1996 results about "Formamide" patented technology

Pharmaceutical compositions including N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1) and methods of using such compositions are described herein.

The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

The present invention relates to solid state forms, for example, crystalline forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, pharmaceutical compositions thereof, and methods therewith.

The invention relates to methods of treating or preventing malaria which comprises administering to a patient in need thereof, an effective amount of a 1H-indazole-3-carboxamide derivative of general formula (I), in the form of a base or of an addition salt with an acid, or in the form of a hydrate or of a solvate of said base or acid addition salt.

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.

The present invention relates to pharmaceutical compositions comprising a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide, methods of manufacturing pharmaceutical compositions of the present invention, and methods of administering pharmaceutical compositions of the present invention.

Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation and R1a, R1b, R1c, R2a, R2b, R3, R4, R5, T, U, W, Y and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula I and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of Formula I. Also disclosed are mixtures and compositions comprising a herbicidally effective amount of a compound of Formula Iz wherein J, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, T, U, W, Y and Z are as defined in the disclosure; and an effective amount of another herbicide or herbicide safener. Also disclosed is a method for selectively controlling undesired vegetation in a crop that involves contacting the locus of a crop with an effective amount of a compound of Formula Iz and a effective amount of a safener.

A topical insect repellent with extended duration of protection was obtained from mixtures of molecules based on two or more volatile repellent organic molecular species occurring naturally on the human skin surface. The novel repellent comprises mixtures of lower, intermediate, and higher volatility organic molecules. Active ingredients for formulations are obtained from homologous series of carboxylic acids, alcohols, ketones, and lactones which span a similar range of volatility and which occur naturally on the skin surface. Volatile silicone fluid imparts mildness and water repellency to the repellent formulations. The new natural repellent exhibits the longevity and repellency that is comparable to N,N-diethyl-m-toluamide (DEET), a synthetic compound employed in almost all commercial formulations, but the inventive natural repellent is more acceptable than DEET, which has an unpleasant odor and imparts a greasy feel to the skin. The inventive insect repellent, formulated in a volatile silicone fluid, was shown to repel and incapacitate stable flies. This finding demonstrated that repellency was not limited to mosquitoes, but extends to other biting flies or insects, thus demonstrating the utility of the novel insect repellent for protecting pets and livestock as well as humans.

A crosslinkable macromer system and related methods of preparing the system and using the system in the form of a crosslinked matrix between a tissue site and an implant article such as a tissue implant or on the porous surface of a prosthetic device. The macromer system includes two or more polymer-pendent polymerizable groups and one or more multifunctional initiator groups. The polymerizable groups and the initiator group(s), when polymer-pendent, can be pendent on the same or different polymeric backbones. The macromer system provides advantages over the use of polymerizable macromers and separate, low molecular weight initiators, including advantages with respect to such properties as nontoxicity, efficiency, and solubility. A macromer system of the invention can be used as an interface between the tissue site and implant article in a manner sufficient to permit tissue growth through the crosslinked matrix and between the tissue site and implant. In a preferred embodiment, polymers with pendent polymerizable groups, for use in the macromer system, are prepared by reacting a polysaccharide polymer with a reactive moiety in an organic, polar solvent such as formamide.

The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.

The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.

A crosslinkable macromer system and related methods of preparing the system and using the system in the form of a crosslinked matrix between a tissue site and an implant article such as a tissue implant or on the porous surface of a prosthetic device. The macromer system includes two or more polymer-pendent polymerizable groups and one or more initiator groups (e.g., polymer-pendent initiator groups). The polymerizable groups and the initiator group(s), when polymer-pendent, can be pendent on the same or different polymeric backbones. The macromer system provides advantages over the use of polymerizable macromers and separate, low molecular weight initiators, including advantages with respect to such properties as nontoxicity, efficiency, and solubility. A macromer system of the invention can be used as an interface between the tissue site and implant article in a manner sufficient to permit tissue growth through the crosslinked matrix and between the tissue site and implant. In a preferred embodiment, polymers with pendent polymerizable groups, for use in the macromer system, are prepared by reacting a polysaccharide polymer with a reactive moiety in an organic, polar solvent such as formamide.

An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1′-carbonyldiimidazole (“CDI”) as carbonyl source; an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide; efficient syntheses for the preparation of intermediates (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride, and the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide including the potassium salt ethanolate and potassium salt hydrate.

Porous ceramic catalyst supports are pre-coated with a passivation layer prior to applying a catalyst or catalyst support coating, the passivation layer consisting of a coating of a liquid mixture comprising at least one coating material selected from the group of polyvinyl alcohol / vinyl amine copolymer, polyvinyl alcohol / vinyl formamide copolymer, and gelatin.

The present invention relates to a process for the preparation of novel pyrrolo [2,1-c][1,4]benzodiazepine hybrids useful as antitumour agents. This invention also relates to a process for the preparation of new pyrrolo[2,1-c][1,4]benzodiazepine hybrids as potential antitumour agents. More particularly, it provides a process for the preparation of 7-methoxy-8-[N-(1''-pyrenyl)-alkane-3'-carboxamide]-oxy-(11aS)-1,2,3,11a-tetraydro 5H-pyrrolo[2,1-c][1,4]benzodiazepine-5-one, with aliphatic chain length variation of these compounds and it also describes the DNA binding, anticancer (antitumour) activity. The structural formula of this novel pyrrolo[2,1-c][1,4]benzodiazepine is given below:

The invention discloses a preparation method of vilazodone or its hydrochloride, which comprises the following steps: the compound of formula (I) is mixed with the compound of formula (II) 5-(1 -piperazinyl)-benzofuran-2-formamide reaction, then collect vilazodone shown in formula 1 from the reaction product; Gained vilazodone 1 is in a solvent, and hydrochloric acid is salified to prepare formula (A ) shown vilazodone hydrochloride. The present invention overcomes the defects and deficiencies in the existing preparation methods of vilazodone and its intermediates, is more suitable for the large-scale industrial preparation of vilazodone hydrochloride, has obvious creativity, and has a relatively large positive progress effect and practical application value. The reaction formula is as follows:

A crosslinkable macromer system and related methods of preparing the system and using the system in the form of a crosslinked matrix between a tissue site and an implant article such as a tissue implant or on the porous surface of a prosthetic device. The macromer system includes two or more polymer-pendent polymerizable groups and one or more multifunctional initiator groups. The polymerizable groups and the initiator group(s), when polymer-pendent, can be pendent on the same or different polymeric backbones. The macromer system provides advantages over the use of polymerizable macromers and separate, low molecular weight initiators, including advantages with respect to such properties as nontoxicity, efficiency, and solubility. A macromer system of the invention can be used as an interface between the tissue site and implant article in a manner sufficient to permit tissue growth through the crosslinked matrix and between the tissue site and implant. In a preferred embodiment, polymers with pendent polymerizable groups, for use in the macromer system, are prepared by reacting a polysaccharide polymer with a reactive moiety in an organic, polar solvent such as formamide.

Compounds of the formulawherein R1, R2, R3, R4, X and Y are as defined, which have a superior cGMP specific phosphodiesterase (PDE) inhibitory activity, and can be used as an agent for the treatment of cardiovascular diseases such as angina pectoris, heart failure, cardiac infarction, hypertension, arteriosclerosis, and the like; allergic diseases such as asthma, or disorders of male or female genital function and the like.

The invention discloses an aluminum-doped zinc oxide film coating and nano-rod array material as well as a preparation method thereof. The aluminum-doped zinc oxide film coating and nano-rod array material comprises the components based on the weight percentage: 95-99% of zinc oxide and 1-5% of aluminum-doped quantity. The preparation method adopts a sol-gel method, zinc acetate and aluminium nitrate are added with organic solvent according to the proportion for heating under reflux; the mixed solution is then added with certain quantity of stabilizing agent for water bath heating at certain temperature and added with organic reagents such as absolute ethyl alcohol, methanamide or methanol and the like to prepare sol according to the need; after that, a spin coating method is adopted to form a film, and the aluminum-doped zinc oxide nano film coating material can be obtained by the processes such as drying, pretreating, repeatedly spin coating, annealing, secondary annealing under the atmosphere of hydrogen and nitrogen and the like; then, a hydrothermal method is adopted for preparing highly oriented aluminum-doped zinc oxide nano-rod and array thereof. The invention has high utilization rate of the raw materials, low cost and simplified preparation technique, and can control the performance and the particle size of the material from the molecular design level.

This invention provides compounds of Formula I, N-oxides and suitable salts thereof wherein Y and V are each independently N or CR4a; W is N, CH or CR6; and R1 through R6, and n are as defined in the disclosure. This invention also pertains to a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula I, an N-oxide thereof or an agronomic or nonagronomic suitable salt of the compound and at least one additional component selected from the group consisting of a surfactant, a solid diluent and a liquid diluent, and optionally further comprising an effective amount of at least one additional biologically active compound or agent. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, an N-oxide thereof or an agronomic or nonagronomic suitable salt of the compound or with the composition described herein.

The invention relates to a preparation process of a metal-organic framework porous adsorption material for C4-C8 normal paraffin and isoparaffin adsorption separation. According to the preparation method of the synthesized metal-organic framework porous adsorption material, metal ion nitrate and an organic ligand are dissolved according to the mass ratio of 1:1-15 in a mixed solution of N,N-dimethylformamide and N,N-diethyl formamide; stirring is carried out for 0.5-12 h; reaction temperature is controlled to 80-250 DEG C, and reaction time is 12-120 h; and by a hydrothermal synthesis method, the metal-organic framework porous adsorption material is prepared. The material has characteristics as follows: specific surface area is large; pore structure height is ordered; pore size is controllable; surface potential energy is controllable; and adsorption capacity of normal paraffin is large. The material can selectively adsorb normal paraffin from mixed materials of normal paraffin and isoparaffin, has high selectivity and has a wide practical application prospect in normal paraffin and isoparaffin separation.

The invention provides a high flame retardancy type soft foam plastic insulation product and a preparation method thereof. The product comprises the following components in parts by weight: 12 to 15 parts of nitrile rubber, 8 to 10 parts of talcum powder, 0.5 to 0.8 parts of polyethylene glycol, 0.2 to 0.4 parts of antiager 4020, 15 to 20 parts of chlorinated paraffin, 0.6 to 0.9 parts of paraffin, 1 to 2 parts of epoxidized soybean oil, 0.1 to 0.3 parts of antiager RD, 0.4 to 0.7 parts of carbon black, 7 to 10 parts of polrvinyl chloride, 26 to 36 parts of fire retardant based on the total amount, 2 to 5 parts of dioctyl ester, 8 to 12 parts of azodicarbonamide, 0.2 to 0.5 parts of stearic acid, 0.4 to 0.7 parts of zinc oxide, 0.4 to 0.7 parts of sulphur, and 1.3 to 1.8 parts of accelerant based on the total amount. By adopting the high flame retardancy type soft foam plastic insulation product, the technical problem that the oxygen index and the smoke density are mutually conflicted in the technological manufacture is solved, and the bottleneck due to mutual limitation is broken through.

The invention provides an ethylene propylene diene terpolymer sponge rubber and a preparation method thereof, relating to a rubber and a preparation method thereof. The ethylene propylene diene terpolymer sponge rubber is prepared from ethylene propylene diene terpolymer, a foaming agent, a filling enhancer, a plasticizer, molecular sieve powder with a hygroscopic effect, a vulcanizing agent and a vulcanizing aid. The ethylene propylene diene terpolymer sponge rubber is characterized in that the molecular sieve powder is used for replacing traditional talc powder or calcium carbonate to be used as a filling agent, a foaming agent azobisformamide (AC) and a foaming agent 4,4'-oxy bis(benzenesulfonyl hydrazide) (OBSH) are combined and matched with an accelerant, and the decomposing rate of the foaming agent and the vulcanizing rate of the ethylene propylene diene terpolymer are matched, thus a microporous sponge rubber sealing product with a hygroscopic function is prepared under die pressing vulcanization conditions. The tensile strength, elongation percentage, stress at definite elongation, compression set and other indexes of the ethylene propylene diene terpolymer sponge rubber can meet the use performance requirements of sponge sealing strips; and at the same time, the sponge rubber has uniform foam pores, small density and hygroscopic function.

The invention discloses a preparation method of pimavanserin. The method comprises the following two steps: firstly, 4-isobutoxy benzene methylamine and carbonyl diimidazole are subjected to acylation reaction to obtain N-(4-isobutoxy phenyl)-1H-imidazole-1-formamide, and the N-(4-isobutoxy phenyl)-1H-imidazole-1-formamide and N-(4-fluorophenyl)-1-methylpiperidine-4-amine are subjected to urea reaction, so as to obtain the pimavanserin. The prepared pimavanserin is good in quality and high in yield, the reagent toxicity is relatively low, the operation is simple and easy to control, and the pimavanserin is suitable for industrial production.