278 results about "Azetidine" patented technology

The invention is related to a cost-effective method for making a silicone hydrogel contact lens having a crosslinked hydrophilic coating thereon. A method of the invention involves heating a silicone hydrogel contact lens in an aqueous solution in the presence of a water-soluble, highly branched, thermally-crosslinkable hydrophilic polymeric material having positively-charged azetidinium groups, to and at a temperature from about 40° C. to about 140° C. for a period of time sufficient to covalently attach the thermally-crosslinkable hydrophilic polymeric material onto the surface of the silicone hydrogel contact lens through covalent linkages each formed between one azetidinium group and one of the reactive functional groups on and/or near the surface of the silicone hydrogel contact lens, thereby forming a crosslinked hydrophilic coating on the silicone hydrogel contact lens. Such method can be advantageously implemented directly in a sealed lens package during autoclave.

The invention is related to azetidinium-containing copolymers and vinylic monomers and their uses in formation of non-silicone hydrogel coatings on silicone hydrogel contact lenses.

The present invention relates to polysaccharides that have been modified by providing azetidinium functionality thereto. Such functionality can be provided by crosslinking a polysaccharide with a resin having azetidinium functional groups. In one or more aspects, the polysaccharide can comprise one or more of starch, guar gum, alginate or derivatives thereof. Polysaccharides having azetidinium functionality according to the present invention are suitable for multiple uses. Such uses include, but are not limited to, removal of one or more solid materials from a liquid, beneficiation of an ore, removal of metallic ions from a liquid; providing oil from bitumen; and removal of mercury from synthetic gypsum. Other uses of the functionalized polysaccharides of the present invention include hydroseeding, dust control and corosion control.

The present invention relates to novel Syn isomers of racemates and optical isomers of 3-(heteroaryl acetamido)-2-oxo-azetidine-1-sulfonic acids of formula (I) and its use in treating the infections caused by gram-negative pathogenic bacteria.

The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

Self-polymerization of mono-aziridine (or azetidine) and multi-aziridine (or azetidine) containing compounds with vinyl group containing organic acid, such as acrylic acid (AA), 2-methylenesuccinic acid, 2,3-dimethylenesuccinic acid and etc, at ambient temperature results in the new type of cross-linked and linear type copolymers, respectively.

The polymerization of multi-functional aziridine (or azetidine) containing compounds with vinyl group containing organic acid results in the formation of high cross-linked polymers. The self-polymerization takes place at ambient temperature and the resultants, cross-linked polymeric networked materials, are solvent insoluble and potential for adhesive, composite matrix and other applications. These insoluble materials are hydrolyzed in an acidic or basic condition to form the water soluble β-amino acids.

A linear poly(β-aminoester) is obtained from the self-polymerization of vinyl group containing organic acid with mono-aziridine (or azetidine) containing compound at ambient temperature. poly(β-aminoester) is applicable for gene transfer, controlled drug release and other applications. This self-polymerization process offers a convenient route for preparing poly(β-aminoesters).

Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

The present invention provides compounds of formula (I), wherein both p's are one or two, R¹ is generally heteroaryl or cycloalkyl, R² is C_3-6cycloalkyl or phenyl and R³ is heteroaryl, and pharmaceutically acceptable salts thereof, as GlyT1 inhibitors for treating schizophrenia, pharmaceutical compositions comprising the same and methods for their preparation.

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, isotopic form or stereoisomer thereof, wherein A is a five-membered heteroaryl comprising 1 or 2 non-adjacent heteroatoms, inclusive of X and Y; W, X, Y, Z, L, L¹, E, R¹, R^2bR^2c and the dotted circle are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and compounds for use in methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided. Preferred compounds are e.g. 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and related compounds such as e.g. the corresponding derivatives with e.g. a benzoimidazole, indole, benzooxazole, imidazopyridine or imidazole core structure, substituted on ring A by e.g. azetidine, pyrrolidine, azepane or bicyclopentane-amine (L¹) each substituted by e.g. propenone (E), and the core structure substituted on the six-membered ring with e.g. 3-hydroxynaphthalene or indazole or hydroxy-, alkoxy- and/or fluoro-substituted phenyl (R¹).

Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): (Formula (I)) or a pharmaceutically acceptable salt, stereoisomer thereof, wherein G, Y, R, R¹, R^2a, R^2b, R^2c, L, L¹ and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided. Preferred compounds are quinazoline and quinazolinone derivatives and in particular 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds.

A process for preparing a compound represented by the formula (I): comprising reacting a compound represented by the formula (II) or salt thereof: with a compound represented by the formula (III): in the presence of a condensation reagent, wherein R 1 represents 1) optionally substituted azetidin-1-yl, 2) optionally substituted pyrrolidin-1-yl, 3) optionally substituted piperidin-1-yl, etc, R2, R3, R4 and R5 may be the same or different and each represents hydrogen or fluorine; and R6 represents hydrogen or fluorine.

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows:

wherein Y, Z, and n are defined herein; and

wherein Y_b and Z_b are as defined herein.

Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-azetidine-carboxylic acids, esters and amides which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.

The invention relates to a preparation method of a ulifloxacin optical isomer, in particular to a preparation method of a 6-fluorine-1-methyl-4-oxo-(1-piperazinyl)-1H and 4H-(1, 3) sulfur azetidine combined with (3, 2-a) quinoline-3-carboxylic acid optical isomer, which comprises the following steps: (+/-) ulifloxacin is taken to be dissolved in dimethyl sulfoxide, a dimethyl sulfoxide solution of D-tartaric acid is dropped into the dimethyl sulfoxide to obtain (S)-ulifloxacin-D-tartrate precipitation, the pH value of the (S)-ulifloxacin-D-tartrate is regulated by a NaOH solution in water after the (S)-ulifloxacin-D-tartrate is recrystallized so as to obtain precipitates, the precipitates are filtered and dried to obtain (S)-ulifloxacin, and the optical purity e.e. of the (S)-ulifloxacin is more than 95 percent. The preparation method of the ulifloxacin optical isomer is simple and convenient without special equipment requests and is beneficial to industrialized batch production, and an obtained optically active body has high purity.

The invention provides a compound of aztreonam and a synthetic method thereof. In the method, general solvents are used, suitable amines are chosen, (2-aminothiazole-4-group)-2-(tert-butoxycarbonyl)-iminodiacetic acid isopropoxide acid-2-ester mercaptobenzothiazole and (3-S-trans form)-3-amino-4-methyl-2-oxo-1-sulfonic acid azetidine are used as intermediates; therefore, the method simplifies reaction and has good effect on depriving protecting groups by the mixed aqueous solution of acetic acid and hydrochloric acid.

The invention discloses a preparation method of regenerated cellulose fiber subjected to cation grafting modification and salt-free dyeing, which adopts cellulose pulp as a main raw material, and orderly comprises the following procedures of dipping, squeezing, crushing, aging, yellowing, dissolving, filtering, defoaming, spinning, post-treatment, and drying; a cellulose cation modifier is added in the dissolving procedure or the spinning procedure; the cellulose cation modifier is one or a mixture of more than one of an amination reagent, a quaternization reagent, a azetidine cation compound, and a modified natural cation reagent. Therefore, the method of the invention prevents the disadvantages of dye waste, uneven dyeing, and the like caused by the adoption of dyes with multiple active groups, and also prevents the problem of process flow increasing caused by the adoption of a pretreatment mode.

The invention relates to the field of chemical synthesis, and discloses a preparation method of tebipenem pivoxil. The preparation method comprises the following steps of: performing condensation reaction on azabicyclo phosphate and 3-mercapto-1-(1,3-thiazoline-2-yl) azetidine hydrochloride by taking acetonitrile as a solvent in the presence of diisopropylethylamine; in a mixed solvent consisting of acetic ether and a potassium bicarbonate aqueous solution, performing hydrogenization on the compound shown by formula I to remove p-nitrobenzyl to obtain tebipenem; and under the catalysis of a phase transfer catalyst, adding anhydrous potassium carbonate into the tebipenem and iodomethyl pivalate to perform condensation reaction to obtain the tebipenem pivoxil. By adopting the preparation method, according to the defects of related solvents and operations of purification and the like in the conventional method for preparing the tebipenem pivoxil, co-adapted solvents and purification operations are selected during preparation according to a reaction mechanism, so that the yield of the tebipenem pivoxil is improved, and the preparation method is suitable for industrial production. The formula I is shown in the description.

The invention provides a water-soluble cationic polyaspartic ester and a synthesis method thereof. The substance has a 3-hydroxyazetidine structure. During synthesis, firstly butene diacid diester reacts with polyethylene polyamine to obtain polyaspartic ester polyamine with unreacted secondary amine group, and then adding epoxy chloropropane for reaction with the secondary amine group so as to obtain water-soluble polyaspartic ester with azetidine cationic group. The cationic polyaspartic ester monomer can be compounded with isocyanate to develop water-soluble polyurea or polyurea/polyurethane coating resin.