The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 09, 2023
Filed:
Aug. 09, 2021
Hina Siddiqui, Karachi, PK;
Muhammad Iqbal Choudhary, Karachi, PK;
Atia-tul- Wahab, Karachi, PK;
Atta-ur- Rahman, Karachi, PK;
Fazila Rizvi, Karachi, PK;
Sheeba Wajid, Karachi, PK;
Hina Siddiqui, Karachi, PK;
Muhammad Iqbal Choudhary, Karachi, PK;
Atia-tul- Wahab, Karachi, PK;
Atta-ur- Rahman, Karachi, PK;
Fazila Rizvi, Karachi, PK;
Sheeba Wajid, Karachi, PK;
Other;
Abstract
One embodiment of the invention relates to the treatment of diseases associated with increased butyrylcholinesterase (BuChE) enzyme activity such Alzheimer's Disease (AD), involving administering an effective amount of a compound selected from a group of new N, N'-disubstituted benzylamine derivatives (1-8) of 4-aminoantipyrine (ampyrone). The kinetic studies of two potent compounds 4-(Bis(4-iodobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (5) (IC=2.43±0.4 and Ki=5.67±0.5 μM) and 4-(Bis(2-bromobenzyl) amino)-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one (6) (IC=0.7±0.2 and Ki=2.4±0.4 μM), revealed them as a competitive and a non-competitive inhibitor of BuChE, respectively. Galantamine Hydrobromide was used as standard inhibitor with IC=40.83±0.4 and Ki=21.5±0.7 μM (Mixed type Inhibitor). The metabolite of aminophenazone, 4-aminoantipyrine (A) is also being reported here as an inhibitor of BuChE for the first time.