78 results about "Azetidine" patented technology

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 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 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.

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 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 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 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 disclosure provides an aerosol generating material for use in a non-combustible aerosol provision system. The aerosol generating material includes an aerosol former, optionally a binder, optionally a non-tobacco botanical material, and at least a substituted 3-(1- methylpyrrolidin-2-yl)pyridine, 3-(azetidin-2-yl)pyridine, or 3-(azetidin-2-ylmethoxy)pyridine as an active agent. The aerosol generating material may be in sheet form, shredded form, bead form, fibrous form, or extrudate form. Further provided are aerosol provision systems including the aerosol generating material.

The present disclosure relates to a compound of Formula (I): Formula (I) or a pharmaceutically acceptable salt thereof for use in the treatment and / or prophylaxis of pathological desert.

The present application relates to a process for the synthesis of diazabicyclo [6.2. 0] decane related compounds. The invention provides a method for synthesizing a diazabicyclo [6.2. 0] decane compound. The synthesis is carried out by stereoselectively synthesizing chiral lactone and then forming azetidine through a series of chemical selective reactions. According to the invention, diazabicyclo [6.2. 0] decane related compounds are formed by means of double cyclization.

The present invention relates to a crystalline form of an imidazo[1,2-a]pyridine compound, and more specifically to a monohydrate crystalline form, crystalline form A, and crystalline form B serving as an active pharmaceutical ingredient of azetidin-1-yl{8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl}methanone and as an intermediate of a final salt addition compound, and a method for preparing same. The monohydrate crystalline form, crystalline form A, and crystalline form B of the compound of chemical formula I according to the present invention have excellent stability under high-humidity or high-temperature conditions, and thus can be usefully applied to the formulation of pharmaceuticals.

The present invention relates to a pharmaceutical formulation, a method for producing the same, and a tablet composition. The pharmaceutical formulation according to the present invention contains azetidin-1-yl{8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl}methanone citrate as an active ingredient and microcrystalline cellulose as an excipient.

The application relates to a compound containing a nitrogen-containing azetidinyl phenyl piperidine-2,6-dione structure, a pharmaceutical composition and application thereof. The compound containing the nitrogen-containing azetidinyl phenyl piperidine-2,6-dione structure has a structure shown in formula (I). The compound has improved proliferation inhibition activity on cancer cells and degradation effect on proteins such as GSPT1, and has practical value.

The invention discloses a synthesis method of 3-hydroxyazetidine hydrochloride, and belongs to the technical field of organic synthesis. According to the method, tert-butylamine and epichlorohydrin are used as starting raw materials, and a target product is prepared through three-step reaction of cyclization, acetylation and deacetylation in sequence. The method is characterized in that in the acetylation reaction step, a step-by-step strategy that hydroxyl is subjected to monoacetylation at low temperature, and then tert-butyl acetylation is carried out by heating under the conditions that Lewis acid is used for catalysis and sodium hydrosulfite is used as a binding agent is adopted; the binding agent can effectively capture fallen tert-butyl, and side reaction between the fallen tert-butyl and the intermediate is avoided. By optimizing the synthesis route and the purification process, the problems of high raw material cost, high hydrogenation deprotection safety risk, more side reactions, difficulty in intermediate purification, poor product crystallization effect and the like in the prior art are solved. The obtained product is high in purity (greater than or equal to 98%) and good in crystal form, and the whole process is good in safety, simple and convenient to operate and more suitable for industrial production.

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.

Liquid aerosolizable compositions adapted for use in an aerosol delivery device are provided. The aerosolizable compositions include an aerosol former and 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 aerosolizable compositions.