RU2015130671A - Соли сульфаты n-(3-(4-(3-(диизобутиламино)пропил)пиперазин-1ил)пропил)-1н-бензо[d]имидазол-2-амина, их получение и их применение - Google Patents
Соли сульфаты n-(3-(4-(3-(диизобутиламино)пропил)пиперазин-1ил)пропил)-1н-бензо[d]имидазол-2-амина, их получение и их применение Download PDFInfo
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- RU2015130671A RU2015130671A RU2015130671A RU2015130671A RU2015130671A RU 2015130671 A RU2015130671 A RU 2015130671A RU 2015130671 A RU2015130671 A RU 2015130671A RU 2015130671 A RU2015130671 A RU 2015130671A RU 2015130671 A RU2015130671 A RU 2015130671A
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- Prior art keywords
- disease
- pharmaceutically acceptable
- sulfate
- propyl
- sulfate salt
- Prior art date
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- -1 SALTS SULPHATES Chemical class 0.000 title claims 5
- OCBFFGCSTGGPSQ-UHFFFAOYSA-N [CH2]CC Chemical class [CH2]CC OCBFFGCSTGGPSQ-UHFFFAOYSA-N 0.000 title 2
- 239000012453 solvate Substances 0.000 claims 9
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 8
- 150000003467 sulfuric acid derivatives Chemical class 0.000 claims 7
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 206010067889 Dementia with Lewy bodies Diseases 0.000 claims 3
- 201000002832 Lewy body dementia Diseases 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 206010059245 Angiopathy Diseases 0.000 claims 2
- 208000012239 Developmental disease Diseases 0.000 claims 2
- 201000010374 Down Syndrome Diseases 0.000 claims 2
- 208000002339 Frontotemporal Lobar Degeneration Diseases 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 208000021642 Muscular disease Diseases 0.000 claims 2
- 201000009623 Myopathy Diseases 0.000 claims 2
- 208000027067 Paget disease of bone Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 208000034799 Tauopathies Diseases 0.000 claims 2
- 208000016738 bone Paget disease Diseases 0.000 claims 2
- 210000000349 chromosome Anatomy 0.000 claims 2
- 210000003000 inclusion body Anatomy 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- SXMCNGUNDUIJCO-UHFFFAOYSA-N n-[3-[4-[3-[bis(2-methylpropyl)amino]propyl]piperazin-1-yl]propyl]-1h-benzimidazol-2-amine;sulfuric acid Chemical compound OS(O)(=O)=O.C1CN(CCCN(CC(C)C)CC(C)C)CCN1CCCNC1=NC2=CC=CC=C2N1 SXMCNGUNDUIJCO-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
- C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
- C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
- C07D235/24—Benzimidazoles; 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
- C07D235/30—Nitrogen atoms not forming part of a nitro radical
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (18)
1. Соль сульфат N-(3-(4-(3-(диизобутиламино)пропил)пиперазин-1-ил)пропил)-1H-бензо[d]имидазол-2-амина и его фармацевтически приемлемые сольваты.
2. Соль сульфат по п. 1, имеющий формулу II
при этом x равен 0,5-4, и его фармацевтически приемлемые сольваты.
3. Соль сульфат по п. 2 и его фармацевтически приемлемые сольваты, отличающиеся тем, что x равен 1,5-2,5.
4. Соль сульфат по п. 2 и его фармацевтически приемлемые сольваты, отличающиеся тем, что x равен 0,5-1,5.
5. Соль сульфат по п. 2 и его фармацевтически приемлемые сольваты, отличающиеся тем, что x равен 2,5-3,5.
6. Соль сульфат по п. 2, имеющий формулу III
при этом
x имеет значения, указанные в п. 2, и
y равен 0,5-5.
7. Фармацевтическая композиция, включающая соль сульфат по любому из пп. 1-6 или его фармацевтически приемлемый сольват и, по меньшей мере, один фармацевтически приемлемый носитель, разбавитель, эксципиент и/или адъювант.
8. Соль сульфат по любому из пп. 1-6 или его фармацевтически приемлемый сольват для применения в качестве лекарственного средства.
9. Соль сульфат по любому из пп. 1-6 или его фармацевтически приемлемый сольват для применения при лечении и/или предупреждении заболевания, выбранного из нейродегенеративных заболеваний, амилоидопатий, тауопатий и болезней развития.
10. Соль сульфат по п. 9, при этом заболевание выбирают из болезни Альцгеймера, деменции с тельцами Леви (DLB), амиотрофического бокового склероза (ALS) с фронтотемпоральной деменцией, миопатии с тельцами включения с болезнью костей Педжета и/или фронтотемпоральной деменцией (IBMPFD), фронтотемпоральной лобарной дегенерации, синуклеопатий, болезни Хантингтона, болезни Паркинсона, амилоидных ангиопатий, фронтотемпоральной деменции с паркинсонизмом, связанным с хромосомой 17, и синдрома Дауна.
11. Соль сульфат по любому из пп. 1-6 или его фармацевтически приемлемый сольват для применения при отсрочке у пациента начала заболевания, выбранного из нейродегенеративных заболеваний, амилоидопатий, тауопатий и болезней развития.
12. Соль сульфат по п. 11, при этом заболевание выбирают из болезни Альцгеймера, деменции с тельцами Леви (DLB), амиотрофического бокового склероза (ALS) с фронтотемпоральной деменцией, миопатии с тельцами включения с болезнью костей Педжета и/или фронтотемпоральной деменцией (IBMPFD), фронтотемпоральной лобарной дегенерации, синуклеопатий, болезни Хантингтона, болезни Паркинсона, амилоидных ангиопатий, фронтотемпоральной деменции с паркинсонизмом, связанным с хромосомой 17, и синдрома Дауна.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12306690 | 2012-12-27 | ||
| EP12306690.4 | 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 (2)
| Publication Number | Publication Date |
|---|---|
| RU2015130671A true RU2015130671A (ru) | 2017-01-30 |
| RU2655454C2 RU2655454C2 (ru) | 2018-05-29 |
Family
ID=47501005
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015130671A RU2655454C2 (ru) | 2012-12-27 | 2013-12-27 | Соли сульфаты n-(3-(4-(3-(диизобутиламино)пропил)пиперазин-1ил)пропил)-1н-бензо[d]имидазол-2-амина, их получение и их применение |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US9562018B2 (ru) |
| EP (1) | EP2938597B1 (ru) |
| JP (1) | JP6384923B2 (ru) |
| KR (1) | KR102115060B1 (ru) |
| CN (1) | CN105008333B (ru) |
| AU (2) | AU2013369288B2 (ru) |
| BR (1) | BR112015015474B1 (ru) |
| CA (1) | CA2895285C (ru) |
| DK (1) | DK2938597T3 (ru) |
| ES (1) | ES2605494T3 (ru) |
| HK (1) | HK1215582A1 (ru) |
| HR (1) | HRP20161612T2 (ru) |
| HU (1) | HUE030930T2 (ru) |
| IL (1) | IL239450B (ru) |
| LT (1) | LT2938597T (ru) |
| MX (1) | MX363367B (ru) |
| NZ (1) | NZ708959A (ru) |
| PL (1) | PL2938597T3 (ru) |
| PT (1) | PT2938597T (ru) |
| RS (1) | RS55511B1 (ru) |
| RU (1) | RU2655454C2 (ru) |
| SI (1) | SI2938597T1 (ru) |
| WO (1) | WO2014102339A1 (ru) |
| ZA (1) | ZA201504521B (ru) |
Families Citing this family (7)
| 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 |
| DK3271335T3 (en) | 2015-03-16 | 2019-04-01 | Inst Nat Sante Rech Med | HIS UNKNOWN 1,4-BIS (3-AMINOPROPYL) PIPERAZINE DERIVATIVES AND USE THEREOF |
| 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 |
| US20230391729A1 (en) | 2020-10-01 | 2023-12-07 | Alzprotect | Succinate 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 |
| EP4225306A1 (en) | 2020-10-07 | 2023-08-16 | Alzprotect | Use of n-(3-(4-(3-(diisobutylamino)propyl)piperazin-1-yl)propyl)-1h-benzo[d]imidazol-2-amine sulphate salts and solvates thereof for the treatment of motor neuron diseases and neuromuscular junction disorders |
| WO2023117990A1 (en) | 2021-12-20 | 2023-06-29 | Alzprotect | USE OF N-(3-(4-(3-(DIISOBUTYLAMINO)PROPYL)PIPERAZIN-1-YL)PROPYL)-1H-BENZO[d]IMIDAZOL-2-AMINE SUCCINATE SALTS AND SOLVATES THEREOF FOR THE TREATMENT OF MOTOR NEURON DISEASES AND NEUROMUSCULAR JUNCTION DISORDERS |
| 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 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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. |
| WO1998056423A1 (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 |
| US20050020582A1 (en) * | 2001-05-25 | 2005-01-27 | Prusiner Stanley B | Optically active compounds clearing malformed proteins |
| US20040116441A1 (en) * | 2002-10-30 | 2004-06-17 | Pfizer Inc | Methods of using sulfonic acid derivatives |
| ES2282731T3 (es) * | 2002-12-23 | 2007-10-16 | Janssen Pharmaceutica N.V. | Derivados de 1-piperidin-4-il-4-azetidin-3-il-piperazina sustituida y su uso como antagonistas de neuroquininas. |
| WO2006051489A1 (en) * | 2004-11-10 | 2006-05-18 | Institut National De La Sante Et De La Recherche Medicale (Inserm) | 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 |
-
2013
- 2013-12-27 PT PT138157805T patent/PT2938597T/pt unknown
- 2013-12-27 RU RU2015130671A patent/RU2655454C2/ru active
- 2013-12-27 EP EP13815780.5A patent/EP2938597B1/en active Active
- 2013-12-27 CN CN201380068524.8A patent/CN105008333B/zh active Active
- 2013-12-27 SI SI201330408A patent/SI2938597T1/sl unknown
- 2013-12-27 WO PCT/EP2013/078068 patent/WO2014102339A1/en active Application Filing
- 2013-12-27 PL PL13815780T patent/PL2938597T3/pl unknown
- 2013-12-27 RS RS20161055A patent/RS55511B1/sr unknown
- 2013-12-27 ES ES13815780.5T patent/ES2605494T3/es active Active
- 2013-12-27 KR KR1020157017192A patent/KR102115060B1/ko active IP Right Grant
- 2013-12-27 MX MX2015008502A patent/MX363367B/es unknown
- 2013-12-27 BR BR112015015474-3A patent/BR112015015474B1/pt active IP Right Grant
- 2013-12-27 NZ NZ70895913A patent/NZ708959A/en unknown
- 2013-12-27 DK DK13815780.5T patent/DK2938597T3/en active
- 2013-12-27 JP JP2015550088A patent/JP6384923B2/ja active Active
- 2013-12-27 CA CA2895285A patent/CA2895285C/en active Active
- 2013-12-27 HU HUE13815780A patent/HUE030930T2/hu unknown
- 2013-12-27 LT LTEP13815780.5T patent/LT2938597T/lt unknown
- 2013-12-27 US US14/655,642 patent/US9562018B2/en active Active
- 2013-12-27 AU AU2013369288A patent/AU2013369288B2/en active Active
-
2015
- 2015-06-16 IL IL239450A patent/IL239450B/en active IP Right Grant
- 2015-06-23 ZA ZA2015/04521A patent/ZA201504521B/en unknown
-
2016
- 2016-03-29 HK HK16103579.5A patent/HK1215582A1/zh unknown
- 2016-12-01 HR HRP20161612TT patent/HRP20161612T2/hr unknown
- 2016-12-22 US US15/388,349 patent/US10537569B2/en active Active
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2018
- 2018-03-28 AU AU2018202218A patent/AU2018202218B2/en active Active
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2019
- 2019-08-27 US US16/552,436 patent/US10772884B2/en active Active
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