IP Library › Granted Patent US 12,528,794
Granted Patent B2
US 12,528,794 · App. 17/904,972 · Granted Jan 20, 2026

MAO-B inhibitor DRG-MAOB-1 for use in treatment of neurodegenerative diseases

Inventors: Serdar Durdagi (Istanbul, TR); Mine Yurtsever (Istanbul, TR); Busecan Aksoydan (Istanbul, TR); Yusuf Serhat Is (Istanbul, TR); Murat Senturk (Istanbul, TR)
Assignees: BAHCESEHIR UNIVERSITESI; ISTANBUL TEKNIK UNIVERSITESI; AGRI IBRAHIM CECEN UNIVERSITESI STRATEJI DAIRE BASK.; ISTANBUL GEDIK UNIVERSITESI
C07D403/12A61K45/06
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Quick Facts
Patent No.
US 12,528,794
App. No.
17/904,972
Granted
Jan 20, 2026
Kind
B2
Abstract

The invention relates to compound shown with formula (I) or a pharmaceutically acceptable derivative thereof for use as a novel inhibitor of MAO-B.

Claims (10)

1 . A compound according to formula I, or a pharmaceutically acceptable derivative thereof,

2 . The compound according to claim 1 , wherein the pharmaceutically acceptable derivative of formula I is a hydrate, a solvate, a prodrug, a stereoisomer, a salt, an ester, a tautomer, an isotopically labeled derivative, or a form of the compound of formula I that forms under physiological conditions of the human body.

3 . A method of treating a disorder mediated by the activity of MAO-B enzyme in a subject in need thereof, the method comprising the step of administering to the subject a therapeutically effective amount of the compound according to claim 1 .

4 . The method of claim 3 , wherein the disorder is a neurodegenerative disease.

5 . The method of claim 4 , wherein the neurodegenerative disease is Alzheimer's disease, Parkinson's disease, Huntington's disease, fronto temporal dementia (or Pick's disease), amyotrophic lateral sclerosis (ALS), spinocerebellar ataxia (SCA), progressive bulbar palsy (PBP), pseudobulbar palsy, progressive muscular atrophy (PMA), primary lateral sclerosis (PLA), monomelic amyotrophy, Spinal muscular atrophy (SMA) type 0, 1, 2, 3 and 4, Creutzfeldt-Jakob disease (CJD), Kuru, Gerstmann-Sträussler-Scheinker syndrome, dementia with Lewy bodies (DLB), or Lafora disease.

6 . The method of claim 5 , wherein the neurodegenerative disease is Alzheimer's disease, Parkinson's disease, Huntington's disease, or amyotrophic lateral sclerosis (ALS).

7 . The method of claim 3 , wherein the compound according to formula I, or a pharmaceutically acceptable derivative thereof, is administered in combination with one or more additional pharmaceutically active agents.

8 . The method of claim 7 , wherein the additional pharmaceutically active agent is selected from the group consisting of acetylcholinesterase inhibitors, NMDA receptor antagonists, sesquiterpene alkaloid compounds, COMT inhibitors, dopamine agonists, other MAO-B inhibitors, neuroleptics, benzodiazepines, selective serotonin reuptake inhibitors, atypical antipsychotic drugs, opioids, levodopa, tetrabenazine, Amantadine, Ramacemide, valproic acid, ethyl-eicosapentoic acid, mirtazapine, riluzole, edaravone, gabapentin, pregabalin, baclofen, tizanidine, scopolamine, amitriptyline, glycopyrrolate, mexiletine, methylphenidate, dextroamphetamine, modafinil, armodafmil, levetiracetam, topiramate, perampanel, and combinations thereof.

9 . A pharmaceutical composition comprising the compound according to claim 1 and at least one pharmaceutically acceptable excipient.

10 . A pharmaceutical composition comprising the compound according to claim 1 and one or more additional pharmaceutically active agent selected from the group consisting of acetylcholinesterase inhibitors, NMDA receptor antagonists, sesquiterpene alkaloid compounds, COMT inhibitors, dopamine agonists, other MAO-B inhibitors, neuroleptics, benzodiazepines, selective serotonin reuptake inhibitors, atypical antipsychotic drugs, opioids, levodopa, tetrabenazine, Amantadine, Ramacemide, valproic acid, ethyl-eicosapentoic acid, mirtazapine, riluzole, edaravone, gabapentin, pregabalin, baclofen, tizanidine, scopolamine, amitriptyline, glycopyrrolate, mexiletine, methylphenidate, dextroamphetamine, modafinil, armodafmil, levetiracetam, topiramate, perampanel, and combinations thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 3, 2023
From: DURDAGI, SERDAR; YURTSEVER, MINE; AKSOYDAN, BUSECAN; IS, YUSUF SERHAT; SENTURK, MURAT
To: BAHCESEHIR UNIVERSITESI; ISTANBUL TEKNIK UNIVERSITESI; AGRI IBRAHIM CECEN UNIVERSITESI STRATEJI DAIRE BASK.; ISTANBUL GEDIK UNIVERSITESI
Reel/Frame 065104/0394 →
Priority Claims (1)
TR 2020/02933 · Feb 26, 2020 · national
Continuity (1)
Related Publication 20230093302A1 · Mar 23, 2023
References Cited (6)
US 6653304B2 · Leftheris · 2003 [cited by examiner]
WO WO2018229195A1 · 2018 [cited by examiner]
International Search Report in International Application No. PCT/TR2021/050170 dated May 31, 2021. [cited by applicant]
Naoi M, Maruyama W, Inaba-Hasegawa K. Type A and B monoamine oxidase in age-related neurodegenerative disorders: their distinct roles in neuronal death and survival. Curr Top Med Chem. 2012;12(20):2177-88. [cited by applicant]
Foley P, Gerlach M, Youdim MB, Riederer P. MAO-B inhibitors: multiple roles in the therapy of neurodegenerative disorders? Parkinsonism Relat Disord. Jan. 2000;6(1):25-47. [cited by applicant]
Tom Thomas, Monoamine oxidase-B inhibitors in the treatment of Alzheimers disease, Neurobiology of Aging, vol. 21, Issue 2, 2000, pp. 343-348. [cited by applicant]