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 T99799 Target Info
Target Name Cholinesterase (BCHE)
Synonyms Pseudocholinesterase; Choline esterase II; CHE1; Butyrylcholine esterase; Acylcholine acylhydrolase
Target Type Successful Target
Gene Name BCHE
Biochemical Class Type-B carboxylesterase/lipase
UniProt ID
CHLE_HUMAN
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) 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 Click to Show More [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
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.
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 Click to Show More [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 Click to Show More [1]
2 D0RS6O Drug Info IC50 = 270 nM [1]
3 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.
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.
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)
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.

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