CN112957334B - 含alpelisib的药物组合物 - Google Patents

含alpelisib的药物组合物 Download PDF

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Publication number
CN112957334B
CN112957334B CN202110187770.1A CN202110187770A CN112957334B CN 112957334 B CN112957334 B CN 112957334B CN 202110187770 A CN202110187770 A CN 202110187770A CN 112957334 B CN112957334 B CN 112957334B
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China
Prior art keywords
tablet
amide
pharmaceutically acceptable
total weight
dispersible
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CN202110187770.1A
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English (en)
Chinese (zh)
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CN112957334A (zh
Inventor
F·艾尔巴茨
C·科赫哈
D·斯丁奇林
M·A·M·博克
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Novartis AG
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Novartis AG
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61JCONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J3/00Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A61J3/10Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • 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
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • 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
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Nutrition Science (AREA)
  • Dispersion Chemistry (AREA)
  • Physiology (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Zoology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202110187770.1A 2014-10-03 2015-10-01 含alpelisib的药物组合物 Active CN112957334B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202110187770.1A CN112957334B (zh) 2014-10-03 2015-10-01 含alpelisib的药物组合物

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462059331P 2014-10-03 2014-10-03
US62/059,331 2014-10-03
CN201580054000.2A CN107106497A (zh) 2014-10-03 2015-10-01 含alpelisib的药物组合物
PCT/IB2015/057523 WO2016051374A1 (en) 2014-10-03 2015-10-01 Pharmaceutical compositions comprising alpelisib
CN202110187770.1A CN112957334B (zh) 2014-10-03 2015-10-01 含alpelisib的药物组合物

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201580054000.2A Division CN107106497A (zh) 2014-10-03 2015-10-01 含alpelisib的药物组合物

Publications (2)

Publication Number Publication Date
CN112957334A CN112957334A (zh) 2021-06-15
CN112957334B true CN112957334B (zh) 2023-08-04

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Application Number Title Priority Date Filing Date
CN202110187770.1A Active CN112957334B (zh) 2014-10-03 2015-10-01 含alpelisib的药物组合物
CN201580054000.2A Pending CN107106497A (zh) 2014-10-03 2015-10-01 含alpelisib的药物组合物

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CN201580054000.2A Pending CN107106497A (zh) 2014-10-03 2015-10-01 含alpelisib的药物组合物

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Country Link
US (3) US20170296523A1 (enExample)
EP (2) EP3200772B1 (enExample)
JP (1) JP6723229B2 (enExample)
KR (2) KR102598782B1 (enExample)
CN (2) CN112957334B (enExample)
AU (1) AU2015326392B2 (enExample)
BR (1) BR112017004694A2 (enExample)
CA (1) CA2962714C (enExample)
ES (1) ES2929554T3 (enExample)
MX (1) MX2017004359A (enExample)
PL (1) PL3200772T3 (enExample)
PT (1) PT3200772T (enExample)
RU (1) RU2690685C2 (enExample)
WO (1) WO2016051374A1 (enExample)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105919957A (zh) * 2016-06-13 2016-09-07 佛山市腾瑞医药科技有限公司 一种艾代拉利司分散片及其制备方法
AR116299A1 (es) 2018-09-07 2021-04-21 Sanofi Sa Sales de 6-(2,4-diclorofenil)-5-[4-[(3s)-1-(3-fluoropropil)pirrolidin-3-il]oxifenil]-8,9-dihidro-7h-benzo[7]anuleno-2-carboxilato de metilo y proceso de preparación de las mismas
TW202146007A (zh) 2020-02-27 2021-12-16 法商賽諾菲公司 包含阿培利司(alpelisib)與6-(2,4-二氯苯基)-5-[4-[(3s)-1-(3-氟丙基)吡咯啶-3-基]氧苯基]-8,9-二氫-7h-苯并[7]輪烯-2-羧酸之組合
US20240156752A1 (en) * 2021-03-11 2024-05-16 Atossa Therapeutics, Inc. Endoxifen for treatment of ovarian cancer

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5747068A (en) * 1994-07-20 1998-05-05 Lilly S. A. Flouxetine pharmaceutical formulations
WO2012175522A1 (en) * 2011-06-21 2012-12-27 Novartis Ag Polymorphs of (s)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide
WO2013144249A1 (en) * 2012-03-29 2013-10-03 Novartis Ag Pharmaceutical diagnostic
WO2013161823A1 (ja) * 2012-04-24 2013-10-31 第一三共株式会社 口腔内崩壊錠及びその製造方法

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5698226A (en) * 1993-07-13 1997-12-16 Glaxo Wellcome Inc. Water-dispersible tablets
UA104147C2 (uk) 2008-09-10 2014-01-10 Новартис Аг Похідна піролідиндикарбонової кислоти та її застосування у лікуванні проліферативних захворювань
WO2011080502A2 (en) * 2009-12-29 2011-07-07 Orexo Ab New pharmaceutical dosage form for the treatment of gastric acid-related disorders
AR082418A1 (es) * 2010-08-02 2012-12-05 Novartis Ag Formas cristalinas de 1-(4-metil-5-[2-(2,2,2-trifluoro-1,1-dimetil-etil)-piridin-4-il]-tiazol-2-il)-amida de 2-amida del acido (s)-pirrolidin-1,2-dicarboxilico
PH12013502077A1 (en) * 2011-04-25 2013-12-16 Novartis Ag Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor
WO2012170488A1 (en) * 2011-06-07 2012-12-13 Zx Pharma, Llc Multiparticulate s-adenosylmethionine compositions and related methods
WO2014007780A1 (en) * 2012-07-06 2014-01-09 Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi Orally-disintegrating formulations of dexketoprofen
EP2742940B1 (en) * 2012-12-13 2017-07-26 IP Gesellschaft für Management mbH Fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-l-aza-bicyclo-[2.2.2]octane for adminstration once daily, twice daily or thrice daily

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5747068A (en) * 1994-07-20 1998-05-05 Lilly S. A. Flouxetine pharmaceutical formulations
WO2012175522A1 (en) * 2011-06-21 2012-12-27 Novartis Ag Polymorphs of (s)-pyrrolidine-1,2-dicarboxylic acid 2-amide 1-({4-methyl-5-[2-(2,2,2-trifluoro-1,1-dimethyl-ethyl)-pyridin-4-yl]-thiazol-2-yl}-amide
WO2013144249A1 (en) * 2012-03-29 2013-10-03 Novartis Ag Pharmaceutical diagnostic
WO2013161823A1 (ja) * 2012-04-24 2013-10-31 第一三共株式会社 口腔内崩壊錠及びその製造方法

Also Published As

Publication number Publication date
AU2015326392B2 (en) 2018-10-04
KR20230008913A (ko) 2023-01-16
US20220331305A1 (en) 2022-10-20
KR102486126B1 (ko) 2023-01-09
RU2017114195A (ru) 2018-11-08
EP3200772B1 (en) 2022-08-03
EP4169508A1 (en) 2023-04-26
KR20170056574A (ko) 2017-05-23
KR102598782B1 (ko) 2023-11-07
JP6723229B2 (ja) 2020-07-15
CN107106497A (zh) 2017-08-29
EP3200772A1 (en) 2017-08-09
US20170296523A1 (en) 2017-10-19
JP2017530143A (ja) 2017-10-12
RU2017114195A3 (enExample) 2018-11-16
BR112017004694A2 (pt) 2017-12-05
CN112957334A (zh) 2021-06-15
ES2929554T3 (es) 2022-11-30
PT3200772T (pt) 2022-10-19
RU2690685C2 (ru) 2019-06-05
WO2016051374A1 (en) 2016-04-07
CA2962714C (en) 2023-09-19
CA2962714A1 (en) 2016-04-07
AU2015326392A1 (en) 2017-03-09
US20190314353A1 (en) 2019-10-17
MX2017004359A (es) 2017-06-23
PL3200772T3 (pl) 2022-12-19

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