183 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 invention discloses polyurethane resin with a super-hydrophobic surface and a preparation method of the polyurethane resin, and belongs to the technical field of modified polyurethane materials. According to the invention, 2, 2 '-diallyl bisphenol A and a fluorine-containing thiol monomer react to introduce a fluorine-containing carbon chain, and then fluorinated modified 2, 2'-diallyl bisphenol A and tetramethoxysilane are used for treating nano zinc oxide, so that the content of active oxygen groups is reduced, a siloxane network structure is formed, the action with water molecules is reduced, and the hydrophobicity is improved. Secondly, the 2, 2 '-diallyl bisphenol A reacts with amino propyl isobutyl POSS to generate a benzoxazine structure, the POSS structure is introduced, the nano-size effect of the benzoxazine structure fills limited movement between molecular chains, a cage-shaped structure serves as a cross-linking point, the mechanical property is improved, and hydrophobicity is achieved. When polyurethane is prepared, 3, 3-bis (hydroxymethyl) azetidine and a benzoxazine structure are subjected to ring opening crosslinking, bonding, dispersity and stability of fluorinated modified nanoparticles and a matrix are enhanced, a complex network structure is formed, the surface roughness is increased, the water contact area is reduced, and super-hydrophobicity is achieved.

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

The invention discloses application of an azetidine compound in preparation of a medicine for preventing and treating triple-negative breast cancer, and belongs to the technical field of biological medicine. By adopting an international common triple-negative breast cancer modeling method, the scheme shows that the compound can effectively inhibit the tumor growth state of nude mouse triple-negative breast cancer, inhibit STAT3 705 site tyrosine phosphorylation and induce tumor cells to generate G2-M phase arrest and apoptosis, and has remarkable prevention and treatment effects on triple-negative breast cancer; the compound is expected to become a novel medicine for treating triple-negative breast cancer.

The invention discloses a deuterated 2-(azetidine-3-yl) ethanone compound as well as a pharmaceutical composition and application of the deuterated 2-(azetidine-3-yl) ethanone compound. The deuterated 2-(azetidine-3-yl) ethanone compound has the structural characteristics of a formula (I), and the definition of each group in the formula (I) is shown in the specification. The compound shown in the formula (I) can be used as a muscarinic M4 receptor positive allosteric modulator, and compared with Emraclidine (CV-231), the compound shown in the formula (I) has better pharmacokinetic characteristics and higher safety. # imgabs0 #

The present disclosure provides, in part, azetidine compounds, and pharmaceutical compositions thereof, and methods of the treatment and prophylaxis of HSV infections.

In the novel salt, crystal form, and production method of the imidazo[1,2-a]pyridine compound of the present invention, the novel salt of the imidazo[1,2-a]pyridine compound is azetidin-1-yl {8-[(2,6-dimethylbenzyl)amino]-2,3-dimethylimidazo[1,2-a]pyridin-6-yl}methanone citrate.

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.

Provided herein is a compound of formula (I), or a pharma- ceutically acceptable salt thereof: (wherein R1 and R2 independently represent a hydrogen atom or a deuterium atom; R3 represents a hydrogen atom, a -COOH group or a -OH group; R3' and R3" independently represent a hydrogen atom, a methyl group, a methoxy group, a chlorine atom, a fluorine atom or a cyano group; R4 represents a hydrogen atom or a fluorine atom; R5 and R5' independently represent a hydrogen atom or a fluorine atom; R6 represents a phenyl group, a fused phenyl group, a bicyclic group containing 5 to 12 carbon atoms, a heteroaryl group containing 2 to 9 carbon atoms and containing 1 to 3 heteroatoms, a cycloalkyl group containing 3 to 7 carbon atoms, a (C3-C6)cycloalkyl(C1-C3)alkyl group, a 4- to 7-membered heterocycloalkyl group, a (C1-C6)alkyl group or a phenyl(C1-C2) ) alkyl group; X represents -CH2-, -O- or -S-; Y represents -CH2-, -O- or -NH-; R7 independently represents a (C1-C3) alkyl group such as a methyl group, a halogen atom such as a fluorine atom, a cyano group, or a (C1-C3) fluoroalkyl group such as trifluoromethyl; R8 represents a hydrogen atom, or a (C1-C3) alkyl group or a cyclopropyl group; n is 0, 1 or 2; m is 0 or 1; p is 0 or 1). Further disclosed are processes for the preparation of the compounds of formula (I), or pharma- ceutically acceptable salts thereof, pharmaceutical compositions containing them, and the use of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, in particular for the treatment of ovulation failure, cancer, endometriosis, osteoporosis, prostatic hyperplasia or inflammation. [Formula 1] TIFF2025513853000144.tif32170

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 invention relates to a preparation method of an N-substituted-3-hydroxy azetidine compound, and belongs to the field of medical intermediates. According to the invention, cheap and easily available N-substituted-3-hydroxy azetidine or 3-hydroxy azetidine is used as a raw material, and in the presence of a metal catalyst, hydrogenation (transfer hydrogenation) deprotection and reductive amination one-pot reaction are carried out on the raw material and various aldehydes to obtain the target N-substituted-3-hydroxy azetidine compound. The method overcomes the defects that in the prior art, when the target N-substituent-3-hydroxy azetidine compound is prepared, the steps are tedious (6-7 steps are needed for reaction to obtain the product), dangerous reagents (LiAlH4 and the like) are used, the preparation reaction conditions are harsh (no water, no oxygen and high temperature), the yield is low and the like, and provides beneficial reference for industrial amplification.

The present disclosure provides adsorbents and contactors, methods of capturing CO2 using the adsorbents and contactors, structures including the adsorbents, and systems and devices for capturing CO2 using the adsorbents and contactors. In one aspect, the disclosure provides an adsorbent comprising a CO2-philic phase and a carrier. The present disclosure provides adsorbents and contactors that include a CO2-philic phase and a support wherein the CO2-philic phase includes a modified amine polymer that is a reaction product of an amine and aziridine or azetidine.

Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (F AAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders:Ar1 is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar2 is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar3 is a divalent radical selected from optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.

The present disclosure provides an improved method of treating non-small cell lung cancer using N-(2-((3S, 4R)-3-fluoro-4-methoxypiperidin-1-yl) pyrimidin-4-yl)-5-isopropyl-8-((2R, 3S)-2-methyl-3-((methylsulfonyl) methyl) azetidin-1-yl) isoquinolin-3-amine represented by the following structure: # imgabs 0 #, or a pharmaceutically acceptable salt thereof.

Provided is a compound in which the balance of the agonist activity against the S1P5 receptor relative to the SIPi receptor has been improved in order to develop a pharmaceutical useful for the treatment of S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases. This compound represented by general formula (V) (in the formula, all symbols are as defined in the specification) has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic for SIPs-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

The invention relates to an absorber (15) of a solar cell, which has a molecular formula of (Cs, AZ) PbI3, (Cs, AZ) Pb (I, Br) 3, (Cs, AZ) Pb (I, Cl) 3 or (Cs, AZ) Pb (I, Br, Cl) 3, and has a perovskite structure, in which AZ represents azetidinium. The invention also relates to a solar cell comprising an absorber (15). The invention also relates to a method for producing an absorber, comprising: a) providing a substrate (1); b) thermally evaporating CsI and / or CsBr and / or CsCl to form a first vapour jet (4), the jet being generated starting from a first evaporation source (7); c) thermally evaporating PbI2 and / or PbBr2 and / or PbCl2 to form a second vapor jet (3), which is generated starting from a second evaporation source (6); d) thermally evaporating AZI, where AZI = azetidine hydroiodide or azetidinium iodide, forming a third steam jet (2), which is generated by a third evaporation source (5); wherein steps b), c) and d) are carried out simultaneously such that the first steam jet (4), the second steam jet (3) and the third steam jet (2) at least partially overlap, thereby forming an absorber on the provided substrate (1).

In the novel salt of the imidazo [1, 2-a] pyridine compound, the crystal form thereof and the preparation method of the novel salt of the imidazo [1, 2-a] pyridine compound, the novel salt of the imidazo [1, 2-a] pyridine compound is azetidine-1-yl {8-[(2, 6-dimethyl benzyl) amino]-2, 3-dimethyl imidazo [1, 2-a] pyridine-6-yl} ketone citrate.

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.