DK2938597T3 - N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1h-benzo[d]imidazol-2-amin sulfatsalte, fremstilling deraf og anvendelse af samme - Google Patents

N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1h-benzo[d]imidazol-2-amin sulfatsalte, fremstilling deraf og anvendelse af samme Download PDF

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Publication number
DK2938597T3
DK2938597T3 DK13815780.5T DK13815780T DK2938597T3 DK 2938597 T3 DK2938597 T3 DK 2938597T3 DK 13815780 T DK13815780 T DK 13815780T DK 2938597 T3 DK2938597 T3 DK 2938597T3
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Denmark
Prior art keywords
propyl
disease
diisobutylamino
pharmaceutically acceptable
amine
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DK13815780.5T
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English (en)
Inventor
Stéphane Burlet
Cécilia Estrella
Mathieu Barrier
Patricia Melnyk
Nicolas Sergeant
Luc Buee
Philippe Verwaerde
Original Assignee
Alzprotect
Inst Nat Sante Rech Med
Université De Lille 2 Droit Et Santé
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Application filed by Alzprotect, Inst Nat Sante Rech Med, Université De Lille 2 Droit Et Santé filed Critical Alzprotect
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Publication of DK2938597T3 publication Critical patent/DK2938597T3/da

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles with 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 in position 2
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Claims (12)

1. A/-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[<^imidazol-2-amin sulfatsalt og farmaceutisk acceptable solvater deraf.
2. Sulfatsaltet ifølge krav 1, der har formlen II
Formel II hvor x er 0,5 til 4, og farmaceutisk acceptable solvater deraf.
3. Sulfatsaltet ifølge krav 2 og farmaceutisk acceptable solvater deraf, kendetegnet ved at x er 1,5 til 2,5.
4. Sulfatsaltet ifølge krav 2 og farmaceutisk acceptable solvater deraf, kendetegnet ved at x er 0,5 til 1,5.
5. Sulfatsaltet ifølge krav 2 og farmaceutisk acceptable solvater deraf, kendetegnet ved at x er 2,5 til 3,5.
6. Sulfatsaltet ifølge krav 2, der har formlen III
hvor x er som defineret i krav 2, og y er 0,5 til 5.
7. Farmaceutisk sammensætning omfattende sulfatsaltet ifølge et hvilket som helst af kravene 1 til 6, eller en farmaceutisk acceptabel solvat deraf, og mindst én farmaceutisk acceptabel bærer, fortynder, excipiens og/eller adjuvans.
8. Sulfatsaltet ifølge et hvilket som helst af kravene 1 til 6, eller en farmaceutisk acceptabel solvat deraf, til anvendelse som et lægemiddel.
9. Sulfatsaltet ifølge et hvilket som helst af kravene 1 til 6, eller en farmaceutisk acceptabel solvat deraf, til anvendelse i behandling og/eller forebyggelse afen sygdom valgt blandt neurodegenerative sygdomme, amyloidopatier, tauopatier og mentale udviklingssygdomme.
10. Sulfatsaltet til anvendelse ifølge krav 9, hvor sygdommen er valgt blandt Alzheimers sygdom, Lewy body demens (DLB), amyotrofisk lateral sklerose (ALS) med frontotemporal demens, inklusionslegeme myopati med Pagets knoglesygdom og/eller frontotemporal demens (IBMPFD), frontotemporal lobar degeneration, synucleopatier, Huntingtons sygdom, Parkinsons sygdom, amyloid angiopatier, frontotemporal demens med Parkinsonisme forbundet til kromosom 17 og Downs syndrom.
11. Sulfatsaltet ifølge et hvilket som helst af kravene 1 til 6, eller en farmaceutisk acceptabel solvat deraf, til anvendelse til udskydelse af optræden hos en patient af en sygdom valgt blandt neurodegenerative sygdomme, amyloidopatier, tauopatier og mentale udviklingssygdomme.
12. Sulfatsaltet til anvendelse ifølge krav 11, hvor sygdommen er valgt blandt Alzheimers sygdom, Lewy body demens (DLB), amyotrofisk lateral sklerose (ALS) med frontotemporal demens, inklusionslegeme myopati med Pagets knoglesygdom og/eller frontotemporal demens (IBMPFD), frontotemporal lobar degeneration, synucleopatier, Huntingtons sygdom, Parkinsons sygdom, amyloid angiopatier, frontotemporal demens med Parkinsonisme forbundet til kromosom 17 og Downs syndrom.
DK13815780.5T 2012-12-27 2013-12-27 N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1h-benzo[d]imidazol-2-amin sulfatsalte, fremstilling deraf og anvendelse af samme DK2938597T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12306690 2012-12-27
PCT/EP2013/078068 WO2014102339A1 (en) 2012-12-27 2013-12-27 Sulphate salts of n-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1h-benzo[d]imidazol-2-amine, preparation thereof and use of the same

Publications (1)

Publication Number Publication Date
DK2938597T3 true DK2938597T3 (da) 2017-01-09

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DK13815780.5T DK2938597T3 (da) 2012-12-27 2013-12-27 N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1h-benzo[d]imidazol-2-amin sulfatsalte, fremstilling deraf og anvendelse af samme

Country Status (24)

Country Link
US (3) US9562018B2 (da)
EP (1) EP2938597B1 (da)
JP (1) JP6384923B2 (da)
KR (1) KR102115060B1 (da)
CN (1) CN105008333B (da)
AU (2) AU2013369288B2 (da)
BR (1) BR112015015474B1 (da)
CA (1) CA2895285C (da)
DK (1) DK2938597T3 (da)
ES (1) ES2605494T3 (da)
HK (1) HK1215582A1 (da)
HR (1) HRP20161612T2 (da)
HU (1) HUE030930T2 (da)
IL (1) IL239450B (da)
LT (1) LT2938597T (da)
MX (1) MX363367B (da)
NZ (1) NZ708959A (da)
PL (1) PL2938597T3 (da)
PT (1) PT2938597T (da)
RS (1) RS55511B1 (da)
RU (1) RU2655454C2 (da)
SI (1) SI2938597T1 (da)
WO (1) WO2014102339A1 (da)
ZA (1) ZA201504521B (da)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2938597T (pt) 2012-12-27 2016-12-09 Université De Lille 2 Droit Et Santé Sais sulfato de n-(3-(4-(3-(isobutilamino)propil)-piperazin-1-il)propil)-1h-benzo[d]imidazol-2-amina, sua preparação e sua utilização
CN107466292B (zh) 2015-03-16 2020-05-01 国家医疗保健研究所 新型1,4-双(3-氨基丙基)哌嗪衍生物及其用途
TWI744300B (zh) * 2016-03-23 2021-11-01 里爾中央醫學中心 改良性熱處理的血小板顆粒裂解液在製備用於治療神經系統疾病的組合物的用途
IL301559A (en) 2020-10-01 2023-05-01 Alzprotect Succinate salts of N-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1H-benzo[D]imidazol-2-amine, their preparation and use
MX2023003715A (es) 2020-10-07 2023-04-24 Alzprotect Uso de sales de sulfato de n-(3-(4-(3-(diisobutilamino)propil)pipe razin-1-il)propil)-1h-benzo[d]imidazol-2-amina y solvatos de los mismos para el tratamiento de enfermedades neuronales motoras y trastornos de la union neuromuscular.
KR20240128694A (ko) 2021-12-20 2024-08-26 알즈프로텍트 운동 뉴런 질환 및 신경근 접합부 장애의 치료를 위한 N-(3-(4-(3-(디이소부틸아미노)프로필)피페라진-1-일)프로필)-1H-벤조[d]이미다졸-2-아민 숙시네이트 염 및 이의 용매화물의 사용
WO2023180537A1 (en) 2022-03-25 2023-09-28 Alzprotect Use of n-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1h-benzo[d]imidazol-2-amine salts and solvates thereof for the treatment of sensory neuron diseases

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FR2674856B1 (fr) * 1991-04-05 1993-07-30 Esteve Labor Dr Nouveaux antihistaminiques non sedatifs, derives de benzimidazole, leur procede de preparation et leur utilisation en tant que medicaments.
CA2263367A1 (fr) * 1997-06-12 1998-12-17 Transgene S.A. Nouveaux complexes lipidiques pour le transfert d'au moins une substance therapeutiquement active, notamment un polynucleotide, dans une cellule cible et utilisation en therapie genique
WO2000018767A2 (en) 1998-09-30 2000-04-06 Neurogen Corporation 2-piperazino alkylamino benzoazole derivatives: dopamine receptor subtype specific ligands
WO2002096431A1 (en) * 2001-05-25 2002-12-05 The Regents Of The University Of California Optically active compounds clearing malformed proteins
US20040116441A1 (en) * 2002-10-30 2004-06-17 Pfizer Inc Methods of using sulfonic acid derivatives
EP1581517B1 (en) * 2002-12-23 2007-02-21 Janssen Pharmaceutica N.V. Substituted 1-piperidin-4-yl-4-azetidin-3-yl-piperazine derivatives and their use as neurokinin antagonists
US9044478B2 (en) * 2004-11-10 2015-06-02 Institut National De La Sante Et De La Recherche Medicale Use of 1,4-bis (3-aminoalkyl) piperazine derivatives in the treatment of neurodegenerative diseases
PT2938597T (pt) * 2012-12-27 2016-12-09 Université De Lille 2 Droit Et Santé Sais sulfato de n-(3-(4-(3-(isobutilamino)propil)-piperazin-1-il)propil)-1h-benzo[d]imidazol-2-amina, sua preparação e sua utilização

Also Published As

Publication number Publication date
CA2895285A1 (en) 2014-07-03
HRP20161612T2 (hr) 2017-02-24
EP2938597B1 (en) 2016-10-26
HK1215582A1 (zh) 2016-09-02
IL239450B (en) 2018-06-28
MX2015008502A (es) 2015-12-16
KR20150105313A (ko) 2015-09-16
RU2015130671A (ru) 2017-01-30
PL2938597T3 (pl) 2017-03-31
US20170151235A1 (en) 2017-06-01
RU2655454C2 (ru) 2018-05-29
BR112015015474A2 (da) 2017-08-15
US20190381036A1 (en) 2019-12-19
AU2013369288A8 (en) 2015-07-16
JP6384923B2 (ja) 2018-09-05
CN105008333A (zh) 2015-10-28
CA2895285C (en) 2021-03-30
NZ708959A (en) 2019-11-29
US20160108003A1 (en) 2016-04-21
US9562018B2 (en) 2017-02-07
ES2605494T3 (es) 2017-03-14
JP2016503813A (ja) 2016-02-08
KR102115060B1 (ko) 2020-05-25
AU2018202218A1 (en) 2018-04-26
AU2013369288A1 (en) 2015-07-02
BR112015015474B1 (pt) 2022-04-19
US10772884B2 (en) 2020-09-15
HUE030930T2 (hu) 2017-06-28
LT2938597T (lt) 2017-01-25
CN105008333B (zh) 2018-02-09
SI2938597T1 (sl) 2017-03-31
WO2014102339A1 (en) 2014-07-03
ZA201504521B (en) 2016-11-30
HRP20161612T1 (hr) 2017-01-27
RS55511B1 (sr) 2017-05-31
AU2013369288B2 (en) 2018-02-22
IL239450A0 (en) 2015-07-30
PT2938597T (pt) 2016-12-09
US10537569B2 (en) 2020-01-21
EP2938597A1 (en) 2015-11-04
MX363367B (es) 2019-03-20
AU2018202218B2 (en) 2019-02-21

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