CN115484933B - 含有bcl2抑制剂的热熔挤出固体分散体 - Google Patents

含有bcl2抑制剂的热熔挤出固体分散体

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Publication number
CN115484933B
CN115484933B CN202180016511.0A CN202180016511A CN115484933B CN 115484933 B CN115484933 B CN 115484933B CN 202180016511 A CN202180016511 A CN 202180016511A CN 115484933 B CN115484933 B CN 115484933B
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China
Prior art keywords
methyl
piperazin
tetrahydro
compound
benzamide
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CN202180016511.0A
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Chinese (zh)
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CN115484933A (zh
Inventor
陈怡�
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Guangzhou Lupeng Pharmaceutical Co Ltd
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Guangzhou Lupeng Pharmaceutical Co Ltd
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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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic 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
    • 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
    • A61K9/146—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 organic macromolecular 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
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • 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
    • A61K9/2009—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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2095—Tabletting processes
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/14—Ortho-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)
CN202180016511.0A 2020-02-24 2021-02-23 含有bcl2抑制剂的热熔挤出固体分散体 Active CN115484933B (zh)

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 (2)

Publication Number Publication Date
CN115484933A CN115484933A (zh) 2022-12-16
CN115484933B true CN115484933B (zh) 2026-03-31

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CN202180016511.0A Active CN115484933B (zh) 2020-02-24 2021-02-23 含有bcl2抑制剂的热熔挤出固体分散体

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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100297194A1 (en) * 2009-04-30 2010-11-25 Nathaniel Catron Formulation for oral administration of apoptosis promoter
CN103282025A (zh) * 2010-10-29 2013-09-04 Abbvie公司 含有细胞凋亡诱导剂的熔体挤出的固体分散体
WO2019040573A1 (en) * 2017-08-23 2019-02-28 Newave Pharmaceutical Inc. Bcl-2 inhibitors

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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
TWI540132B (zh) 2009-06-08 2016-07-01 亞培公司 Ｂｃｌ-２族群抑制劑之口服醫藥劑型
CA3152557A1 (en) 2010-10-29 2012-05-03 Abbvie Inc. Solid dispersions containing an apoptosis-inducing agent
CN106232144B (zh) * 2014-03-18 2019-12-06 武田药品工业株式会社 固体分散体
WO2017132474A1 (en) * 2016-01-30 2017-08-03 Newave Pharmaceutical Inc. Bcl-2 inhibitors
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100297194A1 (en) * 2009-04-30 2010-11-25 Nathaniel Catron Formulation for oral administration of apoptosis promoter
CN103282025A (zh) * 2010-10-29 2013-09-04 Abbvie公司 含有细胞凋亡诱导剂的熔体挤出的固体分散体
WO2019040573A1 (en) * 2017-08-23 2019-02-28 Newave Pharmaceutical Inc. Bcl-2 inhibitors

Also Published As

Publication number Publication date
JP2023514750A (ja) 2023-04-07
WO2021173523A1 (en) 2021-09-02
EP4110298A1 (en) 2023-01-04
MX2022010410A (es) 2022-12-07
JP7849296B2 (ja) 2026-04-21
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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