125 results about "Carbamate esters" patented technology

The present invention provides Lig-and-Drug Conjugates and Drug-Linker Compounds comprising a methylene carbamate unit. The invention provides inter alia, Ligand-Drug Conjugates, wherein the Ligand-Drug Conjugate is comprised of a Self-immolative Assembly Unit having a methylene carbamate unit for conjugation of a drug to a targeting ligand, methods of preparing and using them, and intermediates thereof. The Ligand-Drug Conjugates of the present invention are stable in circulation, yet capable of inflicting cell death once free drug is released from a Conjugate in the vicinity or within tumor cells.

The present invention provides methods of treating skin disorders includes delivering to a mammal a composition containing a compound of formula I, or tautomers thereof, in a regimen, wherein formula I is:and wherein R1-R5 and Q1 are defined as described herein. Specifically, methods for treating acne, hirsutism, and conditioning the skin are described. Also provided are novel PR modulators of formula II.

Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: Formula (I) wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

The present invention is a method for the treatment of Pervasive Developmental Disorders (PDDs) including; Autistic Disorder, Asperger's Disorder, Childhood Disintegrative Disorder (CDD), Rett's Disorder, and PDD-Not Otherwise Specified (PDD-NOS) comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and / or Formula 2 as herein defined and shown below.The present invention is directed to a method for the treatment of Pervasive Developmental Disorders (PDDs) including; Autistic Disorder, Asperger's Disorder, Childhood Disintegrative Disorder (CDD), Rett's Disorder, and PDD-Not Otherwise Specified (PDD-NOS), which includes mono-therapy and alternatively, co-therapy with at least one additional psychoactive medication.

The invention provides eTEC linked glycoconjugates comprising a saccharide covalently conjugated to a carrier protein through a (2-((2-oxoethyl)thio)ethyl)carbamate (eTEC) spacer, immunogenic compositions comprising such glycoconjugates, and methods for the preparation and use of such glycoconjugates and immunogenic compositions.

Novel substituted piperidine carbamates, pharmaceutical compositions comprising them and use thereof in the treatment and / or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and / or prevention of diseases and disorders in which modulation of the activity of hormone sensitive lipase is beneficial.

Film-forming materials include resins and / or crosslinkers having a -Si(OR)3 group. Film-forming resins can include epoxy, acrylic, polyurethane, polycarbonate, polysiloxane, polyvinyl, polyether, aminoplast, and polyester resins. A process to produce a film-forming resin includes reacting various polymers to incorporate a pendent group comprising a -Si(OR)3 group. Crosslinkers for polymerizing a film-forming material include at least two functional groups reactive with a film-forming material and at least one pendent group comprising a -Si(OR)3 group. Functional groups reactive with a film-forming material include isocyanate, blocked isocyanate, uretdione, epoxide, hydroxyl, carboxyl, ester, ether, carbamate, aminoalkanol, aminoalkylether, amide, or amine groups. Film-forming resins and / or crosslinkers having a -Si(OR)3 group can be used in methods of producing coating compositions. Coating compositions can be used to coat a substrate, such as a metal substrate, by electrodeposition. Applied coatings containing the film-forming resins can be cured to form crosslinked films on substrates.

The invention provides a lubricant additive with antioxidant, antiwear and rustproof functions. The lubricant additive with the antioxidant, antiwear and rustproof functions is mainly prepared from the following raw material components in parts by mass: 10-60 parts of alkylbenzene sulfonate, 30-60 parts of alkyl diphenylamine, 20-40 parts of isopropyl beta-(3,5-ditertbutyl-4-hydroxy phenyl) propionate, 10-30 parts of methylene-bis-alkyl dithiocarbamate, 10-30 parts of a sulfur-phosphorus-nitrogen type extreme pressure agent and 5-20 parts of a sulfurized calcium phenate type high temperature clearing agent. A preparation method of the lubricant additive with the antioxidant, antiwear and rustproof functions comprises the following steps: mixing all the raw materials and uniformly stirring, so that the lubricant additive with the antioxidant, antiwear and rustproof functions is obtained. The lubricant additive of the embodiment of the invention is well applied to engine lubricant, hydraulic oil, gear lubricant, steam turbine lubricant and compressor lubricant, is respectively excellent in the antioxidant, antiwear and rustproof aspects and also has excellent clearing function, functionality of the lubricant additive can not be reduced no matter at high temperature or low temperature, and some properties or a certain property of lubricant can be obviously improved.

The present invention discloses a silk-screen printing electrode sensor preparation method based on ionic liquid-multi-wall carbon nano-tube modification, and belongs to the technical field of biological sensors. According to the method, an ionic liquid-multi-wall carbon nano-tube nanometer material is prepared and then coats the surface of a silk-screen printing carbon electrode in a dropwise manner, and then acetylcholine esterase coats the surface of the ionic liquid-multi-wall carbon nano-tube nanometer material modified silk-screen printing work electrode in a dropwise manner so as to prepare the acetylcholine esterase biological sensor for detecting organic phosphorus and carbamate pesticides. According to the present invention, the prepared sensor has characteristics of simple process, easy operation, low cost, high detection sensitivity, strong electrical signal and simple electrode pretreatment, and is suitable for detection of pesticide residues, wherein the detection limit is 0.05 [mu]g / L.

Novel piperazines, pharmaceutical compositions comprising them and use thereof in the treatment and / or prevention of diseases and disorders related to hormone sensitive lipase. More particularly, the compounds are useful for the treatment and / or prevention of diseases and disorders in which modulation of lipolysis, such as decreased lipolysis is beneficial.

The invention provides novel materials for chromatography and chromatography columns. The invention provides a monofunctional silane or a mixture of two or three monofunctional silanes chemically bonded to a substrate, at least one monofunctional silane having at least one unsaturated hydrocarbon group, R′, covalently attached to the substrate, containing the silane structure is of form: Where R′ is independently selected from the group consisting of alkenyl, alkynyl, and phenyl, R″ is selected from the group consisting of alkyl, substitute alkyl, alkenyl, substitute alkenyl, alkynyl, and aryl, substitute aryl, R is selected from the group consisting of alkyl, substitute alkyl, alkenyl, substitute alkenyl, alkynyl, and aryl, substitute aryl, alkylamine, amide, ether, alcohol, carbamate, ester, an anion exchanger, and a cation exchange. Methods for manufacture and design of the columns are also provided and disclosed.

The invention discloses a beta-carboline-cycloenone derivative with a structure as shown in a general formula which is described in the specification. According to the invention, an electron-donatinggroup is introduced into a proper part of beta-carboline, and the 3-site amino group of beta-carboline is connected with cycloenone having anti-tumor activity by utilizing a carbamate bond, so the novel beta-carboline-cycloenone derivative is designed and synthesized. The derivative realizes pH and GSH dual-response fluorescence imaging and diagnosis in a tumor microenvironment, and can selectively target to GSTpi highly-expressed in tumor tissue, so tumor cell proliferation can be significantly inhibited. Such a pH / GSH dual-response fluorescence and cancer-targeting treatment diagnosis and treatment drug provides a new choice for accurate diagnosis and targeting treatment of tumors, and broadens the application of multifunctional molecules in accurate medical treatment.

The invention discloses an anti-wear, anti-friction and anti-oxidant additive and energy-saving hydraulic oil containing the same. Zinc dialkyl thiosulfate, molybdenum phosphate, molybdenum dithiocarbamate, a boron nitrogen compound, borate, organic molybdenum, methylene bisdibutyl dithiocarbamate, polyisobutylene dibutyl diimide, 350N paraffin base oil, polyalphaolefin PAO8 and polyol ester are used as raw materials, and the specific gravity of each component is strictly controlled; the borate has good anti-wear performance, so that the service life of a machine can be prolonged by more thanone time, the bearing capacity is strong, and a sintering accident can be prevented; the friction coefficient is low, and the friction coefficient of oil prepared from a borate agent can be as low as0.05-0.06 at a room temperature; most of the conventional lubricating oil uses an oil-soluble liquid anti-wear agent, and solid anti-wear agents such as graphite, molybdenum disulfide and polytetrafluoroethylene can be applied only when particles thereof are small and stably dispersed in base oil of the lubricating oil; the anti-wear, anti-friction and anti-oxidant additive has very good anti-wearand friction-reducing effects.

The invention discloses a polyethylene / polybutylece terephthalate (PBT) coated coconut shell powder particle blending foam material. The material is prepared from the following materials in part by weight: 60 to 80 parts of LLDPE (Linear low density polyethylene), 20 to 40 parts of HDPE (high-density polyethylene), 30 to 40 parts of PBT, 10 to 15 parts of tourmaline, 15 to 20 parts of water glass, 5 to 10 parts of coconut shell powder, 1 to 2 parts of anilino-methyl-triethoxysilane, 5 to 8 parts of decabromodiphenyl oxide, 4 to 6 parts of di-butyl nylonic acid ester, 5 to 8 parts of epoxy octyl stearate, 3 to 5 parts of foaming agent, 1 to 2 parts of diperoxycarbamate, 1 to 2 parts of zinc oxide, 1 to 2 parts of calcium stearate, 0.5 to 1 part of dibasic lead phosphite, 2 to 3 parts of glycol tristearate, 3 to 5 parts of modified tree ash, and 1 to 2 parts of antioxidant 2461. The polyethylene / PBT coated coconut shell powder particle blending foam material is light in weight, flexible, high in strength, good in resilience, ideal in foaming effect, uniform in cell, compact, high in flame resistance, ageing resistant and durable.

The invention relates to a surface grafted curcumin modified degradable polyurethane composite material as well as a preparation method and application thereof. The polyurethane material is composed of polyurethane and modified curcumin grafted with polyurethane, the polyurethane is connected with the modified curcumin through -CONH- chemical bonds, and the polyurethane material is a polyurethanematerial with a carbamate structure in the molecular formula. The chemical structural formula of the modified curcumin is represented by a formula II, wherein R is C3-C4 straight-chain or branched-chain alkyl.

The present invention relates to a formulation and method for treating an ear infection, especially otomycosis and otitis externa, by administering a one-time only treatment comprising an antibiotic, and antifungal, and an anti-inflammatory in a thick, otic carrier. In one embodiment, the formulation comprises a therapeutically effective amount of active ingredients including a fluoroquinolone, a triazole antifungal, a thiocarbamate antifungal, a corticosteroid and a polyene antifungal, as well as a thickener such that the formulation, upon applying to the infected ear canal, gels and remains in the ear canal, continuously releasing the active ingredients for several days, achieving consistent complete (98-100%) clinical resolution of otomycosis and otitis externa in a single application.

The present invention is directed to a design of and a method to synthesize polycations for gene (DNA and RNA) delivery. According to this design, the polycations (also said cationic polymers) are formed by polymerization of endogenous monomers bearing sufficient amino groups through degradable bonds with linker molecules or with themselves. The amino group-bearing monomers are those naturally existing in or nontoxic to human body. The linker molecules are those which are not only degradable to nontoxic fragments but also able to release the amino group-bearing monomers in their native state upon degradation. Some examples for the endogenous amino group-bearing monomers are spermine, spermidine, serine or N,N-dimethyl serine, and histidine. Examples for the degradable chemical bonds formed between the amino group-bearing monomers are carbamate, imine, amide, carbonate, and ester. In order to improve degradability or proton sponging effect, low pKa (<8) amino group(s) or other electron donating group(s) is incorporated in the linker between the two (or three) reactive groups for linking the amino group-bearing monomers. These polycationic carrier systems can be used for nano-encapsulation and transfection of gene materials.

The invention relates to a preparation method of an overall hydrophobic timber. The timber is dipped by using alkyl isocyanate and dimethylformamide mixed solution, so that alkyl is grafted to a cell wall of the timber through a carbamate key. The method uses a self micron / nanometer roughness structure of the timber as basis, and grafts the alkyl to the cell wall of the timber through the carbamate key to form a low-surface-energy substance; a surface water drop contact angle thereof is about 147-151 degrees; the timber is sawn off in the cross section direction; and a water drop contact angle on the internal surface is about 147 degrees. The overall hydrophobic timber has the performances of mechanical wear resistance and chemical corrosion resistance; and in addition, the related preparation method is simple in steps, excellent in controllability, short in preparation period and easy to realize reaction conditions.

The present invention relates to carbamate derivatives having RNase H, polymerase and / or HIV reverse transcriptase modulatory, and particularly, inhibitory activity. Included in the invention are the carbamate derivatives, compositions containing the derivatives, methods of synthesis of the derivatives, screening methods to identify the derivatives, and methods of treatment using the carbamate derivatives, including the treatment of HIV, AIDS and retrovirus-associated cancer.

The invention relates to a preparation method of high-strength and high-toughness vinyl ester resin. The preparation method comprises the following steps: firstly, reacting diisocyanate with polyether glycol to prepare an isocyanate-terminated polyurethane prepolymer (PUR), then reacting the polyurethane prepolymer (PUR) with hydroxyl of epoxy resin to obtain polyurethane block modified epoxy resin (UE), and finally, reacting with unsaturated monocarboxylic acid to obtain the polyurethane modified vinyl ester resin (VER). According to the preparation method disclosed by the invention, not only is a flexible polyether chain segment blocked into a resin structure, but also the functionality of the vinyl ester resin is increased due to the existence of a carbamate bond. Therefore, the high-strength and high-toughness vinyl ester resin is low in shrinkage rate and high in strength after being cured, the impact resistance is obviously improved, the comprehensive performance is good, the product is stable, and the reaction route is reasonable.

The invention discloses a rapid detection method special for pesticide residues of dichlorvos in fresh fruits and vegetables, and belongs to the technical field of rapid detection of pesticide residues. Based on the specific inhibition effect of organophosphorus pesticides and carbamate pesticides on the activity of acetylcholin esterase (AChE, derived from duck blood extraction), the inhibition degree of AChE is detected by using an ultrahigh-sensitivity fluorescein fluorescent probe. When the addition amount of the dichlorvos in the detection system is the same, the weakened fluorescence intensity (I dichlorvos) of the dichlorvos is 100 times or more lower than that of other pesticides (I other pesticides), thereby showing that even if the content of the dichlorvos is 100 times lower than that of other pesticides, the residual quantity of the dichlorvos can be quantitatively detected. Through diluting a pesticide residue extraction liquid by 100 times, the influence of other pesticide residues on AChE is reduced, the pesticide residue range of specific detection of dichlorvos in fruits and vegetables is 0.02-1.2 mg / kg, the error rate R2 of a detection standard curve is greater than 0.99, and the standard addition recovery rate of the fresh fruits and vegetables reaches 71-86%.

The invention relates to a diesel engine oil composition and application thereof, and mainly solves the problems of insufficient anti-wear and extreme pressure performance of internal combustion engine oil in the prior art. The diesel engine oil composition comprises the following components by weight: a) 2-5 parts of a metal detergent, which is formed by compounding a sulfonate and sulfurized alkyl phenolate; b) 1-5 parts of a polyisobutylene succinimide ashless dispersant; c) 1-3 parts of an anti-wear preservative, which is formed by compounding long chain primary alcohol based zinc dialkyldithiophosphate and primary alcohol based zinc dialkyl dithiophosphate; d) 0.5-3 parts of a composite antioxidant, which is formed by compounding an amine type antioxidant and a phenolic ester antioxidant; e) 0.5-3 parts of an antiwear agent, which is one of or compounded by several of phosphorothioates, thiocarbamates and antimony thiocarbamate; and f) 85-105 parts of base oil. The technical scheme adopted by the invention well solves the problems, and can be used in a vehicle diesel engine system.

Multibiotic agents are disclosed. The multibiotic agents may contain two or more moieties linked through bonds cleavable in vivo. The bonds cleavable in vivo can be ester bonds, amide bonds, azo bonds, glycosidic bonds, carbonate linkers, or carbamate linkers. The moieties can be alcohol cores, amine cores, and / or acyls. Also disclosed are compositions containing multibiotic agents and methods of using the multibiotic agents.

The invention provides a process method for separating talc and chalcopyrite through a three-step method and a collecting agent used in the process method. The method comprises the steps of carrying out ore grinding, carrying out first-step roughing, carrying out second-step concentration, and carrying out third-step table reselection and regrinding operation. The process method aims at separationof the talc and the chalcopyrite, the preferential copper separation technological process is adopted for the first time under the condition that a special-effect talc inhibitor is not added, and effective separation of the talc and the chalcopyrite is achieved. According to the process method, the collecting agent TB-1 formed by mixing isobutyl xanthate propionitrile ester, N-allyl-O-alkyl thiocarbamate and Spans type sorbitan ester is adopted to strengthen flotation of the chalcopyrite, the thickness of a foam layer is adjusted through the defoaming performance of the collecting agent TB-1,and the relative floating speed of the talc and the chalcopyrite is changed; and the flotation and reselection combined technological process is adopted, and effective separation of talc and chalcopyrite is achieved through three steps. The flotation reagent adopted in the process method has the characteristics of low toxicity or no toxicity, environment friendliness, good effect and the like, and an environment-friendly and high-efficiency process method for separating the talc and the chalcopyrite is provided.

The invention provides a gasoline engine lubricating oil composition and a preparation method thereof. The gasoline engine lubricating oil composition comprises a benzotriazole derivative, a succinimide ashless dispersant, a salicylate cleaner, an alkylated diphenylamine antioxidant, a shielded phenol antioxidant, a thiocarbamate antioxidant, an organic molybdenum friction modifier, an OCP viscosity index modifier and lubricant base oil. The gasoline engine lubricating oil composition has the excellent high-temperature antioxidant property, antifriction performance and corrosion resistance, and can meet the requirements of high-performance gasoline engine lubricating oil.