122 results about "Azetidine" patented technology

Disclosed is a pharmaceutical composition for the treatment of tumors, the pharmaceutical composition comprising (6S, 9aS)-N-benzyl-8-({6-[3-(4-ethylpiperazin-1-yl) azetidin-1-yl] pyridin-2-yl} methyl)-6-(2-fluoro-4-hydroxybenzyl)-4, 7-dioxo-2-(propyl-2-en-1-yl) hexahydro-2H-pyrazino [2, 1-c] [1, 2, 3] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [1, 2, 4] triazolo [ The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof and administered in combination with a MEK inhibitor.

The present invention relates to compounds of formula (I), their synthesis and their use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders. [Formula 1] TIFF2023523300000191.tif51156

An aerosol generating material for use in an aerosol delivery device is provided, the aerosol generating material including a fibrous plant material, an aerosol former, and an active agent including at least a substituted 3-(1-methylpyrrolidin-2-yl)pyridine, a 3-(azetidin-2- yl)pyridine, or a 3-(azetidin-2-ylmethoxy)pyridine. The active agent is absorbed or adsorbed in or on the fibrous plant material. The disclosure further provides devices and aerosol provision systems incorporating such aerosol generating material.

To provide crystalline forms of a C-C chemokine receptor type 4 antagonist.SOLUTION: There is provided the compound 2 - ((R) - 3 - (1 - (1 - ((R) - 1 - (2, 4-dichlorophenyl) ethyl) - 3 - (trifluoromethyl) - 1H - pyrazolor3, 4-b] pyrazin-6-yl) azetidin-3-yl) piperidin-1-yl) ethan-1-ol benzenesulfonate in crystalline form.SELECTED DRAWING: Figure 1

The invention is directed to an aqueous binder composition for MMVF fibres comprising one or more protein(s) of non-plant origin; one or more saccharides, a crosslinker comprising at least two azetidinium functional groups and at least one hydrophobic agent. Methods for producing MMVF fibres, MMVF fibre products and uses are also disclosed.

The application discloses a preparation method of baricitinib, and belongs to the technical field of drug synthesis. The method comprises the following steps: firstly, 2-[1-(ethylsulfonyl)-3-azetidinyl]acetonitrile and 4-pyrazole boron pinacol ester are subjected to a Michael addition reaction to obtain 1-(ethylsulfonyl)-3-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]-3-azetidine acetonitrile as an intermediate I; secondly, a protection group is introduced on the amino group of 4-chloropyrrolopyrimidine to obtain an intermediate II; finally, the intermediate I and the intermediate II are subjected to a Suzuki coupling process by adopting a method of combining a nickel pre-catalyst with a supporting ligand to obtain the baricitinib. The preparation method creatively realizes cross coupling of the baricitinib by adopting the cheap metal nickel as a catalyst, avoids the use of a heavy metal palladium catalyst, and has the advantages of low cost, low toxicity, small pollution, green environmental protection and the like.

The invention relates to an adhesive composition comprising:ground pea seeds comprising between 5 wt % and 40 wt % of crude proteins on the total weight of the ground pea seeds,an amine-based azetidinium-functional cross-linker, andwater.The invention also relates to an article and its preparation process, use of the adhesive composition according to the invention, and use of ground pea seeds.

The invention discloses a method for determining L-azetidine-2-carboxylic acid, and provides a method for detecting AZE in food, living body and environment by adopting a liquid chromatography-tandem mass spectrometry and selecting a positive and negative ion switching scanning mode. The method can be used for screening the content of AZE in food and guiding the diet of C9-ALS patients. The method is high in detection sensitivity, the detection limit of AZE is 2.0 ng / L, the accuracy is high, and the method is superior to an existing detection technology.

The present invention relates to compounds of formula (I) or formula (II) or pharmaceutically acceptable salt, solvate or hydrate thereof, wherein said compound of formula (I) and said compound of formula II each comprises at least one ONO2 or ONO moiety; R1 is C1-C3alkyl; R2 is H, C1-C6alkyl, C3-C6cycloalkyl, C1-C2alkoxy, C2-C4alkenyl; R3 is C1-C4alkyl optionally substituted with C1-C2alkoxy, C3-C4cycloalkyl, C2-C4alkenyl; R4 and R5 are each independently H or C1-C6alkyl optionally substituted with F, OH, ONO, ONO2, COOH, C1-C3alkoxy, C3-C6cycloalkyl; or together with the nitrogen atom to which they are attached form a heterocyclic ring, wherein preferably said heterocyclic ring is selected from aziridine, azetidine, pyrollidine, piperidine, morpholine, piperazine, homo-piperazine, 2,5-diazabicyclo[2,2,1]heptane and 3,7-diazabicyclo[3,3,0]octane, wherein said heterocyclic ring is optionally substituted with independently one or more R6; R6 is C1-C6alkyl optionally substituted with independently one or more halogen, OH, ONO, ONO2, C1-C3alkoxy, C1-C3haloalkoxy, COOR7, NR8R9, C═NR10; R7 is H, or C1-C4alkyl optionally substituted with F, OH, ONO, ONO2, NR8R9; R8 and R9 are independently H, or C1-C4alkyl optionally substituted with ONO, ONO2; R10 is C1-C4alkyl optionally substituted with F, ONO, ONO2; C3-C6cycloalkyl; pharmaceutical compositions thereof, and their use in methods of treating or preventing a disease alleviated by inhibition of PDE5 in a human or in a non-human mammal.

A method for the synthesis of diazabicyclo[6.2.0]decane compounds is provided. The synthesis proceeds by stereoselective synthesis of a chiral lactone followed by azetidine formation via a series of chemoselective reactions. Bicyclization results with the formation of diazobicyclo[6.2.0]decane related compounds.

Aerosol generating articles adapted for use in an aerosol delivery device are provided. The aerosol generating articles include an aerosol generating material and an aerosol-modifying agent, wherein the aerosol-modifying agent includes a substituted 3-(1-methylpyrrolidin-2- yl)pyridine, a 3-(azetidin-2-yl)pyridine, or a 3-(azetidin-2-ylmethoxy)pyridine. The disclosure further provides devices incorporating such aerosol generating articles.

The invention discloses a method and a system for preparing a 4-AA medical intermediate through continuous flow ozone oxidation. The method comprises the following steps: continuously introducing a raw material solution containing (3R)-3-((R)-1-((tert-butyldimethylsilyl) oxy) ethyl)-1-(4-methoxyphenyl)-4-oxo azetidine-2-yl acetate and a gas containing ozone into a microreactor for reaction; after the reaction liquid is subjected to reduction quenching, the (3R, 4R) 4-acetoxyl-3-[R-(tert-butyldimethylsiloxy) ethyl]-2-azetidinone is obtained. On one hand, the reaction time is shortened from the hour level to the minute level, and the production efficiency is remarkably improved; and on the other hand, the reaction temperature is increased to 10-30 DEG C from deep cooling, so that the refrigeration energy consumption and the equipment requirement are greatly reduced. According to the invention, local peroxidation is fundamentally avoided, byproducts are obviously reduced, the product purity is improved, the method is suitable for continuous operation, the reaction process is controllable, and the method is safe and reliable.

The present invention relates to a novel salt of an imidazo[1,2-a] pyridine compound, and more specifically, to azetidin-1-yl\{8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl\}methanone diphosphate and a method for preparing same. The azetidin-1-yl\{8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl\}methanone diphosphate according to the present invention has excellent solubility, volume density, light / temperature stability, acid / base stability, and the like, and thus can be usefully used in the formulation of pharmaceuticals.

The present disclosure includes azetidine tryptamines and methods of treating psychiatric disorders with such compounds. Also provided are pharmaceutical compositions comprising azetidine tryptamine.

The present invention provides a method for producing a coated silicone hydrogel contact lens in a cost effective manner. The method comprises: obtaining a preformed silicone hydrogel contact lens, the preformed silicone hydrogel contact lens comprising a bulk silicone hydrogel material, the bulk silicone hydrogel material comprising repeating units of at least one vinyl monomer containing a carboxyl group and at least one vinyl monomer containing an aryl dihydroxy boron group; and a polymer composition comprising a water-soluble and thermally crosslinkable polymer material having an azetidinium group or an epoxy group and a polymer material having 1, 2-or 1, 2, 3, 3, 3, 3-tetrafluoropropene, heating the preformed silicone hydrogel contact lens in an aqueous coating solution of a glycol-containing hydrophilic polymer having a 1, 3-diol moiety to form a coated silicone hydrogel contact lens comprising a bulk silicone hydrogel material and a hydrogel coating, the hydrogel coating comprises a cross-linked polymeric material covalently attached to the bulk silicone hydrogel material and a grafted glycol-containing hydrophilic polymer covalently attached to the bulk silicone hydrogel material and distributed in the cross-linked polymeric material.

The present disclosure relates to amorphous forms of (6-(4-((4-(1H-pyrazol-4- yl)phenyl)amino)pyrimidin-2-yl)-1-methyl-1H-indol-2-yl)(3,3-difluoroazetidin-1-yl)methanone (Compound A) and processes for preparing amorphous forms of Compound A. The present disclosure also provides pharmaceutical dosage forms comprising the amorphous forms of Compound A as an active pharmaceutical ingredient and methods of preparing the pharmaceutical dosage forms.

The present application relates to compounds of formula (Ia) or (Ib): or a salt, solvate, or tautomer thereof; wherein R1, and R2 are independently selected from optionally substituted C1 to C 8 alkyl; or R1 and R2 together with the silicon atom to which they are attached form an optionally substituted 5- or 6-membered ring; R3, and R4 are independently selected from H, optionally substituted C1 to C 8 alkyl; optionally substituted C1 to C 8 haloalkyl; or R3 and R4 together with the nitrogen atom to which they are attached form an optionally substituted azetidine or pyrrolidine ring; R3', and R4' are independently selected from H, optionally substituted C1 to C8 alkyl; optionally substituted C1 to C 8 haloalkyl; or R3' and R4' together with the nitrogen atom to which they are attached form an optionally substituted azetidine or pyrrolidine ring;R5 is selected from a negative charge, H, C1 to C 8 alkyl, or optionally substituted aryl; a is 0 or 1; and Z is a divalent linker group; and to fluorophore compositions comprising such compounds, to assay methods and to kits using such fluorophore compositions.

The invention discloses a synthesis method of 1-(t-butyloxycarboryl)-3-ethoxy azetidine-3-carboxylic acid, and the synthesis route is as follows: the invention discloses a preparation method of 1-(t-butyloxycarboryl)-3-ethoxy azetidine-3-carboxylic acid, which comprises the following steps: by taking 3-oxo azetidine-1-carboxylic acid tert-butyl ester as a raw material, reacting at the temperature of 60-80 DEG C for 2-4 hours, and then adding a catalyst, thereby obtaining the 1-(t-butyloxycarboryl)-3-ethoxy azetidine-3-carboxylic acid. Under an alkaline condition, chloroform and ethanol are mediated, so that a keto carbonyl group of the 3-oxo-azetidine-1-carboxylic acid tert-butyl ester is converted into an ethyoxyl carboxylic acid group, and the target compound 1-(t-butyloxycarbonyl)-3-ethyoxyl azetidine-3-carboxylic acid is obtained. The synthesis method is low in cost, mild in reaction condition, low in potential safety hazard, ideal in yield and simple and efficient in operation, and a potential route is provided for large-scale production of the compound 1-(t-butyloxycarbonyl)-3-ethoxyazetidine-3-carboxylic acid.

The present disclosure provides azetidine compounds of Formula I and their pharmaceutically acceptable salts, their compositions, and methods for their use in determining azetidine compound binding to proteins. The azetidine compounds are useful as probes, for monitoring diacylglycerol kinase activity, and for identifying druggable targets.

The invention provides a method of assessing the appropriate therapeutic dose of 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid to administer to a patient in need thereof, comprising the steps of:(i) testing whether or not the patient has the poor metabolizer genotype; and(ii) if the patient does not have the poor metaboliser genotype, administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient at the standard therapeutic dose; and(iii) if the patient does have the poor metaboliser genotype, either(a) administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient at a therapeutic dose below that of the standard therapeutic dose; or(b) not administering 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid, or a pharmaceutically acceptable salt thereof, to the patient.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a gas emulsification composition as well as a preparation method and application thereof. The gas emulsification composition is prepared from the following components in percentage by mass: 0.1%-2.0% of a compound X, 5%-20% of a solvent, 1%-10% of a nonionic surfactant, 0.5%-5% of an anionic surfactant, 0.3%-0.8% of a rheology modifier, 3%-15% of a propellant and the balance of water, totaling 100%, wherein the compound X is {1-(ethylsulfonyl)-3-[4-(7H-pyrrolo [2, 3-d] pyrimidine-4-yl)-1H-pyrazol-1-yl] azetidine-3-yl} acetonitrile, and the compound X is a compound R2, a compound R3 and a compound R4, the mass ratio of the nonionic surfactant to the anionic surfactant is (1-4): 1. The gas emulsion composition prepared by the invention has excellent foam performance, high skin permeation efficiency and good stability.

The application belongs to the technical field of biological medicine, and discloses a kind of targeted inhibition drug and its application in preparation of prevention and treatment of pancreatic cancer preparation.The drug belongs to azetidine compound, which is the targeted inhibitor of STAT3, and can be directly used in the preparation of prevention and treatment of pancreatic cancer drugs, providing a new approach and technical idea for the treatment of pancreatic cancer.Through the international common pancreatic cancer modeling method, combined with experimental conclusion shows that the compound can effectively inhibit the tumor growth state of nude mice pancreatic cancer, inhibit cell growth related protein expression, inhibit mitochondrial complex enzyme activity and induce cell apoptosis, has a significant prevention and treatment effect on pancreatic cancer, and is expected to become a drug for the treatment of pancreatic cancer.

The present disclosure includes azetidinyl tryptamines and methods of using such compounds to treat psychiatric disorders. Also provided are pharmaceutical compositions comprising azetidinyl tryptamines.

Aerosol generating compositions adapted for use in an aerosol delivery device are provided. The aerosol generating compositions include a thin film. The thin film includes a binder, an aerosol former, and an active agent, wherein the active agent includes at least a substituted 3-(1-methylpyrrolidin-2-yl)pyridine, 3-(azetidin-2-yl)pyridine, or 3-(azetidin-2- ylmethoxy)pyridine. The disclosure further provides articles and devices incorporating such aerosol generating compositions.

The present disclosure provides articles configured for use in an aerosol provision system. The articles include an aerosol generating portion having an aerosol generating material comprising an aerosol former; and a body of material upstream of the aerosol generating portion, wherein the body of material optionally includes a plurality of portions of material. The body of material includes an active agent, the active agent including a substituted 3-(1-methylpyrrolidin- 2-yl)pyridine, 3-(azetidin-2-yl)pyridine, or 3-(azetidin-2-ylmethoxy)pyridine. The disclosure further provides devices incorporating such aerosol generating articles.

The invention belongs to the field of chemical synthesis, and particularly relates to a synthetic method of azetidine-2-yl (methyl) benzyl carbamate hydrochloride. According to the invention, 1-benzyl azetidine-3-alcohol is used as a basic raw material, and a series of reactions such as substitution reaction and the like are carried out to obtain the high-yield and high-purity azetidine-2-yl (methyl) benzyl carbamate hydrochloride, and the method is suitable for industrial production.

The present disclosure relates to the technical field of pharmaceutical formulations and particularly provides, in the specification, a stable imidazo[1,2-a]pyridine derivative pharmaceutical composition, a preparation method therefor, and use thereof. The pharmaceutical composition comprises an active pharmaceutical ingredient and auxiliary materials, wherein the active pharmaceutical ingredient is (azetidin-1-yl)(8-(2,6-dimethylbenzylamino)-2,3-dimethylimidazo[1,2-a]pyridin-6-yl)methanone citrate; the auxiliary materials include one or more selected from cyclodextrin, a salt of cyclodextrin, propylene glycol, and PEG400.

The present invention concerns the compounds of formula (I)wherein R1, R2, R3, X, and Y are as described in the description, and their use as antagonists of the LPA1 receptor, in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s); such as especially pirfenidone and / or nintedanib, in the prevention and / or treatment of fibrotic diseases. The invention further relates to pharmaceutical compositions comprising the compounds of formula (I) in combination with one or more therapeutically active ingredients acting as anti-fibrotic agent(s) such as pirfenidone or nintedanib.

The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders.

The present invention relates to formulations of farnesol X receptor agonists. Specifically, described herein are pharmaceutical formulations of the farnesoid X receptor agonist 3-hydroxyazetidine-trans-1-carboxylic acid 4-((4-(1-(tert-butyl)-1H-pyrazol-4-yl) pyridin-2-yl) ((4-(4-methoxy-3-methylphenyl) bicyclo [2.2. 2] octane-1-yl) methyl) carbamoyl) cyclohexyl, and methods for preparing the pharmaceutical formulations of the farnesoid X receptor agonist 3-hydroxyazetidine-trans-1-carboxylic acid. And methods of treating conditions, diseases, or conditions associated with farnesoid X receptor activity using such pharmaceutical formulations.