Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T30082 Target Info
Target Name Acetylcholinesterase (AChE)
Synonyms YT; N-ACHE; ARACHE
Target Type Successful Target
Gene Name ACHE
Biochemical Class Carboxylic ester hydrolase
UniProt ID
ACES_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2014129989
Title 3-Substituted-6H-Benzo[C]Chromen-6-Ones and 3-Substituted-7,8,9,10-Tetrahydro-6H-Benzo[C]Chromen-6-Ones Against Senile Dementia.
Abstract This invention is related with the conversion of xenobiotics to potent ACHE and BCHE inhibitors that have activity comparable to the current ACHE and BCHE inhibitor drugs (i.e., donepezil, rivastigmine, and galantamine).
Applicant(s) Fargem Farmast
Patent ID WO2013152704
Title 5-Amino-1,4-Dihydro-1,8-Naphthyridine Derivative and Pharmaceutical Composition and Use Thereof.
Abstract Disclosed in the present invention is a class of 5-amino-1,4-dihydro-1,8-naphthyridine derivatives and the pharmaceutical composition and use thereof. The class of 5-amino-1,4-dihydro-1,8-naphthyridin.
Applicant(s) Jiangsu Simcere Pharmaceutical Co., Ltd
Patent ID WO2012065527
Title Compouds and Uses As L-Type Calcium Channel Blocker and/or Acetylcholinesterase Inhibitor Thereof.
Abstract Disclosed in this invention are compounds and the uses as L-type calcium channel blocker and/or acetylcholinesterase inhibitor thereof. The uses of said compounds in the manufactures of a medicament f.
Applicant(s) Jiangsu Simcere Pharmaceutical R & D Co
Representative Drug(s) D0C1UA Drug Info IC50 = 17 nM [2]
Patent ID WO2006070394
Title Substituted Carbamic Acid Quinolin-6-Yl Esters Useful As Acetylcholinesterase Inhibitors.
Abstract The present invention relates to new substituted carbamic acid quinoo-6-yi esters of formulae (1) and (2) where R1= alkyl, and, R2=H, alkyl, aralkyl useful as acetylcholinesterase inhibitors, and which show potent antiacetylcholinesterase activity and have potential therapeutic use for prevention of cure of acetylcholinesterase related disorders including peripheral as well as central nervous system.
Applicant(s) Council of Scientific and Industrial Research
Representative Drug(s) D0T0CB Drug Info IC50 = 3300 nM [2]
Patent ID WO2015075082
Title Novel Uncharged Reactivators Against Op-Inhibition of Human Acetylcholinesterase.
Abstract The present invention deals with compounds of formula (I) which are novel uncharged reactivators of human acetylcholinesterase, pharmaceutical compositions comprising said compounds, and their use for reactivating human acetylcholinesterase inhibited by at least one organophosphorus nerve agent.
Applicant(s) Universite De Strasbourg
Patent ID WO2014210168
Title Activation or Reactivation of Ache.
Abstract Disclosed herein is an in vitro or in vivo method of activating or reversing inactivation of acetylcholinesterase (AChE) or butyrylcholinesterase (BuchE) using compounds of the present disclosure. Also disclosed is a method of treating a subject exposed to a nerve agent using such compounds. Also disclosed is a method of treating organophosphate poisoning in a subject using such compounds. Also disclosed is a method of modulating neuronal signaling and transmission in a subject using such compounds.
Applicant(s) The Trustes of Columbia University In the City of New York
Representative Drug(s) D06GSR Drug Info N.A. [2]
Patent ID WO2014114742
Title Oxidisable Pyridine Derivatives, Their Preparation and Use As Anti-Alzheimer Agents.
Abstract A compound of formula (I) in which the dotted lines indicate the presence of at least one double bond; n = 0 to 4; R3 and R4 are H, or when n = 1, R3 and R4 can also form together a double bond between the carbon atoms, and m = 0, 1 or 2, Z is CH or N or Z is C and - CHR3- is =CH- linked by the double bond to cyclopentanone; or - (-)m- is absent, and Z is NH, >N-alkyl, >N-phenyl, >N-benzyl or >N heteroaryl; R8 is alkyl, aryl or heteroaryl which can be optionally substituted; EWG represents an electron withdrawing group selected from the group comprising COOR, COSR, CONRR', CN, COR, CF3, SOR, SO2R, SONRR', SO2NRR', NO2, halogen, heteroaryl; and the pharmaceutical salts and stereisomers thereof. The compounds of formula (I) are potent in the treatment of neurodegenerative diseases such as Alzheimer's disease.
Applicant(s) Insa (Institut National Des Sciences Applique S) De Rouen Center National De La Recherche Scientifique (Cnrs) Universite De Rouen Vfp Th Apies
Representative Drug(s) D04TGJ Drug Info N.A. [2]
Patent ID WO2012083261
Title Blood Brain Barrier-Penetrating Oximes for Cholistenerases Reactivation.
Abstract The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.
Applicant(s) Human Biomolecular Research Institute
Representative Drug(s) D01RZG Drug Info N.A. [2]
Patent ID WO2009150433
Title Immunogenic Composition.
Abstract This invention relates to the use of a CCR4 antagonist as an adjuvant, in particular in an immunogenic composition comprising an antigen which elicits an immune response against a pathogen or tumour.
Applicant(s) Isis Innovation Limited
Patent ID WO2006103120
Title New Heterocyclic Compounds, Their Preparation and Their Use As Medicaments, In Particular As Anti-Alzheimer Agents.
Abstract The invention is related to compound which comprises at least one radical C=Y, Y being O or S, and an oxidable and non protonable nitrogen atom N wherein the distance (d) between the at least one carbon atom of the radical group C=Y and the nitrogen atom, when oxidized, is comprised between 0.3 and 0.8 nanometers. The invention is related to new heterocyclic compounds defined by formula G, their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of neurodegenerative or Alzheimer disease.
Applicant(s) Insa Rouen Gous Inc
Patent ID WO2005005413
Title Tacrine Derivatives As Inhibitors of Acetylcholinesterase.
Abstract The invention provides compounds of formula: (I) which have a tacrine moiety connected to an heterocyclic moiety through a linker. Through careful selection of the substituents and the linker, the activity and selectivity towards acetylcholinesterase can be modulated. The compounds show potent AChE inhibition activities together with modifications in the gama-amyloid aggregation properties by binding simultaneously to the catalytic and peripheral AChE sites. They are useful in the treatment of AChE mediated diseases, such as the Alzheimer... disease.
Applicant(s) Neuropharma S.A
United States Patent and Trademark Office (USPTO)
Patent ID US20140080860
Title Novel Hybrid Cholinesterase Inhibitors.
Applicant(s) Centrum Medyczne
Representative Drug(s) D01FRI Drug Info IC50 = 7.7 nM Click to Show More [2]
2 D02SQQ Drug Info IC50 = 39 nM [2]
3 D0QJ5H Drug Info IC50 = 3300 nM [2]
Patent ID US2015225343
Title Novel Derivatives of Donepezil.
Representative Drug(s) D0AH3R Drug Info N.A. [2]
Patent ID US20150005328
Title Oximes for The Treatment of Peripheral and Central Nervous System Exposure To Acetyl Cholinesterase Inhibitors.
Applicant(s) Southwest Res Inst
Representative Drug(s) D0HI1R Drug Info Ki = 2300000 Nm [2]
Patent ID US20140350262
Title Reactivators of organophosphorous Inhibited Acetylcholinesterase.
Applicant(s) Southwest Res Inst
Representative Drug(s) D01EGC Drug Info Ki = 230000 nM [2]
Patent ID US20140364443
Title 1,4-Dihydro-Naphthyridine Derivative and Pharmaceutical Composition and Use Thereof.
Representative Drug(s) D0I6UA Drug Info IC50 = 180 nM [2]
Patent ID US20110294850
Title Indoline Derivatives.
Representative Drug(s) D0J3OD Drug Info IC50 = 93000 nM [1]
Patent ID US9227937
Title Phenoxyalkyl Pyridinium Oxime Therapeutics for Treatment of organophosphate Poisoning.
Applicant(s) Mississippi State University
Representative Drug(s) D0G4YS Drug Info N.A. [2]
Patent ID US20150361060
Title Centrally Active and orally Bioavailable Antidotes for organophosphate Exposure and Methods for Making and Using Them.
Applicant(s) Univ California, Scripps Research Inst
Representative Drug(s) D0OG8Z Drug Info N.A. [2]
Patent ID US20140323473
Title Compounds and Methods To Treat organophosphorus Poisoning.
Applicant(s) University of Iowa Research Foundation
Representative Drug(s) D0C0LQ Drug Info N.A. [2]
Patent ID US2014004155
Title 2-Aminothiazole Derivatives and Methods of Preparing and Using The Same.
Applicant(s) Hangzhou Zhongmei Huadong Pharmaceutical Co Ltd
European Patent Office (EPO)
Patent ID EP2727916
Title Neuroprotective Multi-Target Directed Drugs.
Representative Drug(s) D0AA7U Drug Info IC50 = 1800 nM [1]
China National Intellectual Property Administration (CNIPA)
Patent ID CN104788525
Title Triterpene Compounds with Acetylcholinesterase Inhibition Activity, and Preparation Method Thereof.
Applicant(s) Univ Shenyang Chemical Tech
Representative Drug(s) D07HNU Drug Info IC50 = 14000 nM [2]
Patent ID CN104003987
Title Tacrine-Beta-Carboline Conjoined Multifunction Cholinesterase Inhibitor.
Applicant(s) Univ China Pharma
Representative Drug(s) D0I7KU Drug Info IC50 = 63 nM Click to Show More [2]
2 D05QVX Drug Info IC50 = 92 nM [2]
3 D0G9HY Drug Info IC50 = 96 nM [2]
Patent ID CN103059043
Title Clavatine A-C and Preparation Method As Well As Pharmaceutical Composition and Application Thereof.
Applicant(s) Inst Materia Medica Cams
Patent ID CN102617465
Title Tacrine-Caffeic Acid Hetero-Blends, Their Preparation Method and Medicinal Compositions.
Applicant(s) Univ Sun Yat Sen
Representative Drug(s) D05WPG Drug Info EC50 = 26000 nM; IC50 = 0.2 nM Click to Show More [2]
2 D0SW0V Drug Info EC50 = 26000 nM; IC50 = 200 nM [2]
Patent ID CN102746325
Title Compound 1,10-N-Decylene Lycorine Dibromo Salt, Pharmaceutical Composition and Application Thereof In Medicine.
Representative Drug(s) D03VUN Drug Info IC50 = 4300 nM Click to Show More [2]
2 D04XHE Drug Info IC50 = 11000 nM [2]
Patent ID CN101311171
Title Compound with Dual Restraining Activities To Acetyl Cholinesterase and Butyryl Cholinesterase and Use Thereof.
Representative Drug(s) D0RS6O Drug Info IC50 = 210 nM Click to Show More [1]
2 D0B9TI Drug Info IC50 = 640 nM [1]
3 D04FAS Drug Info IC50 = 970 nM [1]
Patent ID CN103387580
Title Stemona Root Alkaloid Monomer Components and Applications Thereof.
Applicant(s) Univ Lanzhou Tech
Representative Drug(s) D02GCZ Drug Info IC50 = 20000 nM Click to Show More [2]
2 D03WGA Drug Info N.A. [2]
Patent ID CN104860955
Title Galantamine Analogue and Application Thereof.
Applicant(s) Univ East China Science & Tech
Patent ID CN103420941
Title 2-Methoxyphenyl-Dimethylamino formic Ether Derivative and Preparation Method and Application Thereof.
Applicant(s) Zhejiang University
Representative Drug(s) D00AQW Drug Info IC50 (rat) = 97 nM [2]
Patent ID CN103333163
Title Coumarone Derivative, and Preparation Method and Applications Thereof.
Applicant(s) Univ Guangzhou Chinese Medicine
Representative Drug(s) D03DIQ Drug Info IC50 = 1400 nM [2]
Patent ID CN102936244
Title Tacrine-Phenothiazine Isodiad Compound and Preparation Method Thereof.
Applicant(s) Univ Hefei Technology
Representative Drug(s) D0I2FM Drug Info IC50 (rat) = 89 nM [2]
Patent ID CN201110359965
Title Tacrine-Caffeic Acid Hetero-Blends, Their Preparation Method and Medicinal Compositions.
Patent ID CN105218529
Title Isochroman-4-Ketone Derivative Having Cholinesterase Inhibiting Activity and Preparation Method Ad Medical Application Thereof.
Representative Drug(s) D0OE6G Drug Info IC50 = 8.9 nM [1]
Patent ID CN104356138
Title Vasicine R-Type Optical Isomer As Well As Preparation Method and Application Thereof.
Representative Drug(s) D01SQO Drug Info IC50 = 980 nM [1]
Patent ID CN102229602
Title Tacrine Heterocomplex, Preparation Method and Use In Medicines for Curing Neurodegenerative Diseases Thereof.
Representative Drug(s) D0CB1C Drug Info IC50 = 4.6 nM [1]
Patent ID CN105764510
Title An H3 Receptor Antagonist Combined with A Cholinesterase Inhibitor for Use In The Treatment of AlzheimerS Disease.
Applicant(s) Sanofi Sa
Patent ID CN104829569
Title Application of 2-Phenyl-Benzo-Five Membered Heterocycle Compound and Derivative of 2-Phenyl-Benzo-Five-Membered Heterocycle Compound.
Applicant(s) Univ Guangzhou Chinese Medicine
Patent ID CN104800209
Title Pyrrolidone Compounds As Well As Medical Composition and Application Thereof.
Applicant(s) Kunming Institute of Botany, Chinese Academy of Sciences
Patent ID CN104327075
Title 9-Amino Substituted Pyrido Acridine Derivative, Preparation Method and Uses Thereof.
Applicant(s) Univ Guangxi Chinese Medicine
Patent ID CN104292280
Title Amino Sugar Thiazole Derivative As Well As Synthetic Method and Application Thereof.
Applicant(s) Huaihai Inst Technology
Patent ID CN103992312
Title 1,2,4-Thiadiazole-3,5-Dione Derivatives, and Pharmaceutical Composition and Application Thereof.
Applicant(s) Jiangsu Simovay Pharmaceutical Co
Patent ID CN101284812
Title Tacrine-Ferulaic Acid Hetero-Blend, Preparation Method and Pharmaceutical Compositions Thereof.
Applicant(s) Univ Sun Yat Sen
References  Top
REF 1 A patent review of butyrylcholinesterase inhibitors and reactivators 2010-2017.Expert Opin Ther Pat. 2018 Jun;28(6):455-465.
REF 2 Recent advances in acetylcholinesterase Inhibitors and Reactivators: an update on the patent literature (2012-2015).Expert Opin Ther Pat. 2017 Apr;27(4):455-476.
REF 3 Sulfonamide inhibitors: a patent review 2013-present.Expert Opin Ther Pat. 2018 Jul;28(7):541-549.

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