Patent(s) and the Corresponding Patented Drug(s) |
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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 |
Representative Drug(s) |
D0X9CR |
Drug Info
|
N.A. |
[1] |
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 |
Representative Drug(s) |
D0ZX8C |
Drug Info
|
IC50 = 720 nM |
[2] |
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 |
Representative Drug(s) |
D0X5KA |
Drug Info
|
N.A. |
[2] |
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 |
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[2] |
2
|
D0UX5I
|
Drug Info
|
IC50 = 20 nM
|
[2] |
3
|
D02SQQ
|
Drug Info
|
IC50 = 39 nM
|
[2] |
4
|
D0QJ5H
|
Drug Info
|
IC50 = 3300 nM
|
[2] |
Patent ID |
US2015225343 |
Title |
Novel Derivatives of Donepezil. |
Representative Drug(s) |
D0AH3R |
Drug Info
|
N.A. |
Click to Show More |
[2] |
2
|
D0XS3N
|
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 |
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[2] |
2
|
D0YF7A
|
Drug Info
|
IC50 = 28000 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 |
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[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 |
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[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 |
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[2] |
2
|
D0Y4CG
|
Drug Info
|
IC50 = 4300 nM
|
[2] |
3
|
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 |
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[1] |
2
|
D0VQ2N
|
Drug Info
|
IC50 = 270 nM
|
[1] |
3
|
D0B9TI
|
Drug Info
|
IC50 = 640 nM
|
[1] |
4
|
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 |
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[2] |
2
|
D03WGA
|
Drug Info
|
N.A.
|
[2] |
3
|
D0V2JR
|
Drug Info
|
N.A.
|
[2] |
Patent ID |
CN104860955 |
Title |
Galantamine Analogue and Application Thereof. |
Applicant(s) |
Univ East China Science & Tech |
Representative Drug(s) |
D0W9ZU |
Drug Info
|
IC50 (rat) = 610 nM |
[2] |
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. |
Representative Drug(s) |
D0W9OC |
Drug Info
|
IC50 = 3200 nM |
[1] |
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 |