HRP20171578T1 - Čvrsta disperzija - Google Patents

Čvrsta disperzija Download PDF

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Publication number
HRP20171578T1
HRP20171578T1 HRP20171578TT HRP20171578T HRP20171578T1 HR P20171578 T1 HRP20171578 T1 HR P20171578T1 HR P20171578T T HRP20171578T T HR P20171578TT HR P20171578 T HRP20171578 T HR P20171578T HR P20171578 T1 HRP20171578 T1 HR P20171578T1
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Croatia
Prior art keywords
solid dispersion
methyl
cellulose
weight
hydroxypropyl
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HRP20171578TT
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English (en)
Inventor
David Shank FRY
Christopher M. Lindemann
Michael PREIGH
Corey Jay BLOOM
Christopher Donovan Craig
Devon Brevard DUBOSE
Jeff GAUTSCHI
Dan SMITHEY
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Array Biopharma, Inc.
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Publication of HRP20171578T1 publication Critical patent/HRP20171578T1/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/498Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Glass Compositions (AREA)
  • Inorganic Insulating Materials (AREA)
  • Optical Communication System (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (15)

1. Čvrsta disperzija, naznačena time što sadrži N4-(4-([1,2,4]triazolo[1,5-a]piridin-7-iloksi)-3-metilfenil)-N6-(4,4-dimetil-4,5-dihidrooksazol-2-il)kinazolin-4,6-diamin i disperzijski polimer.
2. Čvrsta disperzija u skladu s patentnim zahtjevom 1, naznačena time što sadrži amorfni N4-(4-([1,2,4]triazolo[1,5-a]piridin-7-iloksi)-3-metilfenil)-N6-(4,4-dimetil-4,5-dihidrooksazol-2-il)kinazolin-4,6-diamin.
3. Čvrsta disperzija prema patentnim zahtjevima 1 ili 2, naznačena time što se disperzijski polimer bira između vinilnih polimera i kopolimera, PVP-VA, polivinil-alkohola, polivinil-alkoholno-polivinil-acetatnih kopolimera, PVP, akrilatnih i metakrilatnih kopolimera, metilakrilnokiselinski-metil-metakrilatnog kopolimera, polietilenski-polivinil-alkoholnih kopolimera, polioksietilensko-polioksipropilenskih blok kopolimera, nakalamljenog kopolimera, koji se sastoji od polietilen-glikola, polivinilkaprolaktama i polivinil-acetata, celuloznih polimera, poput hidroksipropil(metil)celuloznog acetata, hidroksipropil(metil)celuloze, hidroksipropilceluloze, metilceluloze, hidroksietil(metil)celuloze, hidroksietilceluloze, hidroksietilceluloznog acetata, te hidroksietil(etil)celuloze, hidroksipropil(metil)celuloznog acetat-sukcinata, hidroksipropil(metil)celuloznog ftalata, karboksimetiletilceluloze, celuloznog acetat-ftalata, celuloznog acetat-sukcinata, hidroksipropil(metil)celuloznog acetat-ftalata, celuloznog acetat-trimelitata, hidroksipropil(metil)celuloznog acetat-trimelitata, te karboksimetilceluloznog acetat-butirata.
4. Čvrsta disperzija u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačena time što je disperzijski polimer metilakrilnokiselinski-metil-metakrilatni kopolimer.
5. Čvrsta disperzija u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačena time što je disperzijski polimer hidroksipropilmetilcelulozni ftalat.
6. Čvrsta disperzija u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačena time što je disperzijski polimer celulozni acetat-ftalat.
7. Čvrsta disperzija u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačena time što se disperzijski polimer bira između vinilpirolidin-vinilacetatnog kopolimera i hidroksipropil(metil)celuloze, ili njihovih smjesa.
8. Čvrsta disperzija u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačena time što je disperzijski polimer vinilpirolidin-vinilacetatni kopolimer.
9. Čvrsta disperzija u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačena time što je disperzijski polimer hidroksipropil(metil)celuloza.
10. Čvrsta disperzija u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačena time što je N4-(4-([1,2,4]triazolo[1,5-a]piridin-7-iloksi)-3-metil-fenil)-N6-(4,4-dimetil-4,5-dihidrooksazol-2-il)kinazolin-4,6-diamin prisutan u količini od otprilike 0,1% do otprilike 50%, težinski, u odnosu na disperzijski polimer.
11. Čvrsta disperzija u skladu s bilo kojim od patentnih zahtjeva 1 do 10, naznačena time što je najmanje 80% N4-(4-([1,2,4]triazolo[1,5-a]piridin-7-iloksi)-3-metilfenil)-N6-(4,4-dimetil-4,5-dihidrooksazol-2-il)kinazolin-4,6-diamina u amorfnom obliku.
12. Čvrsta disperzija u skladu s patentnim zahtjevom 11, naznačena time što je najmanje 95% N4-(4-([1,2,4]triazolo[1,5-a]piridin-7-iloksi)-3-metilfenil)-N6-(4,4-dimetil-4,5-dihidrooksazol-2-il)kinazolin-4,6-diamina u amorfnom obliku.
13. Farmaceutski pripravak, naznačen time što sadrži čvrstu disperziju u skladu s bilo kojim od patentnih zahtjeva 1 do 12, kao i jednu ili više farmaceutski prihvatljivih pomoćnih tvari.
14. Farmaceutski pripravak u skladu s patentnim zahtjevom 13, naznačena time što pripravak je tableta.
15. Farmaceutski pripravak u skladu s patentnim zahtjevom 13, naznačen time što sadrži: (a) otprilike 1 do otprilike 70%, težinski, čvrste disperzije u skladu s bilo kojim od patentnih zahtjeva 1 do 12; (b) otprilike 0,1 do 20%, težinski, sredstva za raspadanje; (c) otprilike 0,1 do 25%, težinski, osmogena; (d) otprilike 0,1 do 10%, težinski, sredstva za kliženje; (e) otprilike 0,1 do 10%, težinski, maziva; i (f) otprilike 0,1 do 25%, težinski, veziva. 1. Farmaceutski pripravak u skladu s patentnim zahtjevom 13, naznačen time što sadrži: (a) N4-(4-([1,2,4]triazolo[1,5-a]piridin-7-iloksi)-3-metilfenil)-N6-(4,4-dimetil-4,5-dihidrooksazol-2-il)kinazolin-4,6-diamin; i (b) natrijev bikarbonat. 2. Farmaceutski pripravak u skladu s patentnim zahtjevom 16, naznačen time što sadrži: (a) otprilike 1 do otprilike 70%, težinski, čvrste disperzije u skladu s bilo kojim od patentnih zahtjeva 1 do 12; i (b) otprilike 0,1 do otprilike 30%, težinski, natrijevog bikarbonata. 3. Farmaceutski pripravak u skladu s bilo kojim od patentnih zahtjeva 13 do 17, naznačen time što čvrsta disperzija je otprilike 25 do otprilike 60%-tna, težinski. 4. Čvrsta disperzija u skladu s bilo kojim od patentnih zahtjeva 1 do 18, naznačena time što je namijenjena upotrebi u liječenju bolesti. 5. Čvrsta disperzija, namijenjena upotrebi u skladu s patentnim zahtjevom 19, naznačena time što je bolest rak. 6. Čvrsta disperzija, namijenjena upotrebi u skladu s patentnim zahtjevom 20, naznačena time što se rak bira između raka dojke, želuca, žučovoda, kolorektalnog raka, pluća, velikih stanica pluća, gušterače, glave i vrata, jajnika, maternice i raka na mozgu. 7. Čvrsta disperzija, namijenjena upotrebi u skladu s patentnim zahtjevima 20 ili 21, naznačena time što je rak pozitivan na ErbB2.
HRP20171578TT 2011-10-14 2017-10-17 Čvrsta disperzija HRP20171578T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161547620P 2011-10-14 2011-10-14
US201261606207P 2012-03-02 2012-03-02
PCT/US2012/060044 WO2013056108A2 (en) 2011-10-14 2012-10-12 Solid dispersion
EP12809373.9A EP2765990B1 (en) 2011-10-14 2012-10-12 Solid dispersion

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HRP20171578T1 true HRP20171578T1 (hr) 2017-12-01

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US (5) US9457093B2 (hr)
EP (1) EP2765990B1 (hr)
JP (2) JP5944514B2 (hr)
KR (1) KR102000312B1 (hr)
CN (3) CN114886853A (hr)
AU (3) AU2012322039C1 (hr)
BR (2) BR122020010643B1 (hr)
CA (2) CA2852058C (hr)
CL (1) CL2014000930A1 (hr)
CO (1) CO6960547A2 (hr)
CR (1) CR20140228A (hr)
CY (1) CY1119837T1 (hr)
DK (1) DK2765990T3 (hr)
ES (1) ES2650608T3 (hr)
HR (1) HRP20171578T1 (hr)
HU (1) HUE035247T2 (hr)
IL (1) IL232103B (hr)
LT (1) LT2765990T (hr)
ME (1) ME02913B (hr)
MX (1) MX353970B (hr)
MY (1) MY169072A (hr)
NO (1) NO2021029I1 (hr)
PL (1) PL2765990T3 (hr)
PT (1) PT2765990T (hr)
RS (1) RS56608B1 (hr)
RU (1) RU2648448C2 (hr)
SG (1) SG11201401459YA (hr)
SI (1) SI2765990T1 (hr)
TW (3) TWI594769B (hr)
WO (1) WO2013056108A2 (hr)
ZA (1) ZA201606123B (hr)

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