enable cellular processes essential for survival and augment medical treatments. The phthalazinediones of the invention can modulate functions related to cell growth, differentiation, activity, or death, to correct aberrations and restore homeostasis, and can serve as adjunctive therapy in treating various disease conditions.

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.

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, IKur-associated disorders, and other disorders mediated by ion channel function.

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, IKur-associated disorders, and other disorders mediated by ion channel function.

The invention relates to 5-amino-2,3-dihydro-1,4-phthalazinedione or related compounds, compositions or combinations thereof, for use in the treatment of chronic progressive multiple sclerosis, in particular primary and secondary progressive multiple sclerosis. The invention in particular relates to the use of 5-amino-2,3-dihydro-1,4-phthalazinedione sodium salt for said purposes.

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 invention discloses a phthalazinone compound as well as a preparation method and medical application thereof, and particularly discloses a compound as shown in a formula (I) defined in the description and pharmacologically acceptable salt thereof, and application of the compound as an androgen receptor (AR) for degradation.

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 invention discloses a polymorphism preparation method and an application of 6-(4-chlorophenoxy)-tetrazolo[5,1-a]phthalazine. New crystal forms are comprehensively characterized by utilizing X-ray powder diffraction, thermogravimetic analysis, differential scanning calorimetry, infrared, Raman, hygroscopic analysis and the like. The stability, the hygroscopic property and the dissolvability of four new crystal forms are compared, and references are provided for selecting a best solid form of 6-(4-chlorophenoxy)-tetrazolo[5,1-a]phthalazine used in medicine development. The new crystal form preparation method of 6-(4-chlorophenoxy)-tetrazolo[5,1-a]phthalazine has the advantages of simplicity, easy control, good reappearance, and stable obtaining of target crystal forms.

The invention relates to a pyridazinone compound shown as a formula I or an isomer thereof, or a pharmaceutically acceptable salt, ester, a prodrug or a solvate thereof, a preparation method thereof,a pharmaceutical composition and an application of the pharmaceutical composition for preparing a dengue virus inhibitor. The pyridazinone compound has a structure shown in the formula I. The compoundor the pharmaceutical composition thereof has anti-dengue virus activity and better selectivity, and can be used for preventing and / or treating dengue virus infection.

The invention discloses a novel 4-(aminoalkyl)phthalazine-1-one compound (I) and pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition and use in the preparation of drugs for treating and / or preventing neurological related diseases, including but not limited to vascular dementia, Alzheimer's disease, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, glaucoma, ischemic stroke, hemorrhagic stroke, nerve injury caused by brain trauma and other diseases.

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.