DK2563763T3 - Farmaceutiske sammensætninger, der omfatter n-(4-(2-amino-3-chlorpyridin- 4-yloxy)-3-fluorphenyl)-4-ethoxy-1-(4-fluorphenyl)-2-oxo-1,2-dihydropyridin- 3-carboxamid - Google Patents

Farmaceutiske sammensætninger, der omfatter n-(4-(2-amino-3-chlorpyridin- 4-yloxy)-3-fluorphenyl)-4-ethoxy-1-(4-fluorphenyl)-2-oxo-1,2-dihydropyridin- 3-carboxamid Download PDF

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Publication number
DK2563763T3
DK2563763T3 DK11717917.6T DK11717917T DK2563763T3 DK 2563763 T3 DK2563763 T3 DK 2563763T3 DK 11717917 T DK11717917 T DK 11717917T DK 2563763 T3 DK2563763 T3 DK 2563763T3
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Denmark
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compound
cancer
particles
weight
pxrd pattern
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DK11717917.6T
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English (en)
Inventor
Dilbir S Bindra
Madhushree Yeshwant Gokhale
Cletus John Nunes
Victor W Rosso
Gretchen M Schroeder
Ajit B Thakur
Xiaotian Yin
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Bristol Myers Squibb Co
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Publication of DK2563763T3 publication Critical patent/DK2563763T3/da

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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (7)

  1. FARMACEUTISKE SAMMENSÆTNINGER, DER OMFATTER N-(4-(2-AMINO-3-CHLORPYRIDIN-4-YLOXY)-3-FLUORPHENYL)-4-ETHOXY-l-(4-FLUORPHENYL)-2-OXO-l,2-DIHYDROPYRIDIN-
  2. 3-CARBOXAMID
    1. Farmaceutisk sammensætning, der omfatter (i) partikler af forbindelsen (I) i formen N-l
    (ii) stabilisator; og (iii) mindst én farmaceutisk acceptabel bærer og/eller fortynder; hvor partiklerne har en diameter (D90), der ligger i intervallet fra 1 til 50 uro, og stabilisatoren anbringes på partiklerne; hvor stabilisatoren er en celluloseetherpolymer; hvor formen N-l er kendetegnet ved et af de følgende: a) et simuleret pulverrøntgendiffraktionsmønster (PXRD) i alt væsentligt som vist i figur 1, og/eller et observeret PXRD-mønster i alt væsentligt som vist i figur 1; b) et PXRD-mønster, der omfatter fire eller flere 2Θ værdier (CuKa λ =1,5418 A) udvalgt fra: 6,2±0,2; 7,7±0,2; 11,0±0,2; 12,2±0,2; 18,5±0,2; 21,6±0,2; 22,2±0,2; og 23,0±0,2, hvor PXRD-mønsteret af form N-l måles ved en temperatur på omkring 25 °C; c) et PXRD-mønster, der omfatter fem eller flere 2Θ værdier (CuKa λ = 1,5418 A) udvalgt fra: 6,2±0,2; 7,7±0,2; 11,0±0,2; 12,2±0,2; 18,5±0,2; 21,6±0,2; 22,2±0,2; og 23,0+0,2, hvor PXRD-mønsteret af form N-l måles ved en temperatur på omkring 25 °C; d) enhedscelleparametre i alt væsentligt lig med følgende: celledimensioner: a =14,45 Å b = 19,21 Å c = 8,89 Å α = 90,0° β = 95,7° γ = 90,0° rumgruppe: P2!/c molekyler af forbindelse (I)/asymmetrisk enhed: 1 hvor enhedscelleparametrene af form N-l måles ved en temperatur på omkring 25 °C; e) enhedscelleparametre i alt væsentligt lig med følgende: celledimensioner: a= 14,43 Å b= 19,17 Å c = 8,83 Å α = 90,0° β = 95,4° γ = 90,0° rumgruppe: P2i/c molekyler af forbindelse (l)/asymmetrisk enhed: 1 hvor enhedscelleparametrene af form N-l måles ved en temperatur på omkring -30 °C; og/eller f) et smeltepunkt, der ligger i intervallet fra omkring 211 °C til omkring 217 °C.
    2. Farmaceutisk sammensætning ifølge krav 1, hvor formen N-l er kendetegnet ved ét eller flere af følgende: a) simuleret PXRD-mønster i alt væsentligt som vist i figur 1 og/eller et observeret PXRD-mønster i alt væsentligt som vist i figur 1; b) et PXRD-mønster, der omfatter fire eller flere 2Θ værdier (CuKa λ=1,5418 A) udvalgt fra: 6,2+0,2; 7,7+0,2; 11,0±0,2; 12,2±0,2; 18,5±0,2; 21,6±0,2; 22,2±0,2; og 23,0±0,2, hvor PXRD-mønsteret af form N-l måles ved en temperatur på omkring 25 °C; og/eller c) et PXRD-mønster, der omfatter fem eller flere 2Θ værdier (CuKa λ=1,5418 A) udvalgt fra: 6,2+0,2; 7,7+0,2; 11,0±0,2; 12,2±0,2; 18,5±0,2; 21,6±0,2; 22,2±0,2; og 23,0±0,2, hvor PXRD-mønsteret af form N-l måles ved en temperatur på omkring 25 °C.
    3. Farmaceutisk sammensætning ifølge krav 1, hvor fortynderen er et vandigt medium; og partiklerne af forbindelse (I) i formen N-l dispergeres i det vandige medium.
  3. 4. Farmaceutisk sammensætning ifølge krav 3, der endvidere omfatter: a) fra 0,1 til 5 % (vægt/volumen) celluloseetherpolymer, der er udvalgt fra hydroxypropylcellulose, hydroxypropylmethylcellulose og methylcellulose; b) fra 0,1 til 5 % (vægt/volumen) mikrokrystallinsk cellulose; c) fra 0,01 til 2 % (vægt/volumen) sorbitanester, natriumlaurylsulfat, dodecylsulfat og/eller polyoxyethylen-polyoxypropylen-polyoxyethylenblokcopolymer; d) fra 1 til 40 % (vægt/volumen) sødemiddel; og fra 48 til 98,7% (vægt/volumen) vandigt medium.
  4. 5. Farmaceutisk sammensætning ifølge krav 1, hvor den farmaceutiske sammensætning er en fast oral doseringsform, der omfatter: (i) fra 10 til 40 vægt-% partikler af forbindelse (I) af formen N-l; (ii) fra 2 til 11 vægt-% disintegrationsmiddel; (iii) fra 1 til 7 vægt-% stabilisator; (iv) fra 50 til 86 vægt-% fyldemiddel; (v) 0,1 to 1,1 vægt-% smøremiddel; og (vi) fra 0,1 til 0,7 vægt-% glidemiddel, baseret på tablettens samlede vægt.
  5. 6. Farmaceutisk sammensætning ifølge krav 5, hvor stabilisatoren er en celluloseetherpolymer, der er udvalgt fra hydroxypropylcellulose, hydroxypropylmethylcellulose og methylcellulose.
  6. 7. Forbindelse (I)
    D til anvendelse i behandling af cancer, hvor forbindelsen (I) tilvejebringes som partikler af den krystallinske form N-l som defineret ifølge krav 1, og partiklerne har en diameter (D90), der ligger i intervallet fra 1 til 30 μιτι.
  7. 8. Forbindelse til anvendelse ifølge krav 7, hvor canceren er blærecancer, brystcancer, kolorektal cancer, gastrisk cancer, cancer i hoved eller hals, nyrecancer, levercancer, lungecancer, cancer i æggestokkene, pancreas/galdeblærecancer, prostatacancer, cancer i skjoldbruskkirtelen, osteosarkom, rhabdomyosarkom, melanom, glioblastom/astrocytom, MFH/fibrosarkom eller mesotheliom.
DK11717917.6T 2010-04-30 2011-04-29 Farmaceutiske sammensætninger, der omfatter n-(4-(2-amino-3-chlorpyridin- 4-yloxy)-3-fluorphenyl)-4-ethoxy-1-(4-fluorphenyl)-2-oxo-1,2-dihydropyridin- 3-carboxamid DK2563763T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32971010P 2010-04-30 2010-04-30
PCT/US2011/034417 WO2011137274A1 (en) 2010-04-30 2011-04-29 Pharmaceutical compositions comprising n-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-l-(4-fluorophenyl)-2-oxo- 1,2-dihydropyridine-3 -carboxamide

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US (2) US8911785B2 (da)
EP (1) EP2563763B1 (da)
JP (1) JP5820874B2 (da)
KR (1) KR101897302B1 (da)
CN (1) CN102971296B (da)
DK (1) DK2563763T3 (da)
ES (1) ES2533075T3 (da)
HK (1) HK1179260A1 (da)
HR (1) HRP20150105T1 (da)
MY (1) MY183769A (da)
PL (1) PL2563763T3 (da)
PT (1) PT2563763E (da)
RS (1) RS53790B1 (da)
SG (1) SG184891A1 (da)
SI (1) SI2563763T1 (da)
SM (1) SMT201500069B (da)
WO (1) WO2011137274A1 (da)

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WO2013096858A1 (en) 2011-12-22 2013-06-27 Life Technologies Corporation Cell culture media and methods
KR101545268B1 (ko) 2015-02-05 2015-08-20 보령제약 주식회사 정제 및 이의 제조방법
WO2016126012A1 (en) * 2015-02-05 2016-08-11 Boryung Pharmaceutical Co., Ltd Tablet and method of preparing the same
WO2020150307A1 (en) * 2019-01-15 2020-07-23 The Translational Genomics Research Institute Phosphonate conjugates and uses thereof
US20230257364A1 (en) * 2022-02-16 2023-08-17 Cmg Pharmaceutical Co., Ltd. Pyridazinone-based compounds as axl, c-met, and mer inhibitors and methods of use thereof

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US6214344B1 (en) 1995-06-02 2001-04-10 Genetech, Inc. Hepatocyte growth factor receptor antagonists and uses thereof
ID21762A (id) * 1996-09-24 1999-07-22 Lilly Co Eli Formulasi partikel bersaput
US7459562B2 (en) 2004-04-23 2008-12-02 Bristol-Myers Squibb Company Monocyclic heterocycles as kinase inhibitors
WO2006118210A1 (ja) * 2005-04-28 2006-11-09 Eisai R & D Management Co., Ltd. ジヒドロピリジン系化合物の分解を防止する方法
TR200504775A1 (tr) 2005-11-30 2007-10-22 Esen Beki̇r Kendinden metal takviyeli pvc pencere ve kapı profilleri
US8865722B2 (en) * 2006-01-05 2014-10-21 Teva Pharmaceutical Industries Ltd. Wet formulations of aripiprazole
PL2089364T3 (pl) * 2006-11-08 2013-11-29 Bristol Myers Squibb Co Związki pirydynonu
US20080260837A1 (en) * 2007-04-20 2008-10-23 Qpharma, L.L.C. Physically stable aqueous suspensions of active pharmaceuticals
US8263652B2 (en) * 2007-10-31 2012-09-11 Sk Biopharmaceuticals Co., Ltd. Stabilized pediatric suspension of carisbamate
ES2531396T3 (es) 2008-01-23 2015-03-13 Bristol Myers Squibb Co Proceso para preparar compuestos de piridinona

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AU2011245269A1 (en) 2012-12-20
US20130039989A1 (en) 2013-02-14
MY183769A (en) 2021-03-12
KR101897302B1 (ko) 2018-09-11
CN102971296B (zh) 2015-11-25
WO2011137274A1 (en) 2011-11-03
KR20130100237A (ko) 2013-09-10
PT2563763E (pt) 2015-03-31
US8911785B2 (en) 2014-12-16
EP2563763B1 (en) 2014-12-31
RS53790B1 (en) 2015-06-30
ES2533075T3 (es) 2015-04-07
SMT201500069B (it) 2015-05-05
CN102971296A (zh) 2013-03-13
SI2563763T1 (sl) 2015-03-31
EP2563763A1 (en) 2013-03-06
HRP20150105T1 (hr) 2015-03-13
PL2563763T3 (pl) 2015-06-30
SG184891A1 (en) 2012-11-29
HK1179260A1 (en) 2013-09-27
JP5820874B2 (ja) 2015-11-24
US20150065719A1 (en) 2015-03-05
JP2013525455A (ja) 2013-06-20
US9233948B2 (en) 2016-01-12

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