ECSP21067104A - Forma de un compuesto que tiene biodisponibilidad mejorada y formulaciones de las mismas - Google Patents
Forma de un compuesto que tiene biodisponibilidad mejorada y formulaciones de las mismasInfo
- Publication number
- ECSP21067104A ECSP21067104A ECSENADI202167104A ECDI202167104A ECSP21067104A EC SP21067104 A ECSP21067104 A EC SP21067104A EC SENADI202167104 A ECSENADI202167104 A EC SENADI202167104A EC DI202167104 A ECDI202167104 A EC DI202167104A EC SP21067104 A ECSP21067104 A EC SP21067104A
- Authority
- EC
- Ecuador
- Prior art keywords
- amorphous
- formulations
- compound
- fluoro
- preparing
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 2
- 239000000203 mixture Substances 0.000 title 1
- 238000000034 method Methods 0.000 abstract 2
- 239000008203 oral pharmaceutical composition Substances 0.000 abstract 2
- TWLWOOPCEXYVBE-UHFFFAOYSA-N 5-fluoro-2-(6-fluoro-2-methylbenzimidazol-1-yl)-4-n-[4-(trifluoromethyl)phenyl]pyrimidine-4,6-diamine Chemical compound CC1=NC2=CC=C(F)C=C2N1C(N=1)=NC(N)=C(F)C=1NC1=CC=C(C(F)(F)F)C=C1 TWLWOOPCEXYVBE-UHFFFAOYSA-N 0.000 abstract 1
- 239000006185 dispersion Substances 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
- 239000007962 solid dispersion Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K9/146—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 macromolecular 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
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/485—Inorganic 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
- A61K9/4858—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Inorganic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente descripción en general se relaciona con formas amorfas de compuestos que tienen solubilidad acuosa mejorada y velocidades de disolución y dispersiones sólidas amorfas y formulaciones farmacéuticas orales de las mismas, y a procesos para preparar las mismas. La presente descripción se relaciona específicamente con formas amorfas de 5-fluoro-2-(6-fluoro-2-metil-1H-bencimidazol-1-il)-N-[4-(trifluorometil)fenil]pirimidin-4,6-diamina y dispersiones sólidas amorfas y formulaciones farmacéuticas orales de las mismas, y a procesos para preparar las mismas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962816402P | 2019-03-11 | 2019-03-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP21067104A true ECSP21067104A (es) | 2021-11-18 |
Family
ID=70166162
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI202167104A ECSP21067104A (es) | 2019-03-11 | 2021-09-09 | Forma de un compuesto que tiene biodisponibilidad mejorada y formulaciones de las mismas |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US20220185795A1 (es) |
| EP (1) | EP3938368B1 (es) |
| JP (1) | JP2022524424A (es) |
| KR (1) | KR20210151061A (es) |
| CN (1) | CN113853374B (es) |
| AU (1) | AU2020235825A1 (es) |
| BR (1) | BR112021017353A2 (es) |
| CA (1) | CA3131801A1 (es) |
| CL (1) | CL2021002365A1 (es) |
| CO (1) | CO2021011836A2 (es) |
| EA (1) | EA202192167A1 (es) |
| EC (1) | ECSP21067104A (es) |
| HU (1) | HUE062796T2 (es) |
| IL (1) | IL286163A (es) |
| MX (1) | MX2021010906A (es) |
| PE (1) | PE20212270A1 (es) |
| PL (1) | PL3938368T3 (es) |
| SG (1) | SG11202109503TA (es) |
| WO (1) | WO2020185648A1 (es) |
| ZA (1) | ZA202106437B (es) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2892045C (en) * | 2012-11-21 | 2022-05-31 | Ptc Therapeutics, Inc. | Substituted reverse pyrimidine bmi-1 inhibitors |
| WO2020055544A2 (en) | 2018-08-17 | 2020-03-19 | Ptc Therapeutics, Inc. | Method for treating pancreatic cancer |
| MX2021010398A (es) * | 2019-02-28 | 2022-01-18 | Ptc Therapeutics Inc | Metodo para tratar un mieloma multiple. |
| CA3134648A1 (en) * | 2019-03-27 | 2020-10-01 | Ptc Therapeutics, Inc. | Combinations useful in a method for treating sarcoma |
| KR20220125232A (ko) * | 2019-11-26 | 2022-09-14 | 이케나 온콜로지, 인코포레이티드 | Ahr 억제제 및 이의 용도 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2892045C (en) * | 2012-11-21 | 2022-05-31 | Ptc Therapeutics, Inc. | Substituted reverse pyrimidine bmi-1 inhibitors |
| EA028009B1 (ru) * | 2013-01-22 | 2017-09-29 | Ф.Хоффманн-Ля Рош Аг | Фармацевтическая композиция с улучшенной биодоступностью |
| JP6878398B2 (ja) * | 2015-04-03 | 2021-05-26 | インパクト セラピューティクス インコーポレイティドImpact Therapeutics, Inc | Parp阻害剤固形医薬剤型及びその使用 |
| WO2017149550A1 (en) * | 2016-03-02 | 2017-09-08 | Msn Laboratories Private Limited | Amorphous form of 4-methyl-n-[3-(4-methyl-1h-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide |
-
2020
- 2020-03-09 PE PE2021001490A patent/PE20212270A1/es unknown
- 2020-03-09 BR BR112021017353A patent/BR112021017353A2/pt not_active Application Discontinuation
- 2020-03-09 CA CA3131801A patent/CA3131801A1/en active Pending
- 2020-03-09 WO PCT/US2020/021648 patent/WO2020185648A1/en not_active Ceased
- 2020-03-09 US US17/437,614 patent/US20220185795A1/en not_active Abandoned
- 2020-03-09 AU AU2020235825A patent/AU2020235825A1/en not_active Abandoned
- 2020-03-09 MX MX2021010906A patent/MX2021010906A/es unknown
- 2020-03-09 HU HUE20717027A patent/HUE062796T2/hu unknown
- 2020-03-09 PL PL20717027.5T patent/PL3938368T3/pl unknown
- 2020-03-09 KR KR1020217028865A patent/KR20210151061A/ko not_active Ceased
- 2020-03-09 EP EP20717027.5A patent/EP3938368B1/en active Active
- 2020-03-09 EA EA202192167A patent/EA202192167A1/ru unknown
- 2020-03-09 SG SG11202109503TA patent/SG11202109503TA/en unknown
- 2020-03-09 JP JP2021554628A patent/JP2022524424A/ja active Pending
- 2020-03-09 CN CN202080033442.XA patent/CN113853374B/zh active Active
-
2021
- 2021-09-02 ZA ZA2021/06437A patent/ZA202106437B/en unknown
- 2021-09-05 IL IL286163A patent/IL286163A/en unknown
- 2021-09-09 CO CONC2021/0011836A patent/CO2021011836A2/es unknown
- 2021-09-09 CL CL2021002365A patent/CL2021002365A1/es unknown
- 2021-09-09 EC ECSENADI202167104A patent/ECSP21067104A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2020185648A1 (en) | 2020-09-17 |
| CO2021011836A2 (es) | 2021-12-10 |
| PE20212270A1 (es) | 2021-11-30 |
| EP3938368A1 (en) | 2022-01-19 |
| JP2022524424A (ja) | 2022-05-02 |
| US20220185795A1 (en) | 2022-06-16 |
| EA202192167A1 (ru) | 2022-01-12 |
| BR112021017353A2 (pt) | 2021-11-16 |
| PL3938368T3 (pl) | 2023-12-27 |
| CN113853374B (zh) | 2025-02-28 |
| MX2021010906A (es) | 2021-10-01 |
| ZA202106437B (en) | 2025-01-29 |
| EP3938368B1 (en) | 2023-06-07 |
| CA3131801A1 (en) | 2020-09-17 |
| AU2020235825A1 (en) | 2021-09-30 |
| IL286163A (en) | 2021-10-31 |
| CL2021002365A1 (es) | 2022-04-22 |
| CN113853374A (zh) | 2021-12-28 |
| HUE062796T2 (hu) | 2023-12-28 |
| KR20210151061A (ko) | 2021-12-13 |
| SG11202109503TA (en) | 2021-09-29 |
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