SG11201905528XA - A pharmaceutical composition comprising an oxazine derivative and its use in the treatment or prevention of alzheimer's disease - Google Patents
A pharmaceutical composition comprising an oxazine derivative and its use in the treatment or prevention of alzheimer's diseaseInfo
- Publication number
- SG11201905528XA SG11201905528XA SG11201905528XA SG11201905528XA SG11201905528XA SG 11201905528X A SG11201905528X A SG 11201905528XA SG 11201905528X A SG11201905528X A SG 11201905528XA SG 11201905528X A SG11201905528X A SG 11201905528XA SG 11201905528X A SG11201905528X A SG 11201905528XA
- Authority
- SG
- Singapore
- Prior art keywords
- basel
- postfach
- international
- novartis
- pharma
- Prior art date
Links
- 208000024827 Alzheimer disease Diseases 0.000 title abstract 3
- 150000004893 oxazines Chemical class 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 230000002265 prevention Effects 0.000 title abstract 3
- 238000011282 treatment Methods 0.000 title abstract 3
- 239000003795 chemical substances by application Substances 0.000 abstract 5
- 229940125759 BACE1 protease inhibitor Drugs 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 102220240796 rs553605556 Human genes 0.000 abstract 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
- 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
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- 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
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- 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
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Biophysics (AREA)
- Inorganic Chemistry (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Biochemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 26 July 2018 (26.07.2018) WIP0 I PCT omit VIII °nolo offilmomiloollowo oimIE (10) International Publication Number WO 2018/134760 Al (51) International Patent Classification: A61K 9/16 (2006.01) A61K 31/5377 (2006.01) A61K 9/48 (2006.01) A61P 25/28 (2006.01) A61K 9/14 (2006.01) (21) International Application Number: PCT/IB2018/050312 (22) International Filing Date: 18 January 2018 (18.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 17152481.2 20 January 2017 (20.01.2017) EP (71) Applicant: NOVARTIS AG [CH/CH]; Lichtstrasse 35, 4056 Basel (CH). (72) Inventors: ACHOUR, Miloud; Novartis Pharma AG, Postfach, 4002 Basel (CH). GALLI, Bruno; Novartis Phar- ma AG, Postfach, 4002 Basel (CH). JOHN, Edgar; No- vartis Pharma AG, Postfach, 4002 Basel (CH). JUHNKE, Michael; Novartis Pharma AG, Postfach, 4002 Basel (CH). KNEZIC, Dragutin; 80 Hope Avenue, Apt 112, Waltham, Massachusetts 02453 (US). KORADIA, Vishal Shamji; Novartis Pharma AG, Postfach, 4002 Basel (CH). RAMOS, Rita; Novartis Pharma AG, Postfach, 4002 Basel (CH). Declarations under Rule 4.17: as to applicant's entitlement to apply for and be granted a patent (Rule 4.1700) Published: with international search report (Art. 21(3)) in black and white; the international application as filed contained color or greyscale and is available for download from PATENTSCOPE (74) Agent: NOVARTIS AG; Lichtstrasse 35, 4056 Basel (CH). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. = (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). 00 (54) Title: A PHARMACEUTICAL COMPOSITION COMPRISING AN OXAZINE DERIVATIVE AND ITS USE IN THE TREAT- MENT OR PREVENTION OF ALZHEIMER'S DISEASE \" (57) : The present invention relates to a pharmaceutical composition comprising an oxazine derivative BACE-1 inhibitor, a 0 process for the preparation thereof, and its use in the treatment or prevention of Alzheimer's disease.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17152481 | 2017-01-20 | ||
| PCT/IB2018/050312 WO2018134760A1 (en) | 2017-01-20 | 2018-01-18 | A pharmaceutical composition comprising an oxazine derivative and its use in the treatment or prevention of alzheimer's disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201905528XA true SG11201905528XA (en) | 2019-08-27 |
Family
ID=57890668
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201905528XA SG11201905528XA (en) | 2017-01-20 | 2018-01-18 | A pharmaceutical composition comprising an oxazine derivative and its use in the treatment or prevention of alzheimer's disease |
| SG11201905116PA SG11201905116PA (en) | 2017-01-20 | 2018-01-18 | A free base oxazine derivative in crystalline form |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201905116PA SG11201905116PA (en) | 2017-01-20 | 2018-01-18 | A free base oxazine derivative in crystalline form |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US20200048237A1 (en) |
| EP (2) | EP3571195A1 (en) |
| JP (2) | JP2020505363A (en) |
| KR (1) | KR20190126291A (en) |
| CN (1) | CN110167535A (en) |
| AR (1) | AR110758A1 (en) |
| AU (3) | AU2018208870A1 (en) |
| BR (2) | BR112019014234A2 (en) |
| CA (2) | CA3048346A1 (en) |
| CL (1) | CL2019002020A1 (en) |
| CO (2) | CO2019007670A2 (en) |
| CR (1) | CR20190333A (en) |
| IL (2) | IL267640A (en) |
| JO (2) | JOP20190180A1 (en) |
| MX (2) | MX2019008603A (en) |
| PE (2) | PE20191346A1 (en) |
| RU (1) | RU2019126022A (en) |
| SG (2) | SG11201905528XA (en) |
| TW (1) | TW201828943A (en) |
| UY (1) | UY37572A (en) |
| WO (2) | WO2018134760A1 (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019142111A1 (en) * | 2018-01-18 | 2019-07-25 | Novartis Ag | Salt forms of an oxazine derivative bace inhibitor |
| CN112661667B (en) * | 2020-12-28 | 2023-02-03 | 浦拉司科技（上海）有限责任公司 | Preparation method of trifluoroacetamidine |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2663561E (en) * | 2011-01-13 | 2016-06-07 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
-
2017
- 2017-06-16 JO JOP/2019/0180A patent/JOP20190180A1/en unknown
- 2017-06-16 JO JOP/2019/0178A patent/JOP20190178A1/en unknown
-
2018
- 2018-01-18 WO PCT/IB2018/050312 patent/WO2018134760A1/en unknown
- 2018-01-18 CN CN201880006121.3A patent/CN110167535A/en active Pending
- 2018-01-18 CA CA3048346A patent/CA3048346A1/en not_active Abandoned
- 2018-01-18 CR CR20190333A patent/CR20190333A/en unknown
- 2018-01-18 PE PE2019001432A patent/PE20191346A1/en unknown
- 2018-01-18 WO PCT/IB2018/050314 patent/WO2018134761A1/en unknown
- 2018-01-18 BR BR112019014234-7A patent/BR112019014234A2/en not_active IP Right Cessation
- 2018-01-18 CA CA3046304A patent/CA3046304A1/en not_active Abandoned
- 2018-01-18 US US16/478,736 patent/US20200048237A1/en not_active Abandoned
- 2018-01-18 KR KR1020197020514A patent/KR20190126291A/en not_active Application Discontinuation
- 2018-01-18 MX MX2019008603A patent/MX2019008603A/en unknown
- 2018-01-18 TW TW107101806A patent/TW201828943A/en unknown
- 2018-01-18 MX MX2019008601A patent/MX2019008601A/en unknown
- 2018-01-18 PE PE2019001437A patent/PE20191250A1/en unknown
- 2018-01-18 AU AU2018208870A patent/AU2018208870A1/en not_active Abandoned
- 2018-01-18 SG SG11201905528XA patent/SG11201905528XA/en unknown
- 2018-01-18 US US16/478,704 patent/US20190388428A1/en not_active Abandoned
- 2018-01-18 EP EP18701600.1A patent/EP3571195A1/en not_active Withdrawn
- 2018-01-18 SG SG11201905116PA patent/SG11201905116PA/en unknown
- 2018-01-18 RU RU2019126022A patent/RU2019126022A/en not_active Application Discontinuation
- 2018-01-18 JP JP2019539215A patent/JP2020505363A/en active Pending
- 2018-01-18 BR BR112019014825-6A patent/BR112019014825A2/en not_active Application Discontinuation
- 2018-01-18 EP EP18701232.3A patent/EP3570820A1/en not_active Withdrawn
- 2018-01-18 AU AU2018209442A patent/AU2018209442A1/en not_active Abandoned
- 2018-01-18 JP JP2019539254A patent/JP2020505367A/en active Pending
- 2018-01-19 AR ARP180100124A patent/AR110758A1/en unknown
- 2018-01-19 UY UY0001037572A patent/UY37572A/en not_active Application Discontinuation
-
2019
- 2019-06-25 IL IL267640A patent/IL267640A/en unknown
- 2019-07-17 CO CONC2019/0007670A patent/CO2019007670A2/en unknown
- 2019-07-17 IL IL268131A patent/IL268131A/en unknown
- 2019-07-17 CO CONC2019/0007671A patent/CO2019007671A2/en unknown
- 2019-07-18 CL CL2019002020A patent/CL2019002020A1/en unknown
-
2020
- 2020-12-15 AU AU2020289738A patent/AU2020289738A1/en not_active Abandoned
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