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54 results about "Tacrine" patented technology
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Tacrine is a centrally acting acetylcholinesterase inhibitor and indirect cholinergic agonist (parasympathomimetic). It was the first centrally acting cholinesterase inhibitor approved for the treatment of Alzheimer's disease, and was marketed under the trade name Cognex. Tacrine was first synthesised by Adrien Albert at the University of Sydney. It also acts as a histamine N-methyltransferase inhibitor.
Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase inhibitors
InactiveUS20100227852A1Avoid damageReduce riskBiocideNervous disorderCholinesterase inhibitionRivastigmine
Owner:MERZ PHARMA GMBH & CO KGAA
Combination therapy using 1-aminocyclohexane derivatives and acetylcholinesterase and inhibitors
InactiveUS20090124659A1Avoid damageReduce riskBiocideNervous disorderCholinesterase inhibitionDepressant
The invention relates to a novel drug combination therapy useful in the treatment of dementia comprising administering an 1-aminocyclohexane derivative such as memantine or neramexane and an acetylcholinesterase inhibitor (AChEI) such as galantamine, tacrine, donepezil, or rivastigmine.
Owner:MERZ PHARMA GMBH & CO KGAA
Therapy for neurological diseases
InactiveUS6036973AAvoiding toxic rangeShorten the progressPowder deliveryPill deliveryDiseaseNervous system
A dosage form is disclosed for administering 10 ng to 1200 mg tacrine to a patient in need of tacrine therapy.
Owner:ENCINAL PHARMA INVESTMENTS
Tacrine-ferulaic acid hetero-blend, preparation method and pharmaceutical compositions thereof
The invention relates to a cross-linked body of Tacrine and ferulic acid or a dynamic isomer, medicine salts, a pro-drug or a solvate thereof, wherein, the structural formula is shown in formula (I). The invention also relates to a method for making the same, a combination taking the formula (I) compound as active composition, and application of the compound and the combination thereof taken as the medicine for preventing and curing AChE-mediated diseases, in particular the application in preparation of the medicine for preventing Alzheimer diseases and dementia, in which other oxidative stresses take part.
Owner:SUN YAT SEN UNIV
Tacrine heterocomplex, preparation method and use in medicines for curing neurodegenerative diseases thereof
InactiveCN102229602AStrong inhibitory activityHas anti-free radical activityOrganic active ingredientsNervous disorderCholinesterasePharmaceutical drug
The invention belongs to the field of medicines and chemical industries, and discloses a method for preparing a series of tacrine heterocomplexes and use in medicines for curing neurodegenerative diseases. The invention further relates to use of the tacrine heterocomplex for preparing medicines for curing the neurodegenerative diseases independently or with other medicines. The structural formula of the tacrine heterocomplex is as follows: FORMULA, wherein when X is O or CH2 and Y is N, R1, R2 and R3 are H; n is 2, 3, 4, 5, 6, 8, 9, 10, 11 or 12; when X is O or CH2 and Y is C, R1 is H, OH or OCH3; R2 is H, OH or OCH3; R3 is H, OH or OCH3; R4 is H, OH or OCH3; and n is2, 3, 4, 5, 6, 8, 9, 10, 11 or 12. The tacrine heterocomplex disclosed by the invention has strong inhibitory activity to acetylcholinesterase (AChE) and butyrylcholine esterase (BuChE), which are effectively used for curing the neurodegenerative diseases, such as Alzheimer's diseases.
Owner:SUN YAT SEN UNIV
Cholinesterase Inhibitors In Liposomes And Their Production And Use
InactiveUS20080031935A1Avoid intakeImprove bioavailabilityBiocideNervous disorderEnantiomerRivastigmine
The invention relates to a pharmaceutical composition based on an active ingredient that is enclosed in liposomes for topical, transdermal application. The interior of said liposomes comprises an acidic, aqueous medium containing at least one cholinesterase inhibitor, preferably from the group containing donepezil, rivastigmine, galantamine, physostigmine, heptylphysostigmine, phenserine, tolserine, cymserine, thiatolserine, thiacymserine, neostigmine, huperzine, tacrine, metrifonate and dichlorvos, or an enantiomer or derivative of at least one of said compounds. In addition, the invention relates to a method for producing said composition, optionally in a sterile form and also to the use of the liposomes charged with the active ingredient in various galenic formulations for topical, transdermal application with a depot effect in the epidermis, for the prophylaxis and / or treatment of cutaneous neuropathic pain or the loss of cutaneous sensory function as a result of neuropathy.
Owner:SANOCHEMIA PHARMA AG
Tacrine-coumarin derivative containing triazole and application of derivative
ActiveCN105503840AStrong inhibitory activityLow toxicityNervous disorderOrganic chemistryAmyloid betaHydrolysis
The invention relates to a tacrine-coumarin derivative containing triazole and an application of the derivative and belongs to the technical field of biological medicine. The derivative comprises compounds represented as a formula I and pharmaceutically acceptable salt, and three preparation methods of the derivative are provided; a pharmacological experiment proves that the derivative is acetylcholinesterase inhibitor and can inhibit activity of acetylcholin esterase, butyrylcholine esterase and MAO (monoamine oxidase), and meanwhile, the derivative can inhibit autopolymerization of beta-amyloid protein, delay hydrolysis of acetyl choline and autopolymerization of beta-amyloid protein, improve the function of acetyl choline on synapsis and be used for treating Alzheimer's disease effectively.
Owner:GUANGDONG UNIV OF TECH
Tacrine-8-hydroxyl(amine)quinoline derivative and application thereof
InactiveCN105367553AHas anti-Alzheimer's activityInhibition of self-polymerizationNervous disorderOrganic chemistryQuinolinePharmaceutical medicine
The present invention relates a tacrine-8-hydroxyl(amine)quinoline derivative and applications thereof, and belongs to the technical field of biological medicines. The derivative comprises a compound of a formula I and a pharmaceutically acceptable salt thereof. A preparation method thereof comprises the step of: performing reductive amination and deprotection on the compounds Id and Ii and an intermediate In / In' to obtain a compound I, wherein the compound I can react in an alcohol solution to produce a salt. Pharmacological tests verify that the compound has the activity against Alzheimer's disease and can inhibit acetylcholinesterase and butyrylcholinesterase activity, and meanwhile can inhibit self-polymerization of the beta-amyloid protein, and has a certain chelating effect on metal ions, particularly Cu<2+> and Zn<2+>, so that the hydrolysis of the acetylcholinesterase and the self-polymerization of the beta-amyloid protein are retarded, the effect of the acetylcholinesterase on synapses is improved, and the metal ions in the brain is regulated, and therefore the compound is effective for treating Alzheimer's disease.
Owner:GUANGDONG UNIV OF TECH
Tacrine- nicotinic acid conjugate, preparation method and medical application thereof
The invention relates to the medical field and in particular relates to tacrine- nicotinic acid conjugates. The invention further discloses a preparation method of the tacrine- nicotinic acid conjugates as well as medical salts, pharmaceutical compositions or pharmaceutical agents containing the compounds and application of the compounds in medicines, especially treating Alzheimer disease.
Owner:CHINA PHARM UNIV
Therapies for cognition and learning enhancement
InactiveUS20090252704A1Easy to learnImprove cognitionBiocidePeptide/protein ingredientsDiseaseCognition
The invention relates to a combination comprising an amount of an NO donor, such as ISDN, and / or an amount of another pharmaceutical agent that enhances neurotransmission or which acts as neuroprotectants such as memantine, clomethiazole and tacrine. These compositions can be used in producing cognition and learning enhancement, whereby the invention also provides for a new method of treatment of Alzheimer's disease and related neurodegenerative disorders.
Owner:GREEN ALLAN M +1
Tacrine-pyridinothiophene compounds and preparation method and applications thereof
ActiveCN110143956AImprove memory functionImprove cognitive functionOrganic active ingredientsNervous disorderDiseaseCholinesterase
The invention belongs to the medicine field, and relates to tacrine-pyridinothiophene compounds and applications thereof. The saccharides of tacrine-pyridinothiophene compounds have activity on inhibiting kinase-3beta acetyl cholinesterase dual targets. The compounds can be used as a precursor for preventing Alzheimer's disease by inhibiting the activity of cholinesterase.
Owner:CHINA PHARM UNIV
Gardenamide A-tacrine diad compound as well as preparation method and application thereof
ActiveCN106565675ASimple preparation processSignificant effectOrganic active ingredientsNervous disorderTreatment effectGenipin
The invention belongs to the field of pharmaceutical chemistry, and discloses a gardenamide A-tacrine diad compound as well as a preparation method and application thereof. The structural formula of the compound is shown as formula I. The compound is prepared through the following steps: (1) genipin is adopted as a raw material I and hemiacetal at the C-1 position of genipin is converted into lactone firstly, lactone is converted into lactam secondly, and hydroxyl at the C-10 position is oxidized into aldehyde finally, thereby obtaining an intermediate compound DG; (2) methyl anthranilate is adopted as a raw material II and chloro tacrine is prepared through hydrolysis and cyclization reactions firstly, and an intermediate compound TN-n is prepared through a nucleophilic substitution reaction between chloro tacrine and corresponding diamine secondly; and (3) the target compound is obtained through an amination-reduction reaction between the prepared intermediate compound DG and intermediate compound TN-n. The compound disclosed by the invention is reported for the first time, has a treating effect on neurodegenerative diseases, and can be applied to preparation of a drug for treating the neurodegenerative diseases.
Owner:JINAN UNIVERSITY
Theacrine-based supplement and method of use thereof in a synergistic combination with caffeine
ActiveUS20180104248A1Extended durationIncrease intensityOrganic chemistryAmine active ingredientsCo administrationTheacrine
A human dietary supplement comprises theacrine and optionally other compounds that modulate the effects of theacrine. Uses for the theacrine-containing supplement include improvement of at least one of mood, energy, focus, concentration or sexual desire or a reduction of at least one of anxiety or fatigue. A synergistic composition comprises co-administration of theacrine and caffeine, wherein the co-administered caffeine reduces theacrine oral clearance (CL / F) and oral volume of distribution (Vd / F). In addition, the co-administered caffeine increases area under the plasma concentration time curve (AUC) of theacrine, and increases theacrine maximum plasma concentration (Cmax) in comparison with the corresponding pharmacokinetic parameters when theacrine is administered alone.
Owner:ORTHO NUTRA
Multi-target tacrine derivative and preparation method and application thereof
ActiveCN110551067AInhibitory activityWide range of securityOrganic active ingredientsNervous disorderCholinesteraseHalogen
The invention provides a multi-target tacrine derivative and a preparation method and application thereof. The compound has the structure shown in a formula (I) (please see the specification in the formula (I)), wherein n is a natural number greater than 1; m is 1 or 2; p is 0 or 1; R1 is H or halogen; and Y is selected from the following structures (please see the specification for the structures) or, a pharmaceutically acceptable salt of a compound in a formula (X). According to the compound, activity of histone deacetylase (HDACs), acetylcholinesterase (AChE) or butyryl cholinesterase (BChE) can be effectively inhibited.
Owner:SHANDONG UNIV
CHR20/21-tacrine heterozygote compound as well as preparation method and application thereof
ActiveCN107522691ASimple preparation processSignificant effectNervous disorderOrganic chemistryNeuronal damageCurative effect
The invention belongs to the technical field of medicinal chemistry and discloses a CHR20 / 21-tacrine heterozygote compound, a preparation method thereof and an application of the compound in preparation of a drug for treating neurodegenerative diseases. The CHR20 / 21-tacrine heterozygote compound has the structural formula shown in the formula I, wherein n ranges from 1 to 7. The invention also provides the preparation method of the CHR20 / 21-tacrine heterozygote compound. The CHR20 / 21-tacrine heterozygote compound can be used for preparing the drug for treating the neurodegenerative diseases, has a treatment effect on the neurodegenerative diseases and particularly can be used for preparing a drug for treating the Alzheimer's disease, particularly, a drug for treating the Alzheimer's disease caused by injury of dopaminergic neurons. Compared with other prior arts, the compound is simple to prepare and has the curative effect superior to that of tacrine.
Owner:JINAN UNIVERSITY
Tacrine-phenothiazine isodiad compound and preparation method thereof
ActiveCN102936244ALow toxicityImprove bindingNervous disorderOrganic chemistryStructural formulaPhenothiazine
The invention discloses a tacrine-phenothiazine isodiad compound and a preparation method thereof, wherein the tacrine-phenothiazine isodiad compound has a structural formula shown by a general formula (I) and a general formula (II): the tacrine-phenothiazine isodiad compound is combined with tacrine and phenothiazine parent nucleuses which are used for effectively treating senile dementia, is added with a proper length of a linking group, has dual inhibition functions of Acetylcholinesterase (AchE) and tau protein hyperphosphorylation, is relatively lower in toxicity, and can be used for prevention and treatment of Alzheimer's Dieses (AD).
Owner:HEFEI UNIV OF TECH
Deferasirox-tacrine metal ion chelating agent and pharmaceutical use thereof
InactiveCN104817538AOvercoming the shortcomings of acting on a single targetImprove utilization efficiencyNervous disorderOrganic chemistryDiseaseCarbon chain
The invention provides a deferasirox-tacrine metal ion chelating agent, the structural formula of which is shown as formula I. The invention also provides a preparation method of the deferasirox-tacrine metal ion chelating agent and application of the chelating agent in preparation of drugs treating Alzheimer's disease. According to the invention, deferasirox and tacrine are connected together through carbon chains of different lengths, the metal-chelating properties and antioxidant properties of deferasirox are reserved, and the connected tacrine matrix retains the original acetylcholine esterase inhibitory activity. The obtained novel ion chelating agent has multiple functions and can act on multiple target points. (formula I).
Owner:SOUTHEAST UNIV
Tacrine-bifendate heterocomplex as well as preparation method and application thereof
ActiveCN105111195AAnti-inflammatoryAnti-cancerOrganic active ingredientsNervous disorderDiseaseAcetylcholine esterase
The invention relates to tacrine-bifendate heterocomplex as well as a preparation method and an application thereof, and belongs to the field of medicine and chemical industry. The heterocomplex has a general structure of the following formula (I) or formula (II) as shown in the specification, wherein R1=H or Cl, R2=H or Cl; Y=CH2, NCH3, NH, carbonyl, oxalyl, 1,3- malonyl, p-cyclohexane or OCH2CH2O; m=0 to 4, n=0 to 4; m and n are respectively of an integer, and a carbon end of -CH2-NH- of the formula (II) is disposed at 3-position or 4-position. The compounds expressed by the structural formula (I) and (II) have an excellent effect of inhibiting acetylcholin esterase. The invention further relates to an application of a medicinal composition of the tacrine-bifendate heterocomplex and a medicinal composition adopting the tacrine-bifendate heterocompolex as an active component in treating, improving or preventing relevant diseases mediated by acetylcholin esterase.
Owner:HENAN UNIVERSITY
Sulfydryl-containing tacrine derivative and preparation method and application thereof
InactiveCN102391180AContribute to damageMaintain acetylcholinesterase inhibitory activityOrganic active ingredientsNervous disorderNervous systemOxidative stress
The invention provides a sulfydryl-containing tacrine compound or a dynamic isomer or a medicinal salt thereof. The compound or the dynamic isomer or the medicinal salt thereof have the functions of suppressing acetylcholine esterase, enhancing sea horse LTP (Long-Term Potentiation) and improving learning and memory, and can be used for treating, improving or preventing cognitive function decline-related neurous system diseases such as the Alzheimer's disease, vascular dementia, mild cognitive impairment and other oxidative stress participated dementia.
Owner:HUAZHONG UNIV OF SCI & TECH
Preparation method and application of enzyme regulated nanometer supermolecule vesicle
InactiveCN102580100AEasy to prepareImprove stabilityOrganic active ingredientsNervous disorderBuilding unitSenile dementia
The invention discloses enzyme regulated nanometer supermolecule vesicle of which the building unit takes C4AS as a host and MYC1 as a guest, and a supramolecule assembly is built through inclusion complexation and mutual effect of the host and the gust; and the preparation method is as follows: C4AS and MYC1 are dissolved into water, and supermolecule vesicle solution is obtained after uniform mixing, and choline esterase is added so as to enable supermolecule vesicle in supermolecule vesicle solution to depolymerize gradually by the time. The invention has the advantages as follows: the preparation method is simple and convenient, and the use level of host and guest raw materials are less; the supermolecule vesicle is biocompatible and have excellent stability, has an excellent select responsiveness to choline esterase, can load hydrophilic drug tacrine for curing senile dementia, the loaded tacrine has high selectivity and is released on the target position of the choline esterase properly, and the enzyme regulated nanometer supermolecule vesicle has a wide application scope in the field of loading, transporting and target releasing drug for curing senile dementia.
Owner:NANKAI UNIV
Tacrine-beta-carboline conjoined multifunction cholinesterase inhibitor
The invention relates to the field of medicinal chemistry, and particularly relates to tacrine-beta-carboline conjoined compounds (I, II and III). The pharmacodynamic test proves that the compound disclosed by the invention can be used as a multifunction cholinesterase inhibitor, and can be clinically applied to treatment of an alzheimer disease.
Owner:CHINA PHARM UNIV
2-carboxyl piperazine linked tacrine-8-amino(hydroxyl) quinoline derivative as well as preparation and application
ActiveCN110041309AEnhance the function of synapsesEffective treatmentOrganic active ingredientsNervous disorderChemical synthesisDisease
The invention relates to the technical field of chemical synthesis, and specifically relates to a 2-carboxyl piperazine linked tacrine-8-amino(hydroxyl) quinoline derivative as well as preparation andapplication. The 2-carboxyl piperazine linked tacrine-8-amino(hydroxyl) quinoline derivative is a chemical compound shown in a formula I (the formula I is shown in the description) or a pharmaceutically acceptable salt thereof, and a solvent chemical compound, an enantiomer, a diastereoisomer, a tautomer or a mixture in any proportion of the chemical compound shown in the formula I or the pharmaceutically acceptable salt thereof, and includes a racemic mixture. Confirmed by a pharmacological test, the kind of chemical compound has an inhibiting effect on the activity of acetylcholinesterase(AChE) and butyrylcholinesterase(BuChE), and belongs to a cholinesterase inhibitor; the chemical compound also has an inhibiting effect on self-aggregation of beta-amyloid protein, and has delayed action on hydrolysis of acetylcholine and self-aggregation of the beta-amyloid protein, thereby improving the effect of the acetylcholine on a synapse, and finally realizing the purpose of effectively treating alzheimer's disease (AD).
Owner:GUANGDONG UNIV OF TECH +1
Pyrone compound and application thereof
InactiveCN111592552AGood inhibition rateEnhanced inhibitory effectNervous disorderOrganic chemistryCholinesterase inhibitionAcetylcholine esterase
The invention provides a pyrone compound and application thereof, and belongs to an acetylcholin esterase inhibitor. An acetylcholin esterase inhibition experiment is carried out on the compound, an experiment result shows that the acetylcholin esterase inhibition effect of the compound Id is obviously superior to that of a positive control drug Tacrine, and the compound Id is expected to be developed into a drug or a prodrug thereof for treating and preventing Alzheimer related diseases.
Owner:OCEAN UNIV OF CHINA
Tacrine derivative as CDKs inhibitor and application thereof
ActiveCN114853672ANovel structureStrong antiproliferative activityOrganic active ingredientsOrganic chemistryMedicinePerylene derivatives
The invention relates to a tacrine derivative serving as a CDKs inhibitor and application of the tacrine derivative, the structural general formula of the derivative is shown in the formula I. The tacrine derivative has the advantages of novel structure, high anti-proliferative activity and CDK2 and CDK9 inhibitory activity. Therefore, the compound plays an important role in preparation of drugs for preventing or treating tumors;
Owner:GENERAL HOSPITAL OF THE NORTHERN WAR ZONE OF THE CHINESE PEOPLES LIBERATION ARMY
Tacrine-heteroauxin heterozygous compound as well as preparation method and application thereof
InactiveCN107814787AEasy to prepareRaw materials are easy to getOrganic active ingredientsNervous disorderDiseaseDrugs synthesis
The invention discloses tacrine-heteroauxin heterozygous as well as a preparation method and application thereof, and belongs to the field of medicine synthesis. A structural formula of the compound is shown in a formula (I) which is shown in the description, wherein n is equal to 1 to 7. The compound is not reported in literatures, and has better AChE and BChE double inhibition activity, and potential application prospect on treating AD (Alzheimer's disease).
Owner:UNIV OF JINAN
Cholinesterase inhibitors in liposomes and their production and use
Owner:SANOCHEMIA PHARMA AG
Preparation method and application of tacrine-sinapic acid heterozygote
ActiveCN107652233AStrong inhibitory activityEnhanced inhibitory effectOrganic active ingredientsNervous disorderDiseaseCytotoxicity
The invention discloses a tacrine-sinapic acid heterozygote, a medicinal composition containing the tacrine-sinapic acid heterozygote, and a preparation method and application thereof. The tacrine-sinapic acid heterozygote has the following structure: the formula is as shown in the description. Experiments prove that the tacrine-sinapic acid heterozygote has high inhibitory activity on acetylcholin esterase (AChE) and butyrylcholine esterase (BuChE), has acetylcholin esterase inhibition capability which is 15 times that of tacrine, has strong inhibition effect on amyloid protein (Abeta) self-aggregation, has remarkable anti-oxidation activity, does not have remarkable in-vitro neurocytotoxicity and in-vivo acute hepatotoxicity, shows remarkable in-vitro nerve cell protective activity, andcan be applied to treatment on Alzheimer's disease.
Owner:天津海润家和创新医药研究有限责任公司
1, 2, 3, 4-tetrahydroacridine-9-amine compound as well as preparation method and application thereof
ActiveCN112409335AEasy to prepareRaw materials are easy to getNervous disorderOrganic chemistryCholinergic cellsPharmaceutical medicine
The invention discloses a 1, 2, 3, 4-tetrahydroacridine-9-amine compound as well as a preparation method and application thereof. The compound is characterized in that: tacrine is taken as a parent nucleus; the compound has structural formulas shown in formulas I and II or pharmaceutically acceptable salts, esters or solvates of the compounds shown in the formulas I and II; and the compound can beused for preparing medicines for resisting Alzheimer's disease, medicines for delaying neurodegenerative diseases, medicines for repairing cholinergic neurons in vitro, medicines for resisting oxidative stress injury in vitro and medicines for relieving beta-amyloid protein (A beta) neurotoxicity, improving cognitive disorder through a CREB-ERK pathway or improving cognitive disorder through reducing Tau protein phosphorylation. Thecompound has the advantage of excellent anti-Alzheimer's disease activity.
Owner:NINGBO UNIV
Sulfydryl-containing tacrine derivative and preparation method and application thereof
InactiveCN102391180BOrganic active ingredientsNervous disorderAcetylcholine esterasePerylene derivatives
The invention provides a sulfydryl-containing tacrine compound or a dynamic isomer or a medicinal salt thereof. The compound or the dynamic isomer or the medicinal salt thereof have the functions of suppressing acetylcholine esterase, enhancing sea horse LTP (Long-Term Potentiation) and improving learning and memory, and can be used for treating, improving or preventing cognitive function decline-related neurous system diseases such as the Alzheimer's disease, vascular dementia, mild cognitive impairment and other oxidative stress participated dementia.
Owner:HUAZHONG UNIV OF SCI & TECH
Aldoxime-containing tacrine derivatives selective butyrylcholinesterase inhibitors, preparation method and application thereof
The invention relates to tacrine derivatives containing aldoxime selective butyrylcholinesterase inhibitors, a preparation method and application thereof. The compound has the structure shown in formula I or II. The present invention also relates to pharmaceutical compositions containing compounds of formula I and formula II. The present invention also provides the application of the above compounds and compositions containing one or more of these compounds in the preparation of anti-Alzheimer's disease drugs.
Owner:SHANDONG UNIV
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