JP7849296B2 - Bcl2阻害剤を含むホットメルト押出し固体分散体 - Google Patents

Bcl2阻害剤を含むホットメルト押出し固体分散体

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Publication number
JP7849296B2
JP7849296B2 JP2022550891A JP2022550891A JP7849296B2 JP 7849296 B2 JP7849296 B2 JP 7849296B2 JP 2022550891 A JP2022550891 A JP 2022550891A JP 2022550891 A JP2022550891 A JP 2022550891A JP 7849296 B2 JP7849296 B2 JP 7849296B2
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methyl
tetrahydro
cycloalkyl
piperazine
amino
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JPWO2021173523A5 (https=
JP2023514750A (ja
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チェン,イ
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グアンジョウ・ルペン・ファーマシューティカル・カンパニー・リミテッド
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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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61K9/141Intimate 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
    • A61K9/146Intimate 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 organic macromolecular compounds
    • 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
    • A61K9/1617Organic 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
    • A61K9/14Particulate 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
    • A61K9/1682Processes
    • A61K9/1694Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • 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
    • A61K9/2013Organic 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
    • A61K9/2022Organic 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
    • A61K9/2095Tabletting processes
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems

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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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Inorganic Chemistry (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Extrusion Moulding Of Plastics Or The Like (AREA)
  • Manufacturing Of Micro-Capsules (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2022550891A 2020-02-24 2021-02-23 Bcl2阻害剤を含むホットメルト押出し固体分散体 Active JP7849296B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US202062980700P 2020-02-24 2020-02-24
US62/980,700 2020-02-24
US202063053565P 2020-07-17 2020-07-17
US63/053,565 2020-07-17
PCT/US2021/019181 WO2021173523A1 (en) 2020-02-24 2021-02-23 Hot melt extruded solid dispersions containing a bcl2 inhibitor

Publications (4)

Publication Number Publication Date
JP2023514750A JP2023514750A (ja) 2023-04-07
JPWO2021173523A5 JPWO2021173523A5 (https=) 2024-03-04
JP2023514750A5 JP2023514750A5 (https=) 2024-03-04
JP7849296B2 true JP7849296B2 (ja) 2026-04-21

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JP2022550891A Active JP7849296B2 (ja) 2020-02-24 2021-02-23 Bcl2阻害剤を含むホットメルト押出し固体分散体

Country Status (10)

Country Link
US (1) US20230295183A1 (https=)
EP (1) EP4110298A1 (https=)
JP (1) JP7849296B2 (https=)
KR (1) KR20220158725A (https=)
CN (1) CN115484933B (https=)
AU (1) AU2021228622A1 (https=)
CA (1) CA3173041A1 (https=)
IL (1) IL295803A (https=)
MX (1) MX2022010410A (https=)
WO (1) WO2021173523A1 (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4442685A4 (en) 2021-12-06 2025-11-19 Hangzhou Healzen Therapeutics Co Ltd BCL-2 PROTEIN ANTI-APOPTOTIC INHIBITOR: PHARMACEUTICAL COMPOSITION AND USES
US11964990B2 (en) 2022-01-21 2024-04-23 Abbvie Inc. 1,3,4,7-tetrahydro-2H-pyrrolo[3′,2′:5,6]pyrido[2,3-b][1,4]oxazepine bcl-2 inhibitors
CN115894495B (zh) * 2022-11-29 2024-08-09 大连理工大学 一种基于尿酸与苯硼酸衍生物复合晶体的纯有机室温磷光材料的制备方法
CN116236583A (zh) * 2023-03-30 2023-06-09 广州麓鹏制药有限公司 一种含Bcl-2/Bcl-xl抑制剂的组合物及其制备方法与应用
CN116270660A (zh) * 2023-03-30 2023-06-23 广州麓鹏制药有限公司 一种含Bcl-2/Bcl-xl抑制剂的组合物及其制备方法与应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012529490A (ja) 2009-06-08 2012-11-22 アボット ゲーエムベーハー ウント カンパニー カーゲー Bcl−2ファミリー阻害剤の経口投与用医薬剤形
JP2013540823A (ja) 2010-10-29 2013-11-07 アッヴィ・インコーポレイテッド アポトーシス誘発剤を含む固体分散体
JP2013544804A (ja) 2010-10-29 2013-12-19 アッヴィ・インコーポレイテッド アポトーシス誘発剤を含む溶融押出固体分散体
WO2015141662A1 (ja) 2014-03-18 2015-09-24 武田薬品工業株式会社 固体分散体
WO2017132474A1 (en) 2016-01-30 2017-08-03 Newave Pharmaceutical Inc. Bcl-2 inhibitors
WO2019040573A1 (en) 2017-08-23 2019-02-28 Newave Pharmaceutical Inc. Bcl-2 inhibitors

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19913692A1 (de) 1999-03-25 2000-09-28 Basf Ag Mechanisch stabile pharmazeutische Darreichungsformen, enthaltend flüssige oder halbfeste oberflächenaktive Substanzen
DE19929361A1 (de) 1999-06-25 2001-01-04 Basf Ag Mechanisch stabile pharmazeutische Darreichungsformen, enthaltend flüssige oder halbfeste oberflächenaktive Substanzen
WO2005049593A2 (en) 2003-11-13 2005-06-02 Abbott Laboratories N-acylsulfonamide apoptosis promoters
US7790190B2 (en) 2004-03-20 2010-09-07 Yasoo Health, Inc. Aqueous emulsions of lipophile solubilized with vitamin E TPGS and linoleic acid
WO2008064116A2 (en) 2006-11-16 2008-05-29 Abbott Laboratories Method of preventing or treating organ, hematopoietic stem cell or bone marrow transplant rejection
EP2231159A1 (en) 2007-11-16 2010-09-29 Abbott Laboratories Method of treating arthritis
US20100297194A1 (en) * 2009-04-30 2010-11-25 Nathaniel Catron Formulation for oral administration of apoptosis promoter
EP3333167A1 (en) * 2016-12-09 2018-06-13 LEK Pharmaceuticals d.d. Solid forms of venetoclax
US12220419B2 (en) * 2018-08-22 2025-02-11 Newave Pharmaceutical Inc. BCL-2 inhibitors

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012529490A (ja) 2009-06-08 2012-11-22 アボット ゲーエムベーハー ウント カンパニー カーゲー Bcl−2ファミリー阻害剤の経口投与用医薬剤形
JP2013540823A (ja) 2010-10-29 2013-11-07 アッヴィ・インコーポレイテッド アポトーシス誘発剤を含む固体分散体
JP2013544804A (ja) 2010-10-29 2013-12-19 アッヴィ・インコーポレイテッド アポトーシス誘発剤を含む溶融押出固体分散体
WO2015141662A1 (ja) 2014-03-18 2015-09-24 武田薬品工業株式会社 固体分散体
WO2017132474A1 (en) 2016-01-30 2017-08-03 Newave Pharmaceutical Inc. Bcl-2 inhibitors
WO2019040573A1 (en) 2017-08-23 2019-02-28 Newave Pharmaceutical Inc. Bcl-2 inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Christian Leuner et al.,"Improving drug solubility for oral delivery using solid dispersions",European Journal of Pharmaceutics and Biopharmaceutics,2000年,Vol.50,p.47-60,DOI: 10.1016/s0939-6411(00)00076-X

Also Published As

Publication number Publication date
JP2023514750A (ja) 2023-04-07
WO2021173523A1 (en) 2021-09-02
CN115484933B (zh) 2026-03-31
EP4110298A1 (en) 2023-01-04
MX2022010410A (es) 2022-12-07
AU2021228622A1 (en) 2022-10-13
IL295803A (en) 2022-10-01
CA3173041A1 (en) 2021-09-02
KR20220158725A (ko) 2022-12-01
CN115484933A (zh) 2022-12-16
US20230295183A1 (en) 2023-09-21

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