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75 results about "Ertapenem" patented technology
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Ertapenem is used to prevent and treat a wide variety of bacterial infections.
Ertapenem monosodium salt crystal and preparation method thereof
The invention discloses an ertapenem monosodium salt crystal and a preparation method thereof. The ertapenem monosodium salt crystal has a powder X-ray diffraction spectrum shown by a figure 1. The preparation method of the crystal comprises: dissolving an ertapenem monosodium salt serving as a raw material and a sodium-containing inorganic salt in water at 0 to 5 DEG C; cooling to -2 to 10 DEG C, regulating the pH value to 5 to 6 by using an acidic solution, adding active carbon for decolorization, and filtering; adding methanol and cooling to 0 to -40 DEG C; dripping normal propyl alcohol, stirring and crystallizing; and filtering, washing a filter cake by using an organic solvent, and pumping the solvent completely by using an oil pump. The ertapenem monosodium salt provided by the invention has the advantages of low residual solvent content, high stability and the like. The preparation method disclosed by the invention has the advantages of simple process, low preparation cost, suitability for industrial production and the like and has an industrial application value.
Owner:SHANGHAI ACEBRIGHT PHARMA CO LTD +2
Preparation method of ertapenem and its sodium salt
ActiveCN102731506ASolve dissolveReduce degradationOrganic chemistryBulk chemical productionErtapenemSolvent
The invention relates to a preparation method of ertapenem as shown in the formula 1 and its sodium salt. According to the method, water is used as a reaction solvent, an ertapenem intermediate as shown in the formula 2a undergoes a hydrogenated deprotection reaction in the presence of alkali and a catalyst, so as to generate ertapenem as shown in the formula 1 or its sodium salt. The single solvent water is used as a reaction solvent in the method provided by the invention, thus solving the problem of dissolving the catalyst by the reaction solvent, simplifying post-treatment operational step, reducing product degradation and raising product purity. In addition, the preparation method is economical, safe and environmentally friendly, and is more suitable for industrial operation at large scale.
Owner:CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
Process for the preparation of carbapenem using cabapenem intermediates and recovery of cabapenem
InactiveCN102250145AReduce generationNovel preparation methodOrganic active ingredientsGroup 5/15 element organic compoundsErtapenemMedicinal chemistry
The present invention aims to prepare carbapenem intermediates which can effectivly produce Ertapenem, Meropenem and Doripenem; and provides an effective process for recovering ertapenem compounds.
Owner:SAVIOR LIFETEC CORP
Preparation of carbapenem penicillin ertapenem intermediate
The invention discloses a preparation method of an intermediate for synthesizing carbapenems penicillin etapenem having the formula of VII. The preparation method comprises the following steps: allowing a compound having the formula of I and 4-methoxybenzyl chloride to react to obtain a product; reacting under the action of stannous chloride dehydrate, and regulating pH to 7; performing condensation reaction of above product and activated ester of PNZ L-hydroxyproline; reacting with methylsulfonyl chloride; reacting with potassium thioacetate; and hydrolyzing in acidic or alkaline condition, wherein PMB is shown in figure (1), PNZ is shown in figure (2), Ms is mesyl, and Ac is acetyl. The preparation method can be carried out at the room temperature, with the advantages of mild reaction condition, low cost, and easily realized industrial production.
Owner:SHANGHAI INST OF PHARMA IND CO LTD +1
A kind of method that non-palladium system prepares ertapenem
The invention discloses a method for preparing ertapenem in a non-palladium system. A docking reaction occurs under the action of ertapenem to generate protected ertapenem; 2) Add zinc powder as a reducing agent to remove the protecting group at pH=3.0-6.5; 3) Extract the ertapenem solution and crystallize to obtain Ertapenem. The method has relatively mild reaction conditions, is easy to operate, does not involve heavy metals in the whole process, and the product can be crystallized and separated out in post-treatment, with high purity.
Owner:ZHEJIANG HISOAR PHARMA
Bridged lipoglycopeptides that potentiate the activity of beta-lactam antibacterials
The present invention provides novel lipoglycopeptide compounds which are Type 1 signal peptidase inhibitors (SpsB). Compounds of the present invention are useful for the treatment of various bacterial related infectious diseases, particularly when used as a potentiator of a β-lactam antibiotic such as imipenem and ertapenem. Accordingly, the present invention provides a method for the treatment of bacterial related infections using the compounds described herein, either alone or in combination with a β-lactam antibiotic.
Owner:MERCK SHARP & DOHME CORP +1
Industrial preparation method of ertapenem
InactiveCN102351861AProcess raw materials are cheap and easy to getSimple operation processOrganic chemistryErtapenemBiochemical engineering
The invention discloses an industrial preparation method of ertapenem, comprising the following steps of: firstly synthesizing an ertapenem side chain (a compound V), and using the compound as a raw material together with 1beta-methyl vinyl phosphate (MAP) to prepare ertapenem. The invention has the following advantages of: the technology has fewer steps, the raw materials used are cheap and easily available, and the separation means is simple. Therefore, the preparation method is suitable for industrial production.
Owner:湖南欧亚药业有限公司
Ertapenem and ertapenem side chain, as well as preparation methods of ertapenem and ertapenem side chains
The invention discloses ertapenem and ertapenem side chains, as well as preparation methods of ertapenem and ertapenem side chains. L-hydroxyproline is protected by p-nitrobenzyl ester to obtain (2S,4R)-4-hydroxyl-1-(((4-Nitrobenzformyl)-oxyl)caboyl)pyrrolidine-2-carboxylic acid; then 4-nitro(1S,4S)-3-oxo-2-thia-5-azabicyclo[2.2.1]heptan-5-carboxylic anhydride can be obtained, and reacts with m-aminobenzoic acid p-nitrobenzyl ester to obtain ertapenem side chain III; and the ertapenem can be synthesized through two-step chemical reaction of condensation and deprotection to the ertapenem side chain III and a raw material MAP. An ertapenem side chain I (10), an ertapenem side chain II (13) and the ertapenem side chain III (2) which are prevailing in the market can be synthesized through simple steps, without the need of ultralow temperature, industrialization is easy, and the product purity is high, and the operation is simple and convenient.
Owner:HUNAN CHEMAPI BIOLOGICAL TECH
Method for preparing ertapenem intermediate
ActiveCN102690267AImprove stabilityNot easy to absorb moistureOrganic chemistryBulk chemical productionErtapenemSide chain
The invention provides a preparation method of an ertapenem intermediate or pharmaceutically acceptable salts thereof. The method provided by the invention comprises the following steps: carrying out condensation reaction on ertapenem side chain dimer or pharmaceutically acceptable salts thereof and carbapenem mother nuclide in the presence of a compound R3P and alkali to prepare the ertapenem intermediate or pharmaceutically acceptable salts thereof. The preparation method provided by the invention has the advantages of high reaction activity and high speed, can shorten the working hours and lower the cost in industrial production, and avoids using the ertapenem side chain ES', which can easily absorb moisture, can be easily oxidized and can not be easily preserved due to unstable properties, thereby being beneficial to industrial production.
Owner:SHENZHEN HAIBIN PHARMA +1
Preparation of Carbapenem Intermediate and Their Use
InactiveUS20110288289A1Simple and commercially viableGood yieldOrganic chemistryErtapenemMedicinal chemistry
The present invention relates to preparing carbapenem intermediates that are useful to produce Ertapenem, Meropenem and Doripenem.
Owner:SAVIOR LIFETEC CORP
Novel drug resistant gene of Klebsiella pneumoniae
The invention discloses a novel drug resistant gene of Klebsiella pneumonia. The novel drug resistant gene of the Klebsiella pneumonia is obtained by extracting the Klebsiella pneumonia which is drug resistant against imipenem and ertapenem. The nucleotide sequence of the novel drug resistant gene of the Klebsiella pneumonia is SEQ ID NO. 1 and the amino acid sequence is SEQ ID NO. 2. Functions of the novel gene are researched through a plasmid transduction experiment and a prokaryotic expression experiment, and a result shows that the novel gene is drug-resistant against a plurality of drugs. The novel drug resistant gene of the pneumonia Klebsiella has a great significance on reasonable use of antibiotics, reduction of carbapenems drug-resistant bacteria produced during severe infection, and research and development of new drugs for inhibiting drug-resistance performance of bacteria.
Owner:ACROBIOSYSTEMS INC
Ertapenem pharmaceutical composition
ActiveCN103127097AImprove stabilityInhibit aggregationAntibacterial agentsPowder deliveryErtapenemMedicine
The invention relates to Ertapenem pharmaceutical composition which comprises Ertapenem and protective agents. The Ertapenem pharmaceutical composition obviously improves the stability of active ingredients in the preparation of the composition and a long-term storage process.
Owner:SHANGHAI INST OF PHARMA IND +2
Process for the preparation of carbapenem using cabapenem intermediates and recovery of cabapenem
ActiveUS20110288290A1Increase effective yieldGeneration of impurity can be reducedOrganic active ingredientsGroup 5/15 element organic compoundsErtapenemOrganic chemistry
Owner:SAVIOR LIFETEC CORP
Dual-protection ertapenem crystal and preparation method thereof
The invention discloses a dual-protection ertapenem crystal and a preparation method thereof. The dual-protection ertapenem crystal has a powder X-ray diffraction spectrogram shown as a Figure 1 and is prepared according to the following steps of: firstly, performing condensation reaction of carbapenems mother nucleus MAP and an ertapenem side chain, pouring a reaction liquid into a mixed solvent which is prepared from a buffer solution with a pH value of 4 to 6 and an ester solvent after reaction, extracting and layering; and secondly, adding the buffer solution into an organic layer for washing; and finally, drying the organic layer by using anhydrous sodium sulfate, filtering, stirring and crystallizing at the temperature of 0 to 30 DEG C, filtering, washing a filter cake, and performing vacuum drying. The dual-protection ertapenem crystal provided by the invention is high in stability and purity, and establishes a foundation and provides a guarantee for subsequent preparation of high-purity and stable-quality ertapenem. Moreover, the preparation method is simple, is easy for realizing mass production, meets industrial production requirement and has practical and promotional values, and raw materials are cheap and readily available.
Owner:SHANGHAI ACEBRIGHT PHARMA CO LTD +2
Ertapenem separation and purification method
InactiveCN101838230AHigh purityEasy to operateIon-exchange process apparatusAntibacterial agentsErtapenemPurification methods
The invention relates to an ertapenem purification method, which comprises the following steps: dissolving a crude product of ertapenem by water; using a chromatographic column adopting a porous polystyrene copolymer resin as a separation filler to carry out adsorption; carrying out eluting by using phosphate buffers with different organic phase ratios; and carrying out post treatment on the obtained eluent to obtain an ertapenem purified product. The method has simple operation and high product purity and yield and is suitable for industrial products.
Owner:NANJING UNIV OF TECH
New monosodium ertapenem crystal form and preparation process thereof
InactiveCN104788454AImprove stabilityImprove filtering effectOrganic chemistry methodsErtapenemCombinatorial chemistry
The present invention relates to the technical field of pharmaceutical intermediate synthesis, particularly to a new monosodium ertapenem crystal form and a preparation process thereof, wherein the characteristic peaks exist when the 2[theta] angle is 4.63+ / -0.1 DEG, 5.51+ / -0.1 DEG, 7.32+ / -0.1 DEG, 7.74+ / -0.1 DEG, 8.19+ / -0.1 DEG, 10.99+ / -0.1 DEG, and 12.99+ / -0.1 DEG.
Owner:ZHEJIANG JIUZHOU PHARM CO LTD
Penem derivative containing isothioureido sulfhydryl pyrrolidine
ActiveCN101357918AHigh antibacterial activityBroad spectrum antibacterialAntibacterial agentsOrganic active ingredientsErtapenemPyrrolidine
The invention relates to an ertapenem derivative which contains heter-thioureido sulfhydryl pyrrolidine, the ester which is easy to be hydrolyzed, the salt acceptable in pharmacy, the isomer thereof, the hydrate thereof and the hydrate of ester or salt thereof shown in the formula (I) and a preparing method of the compound shown in the formula (I). The compounds are used as active materials, in particular to be used for preparing the medicine for curing or preventing infectious diseases and to be used as a drug combination containing the compound shown in the formula (I). In the formula (I), the definitions of R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, and n are elaborately described in an introduction.
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD
Penem derivative containing sulfhydryl nitrogen heterocyclic ring and vinyl nitrogen heterocyclic ring
ActiveCN101372490AHigh antibacterial activityShow low toxicityAntibacterial agentsOrganic active ingredientsErtapenemNitrogen
The invention belongs to the technical field of medicine, and more particularly relates to ertapenem derivatives which are shown in general formula (I) and contain hydrosulphonyl nitrogen heterocyclic ring ethylene azacyclonol, salt which can be accepted by the derivatives on pharmacy, ester of the derivatives that is easy to hydrolyze, and isomer of the derivatives; wherein, R1, R2, R3, R4, m, n and are defined as instruction; the invention also relates to a method used for preparing the compounds, medicine combinations containing the compounds, and the application of the compounds in the preparation of the medicine for treating and / or preventing infectious diseases.
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD
Selective enrichment medium for carbapenem-resistant bacteria
The present invention relates to a method for direct detection and differentiation of carbapenem-resistant bacteria in a sample comprising (i) inoculation with said sample of a culture medium comprising at least meropenem and / or ertapenem and at least one chromogenic agent, (ii) incubation of said culture medium under conditions allowing the growth of carbapenem-resistant bacteria, and (iii) detection of colonies formed on said culture medium corresponding to carbapenem-resistant bacteria, as well as a culture medium suitable for use in such a method.
Owner:RAMBACH ALAIN
Carbapenem penicillin ertapenem intermediate, and preparation and use thereof
The invention discloses a preparation method of an intermediate for synthesizing carbapenems penicillin etapenem having the formula of VI, and a preparation method and application in the preparation of the carbapenems penicillin etapenem thereof. The preparation method comprises the following steps: heating a shown compound and potassium thioacetate for reacting, wherein PMB is shown in figure (1), PNZ is shown in figure (2), Ms is mesyl, and Ac is acetyl. The intermediate can be used for preparing etapenem side chain, and further etapenem. The preparation method can be carried out at the room temperature, with the advantages of mild reaction condition, low cost, simple operation, simple experiment condition, no requirement of expensive reagent, high yield, and easily realized industrial production.
Owner:SHANGHAI INST OF PHARMA IND +1
Method for preparing ring-opening impurity of carbapenems
The invention relates to a method for preparing a ring-opening impurity of carbapenems. The ring-opening impurity is of a structure represented by formula I. In the formula I, R represents a meropenem side chain, an ertapenem side chain or a doripenem side chain. The method includes the following steps: (1) adding carbapenems into an alkaline solution, stirring and reacting for 1-4 hours; (2) adjusting the pH to 6.0-9.0; (3) freeze-drying the materials to obtain the ring-opening impurity of carbapenems. The method provided by the invention is simple to operate and short in reaction time; the product has the purity of 95% or above and can be directly used as a reference substance for quantitative and qualitative research on the ring-opening impurity of carbapenem products, so that the product quality can be effectively controlled. The formula I is shown in the description.
Owner:山东安弘制药有限公司
Carbpenem penicillin ertapenem intermediate, and preparation and use thereof
InactiveCN101376636AMild reaction conditionsLow costOrganic compound preparationAmino-carboxyl compound preparationErtapenemPenicillin
The invention discloses an intermediate for synthesizing carbapenems penicillin etapenem having the formula of III, and a preparation method and application in the preparation of carbapenems penicillin etapenem thereof. The preparation method comprises the following steps: heating an intermediate having the formula of II under the action of stannous chloride dehydrate for reacting and regulating pH of reaction solution to greater than 7 with inorganic alkal, wherein PMB is the formula V. The intermediate can be used for preparing etapenem side chain, and further etapenem. The preparation method can be carried out at room temperature, with the advantages of mild reaction condition, low cost, simple operation, simple experiment condition, no requirement for expensive reagent, high yield, no requirement for refining, and easily applicable industrialized production.
Owner:SHANGHAI INST OF PHARMA IND +1
Method for simultaneously classifying and detecting carbapenemase, AmpC enzyme and extended-spectrum beta-lactamase
InactiveCN106047986AAvoid missing detectionIncrease positive rateMicrobiological testing/measurementErtapenemCefoxitin
The invention relates to the technical field of clinical microorganism bacterial detection, in particular to a method for simultaneously classifying and detecting carbapenemase, AmpC enzyme and extended-spectrum beta-lactamase. The method includes the steps that antibiotic test paper and EDTA test paper are selected for use, detected drug-resistant to-be-detected bacteria are prepared into a 0.5 McFarland unit bacterium suspension and evenly smeared to the surface of an M-H plate, the test paper containing EDTA is placed in the center of the surface of the M-H plate coated with the to-be-detected bacteria, ceftazidime (CAZ) antibiotic test paper, ertapenem (ETP) antibiotic test paper, piperacillin / tazobactam (TZP) antibiotic test paper, ceftazidime / clavulanic acid (CAZ / CLAV) antibiotic test paper, imipenem (IMP) antibiotic test paper, and cefoxitin (FOX) antibiotic test paper are attached around the EDTA test paper, gaps are reserved between the EDTA test paper and other antibiotic test paper and between every two pieces of antibiotic test paper, incubation is conducted for 16-18 h at 35 DEG C, and antibacterial zone diameters of the EDTA test paper and other antibiotic test paper are observed and recorded respectively. Cost is low, the detection rate is high, and application and popularization in a clinical laboratory are easy.
Owner:明德松
Penem derivative containing sulfhydryl pyrrolidine formamido triazine
ActiveCN101357920AHigh antibacterial activityLow toxicityAntibacterial agentsOrganic chemistryErtapenemFormamide
The invention belongs to the medicine technology field, which more particularly relates to an ertapenem compound containing hydrosulphonyl pyrrolidine formamide triazine, the salt acceptable in pharmacy thereof, the ester which is easy to be hydrolyzed, the isomer thereof, the hydrate thereof and the hydrate of ester or salt thereof shown in the formula (I) and a preparing method of the compound shown in the formula (I); wherein, the definitions of R<1>, R<2>, R<3>, R<4>, R<5> and R<6> are elaborately described in an introduction. The invention also relates to preparing methods of compounds and the drug combination containing the compounds and the applications of the compounds in preparing the medicine for curing or preventing infectious diseases.
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD
Penem compound containing dihydroimidazole formamido
ActiveCN101357916ABroad-spectrum potent antibacterial activityBroad-spectrum antimicrobial activityAntibacterial agentsOrganic active ingredientsErtapenemStereochemistry
The invention relates to a method for preparing an ertapenem compound as shown in general formula (I) which contains glyoxalidine formamido, the ester which is easy to be hydrolyzed, the pharmaceutically acceptable salt, the isomer, the hydrate, the ester or salt hydrate thereof and the compound as shown in formula (I); the compounds are used for producing medical active materials, particularly preparing medicines for curing and / or preventing infectious diseases and pharmaceutical combination of the compounds as shown in formula (I). Definitions of R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7> and R<8> in the general formula (I) can be seen in the specification.
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD
Dual-protection ertapenem crystal and preparation method thereof
Owner:SHANGHAI ACEBRIGHT PHARMA CO LTD +2
One-pot preparation process of monosodium ertapenem
The present invention relates to the technical field of medicine synthesis, especially to the technical field of monosodium ertapenem preparation, specifically to a one-pot preparation process of monosodium ertapenem. The one-pot preparation process comprises: i) carrying out a condensation reaction of a compound represented by a formula (a) and a compound represented by a formula (b) in the presence of an organic alkali, pouring the reaction solution into a halogenated alkane solvent, washing with a buffer solution, and concentrating the organic layer to obtain a compound represented by a formula (c); and ii) adding tetrahydrofuran to dissolve the concentrated compound represented by the formula (c), cooling to a temperature of -5-10 DEG C, adding a sodium bicarbonate solution with a mass fraction of 0.5-5% in a dropwise manner, adding palladium carbon, introducing hydrogen gas, filtering after completing the reaction, rinsing the filter cake with water, adjusting the pH value of the filtrate with acetic acid / methanol to 5-6, adding an alcoholic solvent / dichloromethane, carrying out stirring layering, adding a solvent A to the obtained water layer, adding a methanol / n-propanol mixed solution in a dropwise manner at a temperature of 0-5 DEG C, filtering, and rinsing the filter cake with acetone to obtain the monosodium ertapenem.
Owner:ZHEJIANG JIUZHOU PHARM CO LTD
Penem derivative containing sulfhydryl formamide benzenesulfonyl pyrrolidine
ActiveCN101357919AHigh antibacterial activityLow toxicityOrganic active ingredientsOrganic chemistryErtapenemPyrrolidine
The invention belongs to the medicine technology field, which particularly relates to an ertapenem derivative containing hydrosulphonyl pyrrolidine formamide benzenesulfonyl, the salt thereof acceptable in pharmacy, the ester which is easy to be hydrolyzed, the isomer thereof, the hydrate thereof and the hydrate of ester or salt thereof shown in the formula (I) and a preparing method of the compound shown in the formula (I); wherein, the definitions of R<1>, R<2>, R<3>, R<4>, R<5> and R<6> are elaborately described in an introduction. The invention also relates to preparing methods of compounds and the drug combination containing the compounds and the applications of the compounds in preparing the medicine for curing or preventing infectious diseases.
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD
Carbpenem penicillin ertapenem intermediate, and preparation and use thereof
InactiveCN101376633AMild reaction conditionsLow costOrganic chemistryOrganic compound preparationErtapenemPenicillin
The invention discloses an intermediate shown as the formula II for synthesizing carbapenem penicillin ertapenem, and a preparation method thereof. The preparation method comprises the following steps: reacting a compound shown as a formular I with 4-methoxybenzyl chloride in the presence of an organic alkali reagent as a catalyst in a nonpolar solvent. The invention also discloses the application of the intermediate on the preparation of the carbapenem penicillin ertapenem. The PMB is the formula III. The intermediate compound can be prepared into ertapenem side chain and then further into ertapenem. The preparation method has the advantages that the conditions of each reaction are mild, the reaction can be carried out at the room temperature, the cost is low, the method is easily applied on an industrialized production, the operation is simple, the experimental condition is simple, no expensive reagent is required, the yield is high and reaches above 90%, and the purity is high.
Owner:SHANGHAI INST OF PHARMA IND +1
Intermediate of ertapenem, a composition comprising the same and preparation methods thereof
ActiveUS20120095209A1High purityGood storage stabilityAntibacterial agentsOrganic active ingredientsErtapenemPresent method
Intermediates of Ertapenem of formula 2a wherein Np represents (I) or (II), and P1 and P2 represent carboxyl protecting groups, and their preparation methods. Compound 2a prepared by the present methods in solid form is amorphous. The present invention also relates to a composition comprising at least 95% of the intermediate of Ertapenem of formula 2a.
Owner:CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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