54 results about "Isonicotinamide" patented technology

The present invention relates to a cyanide-free lytic reagent composition and method for measuring the total hemoglobin concentration in a blood sample, for counting the number of leukocytes and for differential counting of three leukocyte subpopulations including lymphocytes, monocytes, and granulocytes. The cyanide-free lytic reagent composition comprises a hemolytic surfactant selected from the group consisting of quaternary ammonium salts, pyridinium salts, organic phosphate esters, and alkyl sulfonates to lyse erythrocytes and release hemoglobin, and an organic ligand selected from the group consisting of triazole and its derivatives, tetrazole and its derivatives, alkaline metal salts of oxonic acid, melamine, aniline-2-sulfonic acid, quinaldic acid, 2-amino-1,3,4-thiadiazole, triazine and its derivatives, urazole, DL-pipecolinic acid, isonicotinamide, anthranilonitrile, 6-aza-2-thiothymine, adenine, 3-(2-thienyl)acrylic acid, benzoic acid and alkali metal and ammonium salts of benzoic acid, and pyrazine and its derivatives to form a stable chromogen with hemoglobin. Alternatively, the organic ligands can be added to a suitable blood diluent for hemoglobin and leukocyte analysis.

The invention belongs to the field of a medical technology and specifically relates to a co-crystal formed by naringenin and isonicotinamide, wherein stoichiometric ratio of naringenin to isonicotinamide in the co-crystal is 1:2. The co-crystal has an X-ray powder diffraction pattern, a differential scanning calorimetry pattern and an infrared spectrogram which are different from those of naringenin crystals and a physical mixture of naringenin and isonicotinamide, is a novel crystalline form completely different from naringenin, and has remarkably-enhanced solubility.

The invention provides an isonicotinamide eutectic crystal of 17beta estradiol, and a preparation method and application thereof. Particularly, the invention provides the isonicotinamide eutectic crystal of 17beta estradiol. X-ray powder diffraction analysis, thermogravimetic analysis, differential scanning thermometric analysis and other analysis indicate that the eutectic crystal provided by the invention has more excellent physicochemical property and pharmaceutical property. The invention provides the preparation method of the eutectic crystal. The method is simple to operate, easy to control and favorable in reproducibility, and can stably obtain the target eutectic crystal.

The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.

The present invention provides a corrective method for converting cyano-group pyridines compound to niacinamide compound. In particular, the invention relates to the preparation of the niacinamide compound and the isonicotinamide compound, it is used for preparing anti-TB medicine-retozide, and an intermediate of vitamin B12. The invention also relates to catalyst preparing method by niacinamide and isonicotinamide.

The invention belongs to the technical field of the medicine, and specifically provides isonicotinamide methylpyrazine derivative eutectic I, a preparation method thereof, and use thereof for preparing antilipemic agent. The isonicotinamide methylpyrazine derivative eutectic I prepared by the invention uses Cu-Kalpha radiation, an X-ray diffraction spectrum represented by 2theta has characteristicpeaks at 7.2+ / -0.2 degrees, 8.1+ / -0.2 degrees, 14.5+ / -0.2 degrees, and 16.2+ / -0.2 degrees. The prepared isonicotinamide methylpyrazine derivative eutectic prepared is good in stability in the medium,and is high in product purity and good in stability after being placed in a solid state; an animal experimental verifies that the bioavailability is high. The isonicotinamide methylpyrazine derivative eutectic I disclosed by the invention is simple in preparation process and has good industrial application prospect.

The invention discloses a kaempferol and isonicotinamide eutectic compound, a preparation method, a composition thereof and application. Specifically, the invention discloses a novel kaempferol and isonicotinamide eutectic compound which takes kaempferol (as shown in a formula a) as a medicine active component and isonicotinamide (as shown in a formula b) as a eutectic ligand, a preparation methodof the kaempferol and isonicotinamide eutectic Compound, and application of the kaempferol and isonicotinamide eutectic compound as a medicinal active ingredient to preparation of medicines for preventing and treating cancer, resisting cancer, resisting inflammation, resisting oxidation, resisting bacteria or resisting viruses.

The invention discloses a method for preparing cephalonium from 7-aminocephalosporanic acid at one step. The method comprises the following steps: (1) adding 7-aminocephalosporanic acid into water with the temperature of 0-10 DEG C; (2) regulating the pH value of the solution; (3) adding an organic solvent, tiophencacetyl chloride and ethyl acetate, and reacting for 1-3h while stirring at the temperature of 0-10 DEG C; (4) after the reaction is ended, standing for layering; (5) adding activated carbon into a water phase for decoloring, and carrying out suction filtration; (6) adjusting the pH value of the filtrate, then, adding isonicotinamide, and reacting at the temperature of 15-50 DEG C; (7) after the reaction is ended, growing the grain for over 1h; (8) filtering to obtain a crystal, and drying to obtain the cephalonium. The cephalonium is prepared at one step, and an intermediate is not needed to be separated and extracted in the reaction process, so that the method is simple and convenient in operation, simple in reaction step and high in yield; the 7-aminocephalosporanic acid is used as the raw material and is simple and easy to obtain and low in market price, so that the production cost is greatly reduced.

The invention belongs to the field of medicine, and relates to N-(3-azolylphenyl) isonicotinamide compounds as well as a composition comprising the same and a preparation method of the N-(3-azolylphenyl) isonicotinamide compounds. The invention further relates to the application of the compounds and the compositions in anti-gout. The compounds have a general formula I as shown in the specification; the molecular structure of the compounds is more innovative and the activity is greatly enhanced. Moreover, the compounds with the general formula I provided by the invention are simple and feasiblein preparation method, high in yield and easy to be mass-produced.

Nicotinamides and isonicotinamides, used in the preparation of anti-TB drugs i.e. isoniazid and as an intermediate of vitamin B12 are prepared from cyanopyridines and nicotinamides. Catalysts useful for the preparation of nicotinamide and isonicotinamide.

The invention discloses a preparation method of isoniazide, comprising the following steps: carrying out an esterification reaction among isonicotinic acid, alcohol and an acylation reagent to generate isonicotinate, carrying out a reaction between isonicotinate and an ether reagent in an alcoholic solution of hydrogen chloride to generate isonicotinate hydrochloride, condensing with hydrazine hydrate to generate an isoniazide crude product, and refining to obtain the finished product. According to the method, by adding the step of reacting isonicotinate to generate isonicotinate hydrochloride, on one hand, the subsequent condensation hydrazinolysis reaction time can be greatly shortened and preparation efficiency is improved; on the other hand, isonicotinic acid which is not fully reacted, isonicotinamide introduced by an isonicotinic acid raw material and potential 2-picolinic acid impurities can be removed, the purity of the finally obtained isoniazide is as high as 99.99%, and thesingle impurity content is smaller than 0.10%. The preparation method is mild in reaction condition, easy to operate, good in product quality, high in yield, high in preparation speed and suitable forindustrial production.

The invention provides a preparation method of novel multifunctional Alaska pollock polypeptide modified by taurine. The multifunctional polypeptide includes natural polypeptide and a substituent group, wherein the amino acid sequence of the natural polypeptide is SEQ ID NO.1, and taurine is adopted as the substituent group which is combined with the natural polypeptide and introduced for modification. The preparation method of the polypeptide includes preparation of protective peptide fragments, a microwave condensation reaction and a deamination protection reaction. During preparation of theprotective peptide fragments, the natural polypeptide is dissolved in a sodium carbonate solution, an acetone solution containing amino-terminal protection groups and an accelerant is added, stirringis conducted for a reaction, and extraction and precipitation are carried out to obtain the fragments, wherein the accelerant comprises o-aminobenzoic sulfonic acid and isonicotinamide. The providednovel polypeptide has high activity and stability, no spiral structure, high fluidity and a high swelling ratio and can achieve biological activities such as oxidation resistance, removal of free radicals and promotion of brain development. The conversion rate and the yield are high during preparation. The time consumed for synthesis is short, the yield of by-products is low, products are easy topurify, and the production cost is low.

The invention discloses a mezlocillin sodium freeze-dried powder injection. The freeze-dried powder injection is prepared from mezlocillin sodium, isonicotinamide and propylgallate according to a weight ratio of 10:(0.1-0.4):(0.01-0.05). The mezlocillin sodium freeze-dried powder injection is high in stability, high in safety due to few types of auxiliary materials, simple in process and suitable for mass production.

The invention discloses a method for preparing cephalonium from 7-aminocephalosporanic acid at one step. The method comprises the following steps: (1) adding 7-aminocephalosporanic acid into water with the temperature of 0-10 DEG C; (2) regulating the pH value of the solution; (3) adding an organic solvent, tiophencacetyl chloride and ethyl acetate, and reacting for 1-3h while stirring at the temperature of 0-10 DEG C; (4) after the reaction is ended, standing for layering; (5) adding activated carbon into a water phase for decoloring, and carrying out suction filtration; (6) adjusting the pH value of the filtrate, then, adding isonicotinamide, and reacting at the temperature of 15-50 DEG C; (7) after the reaction is ended, growing the grain for over 1h; (8) filtering to obtain a crystal, and drying to obtain the cephalonium. The cephalonium is prepared at one step, and an intermediate is not needed to be separated and extracted in the reaction process, so that the method is simple and convenient in operation, simple in reaction step and high in yield; the 7-aminocephalosporanic acid is used as the raw material and is simple and easy to obtain and low in market price, so that the production cost is greatly reduced.

The invention provides a process for the manufacture of isonicotinic acid hydrazide(INH) useful in the treatment of tuberculosis. The invention relates to the single step conversion of isonicotinamide by hydrazine hydrate to isonicotinic acid hydrazide (INH) of yield greater than 95% (w / w) and purity more than 99%.

The invention discloses a 5-isonicotinamidopyridylisotitanate cadmium complex, and a preparation method and an application thereof, and belongs to the technical field of porous layered materials. Theporous complex has a two-dimensional double-layer network structure, the chemical expression of the porous complex is [Cd2(L)2DMFTHF].2DMF.THF, wherein L is a 5-isonicotinamidopyridylisotitanate ion.The preparation method comprises the following steps: carrying out a solvothermal reaction on 5-isonicotinamidopyridylisotitanic acid and a cadmium salt, and washing and drying the obtained reaction product to obtain the novel porous cadmium complex with a stable structure. The preparation method has the advantages of simple process, convenience in operation, and high yield; and the prepared 5-isonicotinamidopyridylisotitanate cadmium complex can selectively catalyze a Knoevenagel condensation reaction of p-tolualdehyde and malononitrile, has the characteristics of good selectivity and high catalytic activity as a catalyst, and can be used as a fluorescent probe for dichromate ions and permanganate ions.

The preparation method of the eutectic structure of the vanillin and the amide compound comprises the following steps: firstly, preparing a vanillin solution under a stirring condition, then adding nicotinamide or isonicotinamide which is equal to the vanillin in mole into the obtained vanillin solution, and keeping the stirring process until the nicotinamide or isonicotinamide is completely dissolved and becomes a clear solution; adding the silicon dioxide nanoparticles into the clear solution according to the mass ratio to adsorb vanillin, nicotinamide or isonicotinamide, and then separating, freeze-drying, heating, melting and drying to finally obtain a eutectic powder product of vanillin and nicotinamide or vanillin and isonicotinamide; at normal temperature, the eutectic powder product of vanillin and nicotinamide and the eutectic powder product of vanillin and isonicotinamide are dissolved in an organic solvent, after saturation is achieved, the mixture is placed in a constant-temperature and constant-humidity box to be slowly volatilized, the single crystal structure is determined, the yield is very high and can reach 90% or above, the purity reaches 98% or above, and the method is suitable for industrial production.

A cyanide-free lytic reagent composition and method for measuring the total hemoglobin concentration in a blood sample, for counting the number of leukocytes and for deferential counting of leukocyte subpopulations are described. The cyanide-free lytic reagent composition comprises a quaternary ammonium salt or a pyridinium salt to lyse erythrocytes and release hemoglobin, and an organic ligand selected from the group consisting of triazole and its derivatives, tetrazole and its derivatives, alkaline metal salts of oxonic acid, melamine, aniline-2-sulfonic acid, quinaldic acid, 2-amino-1,3,4-thiadiazole, triazine and its derivatives, urazole, DL-pipecolinic acid, isonicotinamide, anthranilonitrile, 6-aza-2-thiothymine, 3-(2-thienyl)acrylic acid, benzoic acid and alkali metal and ammonium salts of benzoic acid, and pyrazine and its derivatives to form a stable chromogen with hemoglobin, and a salt to adjust conductivity of the reagent for impedance measurement. The reagent composition is mixed with a blood sample without pre-dilution and the UV absorption of the sample mixture is measured at the predetermined absorption wavelength. Counting the number of leukocytes and differential counting of leukocyte subpopulations are accomplished simultaneously on an automated cell counter utilizing DC impedance measurement.

The present invention relates to an improved process for conversion of cyanopyridines to nicotinamides More particularly the present invention relates to preparation of nicotinamides and isonicotinamides which finds its usage in the preparation of anti-TB drug i.e. isoniazid and as an intermediate of vitamin B12. The present invention also relates to a process for a catalyst useful for the preparation of nicotinamide and isonicotinamide.

The present invention relates to a topical composition comprising from 0.001 to 10% by weight a compound of formula (I), i.e. N-cyclopropyl nicotinamide, that provides improved antimicrobial effect through generation of antimicrobial peptides when applied to an external surface of the human body. A combination of compound of formula I and at least one ingredient selected from niacinamide, picolinamide and iso-nicotinamide triggers generation of AMPs in a synergistic way.

The invention relates to a co-crystal of nifedipine and isonicotinamide, its preparation method and application. The co-crystal of nifedipine and isonicotinamide was comprehensively characterized by means of X-ray single crystal diffraction analysis, X-ray powder diffraction analysis, thermogravimetric analysis, differential scanning calorimetry analysis, and infrared spectroscopy, and it was found that the Compared with nifedipine, the co-crystal has the advantage of higher light stability. The preparation method of the co-crystal of nifedipine and isonicotinamide is simple, easy to control and good in reproducibility, and stable co-crystal of nifedipine and isonicotinamide can be obtained.

The invention provides a process for the manufacture of HI 6 dimethanesulfonate comprising contacting an O-protected pyridine aidoxime compound with bis(methylsulphonoxymethyl)ether in a suitable solvent to form an intermediate compound, contacting said intermediate compound with isonicotinamide to form an O-protected HI 6 product precursor, and de-protecting the precursor to form HI 6 dimethanesulfonate.

The invention provides an application of an HPMC and naringenin (NGN) isonicotinamide (INT) co-crystal in preparation of a medicine for preventing and treating abdominal aortic aneurysm (AAA). According to the application, firstly the co-crystal (NGN-INT) of the NGN and the INT is prepared, HPMC and PVP are added to the NGN-INT co-crystal separately, the supersaturation effect of the NGN in the HPG / PVP extension co-crystal is investigated, and a blood concentration-time curve of different forms of the NGN in mice is investigated, and results show that the HPMC can significantly increase the oral bioavailability of the NGN in the NGN-INT co-crystal than that of the PVP, and significantly promote the anti-AAA efficacy of the NGN-INT.

The invention discloses two fenbufen pharmaceutical co-crystals and a preparation method thereof, and the two co-crystals both take fenbufen as pharmaceutical active ingredients and take isonicotinamide or nicotinamide as co-crystal formations respectively. The two eutectic crystals are prepared by adopting a solvent evaporation method. The obtained eutectic crystal is characterized by differential scanning calorimetry, powder X-ray diffraction and single crystal X-ray diffraction, and formation of a new crystal form is proved. The solubility of the fenbufen medicine and the two eutectic crystals of the fenbufen medicine in water and a simulated duodenum solution is investigated, the two pharmaceutical eutectic crystals obviously improve the solubility of the fenbufen medicine, and the bioavailability of the fenbufen medicine is improved.

The invention discloses a 5-isonicotinamide-pyridyl-isophthalic acid porous copper complex, as well as a preparation method and application thereof. The porous copper complex comprises a (3,6) dual-node three-dimensional topology lattice structure; the chemical formula of the porous copper complex is [Cu(L)].DMAc.H2O, wherein L is 5-isonicotinamide-pyridyl-isophthalic acid radical ion. The preparation method comprises the following steps: solvent thermal reaction between 5-isonicotinamide-pyridyl-isophthalic acid and nantokite, washing, and drying to obtain the novel porous copper complex of which the structure is stable. The preparation method is simple in process, convenient to operate and high in productivity. The 5-isonicotinamide-pyridyl-isophthalic acid porous copper complex obtained according to the method can catalyze the Knovevenagel condensation reaction between benzaldehyde and malononitrile, is high in catalysis selectivity and catalytic activity, and can be effectively recycled and used repeatedly.

The invention discloses a co-crystal of kaempferol and isonicotinamide, a preparation method, a composition and an application thereof. Specifically, the present invention discloses a new kaempferol and isonicotinamide co-crystal with kaempferol (such as formula a) as the active ingredient of medicine and isonicotinamide (such as formula b) as the eutectic ligand; kaempferol The preparation method of the co-crystal with isonicotinamide; the application of the co-crystal of kaempferol and isonicotinamide as active ingredients in the preparation of anti-cancer, anti-cancer, anti-inflammatory, anti-oxidation, antibacterial or antiviral drugs.

The present invention discloses an isonicotinamide derivative represented by a formula (I) and a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and A are defined in the specification. The present invention further discloses a preparation method of the compounds, a drug composition containing the compound, and applications of the compounds in treatment of mammal, especially human overproliferation diseases and in preparation of drugs for treatment of mammal, especially human overproliferation diseases. The formula (I) is defined in the specification.

The present invention relates to an improved process for conversion of cyanopyridines to nicotinamides. More particularly the present invention relates to preparation of nicotinamides and isonicotinamides which finds its usage in the preparation of anti-TB drug i.e. isoniazid and as an intermediate of vitamin B12. The present invention also relates to a process for a catalyst useful for the preparation of nicotinamide and isonicotinamide.

The invention belongs to the technical field of medicines, and particularly provides an isonicotinamide and acipimox eutectic crystal II, a preparation method thereof and application thereof in preparation of hypolipidemic drugs. The isonicotinamide and acipimox eutectic crystal II prepared by the method is radiated by Cu-K alpha, and an X-ray diffraction pattern expressed by 2theta has characteristic peaks at 10.9 + / -0.2 degrees, 22.0 + / -0.2 degrees, 23.5 + / -0.2 degrees and 26.5 + / -0.2 degrees. The isonicotinamide and acipimox eutectic crystal prepared by the preparation method disclosed by the invention is good in stability in a medium, high in product purity, high in bioavailability and better in drug effect. The method is simple in preparation process and has a good industrial application prospect.