RU2019113752A - Композиции апилимода и способы их применения при лечении болезни альцгеймера - Google Patents
Композиции апилимода и способы их применения при лечении болезни альцгеймера Download PDFInfo
- Publication number
- RU2019113752A RU2019113752A RU2019113752A RU2019113752A RU2019113752A RU 2019113752 A RU2019113752 A RU 2019113752A RU 2019113752 A RU2019113752 A RU 2019113752A RU 2019113752 A RU2019113752 A RU 2019113752A RU 2019113752 A RU2019113752 A RU 2019113752A
- Authority
- RU
- Russia
- Prior art keywords
- apilimod
- cell
- dosage form
- alzheimer
- disease
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims 19
- HSKAZIJJKRAJAV-KOEQRZSOSA-N n-[(e)-(3-methylphenyl)methylideneamino]-6-morpholin-4-yl-2-(2-pyridin-2-ylethoxy)pyrimidin-4-amine Chemical compound CC1=CC=CC(\C=N\NC=2N=C(OCCC=3N=CC=CC=3)N=C(C=2)N2CCOCC2)=C1 HSKAZIJJKRAJAV-KOEQRZSOSA-N 0.000 title claims 9
- 229950002889 apilimod Drugs 0.000 title claims 7
- 208000024827 Alzheimer disease Diseases 0.000 title claims 3
- 239000000203 mixture Substances 0.000 title 1
- 210000004027 cell Anatomy 0.000 claims 6
- 101710137189 Amyloid-beta A4 protein Proteins 0.000 claims 5
- 101710151993 Amyloid-beta precursor protein Proteins 0.000 claims 5
- 102100022704 Amyloid-beta precursor protein Human genes 0.000 claims 5
- DZHSAHHDTRWUTF-SIQRNXPUSA-N amyloid-beta polypeptide 42 Chemical compound C([C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(O)=O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC(O)=O)C(C)C)C(C)C)C1=CC=CC=C1 DZHSAHHDTRWUTF-SIQRNXPUSA-N 0.000 claims 5
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 239000002552 dosage form Substances 0.000 claims 3
- 102000004196 processed proteins & peptides Human genes 0.000 claims 3
- 108090000765 processed proteins & peptides Proteins 0.000 claims 3
- -1 3-methylbenzylidene Chemical group 0.000 claims 2
- 206010012289 Dementia Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 2
- 125000000717 hydrazino group Chemical group [H]N([*])N([H])[H] 0.000 claims 2
- 239000006186 oral dosage form Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 229940122041 Cholinesterase inhibitor Drugs 0.000 claims 1
- 208000031124 Dementia Alzheimer type Diseases 0.000 claims 1
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000001537 neural effect Effects 0.000 claims 1
- 210000002569 neuron Anatomy 0.000 claims 1
- 208000024891 symptom Diseases 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662407186P | 2016-10-12 | 2016-10-12 | |
| US62/407,186 | 2016-10-12 | ||
| PCT/US2017/056147 WO2018071548A1 (en) | 2016-10-12 | 2017-10-11 | Apilimod compositions and methods for using same in the treatment of alzheimer's disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2019113752A true RU2019113752A (ru) | 2020-11-13 |
| RU2019113752A3 RU2019113752A3 (https=) | 2021-01-19 |
Family
ID=60268450
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2019113752A RU2019113752A (ru) | 2016-10-12 | 2017-10-11 | Композиции апилимода и способы их применения при лечении болезни альцгеймера |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20190365771A1 (https=) |
| EP (1) | EP3525794A1 (https=) |
| JP (1) | JP7199349B2 (https=) |
| KR (1) | KR20190067824A (https=) |
| CN (1) | CN110167559A (https=) |
| AU (1) | AU2017342262B2 (https=) |
| BR (1) | BR112019007214A2 (https=) |
| CA (1) | CA3039199A1 (https=) |
| IL (1) | IL265911A (https=) |
| MX (1) | MX2019004179A (https=) |
| RU (1) | RU2019113752A (https=) |
| WO (1) | WO2018071548A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12589097B2 (en) | 2018-02-21 | 2026-03-31 | OrphAl Therapeutics Inc. | Apilimod compositions and methods of use |
| AU2019223014B2 (en) | 2018-02-21 | 2024-10-17 | Orphai Therapeutics Inc. | Combination therapy with apilimod and glutamatergic agents |
| CN116059192B (zh) | 2019-11-13 | 2024-10-29 | 润佳（苏州）医药科技有限公司 | 同位素富集的3-氨基-1-丙磺酸及其衍生物的用途 |
| KR20220140515A (ko) | 2020-01-13 | 2022-10-18 | 버지 애널리틱스, 인크. | 치환된 피라졸로-피리미딘 및 그의 용도 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7923557B2 (en) | 2004-11-10 | 2011-04-12 | Synta Pharmaceuticals Corporation | Process for preparing trisubstituted pyrimidine compounds |
| US7863270B2 (en) | 2005-05-13 | 2011-01-04 | Synta Pharmaceuticals Corp. | IL-12 modulatory compounds |
| WO2006128129A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
| US20130302343A1 (en) | 2011-01-04 | 2013-11-14 | Charité Universitätsmedizin Berlin | Modulators of il-12 and/or il-23 for the prevention or treatment of alzheimer's disease |
| US10206910B2 (en) * | 2014-11-07 | 2019-02-19 | Lam Therapeutics, Inc. | Apilimod for use in the treatment of renal cancer |
| CA2966334A1 (en) * | 2014-11-07 | 2016-05-12 | Lam Therapeutics, Inc. | Apilimod for use in the treatment of colorectal cancer |
| US10729694B2 (en) * | 2015-01-23 | 2020-08-04 | AI Therapeutics, Inc. | Anti-viral compositions containing PIKfyve inhibitors and use thereof |
| US20180015098A1 (en) * | 2015-02-03 | 2018-01-18 | Lam Therapeutics, Inc. | Apilimod compositions and methods for using same |
| US10758545B2 (en) * | 2015-06-25 | 2020-09-01 | University Of Southern California | Methods to treat neurological diseases |
-
2017
- 2017-10-11 KR KR1020197012287A patent/KR20190067824A/ko not_active Ceased
- 2017-10-11 CA CA3039199A patent/CA3039199A1/en active Pending
- 2017-10-11 RU RU2019113752A patent/RU2019113752A/ru not_active Application Discontinuation
- 2017-10-11 WO PCT/US2017/056147 patent/WO2018071548A1/en not_active Ceased
- 2017-10-11 BR BR112019007214A patent/BR112019007214A2/pt not_active Application Discontinuation
- 2017-10-11 US US16/340,845 patent/US20190365771A1/en not_active Abandoned
- 2017-10-11 CN CN201780076520.2A patent/CN110167559A/zh active Pending
- 2017-10-11 AU AU2017342262A patent/AU2017342262B2/en not_active Ceased
- 2017-10-11 EP EP17794818.9A patent/EP3525794A1/en not_active Withdrawn
- 2017-10-11 MX MX2019004179A patent/MX2019004179A/es unknown
- 2017-10-11 JP JP2019519652A patent/JP7199349B2/ja active Active
-
2019
- 2019-04-08 IL IL265911A patent/IL265911A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20190067824A (ko) | 2019-06-17 |
| WO2018071548A1 (en) | 2018-04-19 |
| AU2017342262A1 (en) | 2019-04-18 |
| US20190365771A1 (en) | 2019-12-05 |
| IL265911A (en) | 2019-06-30 |
| JP7199349B2 (ja) | 2023-01-05 |
| BR112019007214A2 (pt) | 2019-07-02 |
| RU2019113752A3 (https=) | 2021-01-19 |
| EP3525794A1 (en) | 2019-08-21 |
| MX2019004179A (es) | 2019-09-02 |
| AU2017342262B2 (en) | 2023-09-28 |
| CA3039199A1 (en) | 2018-04-19 |
| CN110167559A (zh) | 2019-08-23 |
| JP2019530711A (ja) | 2019-10-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20220114 |