AR072062A1 - Formulaciones farmaceuticas solidas que comprenden bibw 2992 - Google Patents
Formulaciones farmaceuticas solidas que comprenden bibw 2992Info
- Publication number
- AR072062A1 AR072062A1 ARP090102042A ARP090102042A AR072062A1 AR 072062 A1 AR072062 A1 AR 072062A1 AR P090102042 A ARP090102042 A AR P090102042A AR P090102042 A ARP090102042 A AR P090102042A AR 072062 A1 AR072062 A1 AR 072062A1
- Authority
- AR
- Argentina
- Prior art keywords
- bibw
- active substance
- immediate release
- dosage form
- pharmaceutical dosage
- Prior art date
Links
- 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 title abstract 3
- 239000007787 solid Substances 0.000 title abstract 3
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000013543 active substance Substances 0.000 abstract 6
- 239000002552 dosage form Substances 0.000 abstract 5
- 239000012729 immediate-release (IR) formulation Substances 0.000 abstract 5
- 239000000543 intermediate Substances 0.000 abstract 5
- 239000000203 mixture Substances 0.000 abstract 5
- USNRYVNRPYXCSP-JUGPPOIOSA-N afatinib dimaleate Chemical class 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 abstract 4
- 238000007907 direct compression Methods 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 238000004090 dissolution Methods 0.000 abstract 2
- 238000000338 in vitro Methods 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000003826 tablet Substances 0.000 abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 2
- 239000008186 active pharmaceutical agent Substances 0.000 abstract 1
- 239000012491 analyte Substances 0.000 abstract 1
- 230000001028 anti-proliverative effect Effects 0.000 abstract 1
- 239000011230 binding agent Substances 0.000 abstract 1
- 239000007963 capsule composition Substances 0.000 abstract 1
- 239000007884 disintegrant Substances 0.000 abstract 1
- 239000012738 dissolution medium Substances 0.000 abstract 1
- 239000007941 film coated tablet Substances 0.000 abstract 1
- 238000009472 formulation Methods 0.000 abstract 1
- 239000008187 granular material Substances 0.000 abstract 1
- 239000012943 hotmelt Substances 0.000 abstract 1
- 239000013067 intermediate product Substances 0.000 abstract 1
- 239000000314 lubricant Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000000771 oncological effect Effects 0.000 abstract 1
- 239000007935 oral tablet Substances 0.000 abstract 1
- 229940096978 oral tablet Drugs 0.000 abstract 1
- 239000000843 powder Substances 0.000 abstract 1
- 238000009490 roller compaction Methods 0.000 abstract 1
- 238000007873 sieving Methods 0.000 abstract 1
- 238000003756 stirring Methods 0.000 abstract 1
- 239000007916 tablet composition Substances 0.000 abstract 1
- 238000005550 wet granulation Methods 0.000 abstract 1
Classifications
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- 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
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Inorganic Chemistry (AREA)
- Gastroenterology & Hepatology (AREA)
- Pulmonology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Una forma de dosificacion farmaceutica que contiene la sustancia activa BIBW 2992 en forma de la sal dimaleato, que proporciona un perfil de liberacion inmediata de la sustancia activa, la presente se refiere a productos intermedios compactados que comprenden sal dimaleato de BIBW 2992 (BIBW2992 MA2) en forma de un polvo preparado al utilizar una etapa de compactacion por rodillos y de tamizado combinada a partir de BIBW 2992 MA2, a mezclas intermedias preparadas a partir de dicho producto intermedio compactado, as¡ como en forma de formulaciones orales solidas que proporcionan un perfil de liberacion inmediata de la sustancia activa, hechas a partir de dicho producto intermedio compactado o a partir de dichas mezclas intermedias listas para su uso/ingesta, p. ej. formulaciones de c psula y comprimido, tales como comprimidos no revestidos o revestidos con pel¡cula preparados mediante compresion directa, y a metodos para su produccion. Reivindicacion 1: Forma de dosificacion farmaceutica de la sustancia activa BIBW 2992 MA2 (sal del API), caracterizada porque proporciona un perfil de disolucion de liberacion inmediata a lo largo del intervalo de pH fisiologicamente relevante de pH 1 - 6,8 y agua, en donde no menos de 85% (Q = 80%) se disuelve en el espacio de 60 minutos o menos in vitro under bajo las siguientes condiciones de disolucion in vitro de acuerdo con la Farmacopea Europea 6.2: aparato 2 (paletas), 900 mL de medio de disolucion de pH 1 - 6,8 o agua, y una velocidad de agitacion de 50 a 150 rpm, preferiblemente 50 o 75 rpm, a una temperatura de 37sC. Reivindicacion 4: Forma de dosificacion farmaceutica de acuerdo con cualquiera de las reivindicaciones 1 a 3, caracterizada porque proporciona un perfil de liberacion inmediata, en la que la concentracion m xima de la sustancia activa en plasma en estado estacionario (Cmax,ss) aumenta de una manera proporcional a la dosis. Reivindicacion 5: Forma de dosificacion farmaceutica de acuerdo con cualquiera de las reivindicaciones 1 a 4, caracterizada porque proporciona un perfil de liberacion inmediata, en la que el rea bajo la curva de concentracion en plasma-tiempo del analito/sustancia activa en plasma en estado estacionario a lo largo de un intervalo de dosificacion t (AUCt,ss) aumenta de una manera proporcional en la dosis. Reivindicacion 13: Forma de dosificacion farmaceutica de acuerdo con la reivindicacion 11 o 12, para uso como una composicion farmaceutica con una actividad antiproliferativa, preferiblemente para el tratamiento de una enfermedad o estado seleccionado de enfermedades oncologicas. Reivindicacion 24: Comprimido oral solido de acuerdo con la reivindicacion 22, caracterizado por ser obtenido mediante compresion directa de una mezcla final de acuerdo con la reivindicacion 20 o 21 o mediante formacion de comprimidos de nodulos o gr nulos obtenidos mediante granulacion en humedo, en seco o en masa fundida caliente, convencional, de una mezcla intermedia de acuerdo con la reivindicacion 20 o 21. Reivindicacion 27: El comprimido de la reivindicacion 24, 25 o 26, caracterizado porque comprende 1 a 150 mg de BIBW 2992, 50 a 500 mg de soporte, aglutinante o una combinacion de los mismos, 0.1 a 5 mg de un deslizante, 1 a 15 mg de un desintegrante, y 1 a 15 mg de un lubricante.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08157800 | 2008-06-06 | ||
| EP09160297 | 2009-05-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR072062A1 true AR072062A1 (es) | 2010-08-04 |
Family
ID=40941955
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP090102042A AR072062A1 (es) | 2008-06-06 | 2009-06-05 | Formulaciones farmaceuticas solidas que comprenden bibw 2992 |
Country Status (33)
| Country | Link |
|---|---|
| US (1) | US8545884B2 (es) |
| EP (1) | EP2299971B1 (es) |
| JP (1) | JP5632367B2 (es) |
| KR (1) | KR101641517B1 (es) |
| CN (1) | CN102056589B (es) |
| AR (1) | AR072062A1 (es) |
| AU (1) | AU2009254574B2 (es) |
| BR (1) | BRPI0913379C1 (es) |
| CA (1) | CA2726472C (es) |
| CL (1) | CL2010001275A1 (es) |
| CO (1) | CO6280463A2 (es) |
| CY (1) | CY1117895T1 (es) |
| DK (1) | DK2299971T3 (es) |
| EA (1) | EA022168B1 (es) |
| EC (1) | ECSP10010650A (es) |
| ES (1) | ES2588031T3 (es) |
| HR (1) | HRP20161061T1 (es) |
| HU (1) | HUE029863T2 (es) |
| IL (1) | IL209054A (es) |
| MA (1) | MA34030B1 (es) |
| ME (1) | ME02478B (es) |
| MX (1) | MX2010012939A (es) |
| MY (1) | MY151240A (es) |
| NZ (1) | NZ589568A (es) |
| PE (1) | PE20100252A1 (es) |
| PL (1) | PL2299971T3 (es) |
| PT (1) | PT2299971T (es) |
| RS (1) | RS54943B1 (es) |
| SI (1) | SI2299971T1 (es) |
| TW (1) | TWI453203B (es) |
| UY (1) | UY31867A (es) |
| WO (1) | WO2009147238A1 (es) |
| ZA (1) | ZA201007805B (es) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MEP45508A (en) | 1999-06-21 | 2011-02-10 | Boehringer Ingelheim Pharma | Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof |
| 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 |
| DK1948180T3 (da) * | 2005-11-11 | 2013-05-27 | Boehringer Ingelheim Int | Kombinationsbehandling af cancer omfattende EGFR/HER2 inhibitorer |
| WO2007054550A1 (en) * | 2005-11-11 | 2007-05-18 | Boehringer Ingelheim International Gmbh | Quinazoline derivatives for the treatment of cancer diseases |
| EP1981863B1 (en) * | 2006-01-26 | 2012-10-10 | Boehringer Ingelheim International GmbH | Process for preparing aminocrotonylamino-substituted quinazoline derivatives |
| NZ576065A (en) * | 2006-09-18 | 2011-12-22 | Boehringer Ingelheim Int | Method for treating cancer harboring egfr mutations |
| UY31867A (es) | 2008-06-06 | 2010-01-29 | Boehringer Ingelheim Int | Nuevas formulaciones farmacéuticas sólidas que comprenden bibw 2992 |
| PT2451445T (pt) | 2009-07-06 | 2019-07-10 | Boehringer Ingelheim Int | Processo para secagem de bibw2992, dos seus sais e de formulações farmacêuticas sólidas compreendendo este ingrediente ativo |
| NO2608792T3 (es) | 2010-08-26 | 2018-03-10 | ||
| 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 |
| WO2015007206A1 (zh) * | 2013-07-16 | 2015-01-22 | 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 (es) | 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 |
| US10525059B2 (en) * | 2015-08-21 | 2020-01-07 | Fresenius Kabi Oncology, Ltd. | Pharmaceutical compositions comprising Afatinib |
| 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 |
| US11446302B2 (en) | 2016-11-17 | 2022-09-20 | Board Of Regents, The University Of Texas System | Compounds with anti-tumor activity against cancer cells bearing EGFR or HER2 exon 20 mutations |
| WO2018140450A1 (en) * | 2017-01-24 | 2018-08-02 | Costigan Timothy E | Granulated feed supplement and methods for making and using |
| WO2018187643A1 (en) | 2017-04-06 | 2018-10-11 | Johnson Matthey Public Limited Company | Novel forms of afatinib dimaleate |
| WO2019070698A1 (en) | 2017-10-02 | 2019-04-11 | Johnson Matthey Public Limited Company | Novel forms of ibrutinib |
| CN112055593B (zh) | 2018-03-01 | 2024-04-09 | 阿斯利康(瑞典)有限公司 | 药物组合物 |
| 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 |
| EP3823627A4 (en) | 2018-07-17 | 2022-04-20 | Insmed Incorporated | CERTAIN (2S)-N-[(1S)-1-CYANO-2-PHENYLETHYL]-1,4-OXAZEPANE-2-CARBOXAMIDES FOR THE TREATMENT OF LUPUS ENEHROPATHY |
| AU2024206233A1 (en) | 2023-01-06 | 2025-08-21 | Insmed Incorporated | Novel, reversible dpp1 inhibitors and uses thereof |
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| MEP45508A (en) * | 1999-06-21 | 2011-02-10 | Boehringer Ingelheim Pharma | Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof |
| 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 |
| WO2007054550A1 (en) * | 2005-11-11 | 2007-05-18 | Boehringer Ingelheim International Gmbh | Quinazoline derivatives for the treatment of cancer diseases |
| DK1948180T3 (da) * | 2005-11-11 | 2013-05-27 | Boehringer Ingelheim Int | Kombinationsbehandling af cancer omfattende EGFR/HER2 inhibitorer |
| EP1981863B1 (en) * | 2006-01-26 | 2012-10-10 | Boehringer Ingelheim International GmbH | Process for preparing aminocrotonylamino-substituted quinazoline derivatives |
| US8338416B2 (en) * | 2006-03-16 | 2012-12-25 | Pharmacylics, Inc. | Indole derivatives as inhibitors of histone deacetylase |
| NZ576065A (en) * | 2006-09-18 | 2011-12-22 | Boehringer Ingelheim Int | Method for treating cancer harboring egfr mutations |
| UY31867A (es) | 2008-06-06 | 2010-01-29 | Boehringer Ingelheim Int | Nuevas formulaciones farmacéuticas sólidas que comprenden bibw 2992 |
| US20120157472A1 (en) * | 2009-01-14 | 2012-06-21 | Boehringer Ingelheim International Gmbh | Method for treating colorectal cancer |
| PT2451445T (pt) | 2009-07-06 | 2019-07-10 | Boehringer Ingelheim Int | Processo para secagem de bibw2992, dos seus sais e de formulações farmacêuticas sólidas compreendendo este ingrediente ativo |
| EP2509592A1 (en) | 2009-12-07 | 2012-10-17 | Boehringer Ingelheim International GmbH | Bibw 2992 for use in the treatment of triple negative breast cancer |
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