- Joint production technology of hydroxylamine, hydroxylammonium salt and cyclohexanone-oxime
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The invention discloses a joint production technology of hydroxylamine, hydroxylammonium salt and cyclohexanone-oxime. The material comprises the steps that reaction liquid obtained by raw materials through an ammoximation reaction and a hydrooximation reaction is extracted and separated to obtain an organic phase, the organic phase is prepared into product cyclohexanone-oxime, or part of the organic phase and part of product cyclohexanone-oxime are adopted as raw materials for an oxime hydrolysis reaction to be hydrolyzed, the organic phase in hydrolysis liquid is circulated to return to a oximation reactor, part of an inorganic phase in the hydrolysis liquid is adopted as a raw material to be circulated to return to a hydroxylamine oximation reactor, and the other part of the inorganic phase is prepared into a hydroxylamine aqueous solution and hydroxylammonium salt. The joint production technology of hydroxylamine, hydroxylammonium salt and cyclohexanone-oxime is simple in procedure, the requirement of the ammoximation reaction for the purity of the raw material cyclohexanone and the catalyst performance is lowered, a high quality cyclohexanone-oxime product without cyclohexanone is obtained, the simplification of the downstream caprolactam technology and the improvement of the product quality are benefited, and the hydroxylamine and hydroxylammonium salt product which have high additional value are obtained simultaneously.
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Paragraph 0015; 0030; 0031
(2017/09/26)
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- MAGNETIC NANOSTRUCTURES AS THERANOSTIC AGENTS
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The present invention relates to magnetic nanostructures as theranostic agents, which provide dual function as diagnostic and therapeutic agents. In particular, the present invention relates to compositions comprising magnetic nanostructures and their use as targeted therapeutic agents for cancers (e.g., medulloblastoma) and Alzheimer's disease and related diseases and conditions.
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- Metalloprotease inhibitors
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Compounds of formula (I) and pharmaceutically-acceptable derivatives thereof, are matrix metalloprotease inhibitors, useful in treatment of conditions mediated by matrix metalloproteases, such as chronic dermal ulcers.
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- Composition for the treatment of damaged tissue
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A pharmaceutical for use in damaged tissue, such as wound, treatment (e.g. healing) is described. The pharmaceutical comprising a composition which comprises: (a) a growth factor; and (b) an inhibitor agent; and optionally (c) a pharmaceutically acceptable carrier, diluent or excipient; wherein the inhibitor agent can inhibit the action of at least one specific adverse protein (e.g. a specific protease) that is upregulated in a damaged tissue, such as a wound, environment.
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- Substituted isoxazolylthiophene compounds
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This invention provides a substituted isoxazolylthiophene compound represented by the formula wherein R1and R2individually represent an alkyl group of 1-5 carbon atoms, R3represents a cyano group or a group CONR5R6(in which R5and R6individually represent a hydrogen atom or an alkyl group of 1-10 carbon atoms), R4represents an alkyl group of 1-5 carbon atoms or a phenyl group, and n is an integer of 0-2, or a salt thereof. The compounds of the invention are useful for the treatment or prevention of various bone diseases or nerve diseases, because they specifically enhance the action of the cell differentiation induction factors found in a living body.
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- Heterocyclic benzenesulphonamide compounds as bradykinine antagonists
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The invention concerns compounds selected among the group consisting of (i) compounds of formula (I) wherein: Het1 represents a nitrogenous heterocycle with 5 apices, in particular imidazole, pyrazole, or triazole; Het2 represents a nitrogenous heterocycle with 4, 5 or 6 apices, selected among the heterocycles: (II) wherein R1and R2are defined as mentioned in the description; and (ii) their additive salts. The invention also concerns the method for preparing said compounds and their use in therapy, in particular for treating pathologies involving bradykinine.
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- Pyridinium compounds
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Methods for using novel quaternary pyridinium compounds in inhibiting acetylcholinesterase in mammals, specifically using the quaternary pyridinium compounds in the prophylaxis and treatment of organophosphate poisoning and mammalian dementia by mimicking or opposing the actions of the natural neurotransmitter acetylcholine.
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- Substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors
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This invention relates to substituted cyclic carbonyls and derivatives thereof useful as retroviral protease inhibitors, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection. A representative compound of the invention is the compound of formula: STR1 wherein R22 and R23 are allyl.
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- Process for the preparation of O-substituted hydroxylammonium salts
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Preparation of O-substituted hydroxylammonium salts I (L=halogen, hydrogensulfate; X=H, alkyl; R1 =unsubst. or subst. phenyl, thienyl, furanyl, pyrrolyl or --CR2 =CR3 R4 ; R2, R3, R4 =H, halogen or alkyl) by reaction of an acetone oxime O-allyl or --O--benzyl ether II STR1 with water and a mineral acid H--L with continuous removal of the acetone formed in this process, by carrying out the hydrolysis batchwise at 0°-50° C. and under a pressure of 10-500 mbar is described. The O-substituted hydroxylammonium salts I are intermediates for plant protection agents and pharmaceuticals.
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- PROTEASE-BINDING COMPOUNDS AND METHODS OF USE
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Non-peptide, protease-binding compounds are described as useful in the detection, labelling, and inhibition of retroviral proteases. Aryl piperidinyl derivatives and other compounds related in structure have been found to be HIV-1 and HIV-2 protease-binding compounds.
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- Amino-oxy esters
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The invention relates to hydroxylamine derivatives of the general formula STR1 in which A denotes a divalent connecting link, R1 can be a hydrogen atom or a C1 -C4 alkyl group, Z stands for an n-valent organic radical, which contains a copolymerizable ethylenically unsaturated group, and n is an integer from 1 to 3, and salts thereof and copolymers thereof.
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- Erythromycin derivatives
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New 9-deoxo-9,12-epoxy erythromycin derivatives are disclosed which have improved antibacterial properties. Compositions comprising the erythromycin derivatives and methods of treating mammalian patients with the erythromycin derivatives are also disclosed.
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- QUATERNARY PYRIDINIUM COMPOUNDS
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Quaternary pyridinium compounds, their use in inhibiting acetylcholinesterase, their roles in the prophylaxis and treatment of organophosphate poisoning, their roles in anticholinesterase therapy and their roles as agents mimicking or opposing the actions of the natural neurotransmitter acetylcholine
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- N-substituted alpha-arylazacycloalkylmethanamines and their use as cardiovascular agents
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Novel compounds of the formula below wherein W is azetidine, pyrrolidine or piperidine, Q is a straight chain hydrocarbon radical of 1-4 carbons and may contain a double bond, and STR1 Ar is phenyl, pyridinyl or pyrimidinyl, a process for their preparation, and novel intermediates are disclosed. The novel compounds and the pharmaceutical compositions of this invention are useful in the treatment of hypertension, arrhythmias and angina.
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- Method for the preparation of N-ethylhydroxylamine hydrochloride
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A process for preparing N-ethylhydroxylamine hydrochloride which comprises reacting hydroxylamine hydrochloride with di-t-butyl dicarbonate in the presence of a base selected from sodium carbonate, potassium carbonate, sodium bicarbonate, potassium bicarbonate, sodium or potassium hydroxide or triethylamine, in a non-reactive solvent, alkylating said reaction product with an alkyl halide and then cleaving with a strong acid the tert-butyloxycarbonyl (BOC) portion of the alkylated product.
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- 1,2,4-oxadiazolyl-phenoxyalkylisoxazoles and their use as antiviral agents
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Compounds of the formulas STR1 wherein: Y is an alkylene bridge of 3-9 carbon atoms; R' is lower-alkyl or hydroxy-lower-alkyl of 1-5 carbon atoms; R1 and R2 are hydrogen, halogen, lower-alkyl, lower-alkoxy, nitro, lower-alkoxycarbonyl or trifluoromethyl; and R8 is hydrogen or lower-alkyl of 1-5 carbon atoms, with the proviso that when R8 is hydrogen R' is hydroxy-lower-alkyl, are useful as antiviral agents, particularly against picornaviruses, including numerous strains of rhinovirus.
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- Work-up of aqueous mother liquors containing hydrochloric acid, sulfuric acid and their hydroxyl-ammonium and ammonium salts
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A process for working up aqueous mother liquors containing hydrochloric acid, sulfuric acid and their hydroxylammonium and ammonium salts, entails the mother liquors being intimately mixed with an excess of cyclohexanone based on the content of hydroxylammonium salts, while maintaining a pH of from 3 to 5.5 by adding alkali metal hydroxide solutions, and the cyclohexanone phase which contains cyclohexanone oxime being removed and washed with water until essentially free of chloride.
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- 1,2,4-oxadiazolyl-phenoxyalkylisoxazoles and their use as antiviral agents
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Compounds of the formulas STR1 wherein: Y is an alkylene bridge of 1-9 carbon atoms; R' is lower-alkyl or hydroxy-lower-alkyl of 1-5 carbon atoms; R1 and R2 are hydrogen, halogen, lower-alkyl, lower-alkoxy, nitro, lower-alkoxycarbonyl or trifluoromethyl; and R8 is hydrogen or lower-alkyl of 1-5 carbon atoms, are useful as antiviral agents, particularly against picornaviruses, including numerous strains of rhinovirus.
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- 5-substituted pyrido[2,3-d]pyrimidine-2,4-diones
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The present invention relates to a novel pyrido[2,3-d]pyrimidine derivative having the formula (I): STR1 wherein each of R1 and R2, which may be the same or different, is a lower alkyl group; and each of R3 and R4, which may be the same or different, is hydrogen, halogen, hydroxy, nitro, amino, hydroxyamino, hydrazino, azido, a lower alkenylamino group or a lower alkylamino group which may optionally have hydroxy; and pharmaceutically acceptable salt thereof. These compounds are useful as anti-allergic agents, for example, for the treatment of bronchial asthma, urticaria, allergic rhinitis, allergic dermatoses or allergic conjunctivitis.
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- Leukotriene antagonists
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This invention provides novel alkane derivatives which are leukotriene antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment of conditions characterized by an excessive release of leukotrienes.
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- 1-Substituted 1,4-dihydropyridines
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A vasodilating or anti-hypertensive composition comprises a pharmaceutical carrier and an effective amount of a 1,4-dihydropyridine compound as an active ingredient. The 1,4-dihydropyridine compound may be represented by the following general formula: STR1 wherein R'1 and R'4 represent a hydrogen atom, R'2 and R'3 represent an alkyl group having 1-5 carbon atoms or a substituted heterocyclic group wherein a substituent is an N-benzylpiperidyl group, R'5 represents a nitro group, and R'6 and R'7 represent an alkyl group having 1-5 carbon atoms.
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- Cephem compounds having a terminal aminocarboxylic acid grouping and containing an azacyclyl(thio)ureido group
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Compounds of the formula STR1 in which the index n represents an integer of from 1 to 4, the index m represents 0 or 1, X represents oxygen, sulphur or the group --NH--, W represents a group --CO--, --CO--NHSO2 -- or --SO2 NH--CO--, or X-W together represent a group --CO-- or --CO--NHSO2 --, A represents optionally substituted phenylene, thienylene or furylene, Z represents oxygen or sulphur, Y represents lower alkylene, the index k represents the value 1 or 2, R4 represents hydrogen, an optionally substituted lower aliphatic or cycloaliphatic radical or acyl, R1 represents hydrogen, lower alkyl, lower alkoxy, halogen or a group of the formula --CH2 --R2 in which R2 represents a free, esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, and R3 represents hydrogen or methoxy, and in which the carboxyl groups are optionally esterified in a form that can be split under physiological conditions, and salts of such compounds having salt-forming groups, are obtained by liberating the functional group(s) in a compound of the formula I in which at least one of the functional groups present is protected. The compounds are effective in vitro and in vivo against gram-positive and gram-negative bacteria and cocci.
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- Insecticidal substituted-biphenylmethyl oxime ethers
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Oxime ethers of the formula STR1 wherein R1 is isopropyl, cyclopropyl, cyclopropylmethyl, or cyclobutyl; X and Y are independently halogen or straight or branched chain alkyl or alkoxy of 1 to 4 carbon atoms optionally substituted with one or more halogen atoms; n is 0-2; and m is 1-4 are disclosed. The insecticidal efficacy and preparation of the compounds are described and exemplified.
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- Acetohydroxamic acids
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The invention provides new acetohydroxamic acid derivatives, having interesting properties on the central nervous system, of the formula: R1 R2 R3 C-CO-NHOH, in which R2 and R3 are each hydrogen or C1-6 alkyl, and R1 is C1-6 alkyl Z1 Z2 N (where Z1 and Z2 are each phenyl, substituted phenyl, or cycloalkyl), substituted hydantoinyl, benzhydroxylcarboxamido, Z3 CH2 -- (where Z3 = optionally substituted aryl), Z4 -A- (where Z4 is optionally substituted phenyl or naphthyl, and A is --NH--, --N(C1-4 alkyl)--, --N(C5-6 cycloalkyl)--, --NHCO--, --N(C1-4 alkyl)CO--, --N(C5-6 cycloalkyl)CO--, --CONH--, --CON(C1-4 alkyl)--, --CON(C5-6 cycloalkyl)--, --NHCONH--, --N(C5 H6)CONH--, or --N(substituted phenyl)CONH--, optionally substituted benzimidazolyl, or an optionally substituted tricyclic radical, and their metal and acid addition salts.
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- Phthaloyl amino acid hydroxamic acids
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A series of phthaloyl amino acid hydroxamic acids are useful as inhibitors of Angiotensin I converting enzyme.
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- N-hydroxy-amidine compounds
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The invention relates to novel biologically active compounds of the formula I: STR1 in which B is a N-hydroxy-amidino group of the general formula: STR2 A represents a methylene-, ethylene- or propylene group, optionally substituted with lower alkyl groups r stands for the number: 0, 1, 2, 3 or 4 R1 is hydroxy, alkyl, alkylthio or alkoxy, halogen (F, Cl, Br or I), trifluoromethyl, nitro, amino or alkylenedioxy (1-4 C), Cn H2n is an alkylene group with 0-4 carbon atoms R2 stands for hydrogen, alkyl, aryl or aralkyl, R3, r4, r5 represent hydrogen, alkyl, aralkyl or acyl, and R6 stands for hydrogen, alkyl, or phenyl or benzyl optionally substituted with methyl groups And pharmaceutically acceptable acid addition salts thereof. The compounds possess anti-hypertensive and vasodilatory activities.
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- Novel chelate formers
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Benzoin oximes of the formula STR1 wherein R1 is alkyl of 3 to 16 carbon atoms, alkenyl of 3 or 4 carbon atoms, 3,7-dimethyl-2,6-octadienyl-1, or -A-S-R4 ; R2 and R3 independently are H, methyl or chlorine; R4 is alkyl or 1 to 8 carbon atoms; and A is alkylene of 3 or 4 carbon atoms, are chelating agents for copper.
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- Selected 3-pyrrolidinones and 2,4-pyrrolidindiones
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Certain 1,5-disubstituted 3-pyrrolidinones and 2,4-pyrrolidindiones have biological properties which resemble those of the natural prostaglandins. Exemplary is 7[N(3-hydroxy-n-octyl)-2,4-dioxopyrrolidin-5-yl] heptanoic acid methyl ester of the formula
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- N-hydroxy-amidine compounds
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The invention relates to novel biologically active compounds of the formula I: SPC1 in which B is a N-hydroxy-amidino group of the general formula: EQU1 or EQU2 A represents a methylene-, ethylene- or propylene group, optionally substituted with lower alkyl groups R stands for the number: 0, 1, 2, 3 or 4 R1 is hydroxy, alkyl, alkylthio or alkoxy, halogen (F, Cl, Br or I), trifluoromethyl, nitro, amino or alkylenedioxy (1-4 C), Cn H2n is an alkylene group with 0-4 carbon atoms R2 stands for hydrogen, alkyl, aryl or aralkyl, R3, r4, r5 represent hydrogen, alkyl, aralkyl or acyl, and R6 stands for hydrogen, alkyl, or phenyl or benzyl optionally substituted with methyl groups And pharmaceutically acceptable acid addition salts thereof.
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