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Analysis

1 / 1
1.20230165833Selective butyrylcholinesterase inhibitor or pharmaceutically acceptable salt thereof, preparation method and use thereof
US - 01.06.2023
Int.Class A61K 31/381
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
38having sulfur as a ring hetero atom
381having five-membered rings
 Appl.No 16967401 Applicant CHINA PHARMACEUTICAL UNIVERSITY Inventor Haopeng Sun

The present invention discloses a selective butyrylcholinesterase inhibitor having a general formula (I) or a pharmaceutically acceptable salt thereof, a preparation method and use thereof. The treatment efficacy of Alzheimer's disease, especially moderate to severe Alzheimer's disease, is tested through butyrylcholinesterase inhibitory activity, selectivity screening and toxicity to nerve cells as a carrier, and it is found that it has good target activity in vitro, extremely high selectivity and drug safety, can be used as a lead substance for further development of the treatment of Alzheimer's disease by selectively inhibiting butyrylcholinesterase.

2.WO/2022/087630INHIBITORS OF AMINO ACID TRANSPORT
WO - 28.04.2022
Int.Class C07C 4/26
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
4Preparation of hydrocarbons from hydrocarbons containing a larger number of carbon atoms
26by splitting polyaryl compounds at a bond between uncondensed six-membered aromatic rings, e.g. biphenyl to benzene
 Appl.No PCT/US2021/071989 Applicant ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI Inventor GREWER, Christof
Disclosed herein are compounds and compositions of formula (I) that are inhibitors of amino acid transport, specifically alanine serine cysteine transporter 2 (ASCT2): These compounds are useful as therapeutic agents for treating various cancers. Methods for inhibiting an ASCT2 transporter are also disclosed. Certain compounds are selective for an ASCT transporter.
3.WO/2021/042410SELECTIVE BUTYRYLCHOLINESTERASE INHIBITOR OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
WO - 11.03.2021
Int.Class C07D 333/38
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
333Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02not condensed with other rings
04not substituted on the ring sulfur atom
26with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
 Appl.No PCT/CN2019/105879 Applicant CHINA PHARMACEUTICAL UNIVERSITY Inventor SUN, Haopeng
Disclosed are a selective butyrylcholinesterase inhibitor having general formula (I) or a pharmaceutically acceptable salt thereof, a preparation method therefor, and use thereof. By testing the efficacy of treatment of Alzheimer’s disease, especially moderate to severe Alzheimer’s disease, by means of the butyrylcholinesterase inhibitory activity and the selective screening as well as the toxicity to nerve cells, it is found that the selective butyrylcholinesterase inhibitor or a pharmaceutically acceptable salt thereof has good in-vitro target activity as well as high selectivity and drug safety, and can be used as a precursor substance for further development of the treatment of Alzheimer's disease by selectively inhibiting butyrylcholinesterase.
4.110627767Selective butyrylcholine esterase inhibitor or pharmaceutically acceptable salt thereof, and preparation method and application thereof
CN - 31.12.2019
Int.Class C07D 333/38
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
333Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02not condensed with other rings
04not substituted on the ring sulfur atom
26with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
 Appl.No 201910841091.4 Applicant CHINA PHARMACEUTICAL UNIVERSITY Inventor SUN HAOPENG
The invention discloses a selective butyrylcholine esterase inhibitor represented by a general formula (I) or a pharmaceutically acceptable salt thereof, and a preparation method and an application thereof. Butyrylcholine esterase inhibitory activity, selective screening and toxicity to nerve cells are used as carriers to examine the curative effect of treating Alzheimer's disease, especially formoderate and severe Alzheimer's disease, it is found that the compound has good in-vitro target activity, extremely high selectivity and drug safety, and can be used as a lead substance for further development of an effect of treating Alzheimer's disease by selectively inhibiting butyrylcholine esterase.
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