19600results about "Organic chemistry methods" patented technology

The invention relates to the technical field of medicines, and provides a use of a heterocyclic anti-tumor compound, in particular a use of the heterocyclic anti-tumor compound in the preparation of a medicine for preventing and / or treating tumors or cancers. The compound has a tri-heterocyclic structure (for example, a structure as shown in formula (B)), has a novel structure, and provides a new direction for the development of SOS1 inhibitor drugs.

The invention relates to a pharmaceutically acceptable salt of a benzothiophene substituted fused ring compound, and a crystal form and application thereof. Specifically, the present disclosure provides a pharmaceutically acceptable salt of 2-amino-7-fluoro-4-((5S, 5aS, 6S, 9R)-1-fluoro-12-((1-((4-(fluoromethylsubunit) piperidine-1-yl) methyl) cyclopropyl) methoxyl)-5-methyl-5a, 6, 7, 8, 9, 10-hexahydro-5H-4-oxa-3, 10a, 11, 13, 14-pentaaza-6, 9-methylbridged naphtho [1, 8-ab] heptano-2-yl) benzo [b] thiophene-3-formonitrile, a crystal form and a preparation method thereof, and a preparation method of the pharmaceutically acceptable salt, the crystal form and the preparation method thereof. Corresponding salts have good stability and can be better used for clinical treatment. # imgabs0 #

Disclosed herein are crystalline forms of phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) isoform alpha (PI3Kα) inhibitors, and formulations and uses of same.

This disclosure provides salts, crystalline forms, and formulations of a KRAS inhibitor, and methods of making and using thereof.

Provided herein are polymorphs and crystalline forms of 2-fluoro-5-((5S,5aS,6S,9R)-1-fluoro-12-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-5-methyl-5a,6,7,8,9,10-hexahydro-5H-4-oxa-3,10a,11,13,14-pentaaza-6,9-methanonaphtho[1,8-ab]heptalen-2-yl)-3-methyl-4-(trifluoromethyl)aniline (Compound of Formula (I)), pharmaceutical compositions thereof, and methods of their use, for example, in the treatment of cancer. Also provided herein are synthetic processes for the manufacture of a compound of Formula (I) (i.e., 2-fluoro-5-((5S,5aS,6S,9R)-1-fluoro-12-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)-5-methyl-5a,6,7,8,9,10-hexahydro-5H-4-oxa-3,10a,11,13,14-pentaaza-6,9-methanonaphtho[1,8-ab]heptalen-2-yl)-3-methyl-4-(trifluoromethyl)aniline). Also provided are compounds useful in its synthesis (e.g., those of Formulae (A), (B), (By), and (H)) and synthetic processes directed thereto.

The invention provides a tetrahydropyridinopyrazole derivative and application thereof in medicine, and particularly relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, a pharmaceutically acceptable salt or eutectic of the compound, and an intermediate and a preparation method of the tetrahydropyridinopyrazole derivative. The invention also relates to application in preparation of related medicines for treating diabetes mellitus. # imgabs0 #

In order to solve the problem that an existing high-voltage lithium ion battery is insufficient in high-temperature performance and safety performance, the invention provides a cyclic carbonate-sulfate compound and application thereof, a non-aqueous electrolyte and a secondary battery, and the cyclic carbonate-sulfate compound comprises a compound as shown in a chemical formula 1, the specific rotation [alpha] of the cyclic carbonate-sulfate compound ranges from-7.982 degrees mL / (dmg) to + 7.982 degrees mL / (dmg), and the specific rotation [alpha] of the cyclic carbonate-sulfate compound ranges from-7.982 degrees mL / (dmg) to + 7.982 degrees mL / (dmg); the chemical formula 1 of the # imgabs0 # is shown in the specification. When the cyclic carbonate-sulfate compound provided by the invention is used as an electrolyte additive, a formed solid electrolyte membrane is smoother and more ordered, so that the cyclic carbonate-sulfate compound has higher high-temperature stability, especially membrane layer stability under a thermal shock condition.

An advantageous isolated morphic form of trilaciclib which is 2′-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7′,8′-dihydro-6′H-spiro[cyclohexane-1,9′-pyrazino[1′,2′:1,5]pyrrolo[2,3-d]pyrimidin]-6′-one, for example in the form of a di-hydrochloride salt or a dihydrochloride, dihydrate.

The invention aims to provide a crystal form of a thyroid hormone receptor agonist, a preparation method, a pharmaceutical composition and application of the crystal form in preparation of a TRbeta selective agonist medicine. Compared with the prior art, the crystal form provided by the invention has one or more improved properties, and is of great significance to further development of the medicine.

A compound having the following structure of Formula (I): or a stereoisomer of the compound, tautomer of the compound, or salt thereof, wherein R1, R2, L, X, Y, A, and B are as defined herein. Pharmaceutical composition comprising the compounds, and their use in methods of treating diseases are also described.

The present disclosure relates generally to various salt forms and compositions thereof useful for the modulation of interleukin-1 receptor-associated kinase 4 ("IRAK4") via ubiquitination and / or degradation and uses of the same in the treatment various diseases.

The disclosure provides methods for treating a subject in need thereof comprising administering to the subject a therapeutically-effective dose of psilocybin. The methods described herein may be used to treat a variety of diseases, disorders, and conditions. For example, the methods may be used to treat anxiety disorders, eating disorders, and headache disorders.

The invention relates to the technical field of fluorescence sensing development, in particular to a Cd (II)-based metal organic framework crystalline material as well as a preparation method and application thereof. The chemical formula of the Cd (II)-based metal organic framework crystalline material is {[Cd3 (H2O) 2 (DMA) 2 (5-CMOIA) 2]. 6 / 5H2O} n, the organic framework material is characterized by an X-ray single crystal diffractometer, and the result shows that the organic framework material is crystallized in a triclinic system P-1 space group, the asymmetric unit of the organic framework material is composed of three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions, three Cd (II) ions and three The complex is composed of two deprotonated (5-CMOIA) 3-ligands, two coordinated DMA solvent molecules, two coordinated water molecules and six fifths of crystal water molecules. The solid fluorescence spectrum of the Cd (II)-based metal organic framework crystalline material is measured, the fluorescence response of the Cd (II)-based metal organic framework crystalline material to metal ions in a solution is explored, and the result shows that the Cd (II)-based metal organic framework crystalline material can effectively recognize Hg < 2 + > from different ions and can be applied to the field of fluorescence sensing.

The invention relates to the technical field of organic synthesis, in particular to a method for constructing Orforglipron pyran ring chirality through enzyme catalysis, which comprises the following steps: step S1, taking SM1 and SM2 as raw materials, and reacting under the action of a palladium catalyst and a ligand to obtain INT-1; step S2; carrying out hydrogenation reduction on double bonds of the INT-1 under the catalysis of Pd / C to obtain INT-2; s3, carrying out hydrolysis resolution on the INT-2 in a solvent, a buffer salt system and enzyme catalysis to obtain a chiral pure intermediate INT-3; step S4, performing ring closing on the INT-3 through a Grignard reaction to synthesize a lactone intermediate INT-4; and S5, carrying out Diball-H reduction, quenching, dichloromethane extraction and anhydrous sodium sulfate drying on the INT-4, and then reducing by using triethyl silane to obtain the compound with the general formula A. Chirality is constructed through enzyme catalysis, isomer impurities do not need to be split and separated through SFC when the chirality is constructed, loss is reduced, the yield is increased, and a target product is obtained with high yield and high chiral selectivity; meanwhile, the cost is relatively reduced, and the cost is saved.

The invention discloses a tetranuclear ladder type organic tin carboxylate complex as well as a preparation method and application thereof, and belongs to the technical field of metal complexes, the tetranuclear ladder type organic tin carboxylate complex is prepared by taking para-position or ortho-position substituted benzoic acid as a ligand and taking organic tin dimethyl tin oxide as a substrate. The preparation method is simple to operate and mild in condition. The tetranuclear ladder type organic tin carboxylate complex can be used as a photocatalyst for photocatalytic production of H2O2, and the photocatalytic H2O2 production rate is as high as 5.12 * 10 < 3 > [mu] mol.g <-1 >. H <-1 > and is higher than the H2O2 production rate of a photocatalyst reported in the existing literature.

The disclosure provides methods for treating a subject in need thereof comprising administering to the subject a therapeutically-effective dose of psilocybin. The methods described herein may be used to treat a variety of diseases, disorders, and conditions. For example, the methods may be used to treat anxiety disorders, eating disorders, and headache disorders.

The invention provides a baricitinib phthalate crystal form, and relates to the technical field of crystal form drug molecules. The crystal form is radiated by Cu-K alpha, and an X-ray diffraction pattern represented by 2 theta has characteristic peaks at 6.20 + / -0.2 degrees, 6.53 + / -0.2 degrees, 14.53 + / -0.2 degrees, 18.29 + / -0.2 degrees, 18.53 + / -0.2 degrees, 18.70 + / -0.2 degrees, 19.44 + / -0.2 degrees and 26.95 + / -0.2 degrees; the crystallographic measurement parameters are as follows: an orthorhombic system is adopted, and the space group is Pbcn; the cell parameters are as follows: # imgabs 0 # alpha = 90 degrees, beta = 90 degrees, gamma = 90 degrees, and the cell volume # imgabs 1 #. The invention also provides a related preparation method and application. The baricitinib phthalate crystal form disclosed by the invention is good in stability and relatively high in solubility and permeability.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof) that degrade and / or otherwise modulate (e.g., inhibit) NIMA Related Kinase 7 (NEK7). Said chemical entities are useful, e.g., for treating a subject (e.g., a human subject) having one or more disorders or diseases associated with NLRP3 inflammasome activation. Said disorders or diseases include but are not limited to, autoinflammatory and autoimmune disorders (e.g., gout, inflammatory bowel disease, rheumatoid arthritis, multiple sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease), cardiovascular and metabolic disorders (eg. pericarditis, atherosclerosis, Type 2 diabetes, obesity, and metabolic syndrome), fibrotic disorders (e.g. interstitial lung disease, chronic kidney disease), hematology (eg. anemia of inflammation) and eye disorders (eg. macular degeneration). In embodiments, and while not wishing to be bound by theory, it is believed that the chemical entities described herein directly target (e.g., directly bind to) NEK7, thereby altering (e.g., attenuating) the inflammatory response modulated by the NLRP3 inflammasome. This disclosure also features compositions containing the same as well as methods of using and making the same.

Embodiments of the present invention provide methods and intermediates for the large scale preparation of 2, 4, 6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl] benzamide hemisuccinate, as well as formulations and product forms prepared by these methods. Embodiments of the present invention further provide for the preparation of lamidetan acetate (2, 4, 6-trifluoro-N-[6-(1-methylpiperidine-4-carbonyl)-2-pyridyl] benzamide acetate) and / or a pharmaceutical composition thereof, and / or the use of lamidetan acetate and formulations thereof in subcutaneous drug delivery.

The disclosure relates to a light-emitting device including a first electrode, a second electrode facing the first electrode, and an interlayer disposed between the first electrode and the second electrode and including an emission layer. The interlayer includes a first compound represented by Formula 1 of the specification, a second compound represented by Formula 2 of the specification, and a third compound, which is a blue phosphorescent compound. The disclosure also relates to an electronic apparatus including the light-emitting device.

The invention relates to a fused heteroaryl compound, a preparation method thereof and application of the fused heteroaryl compound in medicine. Specifically, the invention relates to a fused heteroaryl compound as shown in a general formula (I), a preparation method thereof, a pharmaceutical composition containing the compound and application of the compound as a therapeutic agent, in particular to application of the compound in preparation of drugs for inhibiting KRAS amplification and / or mutant activity. Wherein each group in the general formula (I) is defined in the specification. # imgabs0 #

The disclosure provides methods for treating a subject in need thereof comprising administering to the subject a therapeutically-effective dose of psilocybin. The methods described herein may be used to treat a variety of diseases, disorders, and conditions. For example, the methods may be used to treat neurocognitive disorders (e.g., Alzheimer's disease, Parkinson's disease), ADHD, Epilepsy, Autism, Sleep-wake disorders, Chronic pain, Inflammatory Disorders, IBD, Stroke, ALS, and / or Multiple Sclerosis.

The present disclosure provides a class of compounds represented by formula (I '), or tautomers, stereoisomers or pharmaceutically acceptable salts thereof. The compound disclosed by the invention has a relatively strong agonistic effect on GLP-1R, can be used for treating diseases such as diabetes mellitus, metabolism-related fatty liver diseases, Alzheimer's disease and the like or has an effect of reducing weight. # imgabs0 #

The present disclosure provides crystalline forms, solvates and hydrates of (R)-5-fluoro-2-methyl-1-((R)-5-(pyridin-2-yl)-2,3-dihy dro-lH-indene-2-carbonyl)indoline-6- sulfonamide, and methods of making.