Patent(s) and the Corresponding Patented Drug(s) |
Top |
World Intellectual Property Organization (WIPO) |
Patent ID |
WO2012165981 |
Title |
Novel Hybrid Cholinesterase Inhibitors. |
Abstract |
The invention relates to novel hybrid cholinesterase inhibitors containing the melatonin or its oxidation products unit and tetrahydroacridine unit linked via a carbamate bond. Due to the high selectivity of action, which is expressed with high ratio of IC50 for acetylcholinesterase inhibition to IC50 for butyrylcholinesterase inhibition ([IC50(AChE)]/[IC50(BChE)]), the novel compounds can be used in relief and/or treatment of the neurodegenerative diseases, among them the Alzheimer's disease. |
Applicant(s) |
Univ Warszawski |
Representative Drug(s) |
D0WD0M |
Drug Info
|
IC50 = 0.25 nM |
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[1] |
2
|
D0H3YG
|
Drug Info
|
IC50 = 8.2 nM
|
[1] |
Patent ID |
WO2016151484 |
Title |
Disubstituted Piperidine Derivatives As Butyrylcholinesterase Inhibitors for Use In The Treatment of Alzheimer. |
Abstract |
This invention relates to new inhibitors of butyrylcholinesterase with general formulas I and II, where substituents are described in patent description. Compounds can be in the form of pure enantiomers or as racemic mixtures, or in the form of pharmaceutically acceptable salts. The present invention relates to the use of these inhibitors for the treatment of Alzheimer's disease and other forms of dementia. |
Applicant(s) |
Univerza V Ljubljani |
Representative Drug(s) |
D0K3EB |
Drug Info
|
IC50 = 1.03 nM |
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[1] |
2
|
D00GSF
|
Drug Info
|
N.A.
|
[1] |
3
|
D0BS8I
|
Drug Info
|
N.A.
|
[1] |
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] |
United States Patent and Trademark Office (USPTO) |
Patent ID |
US20110294850 |
Title |
Indoline Derivatives. |
Representative Drug(s) |
D0J3OD |
Drug Info
|
IC50 = 0.36 nM |
[1] |
Patent ID |
US20170258774 |
Title |
Novel Oximes for Reactivating Butyrylcholinesterase. |
Representative Drug(s) |
D0WR9T |
Drug Info
|
N.A. |
[1] |
Patent ID |
US20020094999 |
Title |
Highly Selective Butyrylcholinesterase Inhibitors for The Treatment and Diagnosis of AlzheimerS Disease and Dementias. |
European Patent Office (EPO) |
Patent ID |
EP2727916 |
Title |
Neuroprotective Multi-Target Directed Drugs. |
China National Intellectual Property Administration (CNIPA) |
Patent ID |
CN106831714 |
Title |
Tetrahydroisoquinoline Compound and Preparation Method and Application Thereof. |
Representative Drug(s) |
D02EME |
Drug Info
|
IC50 = 900 nM |
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[1] |
2
|
D0R6RT
|
Drug Info
|
IC50 = 1200 nM
|
[1] |
3
|
D0NB7Z
|
Drug Info
|
IC50 = 3800 nM
|
[1] |
4
|
D04AXC
|
Drug Info
|
IC50 = 5500 nM
|
[1] |
Patent ID |
CN101311171 |
Title |
Compound with Dual Restraining Activities To Acetyl Cholinesterase and Butyryl Cholinesterase and Use Thereof. |
Representative Drug(s) |
D0B9TI |
Drug Info
|
IC50 = 43 nM |
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[1] |
2
|
D0RS6O
|
Drug Info
|
IC50 = 270 nM
|
[1] |
3
|
D0VQ2N
|
Drug Info
|
IC50 = 310 nM
|
[1] |
4
|
D04FAS
|
Drug Info
|
IC50 = 720 nM
|
[1] |
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 |
CN201110359965 |
Title |
Tacrine-Caffeic Acid Hetero-Blends, Their Preparation Method and Medicinal Compositions. |
Representative Drug(s) |
D0W9OC |
Drug Info
|
IC50 = 1.9 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 = 2100 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 = 29 nM |
[1] |
Patent ID |
CN102746325 |
Title |
Compound 1,10-N-Decylene Lycorine Dibromo Salt, Pharmaceutical Composition and Application Thereof In Medicine. |
Representative Drug(s) |
D0Y4CG |
Drug Info
|
IC50 = 3300 nM |
[2] |
Patent ID |
CN102229602 |
Title |
Tacrine Heterocomplex, Preparation Method and Use In Medicines for Curing Neurodegenerative Diseases Thereof. |
Representative Drug(s) |
D0CB1C |
Drug Info
|
IC50 = 3.4 nM |
[1] |
Patent ID |
CN104644704 |
Title |
Medical Application and Preparation Method of Fructus Terminaliae Billericae Pulp Butyrylcholinesterase Inhibitory Activity Extract and Composition of Fructus Terminaliae Billericae Pulp Butyrylcholinesterase Inhibitory Activity Extract. |
Applicant(s) |
Xinjiang Medical Universit (Rmqi, China) |