HRP20161061T1 - Čvrste farmaceutske formulacije koje sadrže bibw 2992 - Google Patents
Čvrste farmaceutske formulacije koje sadrže bibw 2992 Download PDFInfo
- Publication number
- HRP20161061T1 HRP20161061T1 HRP20161061TT HRP20161061T HRP20161061T1 HR P20161061 T1 HRP20161061 T1 HR P20161061T1 HR P20161061T T HRP20161061T T HR P20161061TT HR P20161061 T HRP20161061 T HR P20161061T HR P20161061 T1 HRP20161061 T1 HR P20161061T1
- Authority
- HR
- Croatia
- Prior art keywords
- bibw
- amount
- compaction
- dimaleate
- image
- Prior art date
Links
- 239000007787 solid Substances 0.000 title claims 5
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 239000000203 mixture Substances 0.000 claims 17
- 239000000543 intermediate Substances 0.000 claims 11
- 238000005056 compaction Methods 0.000 claims 9
- 239000003826 tablet Substances 0.000 claims 9
- 238000009472 formulation Methods 0.000 claims 7
- USNRYVNRPYXCSP-JUGPPOIOSA-N afatinib dimaleate Chemical compound OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 USNRYVNRPYXCSP-JUGPPOIOSA-N 0.000 claims 6
- 239000004615 ingredient Substances 0.000 claims 5
- 239000000314 lubricant Substances 0.000 claims 5
- -1 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino }-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline-dimaleate Chemical compound 0.000 claims 3
- ULXXDDBFHOBEHA-ONEGZZNKSA-N Afatinib Chemical compound N1=CN=C2C=C(OC3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-ONEGZZNKSA-N 0.000 claims 3
- 239000011230 binding agent Substances 0.000 claims 3
- 239000007888 film coating Substances 0.000 claims 3
- 238000009501 film coating Methods 0.000 claims 3
- 239000008187 granular material Substances 0.000 claims 3
- 239000000843 powder Substances 0.000 claims 3
- 238000009490 roller compaction Methods 0.000 claims 3
- 239000011521 glass Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000004743 Polypropylene Substances 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 claims 1
- 229910052782 aluminium Inorganic materials 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 238000005266 casting Methods 0.000 claims 1
- 239000007910 chewable tablet Substances 0.000 claims 1
- 239000002274 desiccant Substances 0.000 claims 1
- 238000007907 direct compression Methods 0.000 claims 1
- 239000007919 dispersible tablet Substances 0.000 claims 1
- 238000009826 distribution Methods 0.000 claims 1
- 239000011888 foil Substances 0.000 claims 1
- 239000012458 free base Substances 0.000 claims 1
- 238000005469 granulation Methods 0.000 claims 1
- 230000003179 granulation Effects 0.000 claims 1
- 229920001903 high density polyethylene Polymers 0.000 claims 1
- 239000004700 high-density polyethylene Substances 0.000 claims 1
- 239000012943 hotmelt Substances 0.000 claims 1
- 239000007937 lozenge Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000463 material Substances 0.000 claims 1
- 238000007909 melt granulation Methods 0.000 claims 1
- 239000002808 molecular sieve Substances 0.000 claims 1
- 229920005787 opaque polymer Polymers 0.000 claims 1
- 239000007935 oral tablet Substances 0.000 claims 1
- 229940096978 oral tablet Drugs 0.000 claims 1
- 239000005022 packaging material Substances 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
- 229920001155 polypropylene Polymers 0.000 claims 1
- 229920001296 polysiloxane Polymers 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 238000007873 sieving Methods 0.000 claims 1
- 239000012748 slip agent Substances 0.000 claims 1
- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 claims 1
Classifications
-
- 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
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
- A61K9/143—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 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
- A61K9/14—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
-
- 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
- A61K9/1635—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
- A61K9/2013—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
- A61K9/2027—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
- A61K9/20—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
- A61K9/4891—Coated capsules; Multilayered drug free capsule shells
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
Claims (16)
1. Zbijeni intermedijer koji se sastoji od 4-[(3-kloro-4-fluorofenil)amino]-6-{[4-(N,N-dimetilamino)-1-okso-2-buten-1-il]amino}-7-((S)-tetrahidrofuran-3-iloksi)-kinazolin-dimaleata (BIBW 2992-dimaleata) u obliku praha koji se može dobiti pomoću faze zbijanja valjcima u kombinaciji s najmanje jednom fazom prosijavanja nakon zbijanja, opcijski u mješavini s lubrikantom u količini od 0 do 1,0 % koja se računa na količini od BIBW 2992-dimaleata po masi, naznačen time, da je rasprostranjenost veličine čestice od x10 < 200 μm, 1 μm < x50 < 300 μm, 75 μm < x90 < 600 μm.
2. Zbijeni intermedijer prema zahtjevu 1, naznačen time, da je gustoća rasutosti (ρp) u rasponu od 0,2 g/mL < ρp< 1,0 g/mL i/ili je Hausnerov faktor (HF) u rasponu od 1,00 < HF < 1,30, što se računa pomoću formule gustoća rasutosti/gustoća zbijenosti, pri čemu se gustoća rasutosti mjeri prema Ph.Eur.2.9.15 (Europska farmakopeja, 4. Izdanje) kao gustoća lijevanja i gustoća nabijenosti koje se mjere prema Ph.Eur.2.9.15.
3. Intermedijer ili konačna smjesa, naznačen/a time, da se pripravlja iz zbijenog intermedijera prema zahtjevu 1 ili 2.
4. Intermedijer ili konačna smjesa prema zahtjevu 3, naznačen/a time, da su sadržaji odabrani od sljedećih sastojaka od (a) do (g):
(a) zbijeni intermedijer od BIBW 2992-dimaleata u količini od 1 do 99 % po masi;
(b) opcijski jedan ili više nosača u količini od 10 do 99 % po masi;
(c) jedno ili više vezivnih sredstava u količini od 0 do 99 % po masi;
(d) jedno ili više kliznih sredstava u količini od 0 do 10 % po masi;
(e) jedan ili više dezintegratora u količini od 0 do 10 % po masi;
(f) jedan ili više lubrikanata u količini od 0 do 10 % po masi;
(g) dodatna pomoćna sredstva ili aditivi u količini od 0 do 10 % po masi, pri čemu prisutnost najmanje jednog od sastojaka od (b) do (g) je obavezan, ali je dopušteno također za dva do najviše svih šest od opcijskih sastojaka od (b) do (g) da budu prisutni kao dodatak sastojku (a) u intermedijeru i konačnoj smesi, a zbroj svih sastojaka dodaje se do 100 %.
5. Čvrste oralne formulacije spremne za uporabu/gutanje, naznačene time, da se pripravljaju iz zbijenog intermedijera od BIBW 2992-dimaleata prema bilo kojem od zahtjeva 1 ili 2 ili iz smjese intermedijera zahtjevu 3 ili 4.
6. Čvrste oralne formulacije prema zahtjevu 5, naznačene time, da su odabrane od praškova, granula, zrnaca, tableta, kapsula, tableta za žvakanje, tableta koje se raspršuju, okruglih tableta i tableta za sisanje.
7. Čvrsta oralna tableta prema zahtjevu 5, naznačena time, da se dobiva izravnom kompresijom konačne smjese prema zahtjevu 3 ili 4, ili tabletiranjem zrnaca ili granula koje se dobivaju konvencionalnom granulacijom, bilo vlažnom, suhom ili vruće-topljenom granulacijom smjese intermedijera prema zahtjevu 3 ili 4.
8. Tableta prema zahtjevu 7, naznačena time, da je navedena tableta neobložena ili je obložena primjerice film-oblogom.
9. Tableta prema zahtjevu 7 ili 8, naznačena time, da sadrži BIBW 2992 u količini od 1 do 150 mg (na osnovi slobodne baze).
10. Tableta prema zahtjevu 7, 8 ili 9, naznačena time, da sadrži BIBW 2992 od 1 do 150 mg, nosač, vezivo ili njihovu kombinaciju od 50 do 500 mg, klizno sredstvo od 0,1 do 5 mg, dezintegrator od 1 do 15 mg, i lubrikant od 1 do 15 mg.
11. Tableta prema zahtjevu 7, 8 ili 9, naznačena time, da sadrži BIBW 2992 od 20 do 70 mg, nosač, vezivo ili njihovu kombinaciju od 120 do 500 mg, klizno sredstvo od 0,5 do 5 mg, dezintegrator od 2,5 do 15 mg, i lubrikant od 2,5 do 15 mg.
12. Tableta prema zahtjevu 7, 8 ili 9, naznačena time, da je sastav odabran od sljedećih formulacija A, B, C, D i E:
[image]
[image]
koje su opcijski obložene s film-oblogom koja je naznačena time, da su odabrani sljedeći sastavi za formulacije A, B, C, D i E:
[image]
13. Tableta prema zahtjevu 7, 8 ili 9, naznačena time, da je sastav odabran od sljedećih formulacija F, G, H, I, J i K:
[image]
gdje su formulacije F, G i H opcijski obložene s film-oblogom koja je naznačena time, da su odabrani sljedeći sastavi:
[image]
[image]
14. Čvrsta formulacija prema bilo kojem od zahtjeva 5 do 13, naznačena time, da se pakira u PVC-blistere, PVDC-blistere ili u pakirni materijal otporan na vlagu kao što je blister pakiranje od aluminijske folije, alu/alu-blister, prozirni ili mutni polimerni blister s vrećicom, polipropilenske cijevi, obojani blister materijali, cjevčice, smeđe staklene bočice, staklene bočice i HDPE bočice koje opcijski sadrže svojstva za zaštitu djece, opcijski sadrže sredstvo za sušenje kao što je molekularno sito ili silikonski gel.
15. Postupak proizvodnje zbijenog intermedijera od 4-[(3-kloro-4-fluorofenil)amino]-6-{[4-(N,N-dimetilamino)-1-okso-2-buten-1-il]amino}-7-((S)-tetrahidrofuran-3-iloksi)-kinazolin-dimaleata (BIBW 2992-dimaleata) u obliku praha, naznačen time, da sadrži fazu zbijanja valjcima, u kombinaciji s najmanje jednom fazom prosijavanja, pri čemu se faza zbijanja provodi sa sljedećim:
- sam BIBW 2992-dimaleat, ili opcijski s
- predsmjesom od BIBW 2992-dimaleata s lubrikantom u količini od 0 do 1,0 % u miješalici sa slobodnim padom ili s prevrtanjem za sprečavanje velikog prianjanja valjaka za zbijanje.
16. Postupak prema zahtjevu 15, naznačen time, da se faza zbijanja valjcima provodi u uređaju za zbijanje s valjcima:
- opcijski s horizontalnim položajnim kutom, vertikalnim položajnim kutom ili s položajem valjaka za zbijanje pod pravim kutom,
- koji mogu biti glatki ili s oblicima na svojoj površini;
uporabom sile zbijanja koja varira:
-između 1 kN/cm i 20 kN/cm,
uz brzinu zbijanja valjaka za zbijanje:
- između 1 rpm i 30 rpm,
i sa širinom razmaka između valjaka za zbijanje:
- između 1 mm i 10 mm.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08157800 | 2008-06-06 | ||
| EP09160297 | 2009-05-14 | ||
| EP09757619.3A EP2299971B1 (en) | 2008-06-06 | 2009-06-05 | Solid pharmaceutical formulations comprising bibw 2992 |
| PCT/EP2009/056944 WO2009147238A1 (en) | 2008-06-06 | 2009-06-05 | Solid pharmaceutical formulations comprising bibw 2992 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20161061T1 true HRP20161061T1 (hr) | 2016-10-21 |
Family
ID=40941955
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20161061TT HRP20161061T1 (hr) | 2008-06-06 | 2016-08-21 | Čvrste farmaceutske formulacije koje sadrže bibw 2992 |
Country Status (34)
| Country | Link |
|---|---|
| US (1) | US8545884B2 (hr) |
| EP (1) | EP2299971B1 (hr) |
| JP (1) | JP5632367B2 (hr) |
| KR (1) | KR101641517B1 (hr) |
| CN (1) | CN102056589B (hr) |
| AR (1) | AR072062A1 (hr) |
| AU (1) | AU2009254574B2 (hr) |
| BR (1) | BRPI0913379C1 (hr) |
| CA (1) | CA2726472C (hr) |
| CL (1) | CL2010001275A1 (hr) |
| CO (1) | CO6280463A2 (hr) |
| CY (1) | CY1117895T1 (hr) |
| DK (1) | DK2299971T3 (hr) |
| EA (1) | EA022168B1 (hr) |
| EC (1) | ECSP10010650A (hr) |
| ES (1) | ES2588031T3 (hr) |
| HK (1) | HK1152478A1 (hr) |
| HR (1) | HRP20161061T1 (hr) |
| HU (1) | HUE029863T2 (hr) |
| IL (1) | IL209054A (hr) |
| MA (1) | MA34030B1 (hr) |
| ME (1) | ME02478B (hr) |
| MX (1) | MX2010012939A (hr) |
| MY (1) | MY151240A (hr) |
| NZ (1) | NZ589568A (hr) |
| PE (1) | PE20100252A1 (hr) |
| PL (1) | PL2299971T3 (hr) |
| PT (1) | PT2299971T (hr) |
| RS (1) | RS54943B1 (hr) |
| SI (1) | SI2299971T1 (hr) |
| TW (1) | TWI453203B (hr) |
| UY (1) | UY31867A (hr) |
| WO (1) | WO2009147238A1 (hr) |
| ZA (1) | ZA201007805B (hr) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1731511E (pt) | 1999-06-21 | 2015-11-13 | Boehringer Ingelheim Pharma | Heterociclos bicíclicos, medicamentos contendo estes compostos, a sua utilização e processos para a sua preparação |
| US7019012B2 (en) | 2000-12-20 | 2006-03-28 | Boehringer Ingelheim International Pharma Gmbh & Co. Kg | Quinazoline derivatives and pharmaceutical compositions containing them |
| DE10221018A1 (de) | 2002-05-11 | 2003-11-27 | Boehringer Ingelheim Pharma | Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie |
| US20050043233A1 (en) * | 2003-04-29 | 2005-02-24 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis |
| DE10349113A1 (de) | 2003-10-17 | 2005-05-12 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung von Aminocrotonylverbindungen |
| US20090306101A1 (en) * | 2005-11-11 | 2009-12-10 | Flavio Solca | Combination treatment of cancer comprising egfr/her2 inhibitors |
| JP5688877B2 (ja) * | 2005-11-11 | 2015-03-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 癌疾患の治療用キナゾリン誘導体 |
| JP5241513B2 (ja) * | 2006-01-26 | 2013-07-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | アミノクロトニルアミノ置換キナゾリン誘導体の合成方法 |
| SI2068880T1 (sl) | 2006-09-18 | 2012-08-31 | Boehringer Ingelheim Int | Postopek za zdravljenje raka, ki vsebuje mutacije EGFR |
| PE20100252A1 (es) | 2008-06-06 | 2010-04-12 | Boehringer Ingelheim Int | Nuevas formulaciones farmaceuticas solidas que comprenden dimaleato de 4-[(3-cloro-4-fluorofenil) amino]-6-{[4-(n,n-dimetilamino)-1-oxo-2-buten-1-il] amino}-7-((s)-tetrahidrofuran-3-iloxi)-quinazolina |
| LT2451445T (lt) * | 2009-07-06 | 2019-06-25 | Boehringer Ingelheim International Gmbh | Bibw2992, jo druskų ir kietų farmacinių kompozicijų, apimančių šį aktyvųjį ingredientą, džiovinimo būdas |
| EP2608792B1 (en) | 2010-08-26 | 2017-10-11 | Boehringer Ingelheim International GmbH | Methods of administering an egfr inhibitor |
| US8828391B2 (en) | 2011-05-17 | 2014-09-09 | Boehringer Ingelheim International Gmbh | Method for EGFR directed combination treatment of non-small cell lung cancer |
| US20150368230A1 (en) | 2013-02-01 | 2015-12-24 | Boehringer Ingelheim International Gmbh | Radiolabeled quinazoline derivatives |
| CN106279126B (zh) * | 2013-07-16 | 2019-05-24 | 杭州普晒医药科技有限公司 | 阿法替尼酸加成盐及其晶型、其制备方法及药物组合物 |
| US9242965B2 (en) | 2013-12-31 | 2016-01-26 | Boehringer Ingelheim International Gmbh | Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors |
| NO2699580T3 (hr) | 2014-01-24 | 2018-02-24 | ||
| CN105534920B (zh) * | 2014-10-29 | 2020-07-10 | 江苏豪森药业集团有限公司 | 一种药物组合物及其制备方法 |
| EP3023421A1 (en) | 2014-11-21 | 2016-05-25 | Sandoz Ag | Crystalline forms of afatinib dimaleate |
| CN105769804B (zh) * | 2014-12-23 | 2019-04-30 | 上海复星星泰医药科技有限公司 | 一种阿法替尼片及其制备方法 |
| CN105801568B (zh) | 2015-01-15 | 2019-07-30 | 杭州普晒医药科技有限公司 | 阿法替尼一马来酸盐晶型及其制备方法和药物组合物 |
| AU2016276426B2 (en) | 2015-06-12 | 2019-12-05 | Fresenius Kabi Oncology Ltd. | Polymorphic forms of Afatinib free base and Afatinib dimaleate |
| KR20180066039A (ko) * | 2015-08-21 | 2018-06-18 | 프레세니어스 카비 온콜로지 리미티드 | 아파티닙을 포함하는 약학적 조성물 |
| EP3156047A1 (en) * | 2015-10-12 | 2017-04-19 | Sandoz Ag | Afatinib-containing formulation |
| CN105456222B (zh) * | 2015-12-22 | 2019-03-26 | 河南润弘制药股份有限公司 | 马来酸阿法替尼片及其制备方法 |
| EP3260115A1 (en) * | 2016-06-21 | 2017-12-27 | Omya International AG | Method for the production of a dosage form |
| EP3260114A1 (en) * | 2016-06-21 | 2017-12-27 | Omya International AG | Method for the production of a dosage form |
| CN106074427A (zh) * | 2016-07-31 | 2016-11-09 | 合肥远志医药科技开发有限公司 | 一种马来酸阿法替尼片剂及其制备方法 |
| JP7265985B2 (ja) | 2016-11-17 | 2023-04-27 | ボード オブ リージェンツ，ザ ユニバーシティ オブ テキサス システム | Ｅｇｆｒまたはｈｅｒ２のエクソン２０変異を有するがん細胞に対する抗腫瘍活性を有する化合物 |
| MX2019008506A (es) * | 2017-01-24 | 2019-10-30 | Omnigen Res L L C | Suplemento de alimento granulado y metodos para elaboracion y uso. |
| EP3606916A1 (en) | 2017-04-06 | 2020-02-12 | Johnson Matthey Public Limited Company | Novel forms of afatinib dimaleate |
| WO2019070698A1 (en) | 2017-10-02 | 2019-04-11 | Johnson Matthey Public Limited Company | NEW FORMS OF IBRUTINIB |
| US20210369732A1 (en) * | 2018-03-01 | 2021-12-02 | Astrazeneca Ab | PHARMACEUTICAL COMPOSITIONS COMPRISING (2S)-N-{(1S)-1-CYANO-2-[4-(3-METHYL-2-OXO-2,3-DIHYDRO-1,3-BENZOXAZOL-5-yl)PHENYL]ETHYL}-1,4-OXAZEPANE-2-CARBOXAMIDE |
| WO2019195827A1 (en) | 2018-04-06 | 2019-10-10 | Johnson Matthey Public Limited Company | Novel form of ibrutinib |
| WO2019209908A1 (en) | 2018-04-25 | 2019-10-31 | Johnson Matthey Public Limited Company | Crystalline forms of dasatinib |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1731511E (pt) | 1999-06-21 | 2015-11-13 | Boehringer Ingelheim Pharma | Heterociclos bicíclicos, medicamentos contendo estes compostos, a sua utilização e processos para a sua preparação |
| US7019012B2 (en) | 2000-12-20 | 2006-03-28 | Boehringer Ingelheim International Pharma Gmbh & Co. Kg | Quinazoline derivatives and pharmaceutical compositions containing them |
| DE10063435A1 (de) | 2000-12-20 | 2002-07-04 | Boehringer Ingelheim Pharma | Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| US20030225079A1 (en) | 2002-05-11 | 2003-12-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy |
| DE10221018A1 (de) | 2002-05-11 | 2003-11-27 | Boehringer Ingelheim Pharma | Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie |
| US20050043233A1 (en) | 2003-04-29 | 2005-02-24 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis |
| DE10349113A1 (de) | 2003-10-17 | 2005-05-12 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung von Aminocrotonylverbindungen |
| US20060058311A1 (en) | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| JP5688877B2 (ja) | 2005-11-11 | 2015-03-25 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 癌疾患の治療用キナゾリン誘導体 |
| US20090306101A1 (en) | 2005-11-11 | 2009-12-10 | Flavio Solca | Combination treatment of cancer comprising egfr/her2 inhibitors |
| JP5241513B2 (ja) | 2006-01-26 | 2013-07-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | アミノクロトニルアミノ置換キナゾリン誘導体の合成方法 |
| US8338416B2 (en) * | 2006-03-16 | 2012-12-25 | Pharmacylics, Inc. | Indole derivatives as inhibitors of histone deacetylase |
| SI2068880T1 (sl) | 2006-09-18 | 2012-08-31 | Boehringer Ingelheim Int | Postopek za zdravljenje raka, ki vsebuje mutacije EGFR |
| PE20100252A1 (es) | 2008-06-06 | 2010-04-12 | Boehringer Ingelheim Int | Nuevas formulaciones farmaceuticas solidas que comprenden dimaleato de 4-[(3-cloro-4-fluorofenil) amino]-6-{[4-(n,n-dimetilamino)-1-oxo-2-buten-1-il] amino}-7-((s)-tetrahidrofuran-3-iloxi)-quinazolina |
| US20120157472A1 (en) | 2009-01-14 | 2012-06-21 | Boehringer Ingelheim International Gmbh | Method for treating colorectal cancer |
| LT2451445T (lt) | 2009-07-06 | 2019-06-25 | Boehringer Ingelheim International Gmbh | Bibw2992, jo druskų ir kietų farmacinių kompozicijų, apimančių šį aktyvųjį ingredientą, džiovinimo būdas |
| WO2011069962A1 (en) | 2009-12-07 | 2011-06-16 | Boehringer Ingelheim International Gmbh | Bibw 2992 for use in the treatment of triple negative breast cancer |
-
2009
- 2009-06-04 PE PE2009000775A patent/PE20100252A1/es active IP Right Grant
- 2009-06-04 UY UY0001031867A patent/UY31867A/es active IP Right Grant
- 2009-06-05 US US12/995,715 patent/US8545884B2/en active Active
- 2009-06-05 BR BRPI0913379A patent/BRPI0913379C1/pt active IP Right Grant
- 2009-06-05 TW TW098118819A patent/TWI453203B/zh active
- 2009-06-05 WO PCT/EP2009/056944 patent/WO2009147238A1/en active Application Filing
- 2009-06-05 NZ NZ589568A patent/NZ589568A/xx unknown
- 2009-06-05 AR ARP090102042A patent/AR072062A1/es unknown
- 2009-06-05 CA CA2726472A patent/CA2726472C/en active Active
- 2009-06-05 ES ES09757619.3T patent/ES2588031T3/es active Active
- 2009-06-05 HU HUE09757619A patent/HUE029863T2/en unknown
- 2009-06-05 EA EA201001852A patent/EA022168B1/ru active Protection Beyond IP Right Term
- 2009-06-05 DK DK09757619.3T patent/DK2299971T3/en active
- 2009-06-05 ME MEP-2016-138A patent/ME02478B/me unknown
- 2009-06-05 CN CN2009801210803A patent/CN102056589B/zh active Active
- 2009-06-05 MA MA33400A patent/MA34030B1/fr unknown
- 2009-06-05 AU AU2009254574A patent/AU2009254574B2/en active Active
- 2009-06-05 RS RS20160573A patent/RS54943B1/sr unknown
- 2009-06-05 KR KR1020107027340A patent/KR101641517B1/ko active IP Right Grant
- 2009-06-05 JP JP2011512146A patent/JP5632367B2/ja active Active
- 2009-06-05 EP EP09757619.3A patent/EP2299971B1/en active Active
- 2009-06-05 SI SI200931496A patent/SI2299971T1/sl unknown
- 2009-06-05 MX MX2010012939A patent/MX2010012939A/es active IP Right Grant
- 2009-06-05 PL PL09757619T patent/PL2299971T3/pl unknown
- 2009-06-05 MY MYPI20105644 patent/MY151240A/en unknown
- 2009-06-05 PT PT97576193T patent/PT2299971T/pt unknown
-
2010
- 2010-11-01 ZA ZA2010/07805A patent/ZA201007805B/en unknown
- 2010-11-01 IL IL209054A patent/IL209054A/en active IP Right Grant
- 2010-11-19 CL CL2010001275A patent/CL2010001275A1/es unknown
- 2010-12-01 EC EC2010010650A patent/ECSP10010650A/es unknown
- 2010-12-03 CO CO10152537A patent/CO6280463A2/es not_active Application Discontinuation
-
2011
- 2011-06-24 HK HK11106536.5A patent/HK1152478A1/xx unknown
-
2016
- 2016-08-10 CY CY20161100790T patent/CY1117895T1/el unknown
- 2016-08-21 HR HRP20161061TT patent/HRP20161061T1/hr unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| HRP20161061T1 (hr) | Čvrste farmaceutske formulacije koje sadrže bibw 2992 | |
| HRP20191104T1 (hr) | Pripravci koji sadrže lipofilne aktivne spojeve i postupak za njihovu pripremu | |
| KR20060003362A (ko) | 약물부하가 높은 메살라진 포 | |
| JP2022082823A (ja) | 医薬品 | |
| JP2022082822A (ja) | 医薬組成物 | |
| UA97349C2 (uk) | Стійкі тверді склади сертиндолу | |
| Bhattacharyya et al. | Formulation and evaluation of effervescent granules of Fexofenadine hydrochloride. | |
| Khan et al. | Formulation and evaluation of lumefantrine capsule prepared by using liquisolid technique | |
| Sutradhar et al. | Formulation and evaluation of taste masked oral dispersible tablets of domperidone using sublimation method | |
| MX2013002195A (es) | Agente de revestimiento para preparacion solida farmaceutica, formulacion de pelicula farmaceutica, y preparacion solida farmaceutica revestida. | |
| Jha et al. | Development of natural gum based fast disintegrating tablets of glipizide | |
| Jeganath et al. | Formulation and evaluation of non-effervescent floating tablets of linagliptin using low-density carriers. | |
| Ebere et al. | Comparative study of the functionality of povidone, gelatin and corn starch on Moringa oleifera leaf granule and capsule formulations | |
| Aggarwal et al. | Solubility and dissolution enhancement of poorly aqueous soluble drug atorvastatin calcium using modified gum karaya as carrier: In vitro-In vivo evaluation | |
| Reddy et al. | Formulation and evaluation of fast dissolving tablets of losartan potassium | |
| Laxmi et al. | Formulation and evaluation of aceclofenac matrix tablets using ethyl cellulose and cellulose acetate phthalate | |
| Bhargavi et al. | Formulation and Evaluation of Telmisartan Tablets Employing Solvent Deposited Systems | |
| Kalbhor et al. | DISSOLUATION ENHANCEMENT OF TELMISARTAN BY LIQUISOLID COMPACT | |
| Dasankoppa et al. | Application of SeDeM ODT expert system in formulation development of orodispersible tablets of antihyperlipidemic agent | |
| Sravanthi et al. | Formulation and evaluation of bi-layer floating tablets of amlodipine besylate and metoprolol succinate | |
| Messa et al. | Comparative studies for enhancement of the dissolution profile of pitavastatin | |
| Abd-Alaziz et al. | Enhancement of solubility and dissolution rate of poorly water-soluble domperidone by the formulation of multicomponent solid dispersions using solvent evaporation method | |
| Shailaja et al. | Formulation and In Vitro Evaluation of Gastro Retentive Delivery of Diltiazem Hydrochloride Using Natural Polymers | |
| Singh | FORMULATION DEVELOPMENT AND IN-VITRO EVALUATION OF NIZATIDINE GASTRORETENSIVE TABLET BY USING MELT GRANULATION TECHNIQUE | |
| Patil et al. | Preparation and evaluation of hollow microsphere drug delivery system of zidovudine |