52 results about "Isoindole" patented technology

The present invention provides a water-based dispersion comprising (a) nitrogen compound selected from 3a,4,7,7a-Tetrahydro-1H-isoindole-1,3(2H)-dione and 1,3- Dihydro-2H-isoindole-1,3-dione and (b) sulfonate-based dispersant, and further provides a process for producing phthalimide based fungicide which comprises (1) preparing a water-based dispersion comprising (a) nitrogen compound such as 3 a, 4, 7,7a- Tetrahydro- 1H-isoindole-1,3 (2H)-dione and 1, 3 -Dihydro-2H-i soindole-1,3- dione and (b) sulfonate-based dispersant, (2) reacting the dispersion of step (1) with aqueous alkaline solution, (3) reacting the resulting salt with mercapto-based compound selected from perchloromethyl mercaptan (PCMM) and pentachloro ethyl mercaptan (PCEM) to obtain phthalimide based fungicide such as folpet, captan and / or captafol.

This document relates to crystalline or amorphous forms of oxoisoindole-5-carboxamide compounds, or salts or solvates thereof. It also discloses compositions containing the crystalline or amorphous forms, as well as methods for preparing and using the crystalline or amorphous forms. The resulting crystalline or amorphous forms have excellent solid-state stability and are of great value in drug development, formulation development, and production.

The invention belongs to the field of organic synthesis, and particularly relates to a synthesis method of isoindolone. An N-methylbenzylamine compound as shown in a formula 1 and a 2-fluorobenzoic acid methyl ester compound as shown in a formula 2 are mixed with methyl tert-butyl ether in the presence of bis (trimethylsilyl) lithium amide and cesium fluoride, and the isoindolone as shown in a formula 3 is synthesized through reaction. The isoindolone derivative is synthesized through a one-pot method, and the method has the prominent advantages that raw materials are simple and easy to obtain, operation is easy and convenient, economy and environment friendliness are achieved, and the substrate applicability is wide.

The invention relates to an isoindole thioimine compound, preparation thereof and application of the isoindole thioimine compound as a sigma-2 receptor inhibitor. Catechol and isobutene are subjected to a series of reactions under certain conditions to obtain a solid product; carrying out a series of reactions on o-xylene and chlorosulfonic acid under certain conditions to obtain an oily product; and reacting the solid product with the oily product under a certain condition to obtain the isoindole thioimine compound. Compared with the prior art, when the isoindole thioimine compound prepared by the invention is combined with a sigma-2 receptor and allosteric regulates a sigma-2 receptor compound, the combination of adjacent A beta oligomers and a receptor on synapse is unstable, so that the A beta oligomers are removed from the synapse, the activity of the sigma-2 receptor can be effectively inhibited, and the activity of the sigma-2 receptor can be inhibited. The compound can be further used for preparing new medicines for treating tumors and neurodegenerative diseases.

The present invention relates to an isoindol-sulfilimine compound and its preparation and its use as a sigma-2 receptor inhibitor. Compared with the prior art, the isoindol-sulfilimine compound prepared by the present invention can effectively inhibit the sigma-2 receptor activity by binding to the sigma-2 receptor and deformationally regulating the sigma-2 receptor complex, which will lead to the instability of the binding of adjacent Aβ oligomers to the receptor on the synapse, thus leading to the removal of AB oligomers from the synapse. It can be further used for the preparation of new therapeutic drugs for tumor and neurodegenerative diseases.

The present disclosure discloses a lurasidone hydrochloride oral film composition, preparation method and use thereof. The present disclosure discloses the lurasidone hydrochloride oral film composition including an active pharmaceutical, a film-forming material, a plasticizer and a flavoring agent, wherein the active pharmaceutical is (3aR,4S,7R,7aS)-2-((1R,2R)-2-[4-(1.2-benzisothiazol3-yl)piperazine-1-methyl]cyclohexylmethyl)hexahydro-4.7-methylene-2H-isoindole-1,3-dione hydrochloride denoted by the following formula I. The lurasidone hydrochloride oral film composition of the present disclosure has a good dissolution rate, a uniform appearance, a good flexibility, and a uniformity content meeting the requirement. Moreover, during the preparation process of the film liquid of the composition, sedimentation of the film will not occur. After the composition is dissolved in the user’s mouth, the user does not have any gritty feeling.

The invention discloses application of a metabonomics marker combination in preparation of a product for identifying benign and malignant lung ground glass nodules. The metabonomics marker combination comprises the following 11 metabonomics markers: 5 '-S-methyl-5'-thioadenosine, 5 '-S-methyl-4'-thioadenosine, 5 '-S-methyl-4'-thioadenosine, 5 '-S-methyl-4'-thioadenosine, 5 '-S-methyl-4'- And gamma-glutamylglutamic acid; the component A is N-stearoyl-D-red sphingosine; sphingosine; palmitoyl ethanolamide; 2-(4-(diethylamino) butyl-2-alkyne-1-yl) isoindene-1, 3-diketone is used as a raw material; vesenadine; zolpidem; the preparation method comprises the following steps: adding 4-hydroxyl-3-(2 '-hydroxyl-1, 1'-biphenyl-4-yl)-6-oxo-6, 7-dihydrothieno [2, 3-b] pyridine-5-formonitrile into a reaction kettle, and stirring for 20-30 minutes; and D-erythro-sphingosine; the invention relates to 3-methylpyrrole-2, 4-dicarboxylic acid. According to the invention, 11 specific metabolic markers closely related to benign and malignant lung ground glass nodules are found, the AUC value of a diagnosis model constructed on the basis of the 11 metabolic markers is up to 0.888, and the diagnosis model has extremely high identification accuracy and specificity.

The invention discloses a pyrazolo [5, 1-a] isoindole derivative as well as a synthesis method and application thereof, and belongs to the technical field of organic chemical synthesis. The invention solves the problems of harsh reaction conditions, limited substrate range and the like of continuous multi-step synthesis of a precursor in the existing pyrazolo [5, 1-a] isoindole compound synthesis process. According to the invention, a polarity reversal strategy is adopted, a cyano group is introduced into 1, 5-enyne to change the electronic characteristics of 1, 5-enyne, diazo, olefin and ethynyl benzene are reacted under mild conditions, two rings and three new chemical bonds are constructed through a series of intermolecular [3 + 2] cycloaddition, intramolecular cycloaddition and elimination reactions, and pyrazolo [5, 5-a]-1, 5-a-phenanthrene is efficiently synthesized. According to the present invention, the 1, 1-a] isoindole derivative has characteristics of good synthesis yield, simple operation of the synthesis method, easily available raw materials, good substrate universality and step economy, and provides the effective strategy for the drug design synthesis.

The invention discloses fluoroalkyl substituted azafluorene and pyridopyrimidino isoindole compounds as well as a synthesis method and application thereof, and belongs to the technical field of organic synthesis and drug discovery. The preparation method comprises the following steps: mixing a 3-alkenyl-1, 2, 4-oxadiazolone compound 1, a fluoroalkyl acetylenic ketone compound 2, a catalyst, an additive and an organic solvent, and carrying out heating reaction to prepare a fluoroalkyl substituted azafluorene compound 3 and / or a fluoroalkyl substituted pyridopyrimidino isoindole compound 4. Experimental research discovers that the compound disclosed by the invention has the activity of obviously inhibiting proliferation of Hela and HCT-116 cancer cells, so that the compound disclosed by the invention has obvious anti-cancer activity on cervical cancer and / or colon cancer, has potential medicinal value, and provides a new structural unit for drug screening.

The invention discloses a radionuclide-labeled isoindole-piperidinedione derivative and application thereof, and the structural formula of the radionuclide-labeled isoindole-piperidinedione derivative is shown in the specification. E3 ubiquitin ligase key protein CRBN is used as a new target for nuclear medicine molecular imaging research; dynamic expression of CRBN in a tumor microenvironment is accurately described by constructing a targeted molecular probe with an isoindole-piperidinedione parent nucleus structure, imaging guidance is provided for clinically and accurately screening benefited people and predicting the therapeutic effect of targeted CRBN, and imaging examples are also provided for researching dynamic expression of other key proteins in a ubiquitination system.

The present invention relates to an injectable form comprising: (i) At least 1.5 mg / mL of 2-[6-(4- cyclopropyl-4h-1,2,4-triazol-3-yl)-2-pyridyl]-5-morpholinocarbonyl-1-isoindolinone; (ii) a solvent selected from the group consisting of polyethylene glycol 300 (PEG300), polyethylene glycol 400 (PEG400), and mixtures thereof; and (iii) a co-solvent selected from the group consisting of PEG300, PEG400, propylene glycol, and mixtures thereof.

Substituted derivatives of 5-(4-chlorophenyl)-2,3-dihydroimidazo[1,2-b]isoindol-5-ol and their uses in pharmaceutical compositions for the treatment of central nervous system diseases or disorders are provided.

Substituted derivatives of 5-(4-chlorophenyl)-2,3-dihydroimidazo[1,2-b]isoindol-5-ol and their uses in pharmaceutical compositions for the treatment of central nervous system diseases or disorders are provided.

Relates to a crystal form or an amorphous form of an oxoisoindole-5-carboxamide compound or a salt and a solvate of the oxoisoindole-5-carboxamide compound. The invention also discloses a composition containing the crystal form or the amorphous form, and a preparation method and application thereof. The obtained crystal form or amorphous form has good solid stability, and has very important value for drug development, preparation development and production.

The present disclosure relates to the field of pharmaceutical chemistry. Specifically, the present invention relates to a crystal form of a selective PARP-1 inhibitor hydrochloride, i.e., a crystal form of a hydrochloride of compound A having a structure of 2-(1-cyclohexylpiperidin-4-yl)-3-oxo-2,3-dihydro-1H-isoindole-4-carboxylic acid amide, a preparation method therefor, and a use thereof. The crystal form of the hydrochloride of compound A provided by the present disclosure has at least one of the following excellent characteristics: good stability, high purity, good solubility, good dissolution, high bioavailability, low hygroscopicity, high melting point, good fluidity, good mechanical stress stability, good machinability such as good compressibility, good crystal morphology, good compression resistance, stable storage, avoiding crystal transformation of a drug during development and storage, simple and reliable preparation method, and great development value.

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in a method for the treatment of sepsis in a subject in need thereof. The compounds of the present invention can be used in monotherapy or in combination with another antimicrobial agent.

Isoindole derivatives, the compounds of general formula (I), their stereoisomers are disclosed: #imgabs0# wherein R1, R2, R3 and R4 are as defined in the present disclosure.

The present invention relates to 2,3-dihydro-1H-isoindol-1-one derivatives, their pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the voltage-gated sodium channel Nav1.1.

A lurasidone hydrochloride oral soluble film composition, a preparation method therefor and a use thereof are provided. The lurasidone hydrochloride oral soluble film composition contains an active drug, a film-forming material, a plasticizer and a flavoring agent. The active drug is (3aR,4S,7R,7aS)-2-((1R,2R)-2-[4-(1.2-benzisothiazole 3-yl)piperazine-1-methyl]cyclohexylmethyl)hexahydro-4.7-methylene-2H-isoindole-1,3-dione hydrochloride, as shown in Formula I.

Substituted derivatives of 5-(4-chlorphenyl)-2, 3-dihydroimidazo [1, 2-b] isoindol-5-ol and their use in pharmaceutical compositions for the treatment of central nervous system diseases or disorders are provided.

Provided are a lurasidone hydrochloride orally dissolving film composition, a preparation method and application thereof. The lurasidone hydrochloride orally dissolving film composition comprises an active drug, a film forming material, a plasticizer and a flavoring agent, and the active drug is (3aR,4S,7R,7aS)-2-((1R,2R)-2-[4-(1.2-benzisothiazole 3-yl)piperazine-1-methyl]cyclohexylmethyl)hexahydro-4.7-methylen-2H-isoindole-1,3-dione hydrochloride salt as shown in formula I. The obtained lurasidone hydrochloride orally dissolving film composition has a good dissolution rate, does not have a sand feeling after dissolving in the oral cavity, has a uniform appearance, good flexibility, and does not have sedimentation during the preparation of the film liquid, and the content uniformity meets the requirements.

An isatin-based indolodihydrochromene anti-tumor compound and its synthesis method. The chemical structural formula of the compound is shown in Formula 3. The synthesis method is as follows: The isatin-derived propargyl alcohol and 2-indolylphenol derivative are added to ethyl acetate as reaction raw materials, and under the catalysis of p-toluenesulfonic acid, the reaction is stirred at 25 °C for 8-12 hours. The reaction is tracked by TLC until it is complete, and then filtered, concentrated, and purified to obtain the product. The isatin-based indolodihydrochromene compounds synthesized in the present invention, through bioactivity tests, show that these derivatives have high sensitivity and strong cytotoxic activity against human nasopharyngeal carcinoma cells HONE-1. The reaction conditions of the present invention are relatively conventional, the reaction process is mild, simple, and low-cost, suitable for large-scale industrial production, and broaden the scope of application of this method; the present invention uses a relatively large variety of substrates as reactants, obtaining products with diverse structures and high yields.

The invention belongs to the technical field of organic synthesis, and particularly relates to an isoindole-1, 3-diketone derivative as well as a synthesis method and application thereof. The invention designs and synthesizes a series of isoindole-1, 3-diketone derivatives with novel structures based on a virtual screening method of a protein structure. The isoindole-1, 3-diketone derivatives with different structures are prepared by taking m-nitroaniline as an initial raw material through condensation reaction, reductive hydrogenation and amidation reaction, can prevent and control the magnaporthe oryzae, and shows dose dependence on inhibition of the magnaporthe oryzae. A design thought is provided for the isoindole analogue, and a certain reference is provided for research and development of novel anti-magnaporthe oryzae drugs.

The application discloses a phenyl isoindolinone and zidovudine splicing compound and a preparation method and application thereof. The compound has potential biological activity, provides a compound source for biological activity screening, has important application value for drug screening and the pharmaceutical industry, and through in-vitro anti-tumor activity screening, it is found that the compound can selectively inhibit human lung cancer NCI-H1975 cells, and the selectivity index of the compound to normal cells BEAS-2B is high (the inhibition rate is only 12.51 %), the safety is about 7.2 times of that of osimertinib, and the compound exhibits good tumor cell selectivity and low potential side effects. In combination with the changes of NCI-H1975 cell mitochondrial ROS and membrane potential, it is indicated that the phenyl isoindolinone and zidovudine splicing compound derived from an EGFR allosteric inhibitor can play an anti-tumor role by affecting mitochondrial function.

The invention relates to the technical field of organic synthesis and the technical field of fine chemical engineering, in particular to an eight-membered ring parallel diisoindole heterocyclic hydrazone boron aza fused ring compound as well as a preparation method and application thereof. The structure of the eight-membered ring parallel diisoindole heterocyclic hydrazone boron aza fused ring compound is as shown in a formula (I). Wherein Ar is nitrogen-containing heterocyclic aryl, and R is selected from one of aryl, heterocyclic aryl and alkyl. According to the octatomic ring parallel diisoindole heterocyclic hydrazone boron nitrogen heterocyclic fused ring compound, the solubility, the molecular energy level and the photo-physicochemical properties of the compound are respectively regulated and controlled by regulating and controlling substituent groups on boron of a molecular skeleton, peripheral heteroatoms and fused ring modification, and a series of novel boron nitrogen full fused ring molecules are constructed. Meanwhile, the preparation method of the octatomic-ring parallel diisoindole heterocyclic hydrazone boron aza fused ring compound is simple and convenient, the reaction condition is mild, the raw materials are easy to obtain, the compound is easy to amplify for industrial preparation, and the compound has a wide application prospect.

The invention belongs to the field of organic synthesis medicines, and particularly discloses an isoindolone compound, a compound with a structure as shown in a formula (I) or a formula (II) or a formula (III) or pharmaceutically acceptable salt of the compound, or / and pharmaceutically acceptable salt of the isoindolone compound. The invention provides a series of isoindolone compounds which can be used as GPR139 receptor agonists, and proves that some embodiments of the series of isoindolone compounds can show good agonistic activity on GPR139 receptors, are remarkable in drug-likeness, have good medicinal potential for treating mental system diseases, are wide in market prospect, and can be used for preparing the GPR139 receptor agonists. The preparation method is simple and convenient, mild in reaction condition, convenient to operate and control, low in energy consumption, high in yield, low in cost and suitable for industrial production.

The application discloses a preparation method of a tetrahydrobenzo[f]isoindole compound. The tetrahydrobenzo[f]isoindole compound is prepared by taking 1,6-alkynyl compound as raw material, taking alkaline substance as additive, and performing a cyclization reaction in an organic solvent. The structural formula of the 1,6-alkynyl compound is R is one of phenyl, p-fluorophenyl, p-chlorophenyl, p-bromophenyl, p-tert-butylphenyl, p-benzophenyl, p-methoxyphenyl, p-trifluoromethylphenyl, m-chlorophenyl, m-methoxyphenyl, m-cyanophenyl, m-formylphenyl, 3,5-dimethoxyphenyl, o-methoxyphenyl, o-methylphenyl, 1-naphthyl, 2-thienyl, 3-thienyl and p-methylphenyl. The preparation method of the tetrahydrobenzo[f]isoindole compound is characterized by using cheap and easily obtained alkaline substance as additive, using green and low-toxicity solvent, simple and mild reaction condition, high regioselectivity and the ability to be used for the development of heterocyclic drug molecules.

The invention provides an isoindolone-containing CDK4 / 6 inhibitor and a preparation method and application thereof.The preparation method comprises the steps that ethyl bromoacetate is introduced to a piperazine group of a palbociclib structure to be hydrolyzed into acid, then amido bonds are generated to be linked with different isoindolone, and a series of compounds shown in the formula I are synthesized; the compound can be used for preventing or treating mammalian diseases related to abnormal expression of CDK4 / 6 and anti-tumor, anti-virus, antibacterial and anti-inflammatory related to CDK4 / 6. I.